Results 191 to 200 of about 702,558 (291)

Activation of a Secondary-Messenger Receptor via Allosteric Modulation of a Dynamic Conformational Ensemble. [PDF]

Angew Chem Int Ed Engl
Söldner B, Singh H, Akoury E, Witte G, Linser R.   +4 more
europepmc   +1 more source

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

Enhancement of hippocampal interneuron excitability by NMDA receptor positive allosteric modulation. [PDF]

J Physiol
Xing H, Banke TG, Zhang L, Yu K, Camp CR, Fritzemeier RG, Akins NS, Paladugu S, Arcoria PJ, Brady BR, Prikhodko O, Kennedy MJ, Liotta DC, Yuan H, Traynelis SF.   +14 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

Multiscale computational analysis reveals enhanced allosteric modulation of Nav1.5 by dual binding of dapagliflozin and ertugliflozin. [PDF]

Sci Rep
Chattopadhyay A, Fatehi M, Mosa FES, Gruber B, Light PE, Barakat K.   +5 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

The membrane properties determine protein function: A new aspect of allosteric modulation. [PDF]

Biophys J
Huster D.
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

Allosteric modulation of the solute carrier transporter SLC39A8 potentiates manganese and cadmium uptake. [PDF]

J Clin Invest
Damm-Ganamet KL, Moon C, Wickenden AD, Tichenor M, Ge Y, Mercado-Marin EV, Chiou B, Manughian-Peter A, Mirzadegan T, Venable JD, Xavier RJ, Towne JE, Graham DB, Perrigoue J.   +13 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