Leucine-rich repeat kinase 2 (LRRK2), a key drug target, plays a major role in Parkinson’s disease (PD). Mutations in LRRK2, specifically LRRK2 G2019S which increases LRRK2 kinase activity, have been observed in a majority of PD patients.
Researchers from Massachusetts General Hospital recently detailed the discovery of [11C]SY-08, a new PET radiotracer that detects aggregated α-synuclein (α-Syn) fibrils in individuals with neurological disorders such as Parkinson’s disease, multiple system atrophy and dementia with Lewy bodies.
Aryl hydrocarbon receptor (AhR) signaling regulates gene expression in immune and skin cells and plays a critical role in maintaining skin homeostasis.
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.
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