Researchers from Beijing Institute of Technology (BIT) and affiliated organizations presented the discovery and preclinical characterization of novel soluble epoxide hydrolase 2 (sEH) inhibitors as candidates for the treatment of inflammatory disorders.
The activation of the adenosine A2A receptor, which is mediated by the inhibition of adenosine A1 receptor, has been associated with depression-like behavior and anhedonia. High levels of cortisol, increased oxidative stress and antioxidant enzyme reduction are also contributors to the pathophysiology of depression.
Parkinson’s disease, characterized by progressive dopamine neuron loss, leads to motor deficits such as bradykinesia and rigidity, as well as nonmotor symptoms like cognitive decline and depression. While L-DOPA alleviates motor symptoms, long-term use often results in side effects, including motor fluctuations and dyskinesias, as well as nonmotor (psychotic-like) side effects.
Son of sevenless homolog 1 (SOS1) is an essential guanine nucleotide exchange factor (GEF) in KRAS-driven tumors, and it also functions as a downstream node protein of BCR-ABL, suggesting its critical role in the pathogenesis of chronic myeloid leukemia (CML). Investigators at Shanghaitech University have reported the discovery and preclinical characterization of a novel potent SOS1 proteolysis targeting chimera (PROTAC) – SIAIS-562055 – being developed as an anticancer agent.
Researchers from Vera Salus Ricerca Srl and affiliated organizations have reported the discovery and preclinical characterization of novel sigma-1 receptor (S1R) antagonists as potential new analgesic agents.
Researchers from Gazi University and Friedrich-Schiller-Universität Jena presented the discovery and preclinical characterization of novel microsomal prostaglandin E2 synthase 1 (mPGES-1) inhibitors as potential anti-inflammatory and analgesic drug candidates.
Researchers from UCB SA and affiliated organizations presented the discovery and preclinical characterization of novel NUAK family SnF1-like kinase-1 (NUAK1) inhibitors.
The protease mucosa-associated lymphoid tissue lymphoma translocation 1 (MALT1) is a signaling protein with both molecular scaffolding and protease activity involved in lymphocyte activation. MALT1 is considered a therapeutic target for chronic lymphocytic leukemia (CLL) in patients who develop resistance to Bruton tyrosine kinase (BTK) inhibitors.
Recent research has established that Insulin-like Growth Factor 2 mRNA Binding Protein 3 (IGF2BP3) RNA-binding protein is involved in leukemia development, particularly in the KMT2A-translocated B-acute lymphoblastic leukemia (B-ALL) subtype.
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