Results 201 to 210 of about 131,252 (300)

Advances in the Structural Basis of GluN2A-Selective Negative Allosteric Modulators. [PDF]

ACS Med Chem Lett
Li Y, Yuan H, Liang SH.
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

Structure-based discovery of positive allosteric modulators of the A₁ adenosine receptor. [PDF]

Proc Natl Acad Sci U S A
Nguyen ATN, Panel N, Vo DD, Thai BS, Chia LY, Lu CS, Hellyer SD, Langiu M, Jörg M, Gregory KJ, Kihlberg J, White PJ, Scammells PJ, Christopoulos A, Carlsson J, May LT.   +15 more
europepmc   +1 more source

Discovery of Novel, Potent Metabotropic Glutamate Receptor 5 Allosteric Antagonists

Metabotropic glutamate receptors (mGluR) belong to the G-protein-coupled receptor (GPCR) family and have been divided in three groups. mGluR1 and mGluR5 belong to Group I which couple to phospholipase C and their activation leads to intracellular calcium-
Smits, Gints, Kauss, Valerjans, Muller, Sibylle, Jatzke, Claudia, Erdmane, Elīna, Hechenberger, Mirko, Parsons, Christopher G. R, Weil, Tanja, Zemribo, Ronalds   +8 more
core  

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

Discovering Uncharted Binding Pockets on E3 Ligases Leads to the Identification of FBW7 Allosteric Modulators. [PDF]

Adv Sci (Weinh)
Martínez-Cartró M, Serrano-Morrás Á, Bertran-Mostazo A, Castaño-Muñiz R, Scaffidi S, Ivanova V, Csorba N, Simon J, Ábrányi-Balogh P, Li Y, Keserü GM, Hao B, Barril X, Galdeano C.   +13 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

Antibacterial Benzimidazole-2-Methanamines as Allosteric Modulators of <i>Streptococcus pneumoniae</i> Penicillin-Binding Protein 2x. [PDF]

J Med Chem
Dominguez-Cisneros H, Konai MM, Kim C, Rana N, Feltzer R, Janardhanan J, El-Araby AM, Nguyen VT, Fisher JF, Chang M, Mobashery S.   +10 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

Novel Isoindolin-1-one Derivatives as Metabotropic Glutamate Receptor Positive Allosteric Modulators. [PDF]

ACS Med Chem Lett
Li Y, Liang SH.
europepmc   +1 more source