HSP90


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HSP90

A generic term for a family of molecular chaperones which play a key role in protein folding and quality control for a range of client proteins. Functional HSP90s operate as dimers, have intrinsic ATPase activity, act in concert with other chaperones (e.g., HSP70) and are regulated by co-chaperones/accessory proteins (e.g., HOP, CDC37). HSP90s interact with more than 100 proteins, including kinases (e.g., Raf-1), nuclear hormone receptors (e.g., oestrogen receptor), transcription factors (e.g., P53), GPCRs (e.g., CB2 receptors) and ion channels (e.g. CFTR). In humans, the HSP90-beta isoform is constitutively expressed (i.e., at baseline), whereas HSP90-alpha isoforms are induced by stress. HSP90 plays an important role in some tumour cell types by stabilising mutated oncogenic proteins.
References in periodicals archive ?
Ganetespib has shown anti-tumor activity in heavily pretreated patients with lung cancer, breast cancer, and other tumor types and has been well tolerated with no evidence of severe liver or common ocular toxicities seen with other Hsp90 inhibitors.
Hannah, Clifford Hudis: HSP90 Inhibition is Effective in Breast Cancer: A Phase 2 Trial of Tanespimycin (17AAG) plus Trastuzumab in Patients with HER2-Positive Metastatic Breast Cancer Progressing on Trastuzumab.
The first generation of Hsp90 inhibitors were derived from the natural product geldanamycin, originally identified as an antibiotic.
In the clinic, some 2nd generation Hsp90 inhibitors have shown high rates of ocular toxicity.
However, the clinical efficacy of Hsp90 inhibitors has been disappointing.
Ganetespib is a potent inhibitor of heat shock protein 90 (Hsp90) that is structurally unrelated to first-generation, ansamycin-related Hsp90 inhibitors.
Infinity's presentation, entitled "Antitumor activity of a novel, water-soluble Hsp90 inhibitor IPI-504 in multiple myeloma" (Abstract #6160) discussed data from in vitro and in vivo studies of Infinity's lead investigational anticancer agent.
The Hsp90 chaperone plays a key role in regulating the stability of its client proteins.
We believe that potent inhibition of HSP90 by Debio 0932 with its promising safety profile and convenient oral dosing, in combination with everolimus has the potential to provide improved benefit for patients with kidney cancers," said Ali Fattaey, Ph.
When the stress-related protein FKBP51 partners with another protein known as Hsp90, this formidable chaperone protein complex prevents the clearance from the brain of the toxic tau protein associated with Alzheimer's disease.
The Company's portfolio consists of a series of Hsp90 inhibitors, a novel target therapy for oncology and neurodegenerative disorders, which has attracted an enormous amount of development interest in the past several years.