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Mechanism: Lirafugratinib (RLY-4008) is a highly selective, IRREVERSIBLE (covalent) small-molecule inhibitor of fibroblast growth factor receptor 2 (FGFR2). A methacrylamide (2-methylprop-2-enamide) Michael-acceptor warhead covalently engages Cys491 at the tip of the FGFR2 phosphate-binding (P)-loop (homologous Cys488 in FGFR1). Selectivity…
Read article →Mechanism: A degrader-antibody conjugate is an ADC whose payload is not a cytotoxin but a heterobifunctional protein degrader — a PROTAC or a molecular glue. The antibody supplies antigen-restricted delivery and IgG-like pharmacokinetics; the payload supplies a catalytic, sub-stoichiometric…
Read article →The switch that runs your day Deep in the hypothalamus, a small population of neurons produces two neuropeptides — orexin-A and orexin-B (also called hypocretin-1 and -2). They are the master “stay awake” signal, acting on two G-protein-coupled receptors, OX1R and OX2R. Of…
Read article →In the last five years, targeted protein degradation has gone from an academic curiosity to an industry-wide drug discovery priority. Roughly thirty PROTACs are in human clinical trials as of early 2026. Several are deep into Phase 2…
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