Results 201 to 210 of about 139,314 (301)

ATP Citrate Lyase in Metabolic Disease: Mechanistic Insights and Clinical Potential

iNew Medicine, EarlyView.
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, Xinyan Li, Honglu Shi, Gaolei Song, Zhifu Xie, Jingya Li   +5 more
wiley   +1 more source

α6GABA_A receptor-selective positive allosteric modulator as a novel therapy for fibromyalgia: A proof-of-concept study in mice modeling chronic widespread musculoskeletal pain. [PDF]

Neurotherapeutics
Sant-Cassia M, Lee CH, Phani Babu Tiruveedhula VVN, Cook J, Chen CC, Chiou LC.   +5 more
europepmc   +1 more source

Research Progress of Berberine in Kidney Disease: Targeting Mitochondria and Ferroptosis

iNew Medicine, EarlyView.
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, Rongyu Guo, Xiaojun Feng, Liqin Tang   +3 more
wiley   +1 more source

Targeting PAR-2 with a negative allosteric modulator increases tumor antigen presentation and potentiates anti-PD-1 immunotherapy. [PDF]

J Immunother Cancer
Aouad S, Kadiri M, Allard D, Skora E, Giraud L, Fuselier C, Desroys du Roure P, Mousson A, Janvier A, Baron L, Franchet C, Lecru L, Routy B, Malo J, Brugat T, Blayo AL, Schann S, Stagg J.   +17 more
europepmc   +1 more source

New Hydrazone Derivatives Featuring Isatin and Piperazine Moieties: Synthesis, Cytotoxicity Evaluation, and Molecular Modeling Studies

Journal of Applied Toxicology, EarlyView.
ABSTRACT In this study, ten novel compounds (IPH1–IPH10) were designed by integrating three pharmacophores (isatin, piperazine, and hydrazone) commonly found in the molecular structures of anticancer agents. The target molecules were obtained by the reaction of in‐house prepared 4‐(4‐(pyridin/pyrimidin‐2‐yl)piperazin‐1‐yl)benzohydrazide with various ...
Semiha Köprü, Münevver Baran, Miyase Gözde Gündüz, Şengül Dilem Doğan   +3 more
wiley   +1 more source

Negative allosteric modulator of the metabotropic glutamate receptor 7 ADX71743 increases wakefulness, reduces sleep, and alters stress-induced changes in the brain neurotransmitter levels. [PDF]

Int J Neuropsychopharmacol
Kalinichev M, Gruner JA, Flik G, Heins M, Haddouk H, Royer-Urios I, Bate ST, Poli S, Lütjens R.   +8 more
europepmc   +1 more source

Potential Neuroendocrine Disruption by Benzodiazepines and Its Impact on Male Fertility

Journal of Applied Toxicology, EarlyView.
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, Julia Gonçalves Rodrigues, Marcos de Lucca Moreira Gomes, Fernanda Carolina Ribeiro Dias   +3 more
wiley   +1 more source

First-in-human study on the pharmacokinetics, safety, and tolerability of single escalating doses and multiple doses of XT1061, a novel core protein allosteric modulator, in healthy Chinese subjects. [PDF]

Front Pharmacol
Li Q, Hu Y, Wu D, Zhen W, Zhang H, Xu Q, Zhang H, Sun J, Li M, Ding Y, Jin Q.   +10 more
europepmc   +1 more source

Precision Medicine in Neurodegeneration with Brain Iron Accumulation (NBIA) Disorders: An Update on Emerging Treatments

Movement Disorders Clinical Practice, EarlyView.
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, Divyani Garg, Vassilena Iankova, Thomas Klopstock   +3 more
wiley   +1 more source

The pathway-independent positive allosteric modulator C1 allows for the identification of active Y₄ receptor relevant positions. [PDF]

Cell Mol Life Sci
Schüß C, Vu O, Pelczyk T, Schubert M, Du Y, Stichel J, Weaver CD, Meiler J, Beck-Sickinger AG.   +8 more
europepmc   +1 more source