Nitrogen-containing heteroaromatic-based inhibitors for cytochrome P450 (CYP) in various species contain a crucial coordination between the nitrogen atom and the heme iron. Previous studies suggested that 1,3-oxazole could bind heme-iron with a strength comparable to pyridine, highlighting its potential as a novel heme-iron binding moiety.
The difference between the origin of Alzheimer's disease (AD) and its symptoms is an obstacle to finding effective treatments. Scientists focused on amyloid-β (Aβ) plaques and tau aggregates to slow neurodegeneration and cognitive decline. Without identifying what causes AD, approved treatments do not provide much benefit. However, new findings suggest that restoring lithium levels in the brain could prevent and treat AD. Not just any lithium would work, just the forms that do not bind to Aβ.
Haisco Pharmaceutical Group Co. Ltd. has prepared and tested glucagon-like peptide 1 receptor (GLP-1R) agonists reported to be useful for the treatment of diabetes and obesity.
Researchers from McMaster University and Espervita Therapeutics Inc. have identified the enzyme ATP citrate lyase (ACLY) as a key metabolic regulator of tumor-immune interactions in hepatocellular carcinoma (HCC) driven by metabolic dysfunction-associated steatohepatitis (MASH).
Deep learning tools for protein design can also be used to create molecules that bind to them. Certain peptides, such as intrinsically disordered proteins (IDPs), are challenging to target due to their variable nature. However, scientists from the lab of Nobel laureate David Baker have developed a method to generate binders for IDPs by searching the world’s largest protein database with their AI-powered tool RFdiffusion.
Madrigal Pharmaceuticals Inc.’s long-awaited business development pact became reality by way of an exclusive global license agreement that could be worth more than $2 billion with CSPC Pharmaceutical Group Ltd., of Shijiazhuang, China, for SYH-2086. The candidate is a preclinical oral, small-molecule glucagon-like peptide-1 (GLP-1) receptor agonist and orforglipron derivative.
Researchers from the Cleveland Clinic and National Institutes of Health investigated the role of the neurobeachin (NBEA) gene in predicting weight loss response to glucagon-like peptide-1 receptor agonists.
Indiana University Research and Technology Corp. has divulged peptides acting as dual agonists of amylin receptor and calcitonin (CALCR; CT-R) receptor and its conjugates with incretin reported to be useful for the treatment of obesity.
Madrigal Pharmaceuticals Inc. and CSPC Pharmaceutical Group Ltd. have entered into an exclusive global license agreement for CSPC’s SYH-2086, a preclinical oral small-molecule glucagon-like peptide-1 (GLP-1) receptor agonist and orforglipron derivative. The agreement supports Madrigal’s pipeline strategy to develop combination treatments for metabolic dysfunction-associated steatohepatitis (MASH).