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.
Precision psychiatry got some love at two quite different meetings this week, the European Congress of Neuropsychopharmacology’s New Frontiers meeting and BioEurope Spring. The New Frontiers Meeting, an annual two-day meeting dedicated to cutting-edge issues in brain disease research, focused on big-picture and scientific – at times almost philosophical – questions of how to get to a classification scheme for brain disorders that aligns with the underlying biology.
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.
To Steve Hyman, the manual that clinicians currently use to diagnose mental disorders is an active obstacle to getting a scientific understanding of those disorders. Hyman, who is director of the Stanley Center for Psychiatric Research at the Broad Institute, MIT and Harvard, and a former director of the National Institute of Mental Health (NIMH), listed multiple weaknesses of the American Psychiatric Association’s Diagnostic and Statistical Manual of Mental Disorders (DSM), whose diagnoses, he said, are “arbitrary, rigid, life-stage and context-insensitive,” as well as blind to the fact that mental disorders exist along a continuum.
Patients with amyotrophic lateral sclerosis (ALS) have a median survival of 2 to 5 years. There are 3 FDA-approved drugs for ALS (riluzole, edaravone and Relyvrio [phenylbuturate/taurursodiol]), but they only lead to modest benefit. There are several pathways involved in the disease, but all of them lead to neuroinflammation.
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