Glucagon-like peptide 1 (GLP-1) signaling to intraepithelial lymphocyte (IEL) cells in the gut, where most GLP-1 is made, was important for inflammation in the gut itself, but less so for systemic inflammation. Read More
Identification of selective, ligand-efficient ATP-competitive inhibitors of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) for the potential treatment of cancer was discussed by Bristol Myers Squibb Co. (BMS). Read More
Genentech Inc. presented data on structure-based lead optimization of orally bioavailable hematopoietic progenitor kinase 1 (HPK1) inhibitors. HPK1 is a negative regulator of T-cell receptor signaling in human T cells and target inhibition significantly increases cytokine production, such as IFN-gamma, TNF-alpha and IL-2, and T-cell proliferation, suggesting HPK1 inhibition as an intracellular T-cell target for cancer immunotherapy. Read More
Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd. has described pyrrolopyridazines acting as mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1) inhibitors reported to be useful for the treatment of cancer. Read More
Novartis AG and Les Laboratoires Servier SAS have identified proteolysis targeting chimeras (PROTACs) compounds comprising E3 ubiquitin ligase-binding moiety covalently bonded to Bcl-2-like protein 1 (BCL2L1)-targeting moiety through a linker reported to be useful for the treatment of cancer. Read More
Rappta Therapeutics Oy has divulged protein phosphatase 2A (PP2A) activators reported to be useful for the treatment of cancer, diabetes, neurodegeneration, heart failure, cardiac hypertrophy, autoimmune, chronic obstructive pulmonary and nonalcoholic fatty liver diseases among others. Read More
Shenzhen Targetrx Biotechnology has disclosed epidermal growth factor receptor (EGFR) mutant and/or HER2 mutant inhibitors reported to be useful for the treatment of cancer. Read More
Gilead Sciences Inc. has disclosed the discovery and structure of the potent, oral small molecule programmed cell death 1 ligand 1 (PD-L1) inhibitor GS-4224 (evixapodlin). Read More
Researchers from Baylor College of Medicine and Texas Children's Hospital detailed the discovery of CPK-03-37, a novel fluorescent organic molecule for tumor imaging. Read More
Target ALS Foundation Inc. and the Alzheimer's Drug Discovery Foundation LLC (ADDF) have announced the first four award recipients in a new initiative to identify and develop biomarkers for neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis (ALS) and frontotemporal degeneration (FTD). Read More
Researchers from Kira Pharmaceuticals LLC and University of Pennsylvania have developed a novel mouse model of rapidly progressing lethal C3 glomerulopathy (C3G), with the aim of assessing whether inhibition of proximal alternative pathway (AP) complement components such as factor D (FD) may be more efficacious than C5 inhibition for the treatment of C3G. Read More
