The membrane-associated tyrosine/threonine protein kinase 1 (PKMYT1) regulates cell cycle progression and maintains genomic integrity. If it is dysregulated, cells may enter mitosis prematurely, potentially initiating tumorigenesis.
Investigators at The Scripps Research Institute and Rensselaer Polytechnic Institute have designed novel covalent inhibitors of SARS-CoV-2 papain-like protease (PLpro) and assessed their drug properties in preclinical models.
Combating Antibiotic-Resistant Bacteria Biopharmaceutical Accelerator (CARB-X) will award a seed grant of $610,000 to Justus Liebig University Giessen (JLU) to support the definition of a lead optimization path for the development of a direct-acting peptide therapeutic based on a natural-product scaffold targeting gram-negative pathogens.
Kidney stones are largely composed of calcium oxalate (CaOx), which can cause serious renal inflammation and damage to renal tubular epithelial cells, with the CaOx crystals gradually accumulating and leading to CaOx nephrocalcinosis.
Having 35 copies of the CAG triplet in the gene that causes Huntington’s disease is not a problem. Inheriting 40 could be a sign that goes unnoticed for decades, until reaching 80. From there, the process accelerates and neural death occurs when reaching 150 repeats. Huntington’s disease neurodegeneration is not determined by what, but by how much, according to a study conducted at the Broad Institute.
Bristol Myers Squibb Co. has synthesized proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a DNA-binding protein Ikaros (IKZF1)-, zinc finger protein Helios (IKZF2)-, Aiolos (IKZF3)- and Eos (IKZF4)-targeting moieties through a linker.
A Vanderbilt University patent discloses new muscarinic M4 receptor positive allosteric modulators and agonists reported to be useful for the treatment of Alzheimer’s disease, pain, schizophrenia, sleep disorders and cognitive disorder.
Kymera Therapeutics Inc. has patented new proteolysis targeting chimeras (PROTACs) comprising an E3 ubiquitin ligase-binding moiety coupled to an interleukin-1 receptor-associated kinase 1 (IRAK-4)-targeting moiety via linker.
Work at IFM Due Inc. has led to the identification of stimulator of interferon genes protein receptor (STING; TMEM173) antagonists reported to be useful for the treatment of cancer, systemic lupus erythematosus, autoinflammatory interferonopathy, rheumatoid arthritis and Aicardi-Goutieres syndrome.
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