Merck & Co. has revealed the discovery of novel oral SARS-CoV-2 3C-like proteinase (3CLpro; Mpro) inhibitors for the potential treatment and/or prophylaxis of COVID-19. 3CLpro plays a key role in viral life cycle by cleaving viral protein and helps in replication and infection, which make 3CLpro a target for designing drugs to treat COVID-19.
Researchers from the University of Illinois at Chicago and University of Arizona presented the discovery and preclinical evaluation of a novel BD1-selective BET inhibitor, XL-126, being developed as a potential anti-inflammatory agent.
Kv1.3 is a voltage-gated potassium channel that plays a crucial role in neuroinflammation and neurodegeneration in Parkinson’s disease and other disorders. Preclinical studies have shown that Kv1.3 inhibition confers neuroprotection against neurodegenerative disorders.
Investigators at Ileadbms Co. Ltd. have discovered a new cyclin-dependent kinase 12 (CDK12) and CDK13 inhibitor, IL6-110, which is being developed for the treatment of cancer.
In a new study, researchers from Harvard Medical School and Regulus Therapeutics Inc. further investigated the role of miR-155 in Alzheimer's disease (AD).
The activation of the NLRP3 inflammasome exacerbates neuronal dysfunction in several neurological diseases such as Alzheimer’s and Parkinson’s diseases, as well as multiple sclerosis. Targeting NLRP3 is an approach to overcome brain inflammation, among others.
Since microglia play a critical role in resolving amyloid pathology and it has been previously demonstrated that microglia function can be induced by TREM2 activation, TREM2 agonism has been considered a promising novel therapeutic approach to delay or prevent the progression of Alzheimer’s disease.
Researchers from Bugworks Research Inc. presented the discovery and preclinical evaluation of a novel potent and selective cyclin-dependent kinase 7 (CDK7) inhibitor, BWC-5044, in development for the treatment of cancer.
One-third of patients with acute myeloid leukemia (AML) present mutations in the FMS-like tyrosine kinase 3 (FLT3) gene. Several first- and next-generation FLT3 inhibitors are currently being used in AML management, but there is a need for new options able to achieve complete and sustained FLT3 signaling suppression.
Researchers from St. Jude Children’s Research Hospital have reported the discovery of SJ-3149, a novel selective CK1α degrader being developed for the treatment of cancer.
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