Researchers from Loxo Oncology at Eli Lilly and Co. recently reported the discovery and preclinical evaluation of a new highly potent and selective pan-KRAS inhibitor, LY-4066434, being developed for the treatment of cancer.
Researchers from Hefei Institutes of Physical Science Chinese Academy of Sciences and affiliated organizations have reported the discovery of IHMT-PI3K-455, a novel potent and selective PI3Kγ/δ dual inhibitor as a potential anticancer agent.
Antibody-drug conjugates (ADCs) are effective anti-cancer agents in a wide variety of solid and hematologic cancers. CD30 (TNFRSF8), a member of the TNF receptor superfamily is the target of antibody drug conjugate Adcetris (brentuximab vedotin/BV, Seagen Inc.) approved for use in multiple CD30-expressing lymphomas.
Researchers from Bridge Biotherapeutics Inc. have presented the discovery and preclinical characterization of BBT-4437, a novel brain-penetrable and reversible pan-transcriptional enhancer factor (TEAD) inhibitor, designed to target the Hippo signaling pathway in solid tumors.
KRAS is a GTP-binding protein involved in cell growth control that requires post-translational farnesylation to be active. KRAS G12D mutations are mostly associated with pancreatic, colorectal and non-small-cell lung cancers and occur less commonly in other cancers. There are currently no therapies approved to specifically target this mutation.
A team from Atrogi AB has reported the activity of ATR-127, a novel dual adrenergic agonist targeting β2- and β3-adrenoceptors (ARs), for the potential treatment of steatohepatitis, obesity and diabetes.
Researchers from Yuhan Corp. presented the discovery and preclinical evaluation of a novel long-acting dual agonist of the glucagon like peptide-1 (GLP-1) and growth differentiation factor 15 (GDF-15), YH-40863.
Researchers from East China Normal University and Shanghai Jiao Tong University presented the discovery and preclinical evaluation of new potent antiosteoporosis agents. Synthesis and optimization of a series of heterocyclic ring-fused derivatives of 20(S)-protopanaxadiol (PPD) led to the identification of SH-491 as the lead candidate with the most potent inhibitory effects on RANKL-induced osteoclastogenesis (IC50=11.8 nM).
Researchers from Assembly Biosciences Inc. recently presented details on the discovery and preclinical evaluation of a novel small-molecule hepatitis B virus (HBV) and hepatitis D virus (HDV) entry inhibitor, AB-1659.
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