The simultaneous mapping of DNA mutations and epigenetic changes as colorectal cancer evolves has for the first time tracked their relative contributions and shown epigenetic control of gene transcription is far more important than somatic mutations in enabling tumors to adapt and develop a survival advantage over other cells. In an analysis of 1,373 samples from 30 colorectal cancer samples, epigenetic changes were highly common in cells that had become cancerous and occurred around known cancer driver mutations. These epigenetic alterations were heritable, were passed on at each cell division, and in addition to a direct contribution to the evolution of tumors also influenced how cancer cells accumulated DNA mutations. The modifications to gene regulation conferred survival advantages that meant cancer cells grew faster than normal counterparts. While it is not news that epigenetic changes are involved in tumor development, previously it was not clear what the relative contribution was, and that their effect could be independent of DNA mutations. Read More
Targeting TEAD with small-molecule inhibitors is an emerging therapeutic strategy for YAP/TAZ-dependent human cancers with Hippo pathway alterations. Bridgene Biosciences Inc. identified three hits with the Isobaric Mass Tagged Affinity Characterization (IMTAC) screening platform that covalently bound to TEAD1 with the binding site being cysteine 359, which led to the BGI-9004 compound. Read More
Researchers from Bayer AG presented the discovery of BAY-2927088, a new noncovalent tyrosine kinase inhibitor targeting EGFR exon 20 insertions and C797S resistance mutations in non-small-cell lung cancer (NSCLC). Read More
Researchers from Bridgebio Pharma Inc. presented preclinical characterization of the novel next-generation KRAS G12C GTP/GDP dual inhibitor candidate, BBO-8520, being developed for the treatment of cancer. Read More
Recent findings have unveiled some integrins are associated with Mendelian conditions. In a recent study, researchers directed efforts toward studying integrin-beta 8 (ITGB8) and its association with pathology, especially with neurological pathology, as none of them have been linked to neuropathology to date. Read More
Jacobio Pharmaceuticals Co. Ltd. has patented cellular tumor antigen p53 (TP53) (Tyr220Cys mutant) stabilizers reported to be useful for the treatment of cancer. Read More
Medipure Holdings Inc. has described cannabidiol (CBD) prodrugs reported to be useful for the treatment of pain, epilepsy, cancer, inflammation, psychosis and neurological, eye and immunological disorders. Read More
Dystroglycanopathies are a subset of rare congenital muscular dystrophies (CMDs) caused by dysregulation in the assemblage of glycans on the α-dystroglycan (α-DG) transmembrane glycoprotein. Read More
Hangzhou Innogate Pharma Co. Ltd. has synthesized GTPase KRAS (Gly12Asp mutant) inhibitors reported to be useful for the treatment of cancer. Read More
Leitat Technological Center has patented sigma non-opioid intracellular receptor 1 (SIGMAR1) and/or sigma intracellular receptor 2 (TMEM97) ligands reported to be useful for the treatment of pain and neurological disorders. Read More
Protein glypican 6 (GPC6) belongs to the proteoglycan family, which is linked to glycosylphosphatidylinositol (GPI)-anchored heparan sulfate. Read More
Cosmas Therapeutics Development Inc. has discovered prodrugs of UCM-924 acting as melatonin MT2 receptor agonists reported to be useful for the treatment of pain, depression, diabetes, sleep and anxiety disorders. Read More
