Synonyms: compound 38 [PMID: 36533617] | RMC5552
Compound class:
Synthetic organic
Comment: RMC-5552 is a selective bi-steric inhibitor of mTORC1 [1]. Mechanistically it interacts with both the orthosteric and allosteric binding sites of mTOR, and inhibits phosphorylation of S6K and 4EBP1 (to provide anti-tumour activity) whilst sparing mTORC2-mediated effects on AKT signalling and glucose metabolism. It was developed for potential to treat mTORC1-activated tumours, and is an active clinical lead (Jan 2023).
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References |
1. Burnett GL, Yang YC, Aggen JB, Pitzen J, Gliedt MK, Semko CM, Marquez A, Evans JW, Wang G, Won WS et al.. (2023)
Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors. J Med Chem, 66 (1): 149-169. [PMID:36533617] |