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.
A team of scientists from the Perelman School of Medicine at the University of Pennsylvania and Aum Biotech LLC have described the development of a novel cancer immunotherapy designed to target FOXP3-positive T regulatory cells (Tregs) with a next generation of antisense oligonucleotides (ASOs), termed FOXP3 Aumsilence ASO. In contrast to previous ASOs, FOXP3 Aumsilence ASOs do not require delivery agents, and are capable of highly specific RNA silencing of previously undruggable targets.
Artificial intelligence (AI) drug discovery company Noetik Inc. has closed on an oversubscribed $40 million series A financing round. The company plans to use the money to expand its atlas of human cancer biology with its in vivo CRISPR platform to advance a pipeline of cancer therapeutics to the clinic. In describing its approach, the company said that making a genuine impact on drug discovery requires computational capabilities to understand and simulate disease biology at the patient level, identifying the right targets and matching them with the right therapies.
Scientists at Bristol Myers Squibb Co. and Celgene Corp. have synthesized proteolysis targeting chimera (PROTAC) compounds comprising a cereblon (CRBN) E3 ubiquitin ligase-binding moiety coupled to a protein-targeting moiety through a linker.
Thyroid hormone receptor-interacting protein 13 (TRIP13) is overexpressed in multiple myeloma (MM), where it is associated with progression and poor prognosis.
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.
Celgene Corp. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a MAP kinase-activated protein kinase 2 (MAPKAPK2; MK2)-targeting moiety via a linker.
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.
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