Researchers from Springworks Therapeutics Inc. and affiliated organizations presented the discovery and preclinical characterization of a novel covalent and irreversible YAP/TAZ-TEAD inhibitor, SWTX-143, being developed for the treatment of mesothelioma.
Researchers from Baylor University and collaborators have described the synthesis and evaluation of a series of 6-aryl-3-aroyl-indole analogues acting as tubulin polymerization inhibitors aimed to be used as anticancer agents. Inhibitors of tubulin polymerization are promising antiproliferative agents and their interaction with the colchicine site is linked to its activity as vascular disrupting agents (VDAs).
Researchers from Cybin Inc. presented preclinical data for the potent and selective long-acting serotonin 5-HT2A receptor agonist, CYB-210010, as potential therapeutic candidate for the treatment of neurological disorders.
Researchers from Johns Hopkins University and affiliated organizations have published details on the discovery and preclinical characterization of a purine antimetabolite, Pro-905, which is being developed for the treatment of malignant peripheral nerve sheath tumors (MPNST).
Researchers from Cogent Biosciences Inc. have reported the discovery and preclinical characterization of CGT-4255, a novel EGFR-sparing, ErbB2 inhibitor with activity against oncogenic ErbB2 mutations.
Phosphoinositide 3-kinase (PI3K) is a key cell cycle pathway regulator involved in tumor growth and development. PI3Kα mutations in p110α subunit, H1047R and E542K/E545K are found in patients with several cancer types, including breast cancer and are targeted by approved drugs such as Piqray (alpelisib, Novartis AG).
Researchers from Insilico Medicine Inc. reported on ISM-5043, a novel KAT6A inhibitor aimed to be used for the treatment of refractory ER+ breast cancer.
Researchers from Gilgamesh Pharmaceuticals Inc. and affiliated organizations have presented the discovery and preclinical evaluation of GM-3009, a novel noribogaine analogue being developed for the treatment of opioid use disorder (OUD).
Myeloproliferative neoplasms (MPNs) are a group of disorders of which the main hallmarks are bone marrow fibrosis and atypical megakaryocytes (MK) accumulation. Both Rho kinase (ROCK) and Aurora kinase (ARK) pathways are involved in correct MK maturation.
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