Proteins > Serine/threonine-protein kinase mTOR
Page last updated: 2024-08-07 18:35:09
Serine/threonine-protein kinase mTOR
A serine/threonine-protein kinase mTOR that is encoded in the genome of human. [PRO:CL, UniProtKB:P42345]
Synonyms
EC 2.7.11.1;
FK506-binding protein 12-rapamycin complex-associated protein 1;
FKBP12-rapamycin complex-associated protein;
Mammalian target of rapamycin;
mTOR;
Mechanistic target of rapamycin;
Rapamycin and FKBP12 target 1;
Ra
Research
Bioassay Publications (131)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (0.76) | 18.2507 |
| 2000's | 15 (11.45) | 29.6817 |
| 2010's | 92 (70.23) | 24.3611 |
| 2020's | 23 (17.56) | 2.80 |
Compounds (135)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| caffeine | Homo sapiens (human) | IC50 | 400.0000 | 1 | 1 |
| chloroquine | Homo sapiens (human) | IC50 | 0.2700 | 1 | 1 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | Homo sapiens (human) | IC50 | 4.7474 | 10 | 10 |
| gefitinib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| 3,4-dichloro-n-methyl-n-(2-(1-pyrrolidinyl)cyclohexyl)-benzeneacetamide, (trans)-(+-)-isomer | Homo sapiens (human) | Ki | 0.0007 | 1 | 1 |
| sorafenib | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| wortmannin | Homo sapiens (human) | IC50 | 0.0400 | 1 | 1 |
| 3-(3-pyridyl)-1-propyl-(2s)-1-(3,3-dimethyl-1,2-dioxopentyl)-2-pyrrolidinecarboxylate | Homo sapiens (human) | IC50 | 20.8930 | 1 | 1 |
| tacrolimus | Homo sapiens (human) | IC50 | 0.0021 | 2 | 2 |
| cgp 60474 | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | IC50 | 22.5000 | 2 | 2 |
| ku 55933 | Homo sapiens (human) | IC50 | 7.4400 | 2 | 2 |
| sirolimus | Homo sapiens (human) | IC50 | 0.9906 | 11 | 11 |
| su 11248 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| norbinaltorphimine | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| everolimus | Homo sapiens (human) | IC50 | 0.0022 | 3 | 3 |
| temsirolimus | Homo sapiens (human) | IC50 | 2.0250 | 2 | 2 |
| 17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| px-866 | Homo sapiens (human) | IC50 | 3.1000 | 1 | 1 |
| nu 7026 | Homo sapiens (human) | IC50 | 6.4000 | 3 | 3 |
| 17-hydroxywortmannin | Homo sapiens (human) | IC50 | 0.1930 | 1 | 1 |
| zotarolimus | Homo sapiens (human) | IC50 | 0.0033 | 1 | 1 |
| pi103 | Homo sapiens (human) | IC50 | 0.4746 | 21 | 21 |
| pi103 | Homo sapiens (human) | Ki | 0.0195 | 2 | 2 |
| PI3-Kinase alpha Inhibitor 2 | Homo sapiens (human) | IC50 | 0.0490 | 1 | 1 |
| nu 7441 | Homo sapiens (human) | IC50 | 2.0500 | 2 | 2 |
| idelalisib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| zstk474 | Homo sapiens (human) | IC50 | 0.3633 | 3 | 3 |
| ku-0060648 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| dactolisib | Homo sapiens (human) | IC50 | 0.0233 | 21 | 21 |
| dactolisib | Homo sapiens (human) | Ki | 0.0021 | 2 | 2 |
| 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | Homo sapiens (human) | IC50 | 0.1570 | 2 | 2 |
| buparlisib | Homo sapiens (human) | IC50 | 1.9814 | 5 | 5 |
| buparlisib | Homo sapiens (human) | Ki | 0.1990 | 1 | 1 |
| ku 0063794 | Homo sapiens (human) | IC50 | 0.1182 | 8 | 8 |
| gdc 0941 | Homo sapiens (human) | IC50 | 0.7449 | 10 | 10 |
| gdc 0941 | Homo sapiens (human) | Ki | 0.5775 | 4 | 4 |
| PP121 | Homo sapiens (human) | IC50 | 0.0100 | 3 | 3 |
| pf-04691502 | Homo sapiens (human) | IC50 | 0.0079 | 2 | 2 |
| pf-04691502 | Homo sapiens (human) | Ki | 0.0160 | 2 | 2 |
| gsk 2126458 | Homo sapiens (human) | IC50 | 0.0006 | 8 | 8 |
| gne 477 | Homo sapiens (human) | Ki | 0.0210 | 2 | 2 |
| gdc 0980 | Homo sapiens (human) | Ki | 0.0170 | 2 | 2 |
| wye 125132 | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| azd2014 | Homo sapiens (human) | IC50 | 0.0521 | 4 | 4 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | Homo sapiens (human) | IC50 | 0.0179 | 8 | 8 |
| pki 402 | Homo sapiens (human) | IC50 | 0.0022 | 3 | 3 |
| 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester | Homo sapiens (human) | IC50 | 0.1749 | 5 | 6 |
| pki 587 | Homo sapiens (human) | IC50 | 0.0015 | 6 | 6 |
| cp 466722 | Homo sapiens (human) | IC50 | 4.5900 | 1 | 1 |
| CAY10626 | Homo sapiens (human) | IC50 | 0.0006 | 1 | 1 |
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | Homo sapiens (human) | IC50 | 0.0267 | 4 | 3 |
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | Homo sapiens (human) | Ki | 0.0012 | 2 | 2 |
| (3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)-4-pyrimidinyl]-3-methylmorpholine | Homo sapiens (human) | IC50 | 1.1192 | 5 | 5 |
| etp-46321 | Homo sapiens (human) | IC50 | 4.8800 | 1 | 1 |
| etp-46321 | Homo sapiens (human) | Ki | 4.8800 | 1 | 1 |
| ch 5132799 | Homo sapiens (human) | IC50 | 1.6000 | 1 | 1 |
| torin 1 | Homo sapiens (human) | IC50 | 0.0042 | 4 | 4 |
| gdc-0032 | Homo sapiens (human) | Ki | 1.2000 | 1 | 1 |
| pf-4989216 | Homo sapiens (human) | IC50 | 4.0640 | 1 | 1 |
| pf-4989216 | Homo sapiens (human) | Ki | 1.4400 | 1 | 1 |
| torin 2 | Homo sapiens (human) | IC50 | 0.0068 | 3 | 3 |
| cudc-907 | Homo sapiens (human) | IC50 | 0.3080 | 2 | 2 |
| sar245408 | Homo sapiens (human) | IC50 | 15.0000 | 1 | 0 |
| byl719 | Homo sapiens (human) | IC50 | 4.5203 | 3 | 3 |
| amg 511 | Homo sapiens (human) | IC50 | 12.4000 | 2 | 2 |
| cc214-2 | Homo sapiens (human) | IC50 | 0.2564 | 7 | 7 |
| cc-223 | Homo sapiens (human) | IC50 | 0.0187 | 3 | 3 |
| cc-115 | Homo sapiens (human) | IC50 | 0.0217 | 3 | 3 |
| gne-317 | Homo sapiens (human) | Ki | 0.0090 | 2 | 2 |
| etp-46464 | Homo sapiens (human) | IC50 | 0.0006 | 1 | 1 |
| sar405 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| bay 80-6946 | Homo sapiens (human) | IC50 | 0.0450 | 2 | 2 |
| pp242 | Homo sapiens (human) | IC50 | 1.4284 | 7 | 19 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| imatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| uvitex swn | Homo sapiens (human) | Kd | 130.0000 | 1 | 1 |
| n-phenylpyrrole | Homo sapiens (human) | Kd | 10,000.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| 4(5)-phenylimidazole | Homo sapiens (human) | Kd | 10,000.0000 | 1 | 1 |
| 2-phenylimidazole | Homo sapiens (human) | Kd | 100.0000 | 1 | 1 |
| 2-(2'-pyridyl)benzimidazole | Homo sapiens (human) | Kd | 60.0000 | 1 | 1 |
| 1-phenylimidazole | Homo sapiens (human) | Kd | 10,000.0000 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lestaurtinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| ruboxistaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| canertinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| birb 796 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| enzastaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lapatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| wortmannin | Homo sapiens (human) | Kd | 9.2000 | 1 | 1 |
| pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sirolimus | Homo sapiens (human) | Kd | 0.0006 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| 4-methylesculetin | Homo sapiens (human) | Kd | 1,500.0000 | 1 | 1 |
| bosutinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| everolimus | Homo sapiens (human) | Kd | 0.0020 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pi103 | Homo sapiens (human) | Kd | 0.0120 | 1 | 1 |
| hki 272 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 6244 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bibw 2992 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 0.6200 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| brivanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| kw 2449 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| motesanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| buparlisib | Homo sapiens (human) | Kd | 0.0190 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 0.0987 | 3 | 2 |
| plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gdc 0980 | Homo sapiens (human) | Kd | 0.0033 | 1 | 1 |
| azd2014 | Homo sapiens (human) | Kd | 0.0001 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pki 587 | Homo sapiens (human) | Kd | 0.0009 | 1 | 1 |
| 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine | Homo sapiens (human) | Kd | 0.0001 | 1 | 1 |
| torin 1 | Homo sapiens (human) | Kd | 0.0004 | 1 | 1 |
| torin 2 | Homo sapiens (human) | EC50 | 0.0002 | 1 | 1 |
| cc-223 | Homo sapiens (human) | Kd | 0.0280 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 0.0030 | 2 | 2 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nu 7441 | Homo sapiens (human) | Activity | 1.7000 | 1 | 1 |
Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.European journal of medicinal chemistry, , Sep-18, Volume: 102, 2015
Synthesis and cancer stem cell-based activity of substituted 5-morpholino-7H-thieno[3,2-b]pyran-7-ones designed as next generation PI3K inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells.Bioorganic & medicinal chemistry, , Nov-15, Volume: 19, Issue:22, 2011
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells.Bioorganic & medicinal chemistry, , Mar-15, Volume: 19, Issue:6, 2011
Inhibition of mammalian target of rapamycin signaling by 2-(morpholin-1-yl)pyrimido[2,1-alpha]isoquinolin-4-one.The Journal of biological chemistry, , Aug-17, Volume: 282, Issue:33, 2007
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 14, Issue:24, 2004
Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.Journal of medicinal chemistry, , 12-13, Volume: 61, Issue:23, 2018
Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma.Journal of medicinal chemistry, , Sep-23, Volume: 47, Issue:20, 2004
Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Identification and optimization of 3-bromo-N'-(4-hydroxybenzylidene)-4-methylbenzohydrazide derivatives as mTOR inhibitors that induce autophagic cell death and apoptosis in triple-negative breast cancer.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
Synthesis and anticancer activity of new dihydropyrimidinone derivatives.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 21, Issue:22, 2011
The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain.The Journal of biological chemistry, , May-04, Volume: 282, Issue:18, 2007
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.Journal of medicinal chemistry, , Sep-08, Volume: 48, Issue:18, 2005
Rapamycin analogs with reduced systemic exposure.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Solid-phase/solution-phase combinatorial synthesis of neuroimmunophilin ligands.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Identification and optimization of 3-bromo-N'-(4-hydroxybenzylidene)-4-methylbenzohydrazide derivatives as mTOR inhibitors that induce autophagic cell death and apoptosis in triple-negative breast cancer.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Isolation and structure of homotemsirolimuses A, B, and C.Journal of natural products, , Apr-25, Volume: 74, Issue:4, 2011
Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.Journal of medicinal chemistry, , Jan-27, Volume: 48, Issue:2, 2005
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 14, Issue:24, 2004
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Ring closure strategy leads to potent RIPK3 inhibitors.European journal of medicinal chemistry, , May-05, Volume: 217, 2021
[no title available]ACS medicinal chemistry letters, , Nov-12, Volume: 11, Issue:11, 2020
Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors.European journal of medicinal chemistry, , Oct-15, Volume: 204, 2020
Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 2017
Novel pyrrolopyrimidines as Mps1/TTK kinase inhibitors for breast cancer.Bioorganic & medicinal chemistry, , 04-01, Volume: 25, Issue:7, 2017
Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors.European journal of medicinal chemistry, , Mar-31, Volume: 129, 2017
Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Kα/mTOR inhibitors.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.European journal of medicinal chemistry, , Jul-19, Volume: 117, 2016
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
Design, synthesis and docking studies of novel thienopyrimidine derivatives bearing chromone moiety as mTOR/PI3Kα inhibitors.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors.Bioorganic & medicinal chemistry, , Dec-15, Volume: 22, Issue:24, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.Biochemistry, , Oct-05, Volume: 49, Issue:39, 2010
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.Bioorganic & medicinal chemistry letters, , Dec-20, Volume: 14, Issue:24, 2004
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review.European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 47, 2021
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
Discovery of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 29, Issue:11, 2019
Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3Kα.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
Discovery of a series of N-(5-(quinolin-6-yl)pyridin-3-yl)benzenesulfonamides as PI3K/mTOR dual inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.ACS medicinal chemistry letters, , Aug-11, Volume: 7, Issue:8, 2016
6-Aryl substituted 4-(4-cyanomethyl) phenylamino quinazolines as a new class of isoform-selective PI3K-alpha inhibitors.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.Bioorganic & medicinal chemistry, , Dec-15, Volume: 23, Issue:24, 2015
Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.ACS medicinal chemistry letters, , Apr-09, Volume: 6, Issue:4, 2015
Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity.Bioorganic & medicinal chemistry, , Oct-01, Volume: 23, Issue:19, 2015
Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Recent results in protein kinase inhibition for tropical diseases.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 22, Issue:22, 2012
Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes.Biochemistry, , Oct-05, Volume: 49, Issue:39, 2010
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
[no title available]ACS medicinal chemistry letters, , Jul-12, Volume: 9, Issue:7, 2018
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 2011
Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 47, 2021
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 19, Issue:20, 2009
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.Journal of medicinal chemistry, , 06-23, Volume: 65, Issue:12, 2022
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Class II Phosphoinositide 3-Kinases as Novel Drug Targets.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors.Journal of medicinal chemistry, , 05-11, Volume: 60, Issue:9, 2017
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Design, synthesis, biological evaluation and docking studies of novel 2-substituted-4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as dual PI3Kα/mTOR inhibitors.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Synthesis and anticancer activity of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives bearing chromone moiety.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.ACS medicinal chemistry letters, , Jan-08, Volume: 6, Issue:1, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.Journal of medicinal chemistry, , Nov-10, Volume: 54, Issue:21, 2011
Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
[no title available],
Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
Synthesis and structure-activity relationships of PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 24, Issue:18, 2014
Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.Bioorganic & medicinal chemistry letters, , May-01, Volume: 23, Issue:9, 2013
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.ACS medicinal chemistry letters, , Nov-10, Volume: 2, Issue:11, 2011
Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review.European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
[no title available]European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
[no title available]ACS medicinal chemistry letters, , Nov-11, Volume: 12, Issue:11, 2021
Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.ACS medicinal chemistry letters, , Mar-08, Volume: 9, Issue:3, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 2017
Structure-based optimization leads to the discovery of NSC765844, a highly potent, less toxic and orally efficacious dual PI3K/mTOR inhibitor.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.Journal of medicinal chemistry, , Nov-10, Volume: 54, Issue:21, 2011
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.ACS medicinal chemistry letters, , Apr-14, Volume: 7, Issue:4, 2016
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.Journal of medicinal chemistry, , Nov-10, Volume: 54, Issue:21, 2011
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.Journal of medicinal chemistry, , 01-27, Volume: 65, Issue:2, 2022
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
[no title available]Bioorganic & medicinal chemistry letters, , 07-15, Volume: 27, Issue:14, 2017
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity.Bioorganic & medicinal chemistry, , 08-07, Volume: 26, Issue:14, 2018
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Design, synthesis, and biological evaluation of imidazo[1,2-b]pyridazine derivatives as mTOR inhibitors.European journal of medicinal chemistry, , Mar-31, Volume: 129, 2017
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Phosphatidylinositol 3-Kinase (PI3K) and phosphatidylinositol 3-kinase-related kinase (PIKK) inhibitors: importance of the morpholine ring.Journal of medicinal chemistry, , Jan-08, Volume: 58, Issue:1, 2015
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.Journal of medicinal chemistry, , Jan-28, Volume: 53, Issue:2, 2010
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.Journal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Molecular design of dual inhibitors of PI3K and potential molecular target of cancer for its treatment: A review.European journal of medicinal chemistry, , Jan-15, Volume: 228, 2022
Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.Bioorganic & medicinal chemistry, , 02-15, Volume: 32, 2021
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.Journal of medicinal chemistry, , Mar-25, Volume: 53, Issue:6, 2010
Design, synthesis and biological evaluation of novel hybrids targeting mTOR and HDACs for potential treatment of hepatocellular carcinoma.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-RSC medicinal chemistry, , Oct-01, Volume: 11, Issue:10, 2020
Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.ACS medicinal chemistry letters, , Nov-14, Volume: 10, Issue:11, 2019
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
[no title available],
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Identification of novel PI3K inhibitors through a scaffold hopping strategy.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity.European journal of medicinal chemistry, , Jul-01, Volume: 197, 2020
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.ACS medicinal chemistry letters, , Nov-10, Volume: 2, Issue:11, 2011
Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.Journal of medicinal chemistry, , 08-08, Volume: 62, Issue:15, 2019
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195).Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity.European journal of medicinal chemistry, , Jul-01, Volume: 197, 2020
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021).European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.Journal of medicinal chemistry, , Jul-09, Volume: 58, Issue:13, 2015
Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 47, 2021
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.Journal of medicinal chemistry, , Jul-09, Volume: 58, Issue:13, 2015
Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.ACS medicinal chemistry letters, , Apr-14, Volume: 7, Issue:4, 2016
The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Class 1 PI3K Clinical Candidates and Recent Inhibitor Design Strategies: A Medicinal Chemistry Perspective.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.Journal of medicinal chemistry, , 06-14, Volume: 61, Issue:11, 2018
Non-kinase targets of protein kinase inhibitors.Nature reviews. Drug discovery, , Volume: 16, Issue:6, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 20, Issue:15, 2010
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.Nature chemical biology, , Volume: 4, Issue:11, 2008
Enables
This protein enables 13 target(s):
| Target | Category | Definition |
|---|
| RNA polymerase III type 1 promoter sequence-specific DNA binding | molecular function | Binding to a sequence of DNA that is a part of a type 1 promoter that controls transcription by RNA polymerase III. Type 1 promoters are found in 5S rRNA genes, downstream of the transcription start site within the sequence of the mature RNA, and require TFIIIA for recognition. [GOC:txnOH, PMID:12381659] |
| RNA polymerase III type 2 promoter sequence-specific DNA binding | molecular function | Binding to a sequence of DNA that is a part of a type 2 promoter that controls transcription by RNA polymerase III. Type 2 promoters consist of an A box and a B box downstream of the transcription start site within the sequence within the sequence of the mature RNA. Type 2 promoters are found in many tRNA genes as well as in other small RNAs. [GOC:txnOH, PMID:12381659] |
| RNA polymerase III type 3 promoter sequence-specific DNA binding | molecular function | Binding to a sequence of DNA that is a part of a type 3 promoter that controls transcription by RNA polymerase III (Pol III). A type 3 Pol III promoter is composed of elements upstream of the transcription start site, including a TATA box. The human U6 snRNA gene has a type 3 promoter. Type 3 Pol III promoters have not been observed in S. cerevisiae. [GOC:txnOH, PMID:12381659] |
| TFIIIC-class transcription factor complex binding | molecular function | Binding to a general RNA polymerase III transcription factor belonging to the TFIIC complex, one of the factors involved in formation of the preinitiation complex (PIC) by RNA polymerase III. [GOC:txnOH, PMID:12381659] |
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| kinase activity | molecular function | Catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [ISBN:0198506732] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| ribosome binding | molecular function | Binding to a ribosome. [GOC:go_curators] |
| phosphoprotein binding | molecular function | Binding to a phosphorylated protein. [GOC:ai] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 13 target(s):
| Target | Category | Definition |
|---|
| Golgi membrane | cellular component | The lipid bilayer surrounding any of the compartments of the Golgi apparatus. [GOC:mah] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| mitochondrial outer membrane | cellular component | The outer, i.e. cytoplasm-facing, lipid bilayer of the mitochondrial envelope. [GOC:ai] |
| lysosome | cellular component | A small lytic vacuole that has cell cycle-independent morphology found in most animal cells and that contains a variety of hydrolases, most of which have their maximal activities in the pH range 5-6. The contained enzymes display latency if properly isolated. About 40 different lysosomal hydrolases are known and lysosomes have a great variety of morphologies and functions. [GOC:mah, ISBN:0198506732] |
| lysosomal membrane | cellular component | The lipid bilayer surrounding the lysosome and separating its contents from the cell cytoplasm. [GOC:ai] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| endomembrane system | cellular component | A collection of membranous structures involved in transport within the cell. The main components of the endomembrane system are endoplasmic reticulum, Golgi bodies, vesicles, cell membrane and nuclear envelope. Members of the endomembrane system pass materials through each other or though the use of vesicles. [GOC:lh] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| phagocytic vesicle | cellular component | A membrane-bounded intracellular vesicle that arises from the ingestion of particulate material by phagocytosis. [GOC:go_curators, ISBN:0198506732] |
| nuclear envelope | cellular component | The double lipid bilayer enclosing the nucleus and separating its contents from the rest of the cytoplasm; includes the intermembrane space, a gap of width 20-40 nm (also called the perinuclear space). [ISBN:0198547684] |
Active In
This protein is active in 4 target(s):
| Target | Category | Definition |
|---|
| lysosomal membrane | cellular component | The lipid bilayer surrounding the lysosome and separating its contents from the cell cytoplasm. [GOC:ai] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| TORC1 complex | cellular component | A protein complex that contains at least TOR (target of rapamycin) and Raptor (regulatory-associated protein of TOR), or orthologs of, in complex with other signaling components. Mediates the phosphorylation and activation of S6K. In Saccharomyces, the complex contains Kog1p, Lst8p, Tco89p, and either Tor1p or Tor2p. [GOC:jh, PMID:15780592, PMID:16469695, PMID:21548787] |
| TORC2 complex | cellular component | A protein complex that contains at least TOR (target of rapamycin) and Rictor (rapamycin-insensitive companion of TOR), or orthologs of, in complex with other signaling components. Mediates the phosphorylation and activation of PKB (also called AKT). In Saccharomyces, the complex contains Avo1p, Avo2p, Tsc11p, Lst8p, Bit61p, Slm1p, Slm2p, and Tor2p. [GOC:bf, GOC:jh, PMID:14736892, PMID:15780592, PMID:16469695, PMID:21548787] |
Involved In
This protein is involved in 86 target(s):
| Target | Category | Definition |
|---|
| regulation of cell growth | biological process | Any process that modulates the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
| T-helper 1 cell lineage commitment | biological process | The process in which a CD4-positive, alpha-beta T cell becomes committed to becoming a T-helper 1 cell, a CD4-positive, alpha-beta T cell specialized to promote immunological processes often associated with resistance to intracellular bacteria, fungi, and protozoa, and pathological conditions such as arthritis. [GOC:add, ISBN:0781735149] |
| heart morphogenesis | biological process | The developmental process in which the heart is generated and organized. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:dph, GOC:isa_complete] |
| heart valve morphogenesis | biological process | The process in which the structure of a heart valve is generated and organized. [GOC:mtg_heart] |
| energy reserve metabolic process | biological process | The chemical reactions and pathways by which a cell derives energy from stored compounds such as fats or glycogen. [GOC:mah] |
| 'de novo' pyrimidine nucleobase biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of pyrimidine nucleobases, 1,3-diazine, organic nitrogenous bases, beginning with the synthesis of a pyrimidine ring from simpler precursors. [GOC:mah, ISBN:0716720094] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| DNA damage response | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
| cytoskeleton organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of cytoskeletal structures. [GOC:dph, GOC:jl, GOC:mah] |
| lysosome organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a lysosome. A lysosome is a cytoplasmic, membrane-bounded organelle that is found in most animal cells and that contains a variety of hydrolases. [GOC:mah] |
| germ cell development | biological process | The process whose specific outcome is the progression of an immature germ cell over time, from its formation to the mature structure (gamete). A germ cell is any reproductive cell in a multicellular organism. [GOC:go_curators] |
| response to nutrient | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nutrient stimulus. [GOC:go_curators] |
| regulation of cell size | biological process | Any process that modulates the size of a cell. [GOC:go_curators] |
| cellular response to starvation | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of deprivation of nourishment. [GOC:jl] |
| response to heat | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a heat stimulus, a temperature stimulus above the optimal temperature for that organism. [GOC:lr] |
| post-embryonic development | biological process | The process whose specific outcome is the progression of the organism over time, from the completion of embryonic development to the mature structure. See embryonic development. [GOC:go_curators] |
| negative regulation of autophagy | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of autophagy. Autophagy is the process in which cells digest parts of their own cytoplasm. [GOC:dph, GOC:tb] |
| positive regulation of lamellipodium assembly | biological process | Any process that increases the rate, frequency or extent of the formation of a lamellipodium, a thin sheetlike extension of the surface of a migrating cell. [GOC:dph, GOC:tb] |
| positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| positive regulation of epithelial to mesenchymal transition | biological process | Any process that increases the rate, frequency, or extent of epithelial to mesenchymal transition. Epithelial to mesenchymal transition is where an epithelial cell loses apical/basolateral polarity, severs intercellular adhesive junctions, degrades basement membrane components and becomes a migratory mesenchymal cell. [GOC:BHF, GOC:dph, GOC:tb] |
| positive regulation of myotube differentiation | biological process | Any process that activates, maintains or increases the frequency, rate or extent of myotube differentiation. Myotube differentiation is the process in which a relatively unspecialized cell acquires specialized features of a myotube cell. Myotubes are multinucleated cells that are formed when proliferating myoblasts exit the cell cycle, differentiate and fuse. [GOC:dph, GOC:tb] |
| macroautophagy | biological process | The autophagic process that proceeds via the formation of an autophagosome. [PMID:24366339] |
| regulation of macroautophagy | biological process | Any process that modulates the frequency, rate or extent of macroautophagy. [GOC:krc] |
| phosphorylation | biological process | The process of introducing a phosphate group into a molecule, usually with the formation of a phosphoric ester, a phosphoric anhydride or a phosphoric amide. [ISBN:0198506732] |
| peptidyl-serine phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| neuronal action potential | biological process | An action potential that occurs in a neuron. [GOC:dph, GOC:isa_complete, GOC:tb] |
| protein catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of a protein by the destruction of the native, active configuration, with or without the hydrolysis of peptide bonds. [GOC:mah] |
| positive regulation of cell growth | biological process | Any process that activates or increases the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
| positive regulation of actin filament polymerization | biological process | Any process that activates or increases the frequency, rate or extent of actin polymerization. [GOC:mah] |
| T cell costimulation | biological process | The process of providing, via surface-bound receptor-ligand pairs, a second, antigen-independent, signal in addition to that provided by the T cell receptor to augment T cell activation. [ISBN:0781735149] |
| ruffle organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a ruffle, a projection at the leading edge of a crawling cell. [GOC:mah, PMID:10036235] |
| regulation of myelination | biological process | Any process that modulates the frequency, rate or extent of the formation of a myelin sheath around nerve axons. [GOC:mah] |
| response to nutrient levels | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus reflecting the presence, absence, or concentration of nutrients. [GOC:mah] |
| cellular response to nutrient levels | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus reflecting the presence, absence, or concentration of nutrients. [GOC:mah] |
| cellular response to nutrient | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nutrient stimulus. [GOC:mah] |
| TOR signaling | biological process | The series of molecular signals mediated by TOR (Target of rapamycin) proteins, members of the phosphoinositide (PI) 3-kinase related kinase (PIKK) family that act as serine/threonine kinases in response to nutrient availability or growth factors. [PMID:12372295] |
| positive regulation of phosphoprotein phosphatase activity | biological process | Any process that activates or increases the activity of a phosphoprotein phosphatase. [GOC:mah] |
| cellular response to insulin stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732] |
| regulation of actin cytoskeleton organization | biological process | Any process that modulates the frequency, rate or extent of the formation, arrangement of constituent parts, or disassembly of cytoskeletal structures comprising actin filaments and their associated proteins. [GOC:mah] |
| calcineurin-NFAT signaling cascade | biological process | Any intracellular signal transduction in which the signal is passed on within the cell by activation of a member of the NFAT protein family as a consequence of NFAT dephosphorylation by Ca(2+)-activated calcineurin. The cascade begins with calcium-dependent activation of the phosphatase calcineurin. Calcineurin dephosphorylates multiple phosphoserine residues on NFAT, resulting in the translocation of NFAT to the nucleus. The cascade ends with regulation of transcription by NFAT. The calcineurin-NFAT cascade lies downstream of many cell surface receptors, including G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs) that signal to mobilize calcium ions (Ca2+). [GOC:lm, GOC:mah, PMID:12975316, PMID:15928679] |
| cellular response to amino acid starvation | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of deprivation of amino acids. [GOC:ecd] |
| multicellular organism growth | biological process | The increase in size or mass of an entire multicellular organism, as opposed to cell growth. [GOC:bf, GOC:curators, GOC:dph, GOC:tb] |
| TORC1 signaling | biological process | A series of intracellular molecular signals mediated by TORC1; TOR (target of rapamycin) in complex with at least Raptor (regulatory-associated protein of TOR), or orthologs of, and other signaling components. [GOC:lb] |
| regulation of circadian rhythm | biological process | Any process that modulates the frequency, rate or extent of a circadian rhythm. A circadian rhythm is a biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:dph, GOC:jl, GOC:tb] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| response to amino acid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an amino acid stimulus. An amino acid is a carboxylic acids containing one or more amino groups. [GOC:ef, GOC:mlg] |
| anoikis | biological process | Apoptosis triggered by inadequate or inappropriate adherence to substrate e.g. after disruption of the interactions between normal epithelial cells and the extracellular matrix. [GOC:jl, http://www.copewithcytokines.de/] |
| regulation of osteoclast differentiation | biological process | Any process that modulates the frequency, rate or extent of osteoclast differentiation. [GOC:go_curators] |
| positive regulation of translation | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of proteins by the translation of mRNA or circRNA. [GOC:dph, GOC:go_curators, GOC:tb] |
| negative regulation of cell size | biological process | Any process that reduces cell size. [GOC:go_curators] |
| positive regulation of glycolytic process | biological process | Any process that activates or increases the frequency, rate or extent of glycolysis. [GOC:go_curators] |
| positive regulation of transcription by RNA polymerase III | biological process | Any process that activates or increases the frequency, rate or extent of transcription mediated by RNA polymerase III. [GOC:go_curators, GOC:txnOH] |
| positive regulation of translational initiation | biological process | Any process that activates or increases the frequency, rate or extent of translational initiation. [GOC:go_curators] |
| positive regulation of lipid biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of lipids. [GOC:ai] |
| behavioral response to pain | biological process | Any process that results in a change in the behavior of an organism as a result of a pain stimulus. Pain stimuli cause activation of nociceptors, peripheral receptors for pain, include receptors which are sensitive to painful mechanical stimuli, extreme heat or cold, and chemical stimuli. [GOC:jid] |
| rhythmic process | biological process | Any process pertinent to the generation and maintenance of rhythms in the physiology of an organism. [GOC:jid] |
| oligodendrocyte differentiation | biological process | The process in which a relatively unspecialized cell acquires the specialized features of an oligodendrocyte. An oligodendrocyte is a type of glial cell involved in myelinating the axons of neurons in the central nervous system. [GOC:vp, PMID:15139015] |
| positive regulation of oligodendrocyte differentiation | biological process | Any process that activates or increases the frequency, rate or extent of oligodendrocyte differentiation. [GOC:vp, PMID:15139015] |
| positive regulation of peptidyl-tyrosine phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of the phosphorylation of peptidyl-tyrosine. [GOC:ai] |
| voluntary musculoskeletal movement | biological process | The movement of an organism or part of an organism using mechanoreceptors, the nervous system, striated muscle and/or the skeletal system that can be controlled at will. [GOC:dph] |
| positive regulation of stress fiber assembly | biological process | Any process that activates or increases the frequency, rate or extent of the assembly of a stress fiber, a bundle of microfilaments and other proteins found in fibroblasts. [GOC:ai] |
| positive regulation of keratinocyte migration | biological process | Any process that activates or increases the frequency, rate or extent of keratinocyte migration. [GOC:ai] |
| nucleus localization | biological process | Any process in which the nucleus is transported to, and/or maintained in, a specific location within the cell. [GOC:ai] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| cardiac muscle cell development | biological process | The process whose specific outcome is the progression of a cardiac muscle cell over time, from its formation to the mature state. [GOC:devbiol, GOC:mtg_heart] |
| cardiac muscle contraction | biological process | Muscle contraction of cardiac muscle tissue. [GOC:dph] |
| cellular response to methionine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a methionine stimulus. [GOC:dph, PMID:7891681] |
| negative regulation of calcineurin-NFAT signaling cascade | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the calcineurin-NFAT signaling cascade. [GOC:mah] |
| cellular response to amino acid stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an amino acid stimulus. An amino acid is a carboxylic acids containing one or more amino groups. [GOC:mah] |
| cellular response to L-leucine | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a L-leucine stimulus. [GOC:mah] |
| cellular response to hypoxia | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
| cellular response to osmotic stress | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating an increase or decrease in the concentration of solutes outside the organism or cell. [GOC:mah] |
| regulation of membrane permeability | biological process | Any process that modulates the frequency, rate or extent of the passage or uptake of molecules by a membrane. [GOC:kmv, PMID:22677064] |
| regulation of cellular response to heat | biological process | Any process that modulates the frequency, rate or extent of cellular response to heat. [GOC:TermGenie, GOC:yaf] |
| negative regulation of protein localization to nucleus | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of protein localization to nucleus. [GOC:TermGenie] |
| regulation of signal transduction by p53 class mediator | biological process | Any process that modulates the frequency, rate or extent of signal transduction by p53 class mediator. [GOC:TermGenie] |
| positive regulation of transcription of nucleolar large rRNA by RNA polymerase I | biological process | Any process that activates or increases the frequency, rate or extent of transcription of nuclear large rRNA mediated by RNA polymerase I. [GOC:sart, GOC:TermGenie] |
| positive regulation of wound healing, spreading of epidermal cells | biological process | Any process that activates or increases the frequency, rate or extent of wound healing, spreading of epidermal cells. [GO_REF:0000058, GOC:als, GOC:TermGenie, PMID:18394891] |
| regulation of locomotor rhythm | biological process | Any process that modulates the frequency, rate or extent of locomotor rhythm. [GO_REF:0000058, GOC:TermGenie, PMID:16310969] |
| positive regulation of cytoplasmic translational initiation | biological process | Any process that activates or increases the frequency, rate or extent of cytoplasmic translational initiation. [GO_REF:0000058, GOC:TermGenie, PMID:12242291] |
| negative regulation of lysosome organization | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of lysosome organization. [GO_REF:0000058, GOC:TermGenie, PMID:25561470] |
| positive regulation of pentose-phosphate shunt | biological process | Any process that activates or increases the frequency, rate or extent of pentose-phosphate shunt. [GO_REF:0000058, GOC:TermGenie, PMID:19015259] |
| cellular response to leucine starvation | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of deprivation of leucine. [PMID:19033384] |
| regulation of autophagosome assembly | biological process | Any process that modulates the frequency, rate or extent of autophagosome assembly. [GOC:autophagy, GOC:BHF] |
| negative regulation of macroautophagy | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of macroautophagy. [GOC:go_curators] |