Proteins > Heat shock protein HSP 90-beta
Page last updated: 2024-08-07 15:46:09
Heat shock protein HSP 90-beta
A heat shock protein HSP 90-beta that is encoded in the genome of human. [PRO:DAN]
Synonyms
HSP 90;
Heat shock 84 kDa;
HSP 84;
HSP84
Research
Bioassay Publications (75)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (1.33) | 18.2507 |
| 2000's | 25 (33.33) | 29.6817 |
| 2010's | 34 (45.33) | 24.3611 |
| 2020's | 15 (20.00) | 2.80 |
Compounds (43)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| adenosine diphosphate | Homo sapiens (human) | EC50 | 87.0000 | 1 | 1 |
| ethamivan | Homo sapiens (human) | Kd | 790.0000 | 1 | 1 |
| silybin | Homo sapiens (human) | Kd | 500.0000 | 1 | 1 |
| 5-benzyloxytryptophan | Homo sapiens (human) | Kd | 28.0000 | 1 | 1 |
| 8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-pent-4-yn-1-yl-9H-purin-6-amine | Homo sapiens (human) | EC50 | 1.7000 | 2 | 2 |
| 1,3,6-trimethylpyrimido[5,4-e][1,2,4]triazine-5,7-dione | Homo sapiens (human) | EC50 | 0.9460 | 1 | 1 |
| 1,3,6-trimethylpyrimido[5,4-e][1,2,4]triazine-5,7-dione | Homo sapiens (human) | Kd | 0.4285 | 2 | 2 |
| 1,6-dimethyl-3-propylpyrimido[5,4-e][1,2,4]triazine-5,7-dione | Homo sapiens (human) | EC50 | 0.9170 | 1 | 1 |
| 1,6-dimethyl-3-propylpyrimido[5,4-e][1,2,4]triazine-5,7-dione | Homo sapiens (human) | Kd | 0.3080 | 2 | 2 |
| geldanamycin | Homo sapiens (human) | EC50 | 0.0350 | 1 | 1 |
| geldanamycin | Homo sapiens (human) | Kd | 0.7300 | 6 | 6 |
| 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin | Homo sapiens (human) | EC50 | 0.0237 | 6 | 6 |
| 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin | Homo sapiens (human) | Kd | 0.5000 | 1 | 1 |
| monorden | Homo sapiens (human) | EC50 | 0.0250 | 1 | 1 |
| monorden | Homo sapiens (human) | Kd | 0.0106 | 2 | 2 |
| tanespimycin | Homo sapiens (human) | EC50 | 0.1811 | 8 | 8 |
| tanespimycin | Homo sapiens (human) | Kd | 0.6118 | 4 | 4 |
| 9h-purine-9-propanamine, 6-amino-8-((6-iodo-1,3-benzodioxol-5-yl)thio)-n-(1-methylethyl)- | Homo sapiens (human) | EC50 | 0.0231 | 4 | 4 |
| gambogic acid | Homo sapiens (human) | Kd | 8.1333 | 3 | 3 |
| ipi 493 | Homo sapiens (human) | EC50 | 0.0236 | 5 | 5 |
| ipi 493 | Homo sapiens (human) | Kd | 0.1000 | 1 | 1 |
| cnf 2024 | Homo sapiens (human) | EC50 | 0.0300 | 1 | 1 |
| cnf 2024 | Homo sapiens (human) | Kd | 0.0017 | 1 | 1 |
| snx 2112 | Homo sapiens (human) | Kd | 0.0007 | 1 | 1 |
| novobiocin | Homo sapiens (human) | EC50 | 700.0000 | 1 | 1 |
| novobiocin | Homo sapiens (human) | Kd | 500.0000 | 1 | 1 |
| ver 52296 | Homo sapiens (human) | Kd | 0.0017 | 1 | 1 |
| sta 9090 | Homo sapiens (human) | Kd | 23.5650 | 1 | 1 |
| nms-e973 | Homo sapiens (human) | Kd | 0.0003 | 1 | 1 |
Drugs with Other Measurements
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
Heat shock protein 70 inhibitors. 1. 2,5'-thiodipyrimidine and 5-(phenylthio)pyrimidine acrylamides as irreversible binders to an allosteric site on heat shock protein 70.Journal of medicinal chemistry, , Feb-27, Volume: 57, Issue:4, 2014
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
Orally active purine-based inhibitors of the heat shock protein 90.Journal of medicinal chemistry, , Jan-26, Volume: 49, Issue:2, 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
Discovery and development of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 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
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
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
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
Inhibition of Plasmodium falciparum Hsp90 Contributes to the Antimalarial Activities of Aminoalcohol-carbazoles.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 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
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
A small molecule that preferentially binds the closed conformation of Hsp90.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Heat shock protein 90: inhibitors in clinical trials.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Potent cytotoxic C-11 modified geldanamycin analogues.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
Discovery and development of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Synthesis of Hsp90 dimerization modulators.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 16, Issue:13, 2006
Inhibition of protein-protein association by small molecules: approaches and progress.Journal of medicinal chemistry, , Apr-11, Volume: 45, Issue:8, 2002
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
Synthesis and evaluation of a novel class Hsp90 inhibitors containing 1-phenylpiperazine scaffold.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 24, Issue:6, 2014
Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.European journal of medicinal chemistry, , May-22, Volume: 79, 2014
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
Discovery and development of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Potent cytotoxic C-11 modified geldanamycin analogues.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 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
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
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
Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells.Journal of natural products, , Mar-28, Volume: 77, Issue:3, 2014
Dimeric and trimeric triazole based molecules as a new class of Hsp90 molecular chaperone inhibitors.European journal of medicinal chemistry, , Volume: 65, 2013
Discovery and development of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
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
Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach.Journal of medicinal chemistry, , 02-25, Volume: 64, Issue:4, 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
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
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
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
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
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
Tricyclic series of heat shock protein 90 (Hsp90) inhibitors part I: discovery of tricyclic imidazo[4,5-c]pyridines as potent inhibitors of the Hsp90 molecular chaperone.Journal of medicinal chemistry, , Oct-27, Volume: 54, Issue:20, 2011
Heat shock protein 90: inhibitors in clinical trials.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 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
Discovery and development of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Potent cytotoxic C-11 modified geldanamycin analogues.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 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
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
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
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
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 and development of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
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
Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Heat shock protein 90: inhibitors in clinical trials.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Potent cytotoxic C-11 modified geldanamycin analogues.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
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
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
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
Identification and optimization of novel Hsp90 inhibitors with tetrahydropyrido[4,3-d]pyrimidines core through shape-based screening.European journal of medicinal chemistry, , May-22, Volume: 79, 2014
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
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
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
ATPases as drug targets: insights from heat shock proteins 70 and 90.Journal of medicinal chemistry, , Oct-28, Volume: 53, Issue:20, 2010
Heat shock protein 90: inhibitors in clinical trials.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Discovery and development of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
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
The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
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
Heat shock protein 90: inhibitors in clinical trials.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
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
Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Synthesis and Evaluation of Noviose Replacements on Novobiocin that Manifest Anti-proliferative Activity.ACS medicinal chemistry letters, , Jul-13, Volume: 1, Issue:7, 2010
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
[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
Discovery and development of heat shock protein 90 inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 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
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
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 novel HSP90α/β isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 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
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
Novel 3,4-isoxazolediamides as potent inhibitors of chaperone heat shock protein 90.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
ATPases as drug targets: insights from heat shock proteins 70 and 90.Journal of medicinal chemistry, , Oct-28, Volume: 53, Issue:20, 2010
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
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
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
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 |
|---|
| RNA binding | molecular function | Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah] |
| double-stranded RNA binding | molecular function | Binding to double-stranded RNA. [GOC:jl] |
| 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] |
| 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] |
| protein kinase regulator activity | molecular function | Modulates the activity of a protein kinase, an enzyme which phosphorylates a protein. [GOC:ai] |
| kinase binding | molecular function | Binding to a kinase, any enzyme that catalyzes the transfer of a phosphate group. [GOC:jl] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [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] |
| heat shock protein binding | molecular function | Binding to a heat shock protein, a protein synthesized or activated in response to heat shock. [GOC:mah, GOC:vw] |
| ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
| peptide binding | molecular function | Binding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl] |
| 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] |
| ATP-dependent protein binding | molecular function | Binding to a protein or protein complex using energy from ATP hydrolysis. [GOC:jl] |
| protein folding chaperone | molecular function | Binding to a protein or a protein-containing complex to assist the protein folding process. [GOC:mtg_cambridge_2009] |
| cadherin binding | molecular function | Binding to cadherin, a type I membrane protein involved in cell adhesion. [GOC:bf] |
| protein dimerization activity | molecular function | The formation of a protein dimer, a macromolecular structure consists of two noncovalently associated identical or nonidentical subunits. [ISBN:0198506732] |
| 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] |
| DNA polymerase binding | molecular function | Binding to a DNA polymerase. [GOC:BHF, GOC:mah] |
| 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] |
| receptor ligand inhibitor activity | molecular function | Binds to and decreases the activity of the ligand of a signaling receptor. [PMID:12478285, PMID:1721860] |
| histone methyltransferase binding | molecular function | Binding to a histone methyltransferase enzyme. [GOC:ame, GOC:BHF, PMID:19486527] |
| unfolded protein binding | molecular function | Binding to an unfolded protein. [GOC:ai] |
Located In
This protein is located in 17 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] |
| 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] |
| 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] |
| 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] |
| 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] |
| dynein axonemal particle | cellular component | An aggregation of axonemal dyneins, their specific assembly factors, and broadly-acting chaperones that is located in the cytoplasm. [GOC:krc, PMID:30561330, PMID:32898505, PMID:33263282] |
| 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 3 target(s):
| Target | Category | Definition |
|---|
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
| 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] |
| 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] |
Part Of
This protein is part of 5 target(s):
| Target | Category | Definition |
|---|
| COP9 signalosome | cellular component | A protein complex that catalyzes the deneddylation of proteins, including the cullin component of SCF ubiquitin E3 ligase; deneddylation increases the activity of cullin family ubiquitin ligases. The signalosome is involved in many regulatory process, including some which control development, in many species; also regulates photomorphogenesis in plants; in many species its subunits are highly similar to those of the proteasome. [PMID:11019806, PMID:12186635, PMID:14570571] |
| protein folding chaperone complex | cellular component | A protein complex required for the non-covalent folding or unfolding, maturation, stabilization or assembly or disassembly of macromolecular structures. Usually active during or immediately after completion of translation. Many chaperone complexes contain heat shock proteins. [GOC:bhm, PMID:21855797] |
| 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] |
| aryl hydrocarbon receptor complex | cellular component | A protein complex that acts as an aryl hydrocarbon (Ah) receptor. Cytosolic and nuclear Ah receptor complexes have different subunit composition, but both contain the ligand-binding subunit AhR. [GOC:mah, PMID:7598497] |
| HSP90-CDC37 chaperone complex | cellular component | A protein kinase chaperone complex required for the proper folding, maturation and stabilization of target proteins (mostly signaling protein kinases, some steroid hormone receptors), usually during or immediately after completion of translation. The highly conserved, phosphorylated CDC37-Ser13 (vertebrates) or cdc37-Ser14 (yeast) is essential for complex assembly and target protein binding. CDC37-Ser13 (Ser14) is phosphorylated by Casein kinase II (CK2), which in turn is a target of CDC37 creating a positive feedback loop. Complex binding also prevents rapid ubiquitin-dependent proteosomal degradation of target proteins. [GOC:bhm, GOC:pad, GOC:PARL, PMID:21855797, PMID:22939624] |
Involved In
This protein is involved in 22 target(s):
| Target | Category | Definition |
|---|
| placenta development | biological process | The process whose specific outcome is the progression of the placenta over time, from its formation to the mature structure. The placenta is an organ of metabolic interchange between fetus and mother, partly of embryonic origin and partly of maternal origin. [GOC:add, ISBN:068340007X] |
| 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] |
| virion attachment to host cell | biological process | The process by which a virion protein binds to molecules on the host cellular surface or host cell surface projection. [GOC:bf, GOC:jl, UniProtKB-KW:KW-1161, VZ:956] |
| positive regulation of transforming growth factor beta receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of TGF-beta receptor signaling pathway activity. [GOC:go_curators] |
| 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] |
| negative regulation of proteasomal ubiquitin-dependent protein catabolic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the breakdown of a protein or peptide by hydrolysis of its peptide bonds, initiated by the covalent attachment of ubiquitin, and mediated by the proteasome. [GOC:mah] |
| positive regulation of phosphoprotein phosphatase activity | biological process | Any process that activates or increases the activity of a phosphoprotein phosphatase. [GOC:mah] |
| 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] |
| 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 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 cell differentiation | biological process | Any process that activates or increases the frequency, rate or extent of cell differentiation. [GOC:go_curators] |
| 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] |
| regulation of cell cycle | biological process | Any process that modulates the rate or extent of progression through the cell cycle. [GOC:ai, GOC:dph, GOC:tb] |
| chaperone-mediated protein folding | biological process | The process of inhibiting aggregation and assisting in the covalent and noncovalent assembly of single chain polypeptides or multisubunit complexes into the correct tertiary structure that is dependent on interaction with a chaperone. [GOC:dph, GOC:vw] |
| cellular response to interleukin-4 | 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 interleukin-4 stimulus. [GOC:mah] |
| supramolecular fiber organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a supramolecular fiber, a polymer consisting of an indefinite number of protein or protein complex subunits that have polymerised to form a fiber-shaped structure. [GOC:pr] |
| negative regulation of proteasomal protein catabolic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of proteasomal protein catabolic process. [GOC:BHF, GOC:rl, GOC:TermGenie, PMID:21669198] |
| 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] |
| positive regulation of protein localization to cell surface | biological process | Any process that activates or increases the frequency, rate or extent of protein localization to the cell surface. [GOC:obol] |
| 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] |
| 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] |