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. Read More
Synonymous or silent mutations do not change the sequence of the protein that they encode. With some exceptions, they do not trigger any effect. Last year, however, a study by researchers from the University of Michigan tried to refute this concept after finding that they altered the protein function. But breaking dogmas can have answers. A group of scientists from various institutions has found that this work could have a method error. Read More
Researchers from Novartis AG recently reported on the preclinical activity of IAG-933, a first-in-class YAP1/TAZ pan-TEAD protein-protein interaction... Read More
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. Read More
A recent Hanmi Holdings Co. Ltd. patent describes 1-phosphatidylinositol 3-phosphate 5-kinase (PIKfyve) inhibitors reported to be useful for the treatment of amyotrophic lateral sclerosis, rheumatoid arthritis and Crohn’s disease. Read More
Research at Nextgen Bioscience Co. Ltd. has led to the identification of ectonucleotide pyrophosphatase/phosphodiesterase family member 2 (ENPP2; autotaxin) inhibitors. Read More
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. Read More
Janssen R&D (Ireland) has described respiratory syncytial virus (RSV) inhibiting spiro-bearing derivatives reported to be potentially useful for the treatment of RSV infections. Read More
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. Read More
Researchers at Repare Therapeutics Inc. have prepared and tested N-(5-substituted-[(1,3,4-thiadiazolyl) or (thiazolyl)]) (substituted) carboxamide compounds acting as DNA polymerase θ (POLQ) inhibitors and thus reported to be useful or the treatment of cancer. Read More
