Article
Diptoindonesin G is a middle domain HSP90 modulator for cancer treatment.
The Journal of biological chemistry - 1 Dec 2022
Donahue Kristine, Xie Haibo, Li Miyang, Gao Ang, Ma Min, Wang Yidan, Tipton Rose, Semanik Nicole, Primeau Tina, Li Shunqiang, Li Lingjun, Tang Weiping, Xu Wei
Abstract excerpt
HSP90 inhibitors can target many oncoproteins simultaneously, but none have made it through clinical trials due to dose-limiting toxicity and induction of heat shock response, leading to clinical resistance. We identified diptoindonesin G (dip G) as an HSP90 modulator that can promote degradation of HSP90 clients by binding to the middle domain of HSP90 (Kd = 0.13 ± 0.02 μM) without inducing heat shock response....
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