Researchers from Neophore Ltd. presented the discovery and preclinical evaluation of NP-1867, a small molecule inhibitor of DNA mismatch repair (MMR) protein PMS2, being developed for the treatment of cancer.
Glutaminyl-peptide cyclotransferase-like protein (QPCTL) is a modulator of CD47-SIRPα binding and can be targeted to achieve antitumor responses through myeloid checkpoint blockade. At the recent ESMO meeting in Madrid, researchers from Insilico Medicine Inc. reported the preclinical characterization of ISM-8207, a QPCTL inhibitor with activity against triple-negative breast cancer (TNBC) and diffuse large B-cell lymphoma (DLBCL).
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.
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