Table of Contents
What is Hsp90 inhibitor?
An Hsp90 inhibitor is a substance that inhibits that activity of the Hsp90 heat shock protein. Since Hsp90 stabilizes a variety of proteins required for survival of cancer cells, these substances may have therapeutic benefit in the treatment of various types of malignancies.
How do Hsp90 inhibitors work?
Hsp90 relies on its ability to bind and hydrolyze ATP in order to effectively regulate the maturation of its so-called ‘client’ proteins through a conformationally dynamic ATPase-driven cycle, controlled by an orchestrated set of interactions with a range of co-chaperones (9, 10).
At what temperature do heat shock proteins start to generate?
Hsps are rapidly synthesized in response to temperatures above 42°C and associate with proteins that have begun to unfold as a result of increased temperatures. Moreover, there is also evidence that Hsps can be induced by temperatures within the fever range (38–41°C) (Di et al., 1997; Ostberg et al., 2002).
Where is Hsp90 found?
Two forms, HSP90 alpha and HSP90 beta, are located in the cytoplasm, GRP94 (94-kDa glucose-regulated protein) exists in the ER, and TRAP-1 (tumor necrosis factor receptor-associated protein 1) is present in the mitochondria.
Do humans have Hsp70?
Hsp70-13 (HspA13, Stch) represents the microsome-associated member of the HSP70 family and is constitutively expressed in all human cell types (Otterson et al. 1994).
Who discovered Hsp70?
Ferruccio Ritossa
HSP70: History Heat shock proteins (HSPs) were originally described in the early 1960s by the pioneering work of Ferruccio Ritossa on the fruit fly Drosophila melanogaster 5,6,7.
Where is HSP90 found?
What does HSP90 stand for?
Heat shock protein 90 (Hsp90) is a molecular chaperone involved in the maturation of a plethora of substrates (“clients”), including protein kinases, transcription factors, and E3 ubiquitin ligases, positioning Hsp90 as a central regulator of cellular proteostasis.
Who discovered Hsp90?
HSP90: History In 1987, Bardwell and Craig isolated a gene from E. coli called htpG which is homologous to the gene encoding the Drosophila 83 kDa heat shock protein 2 14.