Proteins > Receptor tyrosine-protein kinase erbB-2
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Receptor tyrosine-protein kinase erbB-2
A receptor tyrosine-protein kinase erbB-2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P04626]
Synonyms
EC 2.7.10.1;
Metastatic lymph node gene 19 protein;
MLN 19;
Proto-oncogene Neu;
Proto-oncogene c-ErbB-2;
Tyrosine kinase-type cell surface receptor HER2;
p185erbB2
Research
Bioassay Publications (160)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (4.38) | 18.2507 |
| 2000's | 47 (29.38) | 29.6817 |
| 2010's | 83 (51.88) | 24.3611 |
| 2020's | 23 (14.38) | 2.80 |
Compounds (158)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.Journal of medicinal chemistry, , Aug-24, Volume: 43, Issue:17, 2000
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 18, Issue:22, 2008
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.Journal of medicinal chemistry, , Aug-16, Volume: 44, Issue:17, 2001
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.Journal of medicinal chemistry, , May-20, Volume: 42, Issue:10, 1999
Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
[no title available]Bioorganic & medicinal chemistry letters, , 08-15, Volume: 30, Issue:16, 2020
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
[no title available]European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Acetylene Group, Friend or Foe in Medicinal Chemistry.Journal of medicinal chemistry, , 06-11, Volume: 63, Issue:11, 2020
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 26, Issue:19, 2016
Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents.Bioorganic & medicinal chemistry, , Jan-15, Volume: 24, Issue:2, 2016
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Tyrosine kinase inhibitors. 18. 6-Substituted 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as soluble, irreversible inhibitors of the epidermal growth factor receptor.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 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
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 18, Issue:22, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.Journal of medicinal chemistry, , Apr-06, Volume: 43, Issue:7, 2000
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.Journal of medicinal chemistry, , Jul-04, Volume: 45, Issue:14, 2002
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
[no title available],
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Acetylene Group, Friend or Foe in Medicinal Chemistry.Journal of medicinal chemistry, , 06-11, Volume: 63, Issue:11, 2020
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
[no title available]European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs.Bioorganic & medicinal chemistry letters, , 10-01, Volume: 26, Issue:19, 2016
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Design, synthesis and molecular modeling of biquinoline-pyridine hybrids as a new class of potential EGFR and HER-2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 24, Issue:18, 2014
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives containing benzodioxole as potential anticancer agents.Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Design, modification and 3D QSAR studies of novel naphthalin-containing pyrazoline derivatives with/without thiourea skeleton as anticancer agents.Bioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Design, synthesis and biological evaluation of pyrazolyl-thiazolinone derivatives as potential EGFR and HER-2 kinase inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Metronidazole acid acyl sulfonamide: a novel class of anticancer agents and potential EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.The Journal of biological chemistry, , May-27, Volume: 286, Issue:21, 2011
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 20, Issue:20, 2010
Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Synthesis and structure-activity relationships of N-benzyl-N-(X-2-hydroxybenzyl)-N'-phenylureas and thioureas as antitumor agents.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Design, synthesis and biological evaluation of thiazolidinone derivatives as potential EGFR and HER-2 kinase inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 18, Issue:1, 2010
Synthesis, molecular modeling, and biological evaluation of cinnamic acid metronidazole ester derivatives as novel anticancer agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
[no title available],
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.Bioorganic & medicinal chemistry letters, , 05-01, Volume: 30, Issue:9, 2020
[no title available]Bioorganic & medicinal chemistry letters, , 08-15, Volume: 30, Issue:16, 2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold.Journal of medicinal chemistry, , 12-27, Volume: 61, Issue:24, 2018
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Design, synthesis and biological evaluation of novel EGFR/HER2 dual inhibitors bearing a oxazolo[4,5-g]quinazolin-2(1H)-one scaffold.European journal of medicinal chemistry, , Sep-14, Volume: 120, 2016
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Identification of quinones as HER2 inhibitors for the treatment of trastuzumab resistant breast cancer.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Synthesis and biological evaluation of 4-[3-chloro-4-(3-fluorobenzyloxy)anilino]-6-(3-substituted-phenoxy)pyrimidines as dual EGFR/ErbB-2 kinase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.Bioorganic & medicinal chemistry, , Jan-01, Volume: 20, Issue:1, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.The Journal of biological chemistry, , May-27, Volume: 286, Issue:21, 2011
Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 20, Issue:20, 2010
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases.Proceedings of the National Academy of Sciences of the United States of America, , Feb-26, Volume: 105, Issue:8, 2008
Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
New thiazole-based derivatives as EGFR/HER2 and DHFR inhibitors: Synthesis, molecular modeling simulations and anticancer activity.European journal of medicinal chemistry, , Nov-05, Volume: 241, 2022
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
N-(3-Cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinJournal of medicinal chemistry, , Nov-16, Volume: 49, Issue:23, 2006
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.Journal of medicinal chemistry, , Volume: 34, Issue:6, 1991
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.Journal of medicinal chemistry, , Volume: 34, Issue:6, 1991
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.Journal of medicinal chemistry, , Volume: 34, Issue:6, 1991
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.Journal of medicinal chemistry, , Aug-26, Volume: 42, Issue:17, 1999
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.Journal of medicinal chemistry, , Volume: 34, Issue:6, 1991
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.Journal of medicinal chemistry, , Oct-23, Volume: 46, Issue:22, 2003
Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins.Journal of medicinal chemistry, , Nov-12, Volume: 36, Issue:23, 1993
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
A small molecule-kinase interaction map for clinical kinase inhibitors.Nature biotechnology, , Volume: 23, Issue:3, 2005
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epiJournal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.Proceedings of the National Academy of Sciences of the United States of America, , Dec-18, Volume: 104, Issue:51, 2007
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.Journal of medicinal chemistry, , Dec-29, Volume: 48, Issue:26, 2005
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Online informatics resources to facilitate cancer target and chemical probe discovery.RSC medicinal chemistry, , Jun-01, Volume: 11, Issue:6, 2020
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
CDK8 as a therapeutic target for cancers and recent developments in discovery of CDK8 inhibitors.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Discovery of novel small-molecule inhibitors of human epidermal growth factor receptor-2: combined ligand and target-based approach.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.ACS chemical biology, , 12-16, Volume: 11, Issue:12, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 29, Issue:4, 2019
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epiderJournal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 2013
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.European journal of medicinal chemistry, , Mar-15, Volume: 214, 2021
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.Journal of medicinal chemistry, , 09-08, Volume: 59, Issue:17, 2016
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer.European journal of medicinal chemistry, , Volume: 69, 2013
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 19, Issue:22, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.Proceedings of the National Academy of Sciences of the United States of America, , Nov-01, Volume: 102, Issue:44, 2005
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 25, Issue:22, 2015
Design and synthesis of novel pyrimido[4,5-b]azepine derivatives as HER2/EGFR dual inhibitors.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Selectively nonselective kinase inhibition: striking the right balance.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
[no title available],
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of quinoline-based irreversible BTK inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis.European journal of medicinal chemistry, , May-01, Volume: 169, 2019
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors.MedChemComm, , Apr-01, Volume: 9, Issue:4, 2018
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Discovery of (R)-5-(benzo[d][1,3]dioxol-5-yl)-7-((1-(vinylsulfonyl)pyrrolidin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (B6) as a potent Bmx inhibitor for the treatment of NSCLC.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 27, Issue:17, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy.Bioorganic & medicinal chemistry, , 01-01, Volume: 25, Issue:1, 2017
Recent progress on third generation covalent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of quinoline-based irreversible BTK inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
[no title available],
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Recent progress on third generation covalent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.Cancer research, , Jun-15, Volume: 68, Issue:12, 2008
Enables
This protein enables 12 target(s):
| Target | Category | Definition |
|---|
| RNA polymerase I core binding | molecular function | Binding to a RNA polymerase I core enzyme, a multisubunit eukaryotic nuclear RNA polymerase typically composed of seventeen subunits. [GOC:txnOH] |
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| transmembrane receptor protein tyrosine kinase activity | molecular function | Combining with a signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP + a protein-L-tyrosine = ADP + a protein-L-tyrosine phosphate. [EC:2.7.10.1, GOC:mah] |
| transmembrane signaling receptor activity | molecular function | Combining with an extracellular or intracellular signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity or state as part of signal transduction. [GOC:go_curators, Wikipedia:Transmembrane_receptor] |
| signaling receptor binding | molecular function | Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732] |
| 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] |
| coreceptor activity | molecular function | Combining with an extracellular or intracellular messenger, and in cooperation with a nearby primary receptor, initiating a change in cell activity. [GOC:go_curators] |
| receptor tyrosine kinase binding | molecular function | Binding to a receptor that possesses protein tyrosine kinase activity. [GOC:mah] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| ErbB-3 class receptor binding | molecular function | Binding to the protein-tyrosine kinase receptor ErbB-3/HER3. [GOC:jl] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
Located In
This protein is located in 14 target(s):
| Target | Category | Definition |
|---|
| 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] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| early endosome | cellular component | A membrane-bounded organelle that receives incoming material from primary endocytic vesicles that have been generated by clathrin-dependent and clathrin-independent endocytosis; vesicles fuse with the early endosome to deliver cargo for sorting into recycling or degradation pathways. [GOC:mah, NIF_Subcellular:nlx_subcell_20090701, PMID:19696797] |
| 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] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| endosome membrane | cellular component | The lipid bilayer surrounding an endosome. [GOC:mah] |
| 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] |
| basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| neuromuscular junction | cellular component | The junction between the axon of a motor neuron and a muscle fiber. In response to the arrival of action potentials, the presynaptic button releases molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane of the muscle fiber, leading to a change in post-synaptic potential. [GOC:nln] |
| ruffle membrane | cellular component | The portion of the plasma membrane surrounding a ruffle. [GOC:mah] |
| presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
| myelin sheath | cellular component | An electrically insulating fatty layer that surrounds the axons of many neurons. It is an outgrowth of glial cells: Schwann cells supply the myelin for peripheral neurons while oligodendrocytes supply it to those of the central nervous system. [GOC:cjm, GOC:jl, NIF_Subcellular:sao593830697, Wikipedia:Myelin] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| basal plasma membrane | cellular component | The region of the plasma membrane located at the basal end of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
Part Of
This protein is part of 3 target(s):
| Target | Category | Definition |
|---|
| semaphorin receptor complex | cellular component | A stable binary complex of a semaphorin and a plexin, together forming a functional semaphorin receptor. [GOC:hjd, PMID:10934324, PMID:12367632, PMID:12613544] |
| ERBB3:ERBB2 complex | cellular component | A heterodimeric complex between the tyrosine kinase receptor ERBB2 and a ligand-activated receptor ERBB3. ERBB2, which does not bind any known ligand, is activated through formation of a heterodimer with another ligand-activated ERBB family member such as ERBB3. [GOC:signaling, PMID:16460914, PMID:8665853, Reactome:R-HSA-1247502, Reactome:R-HSA-1963573, Reactome:R-HSA-1963589] |
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 42 target(s):
| Target | Category | Definition |
|---|
| positive regulation of protein phosphorylation | biological process | Any process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| enzyme-linked receptor protein signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell, where the receptor possesses catalytic activity or is closely associated with an enzyme such as a protein kinase, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| cell surface receptor protein tyrosine kinase signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| heart development | biological process | The process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948] |
| neuromuscular junction development | 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 neuromuscular junction. [GOC:mtg_OBO2OWL_2013] |
| motor neuron axon guidance | biological process | The process in which the migration of an axon growth cone of a motor neuron is directed to a specific target site in response to a combination of attractive and repulsive cues. [CL:0000100, GOC:pr, ISBN:0878932437] |
| Schwann cell development | biological process | The process aimed at the progression of a Schwann cell over time, from initial commitment of the cell to a specific fate, to the fully functional differentiated cell. Schwann cells are found in the peripheral nervous system, where they insulate neurons and axons, and regulate the environment in which neurons function. [GOC:dgh, GOC:ef] |
| peptidyl-tyrosine phosphorylation | biological process | The phosphorylation of peptidyl-tyrosine to form peptidyl-O4'-phospho-L-tyrosine. [RESID:AA0039] |
| 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] |
| regulation of microtubule-based process | biological process | Any process that modulates the frequency, rate or extent of any cellular process that depends upon or alters the microtubule cytoskeleton. [GOC:mah] |
| immature T cell proliferation in thymus | biological process | The expansion of an immature T cell population by cell division in the thymus. [GOC:add, ISBN:0781735149] |
| negative regulation of immature T cell proliferation in thymus | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of immature T cell proliferation in the thymus. [GOC:add, GOC:mah] |
| positive regulation of Rho protein signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of Rho protein signal transduction. [GOC:bf] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| ERBB2-ERBB3 signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to a ERBB3 receptor on the surface of a cell, followed by transmission of the signal by a heterodimeric complex of ERBB2 and ERBB3. ERBB2, which does not bind any known ligand, is activated through formation of a heterodimer with another ligand-activated ERBB family member such as ERBB3. ERBB3 also has impaired kinase activity and relies on ERBB2 for activation and signal transmission. [GOC:signaling, PMID:16460914, Reactome:R-HSA-1963589] |
| ERBB2-EGFR signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to an epidermal growth factor receptor (EGFR/ERBB1) on the surface of a cell, followed by transmission of the signal by a heterodimeric complex of ERBB2 and EGFR. ERBB2, which does not bind any known ligand, is activated through formation of a heterodimer with another ligand-activated ERBB family member such as EGFR. [GOC:signaling, PMID:16460914, Reactome:R-HSA-1963589] |
| ERBB2-ERBB4 signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to a ERBB4 receptor on the surface of a cell, followed by transmission of the signal by a heterodimeric complex of ERBB2 and ERBB4. ERBB2, which does not bind any known ligand, is activated through formation of a heterodimer with another ligand-activated ERBB family member such as ERBB4. [GOC:signaling, PMID:16460914, Reactome:R-HSA-1963589] |
| wound healing | biological process | The series of events that restore integrity to a damaged tissue, following an injury. [GOC:bf, PMID:15269788] |
| myelination | biological process | The process in which myelin sheaths are formed and maintained around neurons. Oligodendrocytes in the brain and spinal cord and Schwann cells in the peripheral nervous system wrap axons with compact layers of their plasma membrane. Adjacent myelin segments are separated by a non-myelinated stretch of axon called a node of Ranvier. [GOC:dgh, GOC:mah] |
| positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | An intracellular signaling cassette that starts with phosphatidylinositol 3-kinase (PI3K) activation, production of phosphatidylinositol 3-phosphate (PI3P), activation of PDK1, which recruits and ending with the activation of protein kinase B (PKB, also known as Akt). PI3K is activated by cell surface receptors. Note that PTEN is an inhibitor of the pathway. [PMID:20517722, PMID:22952397] |
| 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] |
| regulation of angiogenesis | biological process | Any process that modulates the frequency, rate or extent of angiogenesis. [GOC:go_curators] |
| positive regulation of cell adhesion | biological process | Any process that activates or increases the frequency, rate or extent of cell adhesion. [GOC:go_curators] |
| positive regulation of transcription by RNA polymerase I | biological process | Any process that activates or increases the frequency, rate or extent of transcription mediated by RNA polymerase I. [GOC:go_curators, GOC:txnOH] |
| 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 epithelial cell proliferation | biological process | Any process that activates or increases the rate or extent of epithelial cell proliferation. [GOC:ai] |
| regulation of ERK1 and ERK2 cascade | biological process | Any process that modulates the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:add, ISBN:0121245462, ISBN:0896039986] |
| cellular response to growth factor 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 a growth factor stimulus. [GOC:mah] |
| cellular response to epidermal growth factor 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 epidermal growth factor stimulus. [GOC:mah] |
| semaphorin-plexin signaling pathway | biological process | The series of molecular signals generated as a consequence of a semaphorin receptor (composed of a plexin and a neurophilin) binding to a semaphorin ligand. [GOC:BHF, GOC:mah, GOC:vk, PMID:15239959] |
| positive regulation of protein targeting to membrane | biological process | Any process that increases the frequency, rate or extent of the process of directing proteins towards a membrane, usually using signals contained within the protein. [GOC:tb] |
| neurotransmitter receptor localization to postsynaptic specialization membrane | biological process | A process in which a neurotransmitter is transported to, or maintained in, a location within the membrane adjacent to a postsynaptic specialization (e.g. postsynaptic density). [GOC:dos] |
| neurogenesis | biological process | Generation of cells within the nervous system. [GO_REF:0000021, GOC:cls, GOC:curators, GOC:dgh, GOC:dph, GOC:jid] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| 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] |
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |
| multicellular organism development | biological process | The biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| neuron differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a neuron. [GOC:mah] |