The synthesis of RP-1664, a highly potent, selective and bioavailable PLK4 inhibitor for the potential treatment of cancer, was recently reported by Repare Therapeutics Inc.
Prelude Therapeutics Inc. described the discovery of PRT-3789, a first-in-human, highly potent and selective SMARCA2-targeted protein degrader, for the potential treatment of cancer.
Fibroblast activation protein (FAP) is a serine protease, the expression of which increases with pathogenic fibroblasts in the fibrotic liver during metabolic dysfunction-associated steatohepatitis (MASH) and might induce fibrosis by cleaving several proteins that regulate extracellular matrix turnover and metabolism, including α2-antiplasmin (α2-AP) and fibroblast growth factor 21 (FGF21). Astrazeneca plc recently presented new results on their research regarding their oral small-molecule FAP inhibitor, AZD-2389, as a candidate drug for treating MASH.
At last week’s American Chemical Society Spring meeting, Bristol Myers Squibb Co. discussed the development of a potent, orally bioavailable and highly selective cereblon (CRBN)-mediated ligand-directed degrader (LDD) of B-cell lymphoma 6 protein (BCL6), BMS-986458, for the treatment of B-cell non-Hodgkin lymphoma.
At this week’s American Chemical Society Spring meeting, Galderma SA reported the discovery of novel, oral and selective macrocyclic inhibitors of protein kinase C θ (PKCθ) for the potential treatment of atopic dermatitis (AD) and psoriasis.
