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.
Psoriasis is an autoimmune disorder characterized by abnormal differentiation of keratinocytes and chronic inflammation where current treatments frequently are associated with severe side effects.
Previous research has shown high expression of angiotensin-converting enzyme 1 (ACE1) in the triple-negative breast cancer (TNBC) cell line MDA-MB-231, suggesting the potential of ACE1 as a novel target for this disease. In the current study, researchers from Peking University Cancer Hospital presented the discovery of [68Ga]DOTA-BPP, a novel peptide nuclide molecular imaging probe targeting ACE1 for the imaging of TNBC.
Researchers from Technische Universität München and Universitätsklinikum Augsburg recently presented the discovery of novel radiohybrid-based minigastrin analogues.
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