NSC49652 is a orally active, potent and selective inhibitor of death receptor p75NTR (p75 neurotrophin receptor) that targets the interfaces between transmembrane domains (TMDs). NSC49652 induces profound conformational changes and triggers p75NTR dependent cancer cell death. It inhibits the growth of cancer in melanoma mouse model.
orally active, potent and selective inhibitor of death receptor p75NTR that targets the interfaces between transmembrane domains
Cell chemical biology, 25(12), 1485-1494 (2018-10-09)
Small molecules offer powerful ways to alter protein function. However, most proteins in the human proteome lack small-molecule probes, including the large class of non-catalytic transmembrane receptors, such as death receptors. We hypothesized that small molecules targeting the interfaces between
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