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 [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 522229ClinicalTrials.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 522586ClinicalTrials.gov (NCT00847678) Efficacy and Safety of Mycograb as Adjunctive Therapy for Cryptococcal Meningitis in Patients With AIDS. U.S. National Institutes of Health.
Ref 522945ClinicalTrials.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 524290ClinicalTrials.gov (NCT01854034) Phase 2 Study of AUY922 in NSCLC Patients With Exon 20 Insertion Mutations in EGFR. U.S. National Institutes of Health.
Ref 531690Advances in the clinical development of heat shock protein 90 (Hsp90) inhibitors in cancers. Biochim Biophys Acta. 2012 Mar;1823(3):742-55.
Ref 532267The HSP90 inhibitor NVP-AUY922 potently inhibits non-small cell lung cancer growth. Mol Cancer Ther. 2013 Jun;12(6):890-900.
Ref 536429Sodium cromoglicate: an ineffective drug or meta-analysis misused? Pharm Stat. 2007 Apr-Jun;6(2):123-37.
Ref 545916Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005345)
Ref 547699Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018517)
Ref 547800Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019408)
Ref 547870Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020039)
Ref 548581Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026781)
Ref 548611Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027019)
Ref 549754Inhibition 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 550048Heat shock protein 90 (Hsp90). SciBX 4(18).
Ref 550597Clinical pipeline report, company report or official report of Debiopharm (2011).
Ref 525501Bioorg Med Chem Lett. 1999 May 3;9(9):1233-8.Synthesis and evaluation of geldanamycin-estradiol hybrids.
Ref 527601J 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 529815Bioorg Med Chem. 2009 Mar 15;17(6):2225-35. Epub 2008 Nov 6.Discovery and development of heat shock protein 90 inhibitors.
Ref 530083BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol Cancer Ther. 2009 Apr;8(4):921-9.
Ref 530401Efungumab: a novel agent in the treatment of invasive candidiasis. Ann Pharmacother. 2009 Nov;43(11):1818-23.
Ref 530621J Med Chem. 2010 Jan 14;53(1):3-17.Heat shock protein 90: inhibitors in clinical trials.
Ref 531262Bioorg 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 531977Anti-tumor activity against multiple myeloma by combination of KW-2478, an Hsp90 inhibitor, with bortezomib. Blood Cancer J. 2012 Apr;2(4):e68.
Ref 532267The HSP90 inhibitor NVP-AUY922 potently inhibits non-small cell lung cancer growth. Mol Cancer Ther. 2013 Jun;12(6):890-900.
Ref 532433Phase 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 535689Endothelial nitric oxide synthase: the Cinderella of inflammation? Trends Pharmacol Sci. 2003 Feb;24(2):91-5.
Ref 535743Hsp90 is a direct target of the anti-allergic drugs disodium cromoglycate and amlexanox. Biochem J. 2003 Sep 1;374(Pt 2):433-41.
Ref 535935High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity. Anal Biochem. 2004 Apr 15;327(2):176-83.
Ref 536886Recent advances in Hsp90 inhibitors as antitumor agents. Anticancer Agents Med Chem. 2008 Oct;8(7):761-82.
Ref 537541Heat shock protein 90 regulates the stability of MEKK3 in HEK293 cells. Cell Immunol. 2009 Jun 6.
Ref 550171WO patent application no. 2013,1734,36, Pre-selection of subjects for therapeutic treatment with an hsp90 inhibitor based on hypoxic status.
Ref 550288Clinical pipeline report, company report or official report of AstraZeneca (2009).
Ref 550524National Cancer Institute. NCI Drug Dictionary. 2009 (CdrID=610131)
Ref 550597Clinical pipeline report, company report or official report of Debiopharm (2011).
Ref 550842US patent application no. 2014,0079,636, Targeted therapeutics.
Ref 550909US patent application no. 2013,0023,420, Susceptibility to hsp90-inhibitors.

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