Obesity is a chronic disorder tied to other disorders such as hyperglycemia, type 2 diabetes or cardiovascular disease, among others. Recent findings have suggested that EphB tyrosine kinase receptor and its ligand, ephrin B, may be involved in insulin signaling.
M-9140 (Merck KGaA) is an antibody-drug conjugate (ADC) that carries a DNA topoisomerase 1 (TOP1) inhibitor payload plus an antibody directed against carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5). CEACAM5 is a cell surface protein that is overexpressed in colorectal cancer and other solid tumors.
Work at Escient Pharmaceuticals Inc. has led to the discovery of novel Mas-related G protein-coupled receptor member X4 (MRGPRX4) antagonists as potential therapeutic candidates for the treatment of cholestatic and uremic pruritus.
Windtree Therapeutics Inc. has entered into an asset purchase agreement with Varian Biopharmaceuticals Inc. to acquire certain Varian assets, including a proprietary atypical protein kinase C iota inhibitor (aPKCi).
Vernalis (R&D) Ltd., a subsidiary of Hitgen Inc., and C4x Discovery Holdings plc have entered into a collaboration to identify modulators of an undisclosed, hard-to-drug, high-value target involved in inflammatory disease.
ABM Therapeutics Inc. presented a novel small-molecule, ATP-uncompetitive, phosphorylated MEK (pMEK) inhibitor – ABM-4095 – that potently prevents phosphorylation of MEK by RAF with moderate inhibition of MEK kinase activity; it is being investigated for the potential treatment of pancreatic cancer.
Basilea Pharmaceutica Ltd. has been awarded a grant from CARB-X (Combating Antibiotic-Resistant Bacteria Biopharmaceutical Accelerator) to support initial preclinical activities on the antibiotics program recently acquired from Spexis.
At the AACR meeting, Innovent Biologics Inc. discussed the discovery and preclinical evaluation of a B7-H3/EGFR bispecific antibody-drug conjugate (bsADC).
The formation of neutrophil extracellular traps (NETs) is a common feature in the renal glomeruli of patients with antineutrophil cytoplasmic autoantibody (ANCA) vasculitis. The use of a DNA repair antibody, such as PAT-DX-1 from Patrys Ltd., could inhibit NET formation by interfering with DNA damage responses in the neutrophil, which lead to the release of DNA.
A small molecule could provide a new therapeutic approach against organ fibrosis. Using genome-wide association (GWA) assays, a group of researchers from the Westmead Institute for Medical Research in Sydney identified Mer tyrosine kinase (MERTK) as a candidate to study fibrosis and showed that its inhibition with the experimental compound reduced this condition in mouse models’ liver, kidneys and lungs. “There were some studies on the role of MERTK in liver fibrosis, but its therapeutic potential for various organ fibrosis has not been explored before. This study provides unequivocal evidence that MERTK is a potent nodal regulator of fibrosis supported by detailed mechanistic studies,” the senior author Mohammed Eslam told BioWorld.
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