A Pelemed Co. Ltd. patent details new indirubin derivatives acting as inhibitors of FLT3 (FLK2/STK1) and/or proto-oncogene tyrosine-protein kinase receptor Ret (RET; CDHF12; PTC) and its mutants. They are reported to be useful for the treatment of acute myeloid leukemia.
Research at Pharos Ibio Co. Ltd. has led to the identification of son of sevenless homolog 1 (SOS1) inhibitors reported to be useful for the treatment of cancer.
Gilead Sciences Inc. and Novartis AG have jointly reported pyrazolopyridinone compounds potentially useful for the treatment of herpes virus infections.
Aurigene Oncology Ltd. has reported the discovery of proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase binding agent coupled to probable global transcription activator SNF2L2 (SMARCA2; BAF190B; SNF2-α) and/or transcription activator BRG1 (SMARCA4; BAF190A; SNF2-β) targeting moiety via linker. They act as SMARCA2 and/or SMARCA4 degradation inducers and are reported to be useful for the treatment of cancer.
Synthesis and optimization of a series of 1H-pyrazolo[4,3d]pyrimidine molecules at Bristol Myers Squibb Co. led to the identification of compound [I] as the lead Toll-like receptor 7 (TLR7) agonist, with EC50 values of 21 and 94 nM for human and mouse TLR7, respectively.
Interleukin-17A (IL-17A) is a pro-inflammatory cytokine involved in the pathogenesis of inflammatory, immune-mediated diseases such as psoriasis, psoriatic arthritis and others.
Apolipoprotein C3 (APOC3) is one of the main regulators of triglyceride metabolism. Hypertriglyceridemia (HTG) is a major risk factor for cardiovascular disease and there is evidence that loss-of-function mutations in APOC3 correlate with decreased plasma triglyceride levels and subsequent reduced cardiometabolic dysfunction.
Longaevus Technologies Ltd. has announced the spin-off of Elastin Biosciences following breakthrough preclinical results of three of its assets. Elastin Biosciences has successfully conducted experiments and identified three novel drug combinations that inhibit elastin degradation and foster its deposition, leading to an increase in elastin expression by 5-fold, and improving aortic elasticity in aged mice in vivo.
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