Researchers from Arvinas Inc. and affiliated organizations presented the discovery and preclinical evaluation of ARV-766, a novel androgen receptor (AR) degrading proteolysis targeting chimera (PROTAC), being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC).
Tumor-associated calcium signal transducer 2 (TROP2), a clinically validated target in oncology, is a glycoprotein overexpressed in several solid tumors such as breast, lung, pancreatic, ovarian and prostate cancer. TROP2 antibody-drug conjugates (ADCs) have shown significant efficacy in a large number of cancer types but still are linked to substantial safety issues.
Researchers at 1200 Pharma LLC have undertaken preclinical analysis of KRAS G12C inhibitors in clinical phases with the aim of finding an explanation for the differences observed in therapeutic efficacy in tumor sites other than lung, including lung-derived metastases. Results pointed to potency and pharmacokinetics as key drivers of efficacy.
Carcinoembryonic antigen-related cell adhesion molecule 1 (CEACAM1) is an inhibitory factor on natural killer (NK) and T cells and is expressed in several cancer types and immune cells such as macrophages and neutrophils. Researchers from Suzhou Neologics Bioscience Co. Ltd. have investigated CEACAM1 as a potential target for cancer immunotherapy.
Researchers from Novartis AG recently reported on the preclinical activity of IAG-933, a first-in-class YAP1/TAZ pan-TEAD protein-protein interaction...
Researchers have identified a druggable pocket on the phosphatase Wip1, which regulates the tumor suppressor TP53 as well as DNA damage repair proteins. The work, which was published in Frontiers in Molecular Biosciences on April 18, 2023, by researchers from the University of Pennsylvania, could lead to therapeutics targeting Wip1. And the computational deep learning methods used to identify the pocket are broadly useful for identifying what the authors call “cryptic” pockets.
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