Unc-51-like autophagy-activating kinases 1 and 2 (ULK1/2) are enzymes that play a key role in initiating and regulating autophagy, with ULK1/2 autophagy being an adaptive stress response to multiple cancer therapies, supporting cell proliferation and tumor progression. At the recently concluded ACS meeting in New Orleans, Deciphera Pharmaceuticals LLC presented the discovery of a first-in-class ULK1/2 inhibitor as a potential new anticancer agent.
After many years of testing different monoclonal antibodies against amyloid-β protein, the results obtained are far from being outstanding, and the control of the progression and symptoms of Alzheimer’s disease (AD) remains elusive. At the recent AD/PD 2024 conference held in Lisbon, new non-anti-amyloidogenic strategies in the starting line against AD were discussed. Professor Einar Sigurdsson from New York University gave a presentation entitled, “Single domain antibodies for therapy and diagnosis of synucleinopathies and tauopathies.”
Researchers from Viiv Healthcare Ltd. presented preclinical data for the next-generation maturation inhibitor (MI) VH-3739937 (VH-937, zegruvirimat), currently in clinical testing for the treatment of HIV.
Development and optimization of novel oral selective hematopoietic progenitor kinase 1 (HPK1) inhibitors for immuno-oncology (IO) treatment were reported by scientists from Astrazeneca plc in two presentations during the ACS meeting this week.
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).
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