Immune checkpoint inhibitors (ICIs), such as anti-CTLA-4 antibodies, are widely used in cancer immunotherapy. CTLA-4 blockers such as Yervoy (ipilimumab, Bristol Myers Squibb Co.) stimulate antitumoral immune responses, but may also induce toxicity, such as colitis, a common immune-related adverse event that can lead to treatment discontinuation.
F. Hoffmann-La Roche Ltd. and Hoffmann-La Roche, Inc. have described fluorescent probes acting as monoglyceride lipase (MGLL; MAGL) inhibitors reported to be useful for diagnostic imaging of MAGL.
University of Ottawa has synthesized ferroptosis inhibitors reported to be useful for the treatment of cancer, diabetes, myocardial infarction, amyotrophic lateral sclerosis, sepsis, shock, transplant rejection and Alzheimer’s dementia.
Ensem Therapeutics Inc. has disclosed quinazoline derivatives acting as GTPase KRAS (G12D mutant) inhibitors reported to be useful for the treatment of cancer.
Synthesis and optimization of several series of G-protein coupled receptor 183 (GPR183) antagonists at Immunophage Biomedical Co. Ltd. led to the discovery of a lead candidate with promising potency (IC50=31.3 nM), reduced hERG inhibition and improved aqueous solubility.
Malaria cases increase at a slow but continued rate. There is a vital need for new antimalarial treatments able to overcome drug resistance for a more sustained control of the disease.
Syntheticgestalt Ltd. and Enamine Ltd. have begun a joint effort to create a suite of artificial intelligence (AI) models that will enable the generation of synthetically accessible biologically active compounds with optimized physicochemical and ADME/Tox properties.
Proabtech Co. Ltd. investigators have published findings from the preclinical characterization of PAT-101, a novel recombinant human albumin (rHA)-conjugated urate oxidase (Uox) variant, being developed for the treatment of gout.
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