Researchers from the University of Zaragoza and Promontory Therapeutics Inc. have discovered that PT-112, which has a multimodal mechanism of action, could have different clinical applications in cancer treatment due to its effects on mitochondria in castration-resistant prostate cancer (CRPC). PT-112 is an immunogenic small molecule currently in phase II development in metastatic castration-resistant prostate cancer (mCRPC). The researchers designed PT-112 to target advanced solid tumors, such as thymus, small-cell, non-small-cell lung or CRPC.
Diwali, the Festival of Light, marks different events depending on where it is celebrated. In some areas of India, it marks the return of Lord Rama to his birthplace of Ayodhya after defeating the demon Ravana.
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.
Jacobio Pharmaceuticals Co. Ltd. has patented cellular tumor antigen p53 (TP53) (Tyr220Cys mutant) stabilizers reported to be useful for the treatment of cancer.
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.
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).
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.
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.
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