Researchers from Fudan University and affiliated organizations presented the discovery of novel PIM kinase inhibitors for the treatment of acute myeloid leukemia (AML). A literature-aided molecular hybridization strategy was applied to synthesize a structurally novel compound, based on an N-pyridinyl amide scaffold. Subsequent optimization showed that the positional isomerization of pyridine N toward to Lys67 resulted in a decrease of potency while increased freedom of solvent fragment toward Asp128/Glu171 led to an increase in activity.
An2 Therapeutics Inc. has received a research grant from the Bill & Melinda Gates Foundation to discover novel, boron-containing small molecules for the treatment of tuberculosis (TB) and malaria.
Methicillin-resistant S. aureus (MRSA) causes difficult-to-treat infections due to its inherent resistance. Thus finding new strategies to overcome MRSA resistance is critical. Researchers from China Agricultural University reported on the discovery and optimization of a novel series of pleuromutilin derivatives containing benzoxazole-2-thiol.
Sarcoidosis is a multisystem disorder characterized by the formation of granulomatous inflammatory nodules mainly located in the lungs, lymphatic system, skin and eyes. In patients with pulmonary involvement, targeting IFN-γ has proven ineffective. Researchers from Baylor College of Medicine and collaborators reported on the use of nonreceptor tyrosine phosphatase Src homolog-2 domain-containing phosphatase 2 (SHP2) inhibition as a potential strategy to treat sarcoidosis-like diseases.
Arialys Therapeutics Inc. launched this month with $58 million in seed funding, an experimental compound it is developing for autoimmune encephalitis and autoimmune psychosis, and high aspirations for its field. “Yes, I want to treat these patients, I want these patients to have a better life. But I also want drug discovery and development folks to think differently about discovering new drugs for the CNS,” Jay Lichter told BioWorld.
Glycotope GmbH and the Max Delbrück Center for Molecular Medicine in the Helmholtz Association have signed an agreement to explore the potential of combining Glycotope’s antibodies against protein/carbohydrate combined glyco-epitopes (Glycotargets) with chimeric antigen receptor (CAR) technology developed by the Max Delbrück Center.
Acurastem Inc. has entered into a license agreement with Takeda Pharmaceutical Company Ltd. to develop and commercialize Acurastem’s PIKFYVE-targeted therapeutics, including AS-202, an innovative antisense oligonucleotide (ASO) for the treatment of amyotrophic lateral sclerosis (ALS).
Orexia Therapeutics Ltd. has identified bicyclic-heterocycle derivatives acting as orexin OX2 receptor agonists. As such, they are reported to be useful for the treatment of narcolepsy, circadian rhythm disorder, genetic disorders, coma, metabolic syndrome, neurodegeneration, osteoporosis and sleep apnea, among others.
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