University of Maryland has presented proteolysis targeting chimeras (PROTACs) comprised of E3 ubiquitin ligase cereblon (CRBN)-binding moiety covalently linked to induced myeloid leukemia cell differentiation protein Mcl-1-binding moiety through a linker reported to be useful for the treatment of cancer.
Avelos Therapeutics Inc. has identified substituted 1,2-diaminoheterocyclic compound derivatives acting as serine/threonine-protein kinase greatwall (MASTL) inhibitors reported to be useful for the treatment of cancer, diabetes, obesity, stroke, thrombosis deep venous, thrombocytopenia and cardiovascular disorders.
Hangzhou Zhongmei Huadong Pharmaceutical Co. Ltd. has divulged pyrrolopyridines acting as mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1) inhibitors reported to be useful for the treatment of cancer.
Genfleet Therapeutics (Shanghai) Inc. has patented receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors reported to be useful for the treatment of stroke, rheumatoid arthritis, psoriasis, heart failure, nonalcoholic steatohepatitis and inflammatory bowel disease.
Alagille syndrome (ALGS) is a rare JAG1 (encodes for a Notch ligand) autosomal dominant disease affecting approximately 1 in 30,000-40,000 individuals. ALGS developmental defects cause an absence of bile ducts (intrahepatic duct paucity, IHDP) with an inability to transport bile from the liver to bile ducts (cholestasis) as well as heart problems.
G-protein coupled receptor family C group 5 member D (GPRC5D) is a tumor-associated receptor that is highly expressed in multiple myeloma (MM) and is a potential target for therapy in MM. Preclinical data have been presented for FT-555, an induced pluripotent stem cell (iPSC)-derived CAR-NK (CAR-iNK) cell product that exerts dual targeting on GPRC5D and CD38 in combination with daratumumab.
Peptide-drug conjugates are an emerging class of molecules that allow efficient targeted drug delivery into tumors. Researchers from Oncopeptides AB and their collaborators presented data on the novel peptide-drug conjugate OPDC3, which has a novel alkylating payload, in models of diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML).
Satellos Bioscience Inc. has designated SAT-3153 as a development candidate for Duchenne muscular dystrophy and will move the candidate into pre-IND-enabling studies and toward an IND filing. SAT-3153 is a small molecule designed to inhibit a particular kinase protein which the company believes controls Notch polarity within muscle stem cells.
Umecrine Cognition AB has announced results showing that its GABA-A receptor-modulating steroid antagonist golexanolone reversed fatigue, anxiety, depression, and some cognitive and motor alterations in a preclinical model of Parkinson's disease. Compared to a control-operated group, models with Parkinson's disease showed increased fatigue in the treadmill test and anxiety in the open field test.
Hotspot Therapeutics Inc. has received FDA clearance of its IND application for HST-1011, the company's investigational small-molecule allosteric inhibitor of casitas B-lineage lymphoma-B (CBL-B), an E3 ubiquitin protein ligase critically involved in immune cell response.
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