Siteone Therapeutics Inc. has provided details on the discovery of highly selective, potent, state-independent inhibitors of Nav1.7, a nonopioid target for the potential treatment of pain. While prior Nav1.7 inhibitors appear to bind the inactivated state preferentially, it was hypothesized that superior efficacy would be achievable by engaging all states/conformations of the channel.
Prosetta Biosciences Inc. has presented data on small molecules that inhibit cellular host factors needed for viral replication as a discovery tool to identify molecular interfaces upstream of Alzheimer’s disease cellular pathology.
It has been previously demonstrated that genetic loss-of-function of triggering receptor expressed on myeloid cells 2 (TREM2) impairs microglia migration, with the TREM2 R47H variant having been linked to increased risk of Alzheimer’s disease (AD) due to impaired microglia clustering and enhanced neuronal damage.
Rigel Pharmaceuticals Inc. presented findings from collaborative work with Medpharm that identified R-209, an interleukin-1 receptor-associated kinase 1 and 4 (IRAK-1/4) inhibitor with optimized properties for topical application.
Idorsia Pharmaceuticals Ltd. has reported the discovery of novel galectin-3 (Gal-3) inhibitors for the potential treatment of fibrotic and inflammatory diseases. Galactins are a family of glycan-binding proteins associated with various biological processes, including apoptosis, inflammation, fibrosis, angiogenesis, immunomodulation or tumor proliferation.
Nuclear factor erythroid 2-related factor 2 (NRF2) is a master regulator of cytoprotective mechanisms, and the cellular levels of this transcription factor are maintained low under normal conditions via actions of a CUL3-based E3 ligase, Kelch-like ECH-associated protein 1 (KEAP1).
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.
For the treatment of HIV infection, non-nucleoside reverse transcriptase inhibitors (NNRTIs) are used to prevent viral replication by binding to a pocket near the polymerase active site of HIV-1 reverse transcriptase.
At the ongoing ACS meeting in New Orleans, Rezubio Pharmaceuticals Co. Ltd. detailed the discovery and preclinical evaluation of novel small-molecule gut-restricted GPR40 agonists using membrane-anchored drug (MADD) design.
LX-101 from Lirum Therapeutics Inc. is an insulin-like growth factor 1 receptor (IGF-1R) inhibitor consisting of an IGF-1 variant coupled to a cytotoxic methotrexate payload. There are several aggressive cancer types of unmet need that have altered IGF-1R pathways and/or high IGF-1R expression, which correlates with poor prognosis.
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