Novartis AG described the identification and activity of TAK-756, a novel, selective and potent TAK1 inhibitor, as a potential intra-articular therapy for the treatment of osteoarthritis. Previous studies demonstrated that TAK1 appears to be a potential target for controlling inflammation and catabolism through NF-κB and MAPK pathways.

Immortality and eternal youth have been the stuff of myths and legends from ancient times on. Now, in the 21st century, real studies of current medicine could be applied to repair tissues and organs damaged by age. During the 11th Aging Research & Drug Discovery (ARDD) Meeting held at the University of Copenhagen at the end of August, scientists explained the molecular keys of rejuvenation, as many artists imagined in the past.

Essential branched-chain amino acids (BCAA) such as leucine, isoleucine or valine, cannot be synthesized by mammals, making them an obligate part of the diet.

At the European Federation for Medicinal chemistry and Chemical biology’s International Symposium on Medicinal Chemistry (EFMC-ISMC) held this week in Rome, Novartis Biomedical Research reported the discovery and evaluation of NVP-EVS-459, a low molecular weight folate receptor (FR)-targeting radioconjugate, for the potential treatment and diagnosis of cancer.

Researchers from Astrazeneca plc presented the structure and preclinical characterization of a novel PCSK9 inhibitor, AZD-0780, being developed for the treatment of cardiovascular disease. A new potentially druggable functional binding pocket was identified on the PCSK9 C-terminal domain (CTD), and multiple fragment screens generated a single CTD-binding hit.

Researchers from the National University of Singapore and affiliated organizations presented data from a study that investigated the potential of targeting chondroitin sulfate (CS) synthesis as a therapeutic strategy for ameliorating hyperplastic arterial remodeling.

Researchers from Bristol Myers Squibb Co. disclosed the structure and presented preclinical data for the dual inhibitor of diacylglycerol kinases (DGK) α and ζ, BMS-986408. Optimization of a DGK-α-selective hit led to the synthesis of dual DGK-α and -ζ inhibitors.

Genetic or pharmacologic inhibition of casein kinase 1α (CK1α) has proven effective in suppressing the proliferation of acute myeloid leukemia (AML) cell lines with wild-type TP53. Researchers from Bristol Myers Squibb Co. recently presented the discovery and preclinical characterization of BMS-986397, a cereblon E3 ligase modulatory drug (CELMoD) designed as a molecular glue degrader of CK1α.