Target Information

Target General Infomation
Target ID
T66719
Former ID
TTDS00274
Target Name
Heat shock protein HSP90
Synonyms
HSP90; HSP90 molecular chaperone; Heat shock protein HSP 90; Heat-shock protein 90 molecularchaperone; Hsp90 chaperone
Target Type
Clinical Trial
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).
Target Validation
T66719
Drugs and Mode of Action
Drug(s) AUY922 Drug Info Phase 2 Myeloma [1]
BIIB-021 Drug Info Phase 2 Breast cancer [2]
Efungumab Drug Info Phase 2 Breast cancer [3]
KW-2478 Drug Info Phase 2 Cancer [4]
NVP-AUY922 Drug Info Phase 2 Cancer [5]
VER 50589 Drug Info Phase 2 Breast cancer [6]
BIIB 028 Drug Info Phase 1 Solid tumours [7]
Debio 0932 Drug Info Phase 1 Cancer [8]
PU3 Drug Info Phase 1 Cancer [9]
CCT-018159 Drug Info Preclinical Cancer [10]
KOS-2484 Drug Info Preclinical Cancer [11]
HBP-347 Drug Info Discontinued in Phase 3 Autoimmune diabetes [12]
Geldanamycin Drug Info Discontinued in Phase 2 Kidney cancer; Peripheral nerve damage [13]
IPI-493 Drug Info Discontinued in Phase 1 Gastric cancer [14]
Cromoglicate Drug Info Terminated Allergic rhinitis [15]
EC-154 Drug Info Terminated Cancer [16]
Inhibitor 17-allylamino-17-desmethoxy-geldanamycin Drug Info [17]
17-desmethoxy-17-aminogeldanamycin Drug Info [18]
AUY922 Drug Info [6]
BIIB 028 Drug Info [19]
BIIB-021 Drug Info [20]
CCT-018159 Drug Info [21]
Cromoglicate Drug Info [22]
Debio 0932 Drug Info [8]
Disodium cromoglycate Drug Info [22]
EC-154 Drug Info [23]
Geldanamycin Drug Info [24], [25], [26]
Geldanamycin-estradiol hybrid Drug Info [27]
GNF-PF-67 Drug Info [28]
IPI-493 Drug Info [29], [30]
KOS-2484 Drug Info [31]
KOSN1559 Drug Info [21]
Macbecin Drug Info [21]
NVP-AUY922 Drug Info [21]
PU24S Drug Info [21]
PU3 Drug Info [21]
Radicicol Drug Info [24], [25]
RHEIN Drug Info [28]
SNX-2112 Drug Info [18]
VER 50589 Drug Info [21]
VER-49009 Drug Info [32]
ZEARALANONE Drug Info [28]
Modulator HBP-347 Drug Info [33]
KW-2478 Drug Info [34]
References
REF 1ClinicalTrials.gov (NCT01854034) Phase 2 Study of AUY922 in NSCLC Patients With Exon 20 Insertion Mutations in EGFR. U.S. National Institutes of Health.
REF 2ClinicalTrials.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 3ClinicalTrials.gov (NCT00847678) Efficacy and Safety of Mycograb as Adjunctive Therapy for Cryptococcal Meningitis in Patients With AIDS. U.S. National Institutes of Health.
REF 4ClinicalTrials.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 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027019)
REF 6The HSP90 inhibitor NVP-AUY922 potently inhibits non-small cell lung cancer growth. Mol Cancer Ther. 2013 Jun;12(6):890-900.
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020039)
REF 8Clinical pipeline report, company report or official report of Debiopharm (2011).
REF 9Advances in the clinical development of heat shock protein 90 (Hsp90) inhibitors in cancers. Biochim Biophys Acta. 2012 Mar;1823(3):742-55.
REF 10Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018517)
REF 11Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019408)
REF 12Heat shock protein 90 (Hsp90). SciBX 4(18).
REF 13Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005345)
REF 14Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026781)
REF 15Sodium cromoglicate: an ineffective drug or meta-analysis misused? Pharm Stat. 2007 Apr-Jun;6(2):123-37.
REF 16Inhibition of heat shock protein 90 (Hsp90) modulates macrophage stimulating-1 receptor (MSR1) expression and signaling, and reduces pancreatic tumor growth. Cancer Res May 1, 2009 69; 2835.
REF 17Bioorg Med Chem. 2009 Mar 15;17(6):2225-35. Epub 2008 Nov 6.Discovery and development of heat shock protein 90 inhibitors.
REF 18J Med Chem. 2010 Jan 14;53(1):3-17.Heat shock protein 90: inhibitors in clinical trials.
REF 19Phase 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 20BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol Cancer Ther. 2009 Apr;8(4):921-9.
REF 21Recent advances in Hsp90 inhibitors as antitumor agents. Anticancer Agents Med Chem. 2008 Oct;8(7):761-82.
REF 22Hsp90 is a direct target of the anti-allergic drugs disodium cromoglycate and amlexanox. Biochem J. 2003 Sep 1;374(Pt 2):433-41.
REF 23WO patent application no. 2013,1734,36, Pre-selection of subjects for therapeutic treatment with an hsp90 inhibitor based on hypoxic status.
REF 24Endothelial nitric oxide synthase: the Cinderella of inflammation? Trends Pharmacol Sci. 2003 Feb;24(2):91-5.
REF 25High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity. Anal Biochem. 2004 Apr 15;327(2):176-83.
REF 26Heat shock protein 90 regulates the stability of MEKK3 in HEK293 cells. Cell Immunol. 2009 Jun 6.
REF 27Bioorg Med Chem Lett. 1999 May 3;9(9):1233-8.Synthesis and evaluation of geldanamycin-estradiol hybrids.
REF 28Bioorg 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 29Clinical pipeline report, company report or official report of AstraZeneca (2009).
REF 30National Cancer Institute. NCI Drug Dictionary. 2009 (CdrID=610131)
REF 31US patent application no. 2014,0079,636, Targeted therapeutics.
REF 32J 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 33US patent application no. 2013,0023,420, Susceptibility to hsp90-inhibitors.
REF 34Anti-tumor activity against multiple myeloma by combination of KW-2478, an Hsp90 inhibitor, with bortezomib. Blood Cancer J. 2012 Apr;2(4):e68.

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