Target Information
Target General Infomation | |||||
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Target ID |
T66719
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Former ID |
TTDS00274
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Target Name |
Heat shock protein HSP90
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Synonyms |
HSP90; HSP90 molecular chaperone; Heat shock protein HSP 90; Heat-shock protein 90 molecularchaperone; Hsp90 chaperone
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Target Type |
Clinical Trial
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Disease | Autoimmune diabetes [ICD10: E08-E13] | ||||
Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4] | |||||
Breast cancer [ICD9: 174, 175; ICD10: C50] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Gastric cancer [ICD9: 151; ICD10: C16] | |||||
Kidney cancer; Peripheral nerve damage [ICD9: 140-229, 356.0, 356.8; ICD10: G64, G90.0] | |||||
Myeloma [ICD9: 203; ICD10: C90] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Molecular chaperone. Has atpaseactivity (by similarity).
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Target Validation |
T66719
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Drugs and Mode of Action | |||||
Drug(s) | AUY922 | Drug Info | Phase 2 | Myeloma | [524290] |
BIIB-021 | Drug Info | Phase 2 | Breast cancer | [522229] | |
Efungumab | Drug Info | Phase 2 | Breast cancer | [522586] | |
KW-2478 | Drug Info | Phase 2 | Cancer | [522945] | |
NVP-AUY922 | Drug Info | Phase 2 | Cancer | [548611] | |
VER 50589 | Drug Info | Phase 2 | Breast cancer | [532267] | |
BIIB 028 | Drug Info | Phase 1 | Solid tumours | [547870] | |
Debio 0932 | Drug Info | Phase 1 | Cancer | [550597] | |
PU3 | Drug Info | Phase 1 | Cancer | [531690] | |
CCT-018159 | Drug Info | Preclinical | Cancer | [547699] | |
KOS-2484 | Drug Info | Preclinical | Cancer | [547800] | |
HBP-347 | Drug Info | Discontinued in Phase 3 | Autoimmune diabetes | [550048] | |
Geldanamycin | Drug Info | Discontinued in Phase 2 | Kidney cancer; Peripheral nerve damage | [545916] | |
IPI-493 | Drug Info | Discontinued in Phase 1 | Gastric cancer | [548581] | |
Cromoglicate | Drug Info | Terminated | Allergic rhinitis | [536429] | |
EC-154 | Drug Info | Terminated | Cancer | [549754] | |
Inhibitor | 17-allylamino-17-desmethoxy-geldanamycin | Drug Info | [529815] | ||
17-desmethoxy-17-aminogeldanamycin | Drug Info | [530621] | |||
AUY922 | Drug Info | [532267] | |||
BIIB 028 | Drug Info | [532433] | |||
BIIB-021 | Drug Info | [530083] | |||
CCT-018159 | Drug Info | [536886] | |||
Cromoglicate | Drug Info | [535743] | |||
Debio 0932 | Drug Info | [550597] | |||
Disodium cromoglycate | Drug Info | [535743] | |||
EC-154 | Drug Info | [550171] | |||
Geldanamycin | Drug Info | [535689], [535935], [537541] | |||
Geldanamycin-estradiol hybrid | Drug Info | [525501] | |||
GNF-PF-67 | Drug Info | [531262] | |||
IPI-493 | Drug Info | [550288], [550524] | |||
KOS-2484 | Drug Info | [550842] | |||
KOSN1559 | Drug Info | [536886] | |||
Macbecin | Drug Info | [536886] | |||
NVP-AUY922 | Drug Info | [536886] | |||
PU24S | Drug Info | [536886] | |||
PU3 | Drug Info | [536886] | |||
Radicicol | Drug Info | [535689], [535935] | |||
RHEIN | Drug Info | [531262] | |||
SNX-2112 | Drug Info | [530621] | |||
VER 50589 | Drug Info | [536886] | |||
VER-49009 | Drug Info | [527601] | |||
ZEARALANONE | Drug Info | [531262] | |||
Modulator | HBP-347 | Drug Info | [550909] | ||
KW-2478 | Drug Info | [531977] | |||
References | |||||
Ref 522229 | ClinicalTrials.gov (NCT00618319) An Open-Label, 18FDG-PET Pharmacodynamic Assessment of the Effect of BIIB021 in Subjects With Gastrointestinal Stromal Tumors (GIST). U.S. National Institutes of Health. | ||||
Ref 522586 | ClinicalTrials.gov (NCT00847678) Efficacy and Safety of Mycograb as Adjunctive Therapy for Cryptococcal Meningitis in Patients With AIDS. U.S. National Institutes of Health. | ||||
Ref 522945 | ClinicalTrials.gov (NCT01063907) A Study of KW-2478 in Combination With Bortezomib in Subjects With Relapsed and/or Refractory Multiple Myeloma. U.S. National Institutes of Health. | ||||
Ref 524290 | ClinicalTrials.gov (NCT01854034) Phase 2 Study of AUY922 in NSCLC Patients With Exon 20 Insertion Mutations in EGFR. U.S. National Institutes of Health. | ||||
Ref 531690 | Advances in the clinical development of heat shock protein 90 (Hsp90) inhibitors in cancers. Biochim Biophys Acta. 2012 Mar;1823(3):742-55. | ||||
Ref 532267 | The HSP90 inhibitor NVP-AUY922 potently inhibits non-small cell lung cancer growth. Mol Cancer Ther. 2013 Jun;12(6):890-900. | ||||
Ref 536429 | Sodium cromoglicate: an ineffective drug or meta-analysis misused? Pharm Stat. 2007 Apr-Jun;6(2):123-37. | ||||
Ref 545916 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005345) | ||||
Ref 547699 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018517) | ||||
Ref 547800 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019408) | ||||
Ref 547870 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020039) | ||||
Ref 548581 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026781) | ||||
Ref 548611 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027019) | ||||
Ref 525501 | Bioorg Med Chem Lett. 1999 May 3;9(9):1233-8.Synthesis and evaluation of geldanamycin-estradiol hybrids. | ||||
Ref 527601 | J Med Chem. 2005 Jun 30;48(13):4212-5.Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. | ||||
Ref 529815 | Bioorg Med Chem. 2009 Mar 15;17(6):2225-35. Epub 2008 Nov 6.Discovery and development of heat shock protein 90 inhibitors. | ||||
Ref 530083 | BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol Cancer Ther. 2009 Apr;8(4):921-9. | ||||
Ref 530401 | Efungumab: a novel agent in the treatment of invasive candidiasis. Ann Pharmacother. 2009 Nov;43(11):1818-23. | ||||
Ref 531262 | Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). | ||||
Ref 531977 | Anti-tumor activity against multiple myeloma by combination of KW-2478, an Hsp90 inhibitor, with bortezomib. Blood Cancer J. 2012 Apr;2(4):e68. | ||||
Ref 532267 | The HSP90 inhibitor NVP-AUY922 potently inhibits non-small cell lung cancer growth. Mol Cancer Ther. 2013 Jun;12(6):890-900. | ||||
Ref 532433 | Phase I study of BIIB028, a selective heat shock protein 90 inhibitor, in patients with refractory metastatic or locally advanced solid tumors. Clin Cancer Res. 2013 Sep 1;19(17):4824-31. | ||||
Ref 535689 | Endothelial nitric oxide synthase: the Cinderella of inflammation? Trends Pharmacol Sci. 2003 Feb;24(2):91-5. | ||||
Ref 535743 | Hsp90 is a direct target of the anti-allergic drugs disodium cromoglycate and amlexanox. Biochem J. 2003 Sep 1;374(Pt 2):433-41. | ||||
Ref 535935 | High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity. Anal Biochem. 2004 Apr 15;327(2):176-83. | ||||
Ref 536886 | Recent advances in Hsp90 inhibitors as antitumor agents. Anticancer Agents Med Chem. 2008 Oct;8(7):761-82. | ||||
Ref 537541 | Heat shock protein 90 regulates the stability of MEKK3 in HEK293 cells. Cell Immunol. 2009 Jun 6. |
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