PD alleviates APAP‐induced ALI by inhibiting the NLRP3 inflammasome signaling pathway. C/EBPβ is identified as a direct target via multimethod validation. PD promotes the deacetylation of C/EBPβ via Sirt1. The Sirt1/C/EBPβ/NLRP3 signaling axis is defined for PD's hepatoprotective effect.
Tian‐Yu Yang +6 more
wiley +1 more source
Discovery of VU6052959/BI'7927: A Selective mGlu<sub>3</sub> Positive Allosteric Modulator (PAM) from an Orthogonal Benzoxazine Chemotype. [PDF]
Jones CA +30 more
europepmc +1 more source
ATP Citrate Lyase in Metabolic Disease: Mechanistic Insights and Clinical Potential
ATP citrate lyase (ACLY) is a central metabolic hub that diverts mitochondrial citrate to fuel de novo lipogenesis, cholesterol biosynthesis, and protein acetylation. Given its robust correlation with pathological changes in multiple human diseases, ACLY inhibitors featuring distinct pharmacological strengths have been developed for therapeutic ...
Wenbiao Wang +5 more
wiley +1 more source
UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors. [PDF]
Benton AJ +10 more
europepmc +1 more source
Research Progress of Berberine in Kidney Disease: Targeting Mitochondria and Ferroptosis
This figure illustrates the model‐specific renoprotective mechanisms of berberine (BBR) across three major kidney diseases. From left to right, the diagram shows that BBR targets distinct core pathways depending on the pathological context: in diabetic nephropathy (DN), BBR activates AMPK to improve mitochondrial energy metabolism; in acute kidney ...
Liuqing Wang +3 more
wiley +1 more source
Potential Neuroendocrine Disruption by Benzodiazepines and Its Impact on Male Fertility
ABSTRACT Neuroactive substances have emerged as potent endocrine disruptors affecting male reproductive health through central and peripheral mechanisms. Among these, benzodiazepines, which are widely used for the management of anxiety, insomnia, epilepsy, and neuromuscular disorders, are known as GABA A (gamma‐aminobutyric acid type A) receptor ...
Ana Clara Melo Andrade de Rodrigues +3 more
wiley +1 more source
Phase 1 randomized trial of HS-10353, a novel GABA(A) positive allosteric modulator for treatment of major depressive disorder. [PDF]
Wang Z +9 more
europepmc +1 more source
Abstract Background Neurodegeneration with Brain Iron Accumulation (NBIA) is a heterogeneous group of heritable, mostly recessive, progressive neurodegenerative diseases characterized by iron deposition in the basal ganglia and brainstem. There are no solid global epidemiological data on prevalence and incidence of NBIA subtypes, but registry data and ...
Susanne A. Schneider +3 more
wiley +1 more source
Neuroprotective activity of the α7-nAChR positive allosteric modulator PNU-120596 on short term outcomes after traumatic brain injury. [PDF]
Winzer-Serhan UH +4 more
europepmc +1 more source
Small‐Molecule Kinase Inhibitors Modulating Circadian Rhythms
ABSTRACT The circadian clock mechanism generates 24‐h rhythms crucial for regulating various physiological processes, and its dysregulation has been implicated in numerous diseases. In cells, the circadian clock operates through a transcriptional‐translational feedback loop, where phosphorylation plays a pivotal role in maintaining accurate circadian ...
Irene Castellino +3 more
wiley +1 more source

