Proteins > Heat shock protein HSP 90-alpha
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Heat shock protein HSP 90-alpha
A heat shock protein HSP 90-alpha that is encoded in the genome of human. [PRO:DAN]
Synonyms
EC 3.6.4.10;
Heat shock 86 kDa;
HSP 86;
HSP86;
Lipopolysaccharide-associated protein 2;
LAP-2;
LPS-associated protein 2;
Renal carcinoma antigen NY-REN-38
Research
Bioassay Publications (105)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (1.90) | 18.2507 |
| 2000's | 25 (23.81) | 29.6817 |
| 2010's | 52 (49.52) | 24.3611 |
| 2020's | 26 (24.76) | 2.80 |
Compounds (60)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| n(6),n(6)-dimethyladenine | Homo sapiens (human) | IC50 | 1,500.0000 | 1 | 1 |
| ns 1619 | Homo sapiens (human) | IC50 | 42.1600 | 2 | 2 |
| vorinostat | Homo sapiens (human) | IC50 | 167.3333 | 3 | 3 |
| adenosine diphosphate | Homo sapiens (human) | IC50 | 59.3080 | 1 | 1 |
| 2-chloroadenosine | Homo sapiens (human) | IC50 | 1,250.0000 | 1 | 1 |
| 2-chloroadenosine | Homo sapiens (human) | Ki | 2.2000 | 1 | 1 |
| 9-fluorenone | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| adenosine | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| 2-acetylamino-3-chloro-1,4-naphthoquinone | Homo sapiens (human) | IC50 | 6.6000 | 1 | 1 |
| adenosine-5'-carboxylic acid | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| adenosine 5'-carboxamide | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| isopentaquine | Homo sapiens (human) | IC50 | 14.4000 | 1 | 1 |
| 5'-n-methylcarboxamideadenosine | Homo sapiens (human) | Ki | 1.7000 | 1 | 1 |
| n-methyladenosine | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| deguelin | Homo sapiens (human) | IC50 | 1.6300 | 1 | 1 |
| adenosine 5'-phosphoramidate | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| adenosine-5'-(n-ethylcarboxamide) | Homo sapiens (human) | Ki | 2.7000 | 1 | 1 |
| 8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-pent-4-yn-1-yl-9H-purin-6-amine | Homo sapiens (human) | IC50 | 9.5286 | 7 | 7 |
| cct018159 | Homo sapiens (human) | IC50 | 1.7520 | 4 | 4 |
| adenosine-5'-(N-propyl)carboxamide | Homo sapiens (human) | Ki | 1.8000 | 1 | 1 |
| ver-49009 | Homo sapiens (human) | IC50 | 0.2372 | 4 | 4 |
| geldanamycin | Homo sapiens (human) | IC50 | 0.0917 | 20 | 20 |
| 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin | Homo sapiens (human) | IC50 | 0.1699 | 7 | 7 |
| 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin | Homo sapiens (human) | Ki | 0.6800 | 1 | 1 |
| derrubone | Homo sapiens (human) | IC50 | 14.0000 | 1 | 1 |
| monorden | Homo sapiens (human) | IC50 | 0.2092 | 5 | 5 |
| monorden | Homo sapiens (human) | Ki | 20.0000 | 1 | 1 |
| tanespimycin | Homo sapiens (human) | GI50 | 0.0320 | 1 | 1 |
| tanespimycin | Homo sapiens (human) | IC50 | 12.2263 | 30 | 30 |
| tanespimycin | Homo sapiens (human) | Ki | 0.0168 | 2 | 2 |
| 1-aminoadenosine | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| 9h-purine-9-propanamine, 6-amino-8-((6-iodo-1,3-benzodioxol-5-yl)thio)-n-(1-methylethyl)- | Homo sapiens (human) | IC50 | 0.0660 | 8 | 8 |
| reblastatin | Homo sapiens (human) | IC50 | 0.0050 | 1 | 1 |
| 5'-amino-5'-deoxyadenosine | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| gambogic acid | Homo sapiens (human) | IC50 | 21.9800 | 1 | 1 |
| n-cyclopropyl adenosine-5'-carboxamide | Homo sapiens (human) | Ki | 3.0000 | 1 | 1 |
| ec 144 | Homo sapiens (human) | IC50 | 0.0011 | 1 | 1 |
| ec 144 | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| snx-7081 | Homo sapiens (human) | IC50 | 1.7592 | 4 | 4 |
| at 13387 | Homo sapiens (human) | IC50 | 0.0437 | 5 | 5 |
| cnf 2024 | Homo sapiens (human) | IC50 | 20.2621 | 8 | 8 |
| cnf 2024 | Homo sapiens (human) | Ki | 0.0018 | 4 | 4 |
| snx 2112 | Homo sapiens (human) | IC50 | 28.6796 | 8 | 9 |
| snx 2112 | Homo sapiens (human) | Ki | 0.0040 | 1 | 1 |
| debio 0932 | Homo sapiens (human) | IC50 | 0.0330 | 1 | 1 |
| pf 04929113 | Homo sapiens (human) | IC50 | 0.0380 | 1 | 1 |
| tas-116 | Homo sapiens (human) | IC50 | 0.0690 | 1 | 1 |
| tas-116 | Homo sapiens (human) | Ki | 0.0347 | 2 | 2 |
| 2-(3,4-dimethoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2h-chromen-6-yl)ethanone | Homo sapiens (human) | IC50 | 0.0900 | 1 | 1 |
| ver-246608 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ver-246608 | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| ver-50589 | Homo sapiens (human) | IC50 | 0.0280 | 1 | 1 |
| ver 52296 | Homo sapiens (human) | IC50 | 2.9214 | 15 | 15 |
| ver 52296 | Homo sapiens (human) | Ki | 0.0055 | 2 | 2 |
| sta 9090 | Homo sapiens (human) | IC50 | 1.3771 | 4 | 4 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.1100 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| adenosine diphosphate | Homo sapiens (human) | Activity | 46.0000 | 2 | 2 |
| geldanamycin | Homo sapiens (human) | Concentration | 5.0000 | 1 | 1 |
| ver-246608 | Homo sapiens (human) | Activity | 80.0000 | 1 | 1 |
| nms-e973 | Homo sapiens (human) | DC50 | 0.0100 | 2 | 2 |
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.European journal of medicinal chemistry, , Mar-15, Volume: 190, 2020
N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Synthesis of a red-shifted fluorescence polarization probe for Hsp90.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Biological Evaluation of 5'-(ACS medicinal chemistry letters, , Mar-11, Volume: 12, Issue:3, 2021
Rational Design of Selective Adenine-Based Scaffolds for Inactivation of Bacterial Histidine Kinases.Journal of medicinal chemistry, , 10-12, Volume: 60, Issue:19, 2017
Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Synthesis of a red-shifted fluorescence polarization probe for Hsp90.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.Journal of medicinal chemistry, , Apr-21, Volume: 48, Issue:8, 2005
Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
4-Amino derivatives of the Hsp90 inhibitor CCT018159.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
[no title available],
Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 30, Issue:11, 2020
Why Some Targets Benefit from beyond Rule of Five Drugs.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90).Bioorganic & medicinal chemistry letters, , 05-01, Volume: 28, Issue:8, 2018
Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
Targeting the entry region of Hsp90's ATP binding pocket with a novel 6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl amide.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
C15-methoxyphenylated 18-deoxy-herbimycin A analogues, their in vitro anticancer activity and heat shock protein 90 binding affinity.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 26, Issue:17, 2016
Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Identification of a new series of potent diphenol HSP90 inhibitors by fragment merging and structure-based optimization.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 24, Issue:11, 2014
Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 21, Issue:15, 2011
Discovery of a macrocyclic o-aminobenzamide Hsp90 inhibitor with heterocyclic tether that shows extended biomarker activity and in vivo efficacy in a mouse xenograft model.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Design and SAR of macrocyclic Hsp90 inhibitors with increased metabolic stability and potent cell-proliferation activity.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90.Journal of medicinal chemistry, , Feb-14, Volume: 51, Issue:3, 2008
Synthesis of Hsp90 dimerization modulators.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
Crystal structures of human HSP90alpha-complexed with dihydroxyphenylpyrazoles.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 15, Issue:5, 2005
Inhibition of protein-protein association by small molecules: approaches and progress.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin.Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
Synthesis and evaluation of geldanamycin-estradiol hybrids.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
Structure-activity relationship of Garcinia xanthones analogues: Potent Hsp90 inhibitors with cytotoxicity and antiangiogenesis activity.Bioorganic & medicinal chemistry, , 10-01, Volume: 24, Issue:19, 2016
Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-diflJournal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 18, Issue:23, 2008
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Structure-based design of 7-carbamate analogs of geldanamycin.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
[no title available]Journal of natural products, , 03-26, Volume: 84, Issue:3, 2021
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Fusicoccane Diterpenes from Hypoestes forsskaolii as Heat Shock Protein 90 (Hsp90) Modulators.Journal of natural products, , 03-22, Volume: 82, Issue:3, 2019
Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase.Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.The Journal of biological chemistry, , Feb-14, Volume: 289, Issue:7, 2014
A chemical-biological study reveals C9-type iridoids as novel heat shock protein 90 (Hsp90) inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors.Journal of medicinal chemistry, , Aug-24, Volume: 49, Issue:17, 2006
Structure-based discovery of a new class of Hsp90 inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Structural basis for inhibition of the Hsp90 molecular chaperone by the antitumor antibiotics radicicol and geldanamycin.Journal of medicinal chemistry, , Jan-28, Volume: 42, Issue:2, 1999
2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach.Journal of medicinal chemistry, , 02-25, Volume: 64, Issue:4, 2021
N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression.European journal of medicinal chemistry, , Jan-01, Volume: 185, 2020
Quinazoline Based HSP90 Inhibitors: Synthesis, Modeling Study and ADME Calculations Towards Breast Cancer Targeting.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 30, Issue:15, 2020
Fusicoccane Diterpenes from Hypoestes forsskaolii as Heat Shock Protein 90 (Hsp90) Modulators.Journal of natural products, , 03-22, Volume: 82, Issue:3, 2019
Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 27, Issue:2, 2017
Design and synthesis of neolamellarin a derivatives targeting heat shock protein 90.European journal of medicinal chemistry, , Jul-28, Volume: 135, 2017
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 25, Issue:6, 2015
Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Differences in conformational dynamics between Plasmodium falciparum and human Hsp90 orthologues enable the structure-based discovery of pathogen-selective inhibitors.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Bioactive limonoids from the leaves of Azaridachta indica (Neem).Journal of natural products, , Mar-28, Volume: 77, Issue:3, 2014
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Synthesis and biological activities of a new class of heat shock protein 90 inhibitors, designed by energy-based pharmacophore virtual screening.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
A chemical-biological study reveals C9-type iridoids as novel heat shock protein 90 (Hsp90) inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
EC144 is a potent inhibitor of the heat shock protein 90.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Lead identification of β-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
Lead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 21, Issue:19, 2011
Heat shock protein 90: inhibitors in clinical trials.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
Synthesis of pochoxime prodrugs as potent HSP90 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 19, Issue:14, 2009
Potent non-benzoquinone ansamycin heat shock protein 90 inhibitors from genetic engineering of Streptomyces hygroscopicus.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Synthesis of a red-shifted fluorescence polarization probe for Hsp90.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
4-Amino derivatives of the Hsp90 inhibitor CCT018159.Bioorganic & medicinal chemistry letters, , May-01, Volume: 16, Issue:9, 2006
Synthesis of Hsp90 dimerization modulators.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Structure-based discovery of a new class of Hsp90 inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.Bioorganic & medicinal chemistry letters, , Jan-19, Volume: 14, Issue:2, 2004
Synthesis of novel fluorescent probes for the molecular chaperone Hsp90.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.Bioorganic & medicinal chemistry letters, , Apr-09, Volume: 11, Issue:7, 2001
Design and Synthesis of TRAP1 Selective Inhibitors: H-Bonding with Asn171 Residue in TRAP1 Increases Paralog Selectivity.ACS medicinal chemistry letters, , Jul-08, Volume: 12, Issue:7, 2021
Discovery of 2-((4-resorcinolyl)-5-aryl-1,2,3-triazol-1-yl)acetates as potent Hsp90 inhibitors with selectivity over TRAP1.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 27, Issue:2, 2017
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94.Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling.Bioorganic & medicinal chemistry, , Jul-15, Volume: 16, Issue:14, 2008
Synthesis of a red-shifted fluorescence polarization probe for Hsp90.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 16, Issue:17, 2006
[no title available],
Structure-activity relationship of Garcinia xanthones analogues: Potent Hsp90 inhibitors with cytotoxicity and antiangiogenesis activity.Bioorganic & medicinal chemistry, , 10-01, Volume: 24, Issue:19, 2016
Gambogic acid, a natural product inhibitor of Hsp90.Journal of natural products, , May-27, Volume: 74, Issue:5, 2011
Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Structure-based design of 7-carbamate analogs of geldanamycin.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer.Journal of medicinal chemistry, , 02-13, Volume: 63, Issue:3, 2020
Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.Journal of medicinal chemistry, , 11-08, Volume: 61, Issue:21, 2018
Design, synthesis and pharmacological evaluation of ALK and Hsp90 dual inhibitors bearing resorcinol and 2,4-diaminopyrimidine motifs.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Novel Tetrahydropyrido[4,3-d]pyrimidines as Potent Inhibitors of Chaperone Heat Shock Protein 90.Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.European journal of medicinal chemistry, , Mar-15, Volume: 190, 2020
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
Fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides as antitumor agents against CRC and NSCLC cancer cells.European journal of medicinal chemistry, , Oct-01, Volume: 203, 2020
1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Synthesis and in vitro antiproliferative activity of C5-benzyl substituted 2-amino-pyrrolo[2,3-d]pyrimidines as potent Hsp90 inhibitors.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 27, Issue:2, 2017
Paralog Specificity Determines Subcellular Distribution, Action Mechanism, and Anticancer Activity of TRAP1 Inhibitors.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
EC144 is a potent inhibitor of the heat shock protein 90.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Heat shock protein 90: inhibitors in clinical trials.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.Journal of medicinal chemistry, , 11-08, Volume: 61, Issue:21, 2018
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).Bioorganic & medicinal chemistry, , Nov-15, Volume: 21, Issue:22, 2013
EC144 is a potent inhibitor of the heat shock protein 90.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
Using NMR to identify binding regions for N and C-terminal Hsp90 inhibitors using Hsp90 domains.RSC medicinal chemistry, , Mar-01, Volume: 12, Issue:3, 2021
From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition.ACS medicinal chemistry letters, , Aug-13, Volume: 11, Issue:8, 2020
Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors.Journal of medicinal chemistry, , 03-11, Volume: 64, Issue:5, 2021
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Discovery of 3-Ethyl-4-(3-isopropyl-4-(4-(1-methyl-1 H-pyrazol-4-yl)-1 H-imidazol-1-yl)-1 H-pyrazolo[3,4- b]pyridin-1-yl)benzamide (TAS-116) as a Potent, Selective, and Orally Available HSP90 Inhibitor.Journal of medicinal chemistry, , 01-24, Volume: 62, Issue:2, 2019
[no title available]Journal of medicinal chemistry, , 09-26, Volume: 62, Issue:18, 2019
Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase.Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
Fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides as antitumor agents against CRC and NSCLC cancer cells.European journal of medicinal chemistry, , Oct-01, Volume: 203, 2020
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of novel heat shock protein (Hsp90) inhibitors based on luminespib with potent antitumor activity.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 30, Issue:12, 2020
Design, synthesis and pharmacological evaluation of ALK and Hsp90 dual inhibitors bearing resorcinol and 2,4-diaminopyrimidine motifs.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Design, synthesis and pharmacological evaluation of 4,5-diarylisoxazols bearing amino acid residues within the 3-amido motif as potent heat shock protein 90 (Hsp90) inhibitors.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Synthesis and biological evaluation of 3,5-disubstituted-4-alkynylisoxozales as a novel class of HSP90 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 25, Issue:16, 2015
Identification of a new series of potent diphenol HSP90 inhibitors by fragment merging and structure-based optimization.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 24, Issue:11, 2014
Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
4,5,6,7-Tetrahydro-isoxazolo-[4,5-c]-pyridines as a new class of cytotoxic Hsp90 inhibitors.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Discovery of potent N-(isoxazol-5-yl)amides as HSP90 inhibitors.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Synthesis and evaluation of new Hsp90 inhibitors based on a 1,4,5-trisubstituted 1,2,3-triazole scaffold.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
EC144 is a potent inhibitor of the heat shock protein 90.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Heat shock protein 90: inhibitors in clinical trials.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
[no title available],
Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC) dual inhibitors for the treatment of azoles-resistant Candida albicans.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities.Bioorganic & medicinal chemistry, , 05-01, Volume: 28, Issue:9, 2020
Discovery of 2-((4-resorcinolyl)-5-aryl-1,2,3-triazol-1-yl)acetates as potent Hsp90 inhibitors with selectivity over TRAP1.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
Experimental and structural testing module to analyze paralogue-specificity and affinity in the Hsp90 inhibitors series.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
[no title available],
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 NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).Bioorganic & medicinal chemistry, , Nov-15, Volume: 21, Issue:22, 2013
Enables
This protein enables 28 target(s):
| Target | Category | Definition |
|---|
| UTP binding | molecular function | Binding to UTP, uridine 5'-triphosphate. [GOC:hjd, ISBN:0198506732] |
| CTP binding | molecular function | Binding to CTP, cytidine 5'-triphosphate. [GOC:hjd, ISBN:0124020607] |
| RNA binding | molecular function | Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah] |
| mRNA binding | molecular function | Binding to messenger RNA (mRNA), an intermediate molecule between DNA and protein. mRNA includes UTR and coding sequences, but does not contain introns. [GOC:kmv, GOC:pr, SO:0000234] |
| 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] |
| GTP binding | molecular function | Binding to GTP, guanosine triphosphate. [GOC:ai] |
| ATP hydrolysis activity | molecular function | Catalysis of the reaction: ATP + H2O = ADP + H+ phosphate. ATP hydrolysis is used in some reactions as an energy source, for example to catalyze a reaction or drive transport against a concentration gradient. [RHEA:13065] |
| sulfonylurea receptor binding | molecular function | Binding to a sulfonylurea receptor, a regulatory subunit of the ATP-sensitive potassium ion channel. [GOC:ceb, PMID:11938023] |
| protein phosphatase binding | molecular function | Binding to a protein phosphatase. [GOC:jl] |
| MHC class II protein complex binding | molecular function | Binding to a class II major histocompatibility complex. [GOC:mtg_signal, GOC:vw] |
| nitric-oxide synthase regulator activity | molecular function | Binds to and modulates the activity of nitric oxide synthase. [GOC:mah] |
| TPR domain binding | molecular function | Binding to a tetratricopeptide repeat (TPR) domain of a protein, the consensus sequence of which is defined by a pattern of small and large hydrophobic amino acids and a structure composed of helices. [GOC:mah] |
| ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
| dATP binding | molecular function | Binding to dATP, deoxyadenosine triphosphate. [GOC:mah] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| histone deacetylase binding | molecular function | Binding to histone deacetylase. [GOC:jl] |
| transmembrane transporter binding | molecular function | Binding to a transmembrane transporter, a protein or protein complex that enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:BHF, GOC:jl, PMID:33199372] |
| tau protein binding | molecular function | Binding to tau protein. tau is a microtubule-associated protein, implicated in Alzheimer's disease, Down Syndrome and ALS. [GOC:jid] |
| GTPase binding | molecular function | Binding to a GTPase, any enzyme that catalyzes the hydrolysis of GTP. [GOC:ai] |
| Rho GDP-dissociation inhibitor binding | molecular function | Binding to a Rho GDP-dissociation inhibitor protein. [GOC:ai] |
| DNA polymerase binding | molecular function | Binding to a DNA polymerase. [GOC:BHF, GOC:mah] |
| scaffold protein binding | molecular function | Binding to a scaffold protein. Scaffold proteins are crucial regulators of many key signaling pathways. Although not strictly defined in function, they are known to interact and/or bind with multiple members of a signaling pathway, tethering them into complexes. [GOC:BHF, GOC:sjp, PMID:10433269, Wikipedia:Scaffold_protein] |
| disordered domain specific binding | molecular function | Binding to a disordered domain of a protein. [GOC:gg, PMID:11746698] |
| ATP-dependent protein folding chaperone | molecular function | Binding to a protein or a protein-containing complex to assist the protein folding process, driven by ATP hydrolysis. [PMID:27365453] |
| protein tyrosine kinase binding | molecular function | Binding to protein tyrosine kinase. [PMID:25499537] |
| unfolded protein binding | molecular function | Binding to an unfolded protein. [GOC:ai] |
Located In
This protein is located in 25 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| 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] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
| 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] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| 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] |
| brush border membrane | cellular component | The portion of the plasma membrane surrounding the brush border. [GOC:mah] |
| secretory granule lumen | cellular component | The volume enclosed by the membrane of a secretory granule. [GOC:rph] |
| melanosome | cellular component | A tissue-specific, membrane-bounded cytoplasmic organelle within which melanin pigments are synthesized and stored. Melanosomes are synthesized in melanocyte cells. [GOC:jl, PMID:11584301] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| lysosomal lumen | cellular component | The volume enclosed within the lysosomal membrane. [GOC:jl, PMID:15213228] |
| dendritic growth cone | cellular component | The migrating motile tip of a growing nerve cell dendrite. [GOC:jl] |
| axonal growth cone | cellular component | The migrating motile tip of a growing nerve cell axon. [GOC:jl, NIF_Subcellular:sao203987954] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| collagen-containing extracellular matrix | cellular component | An extracellular matrix consisting mainly of proteins (especially collagen) and glycosaminoglycans (mostly as proteoglycans) that provides not only essential physical scaffolding for the cellular constituents but can also initiate crucial biochemical and biomechanical cues required for tissue morphogenesis, differentiation and homeostasis. The components are secreted by cells in the vicinity and form a sheet underlying or overlying cells such as endothelial and epithelial cells. [GOC:BHF, GOC:rph, PMID:21123617] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
| endocytic vesicle lumen | cellular component | The volume enclosed by the membrane of an endocytic vesicle. [GOC:pde] |
| sperm mitochondrial sheath | cellular component | The tightly packed helical sheath of ATP-producing mitochondria restricted to the midpiece of the sperm flagellum. [GOC:cjm, MP:0009832, PMID:32791035] |
| sperm plasma membrane | cellular component | A plasma membrane that is part of a sperm cell. [GOC:cjm] |
| ficolin-1-rich granule lumen | cellular component | Any membrane-enclosed lumen that is part of a ficolin-1-rich granule. [GO_REF:0000064, GOC:TermGenie, PMID:23650620] |
Active In
This protein is active in 6 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] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| 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] |
| 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] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
Involved In
This protein is involved in 39 target(s):
| Target | Category | Definition |
|---|
| neuron migration | biological process | The characteristic movement of an immature neuron from germinal zones to specific positions where they will reside as they mature. [CL:0000540, GOC:go_curators] |
| 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] |
| activation of innate immune response | biological process | Any process that initiates an innate immune response. Innate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. Examples of this process include activation of the hypersensitive response of Arabidopsis thaliana and activation of any NOD or TLR signaling pathway in vertebrate species. [GO_REF:0000022, GOC:add, GOC:mtg_sensu, ISBN:0781735149, PMID:15199967, PMID:16177805] |
| positive regulation of defense response to virus by host | biological process | Any host process that results in the promotion of antiviral immune response mechanisms, thereby limiting viral replication. [GOC:add, GOC:dph, GOC:tb, ISBN:0781735149] |
| skeletal muscle contraction | biological process | A process in which force is generated within skeletal muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. In the skeletal muscle, the muscle contraction takes advantage of an ordered sarcomeric structure and in most cases it is under voluntary control. [GOC:mtg_cardio, GOC:mtg_muscle] |
| mitochondrial transport | biological process | Transport of substances into, out of or within a mitochondrion. [GOC:ai] |
| response to unfolded protein | 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 unfolded protein stimulus. [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] |
| response to cold | 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 cold stimulus, a temperature stimulus below the optimal temperature for that organism. [GOC:lr] |
| response to xenobiotic stimulus | 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 from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| response to salt stress | 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 indicating an increase or decrease in the concentration of salt (particularly but not exclusively sodium and chloride ions) in the environment. [GOC:jl] |
| 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] |
| cardiac muscle cell apoptotic process | biological process | A form of programmed cell death induced by external or internal signals that trigger the activity of proteolytic caspases, whose actions dismantle a cardiac muscle cell and result in its death. Cardiac muscle cells are striated muscle cells that are responsible for heart contraction. [CL:0000746, GOC:dph, GOC:mtg_apoptosis, GOC:tb] |
| regulation of protein ubiquitination | biological process | Any process that modulates the frequency, rate or extent of the addition of ubiquitin groups to a protein. [GOC:mah] |
| positive regulation of protein polymerization | biological process | Any process that activates or increases the frequency, rate or extent of the process of creating protein polymers. [GOC:mah] |
| positive regulation of interferon-beta production | biological process | Any process that activates or increases the frequency, rate, or extent of interferon-beta production. [GOC:mah, PMID:15546383] |
| regulation of protein localization | biological process | Any process that modulates the frequency, rate or extent of any process in which a protein is transported to, or maintained in, a specific location. [GOC:dph, GOC:mah, GOC:tb] |
| protein refolding | biological process | The process carried out by a cell that restores the biological activity of an unfolded or misfolded protein, using helper proteins such as chaperones. [GOC:mb] |
| response to cocaine | 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 cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
| positive regulation of protein import into nucleus | biological process | Any process that activates or increases the frequency, rate or extent of movement of proteins from the cytoplasm into the nucleus. [GOC:jl] |
| regulation of apoptotic process | biological process | Any process that modulates the occurrence or rate of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| regulation of protein-containing complex assembly | biological process | Any process that modulates the frequency, rate or extent of protein complex assembly. [GOC:jl] |
| protein unfolding | biological process | The process of assisting in the disassembly of non-covalent linkages in a protein or protein aggregate, often where the proteins are in a non-functional or denatured state. [GOC:mlg] |
| response to estrogen | 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 stimulus by an estrogen, C18 steroid hormones that can stimulate the development of female sexual characteristics. [GOC:jl, ISBN:0198506732] |
| protein insertion into mitochondrial outer membrane | biological process | The process comprising the insertion of proteins from outside the organelle into the mitochondrial outer membrane, mediated by large outer membrane translocase complexes. [GOC:mcc, GOC:vw, PMID:18672008] |
| positive regulation of nitric oxide 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 nitric oxide. [GOC:go_curators] |
| positive regulation of protein catabolic process | biological process | Any process that activates or increases the frequency, rate or extent of 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:go_curators] |
| positive regulation of cell size | biological process | Any process that increases cell size. [GOC:go_curators] |
| response to antibiotic | 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 antibiotic stimulus. An antibiotic is a chemical substance produced by a microorganism which has the capacity to inhibit the growth of or to kill other microorganisms. [GOC:ai, GOC:ef] |
| protein stabilization | biological process | Any process involved in maintaining the structure and integrity of a protein and preventing it from degradation or aggregation. [GOC:ai] |
| chaperone-mediated protein complex assembly | biological process | The aggregation, arrangement and bonding together of a set of components to form a protein complex, mediated by chaperone molecules that do not form part of the finished complex. [GOC:ai] |
| positive regulation of cardiac muscle contraction | biological process | Any process that increases the frequency, rate or extent of cardiac muscle contraction. [GOC:dph, GOC:tb] |
| chaperone-mediated autophagy | biological process | The autophagy process which begins when chaperones and co-chaperones recognize a target motif and unfold the substrate protein. The proteins are then transported to the lysosome where they are degraded. [GOC:pad, GOC:PARL, PMID:22743996, PMID:23434281] |
| cellular response to virus | 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 from a virus. [GOC:dos] |
| regulation of postsynaptic membrane neurotransmitter receptor levels | biological process | Any process that regulates the the local concentration of neurotransmitter receptor at the postsynaptic membrane. [GOC:dos] |
| positive regulation of tau-protein kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of tau-protein kinase activity. [GO_REF:0000059, GOC:sjp, GOC:TermGenie, PMID:15897157, PMID:22986780] |
| telomerase holoenzyme complex assembly | biological process | The aggregation, arrangement and bonding together of a set of components to form a telomerase holoenzyme complex. [GO_REF:0000079, GOC:TermGenie, PMID:26305931] |
| cellular response to heat | 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 heat stimulus, a temperature stimulus above the optimal temperature for that organism. [GOC:mah] |
| protein folding | biological process | The process of assisting in the covalent and noncovalent assembly of single chain polypeptides or multisubunit complexes into the correct tertiary structure. [GOC:go_curators, GOC:rb] |