Results 141 to 150 of about 139,314 (301)

Structural pharmacology of SV2A reveals an allosteric modulation mechanism in the major facilitator superfamily

Nature Communications
The synaptic vesicle glycoprotein 2A (SV2A), a member of the major facilitator superfamily (MFS), is a key target for antiseizure medications and a biomarker for synaptic density imaging.
Shabareesh Pidathala, Xiao Chen, Yaxin Dai, Long N. Nguyen, Christoph Gorgulla, Yiming Niu, Fangyu Liu, Chia-Hsueh Lee   +7 more
doaj   +1 more source

The free fatty acid 2 receptor regulates C5a induced neutrophil superoxide production and its sensitivity to inhibition by the antagonist avacopan

Frontiers in Immunology
IntroductionReceptor transactivation is a novel signaling mechanism used by several different neutrophil G protein-coupled receptors (GPCRs) to activate an allosterically modulated receptor that recognizes short chain free fatty acids.
Zahra Khan, Zahra Khan, Neele K. Levin, Claes Dahlgren, Martina Sundqvist, Fariha Khan, Huamei Forsman, Huamei Forsman, Lena Björkman   +8 more
doaj   +1 more source

Hederagenin Attenuates Morphine Addiction via GABAA1‐Mediated Modulation of Ca2+–CaMK–CREB Signaling in Ventral Tegmental Dopaminergic Neurons

Advanced Science, EarlyView.
Hederagenin is identified as a GABAA1‐targeting natural compound that suppresses morphine‐associated reward by restraining Ca2+–CaMK–cAMP–CREB signaling in ventral tegmental dopaminergic neurons. RVG29‐modified liposomal delivery further enhances brain accumulation and behavioral efficacy, providing a mechanistically defined strategy for natural ...
Hongyang Jiang, Ziting Zhou, Nannan Xue, Jiasi Deng, Yuanyuan Zhou, Xinying Lv, Yuxuan Wang, Yi Zhang, Haotian Pan, Geyan Xu, Yinkun Tao, Mengran Li, Xin Cui, Hongyue Ma, Qian Wang, Zhigang Lu   +15 more
wiley   +1 more source

Supramolecular Allostery Achieves Tunable Luminescence Aromatic Bridged Phenothiazine Noncovalent Frameworks

Advanced Science, EarlyView.
Tunable luminescent supramolecular organic framework enabled by multiple allosteric effects, composed of a tetracation vinylphenylpyridinium‐modified aromatic‐bridged phenothiazine guest and cucurbit[8]uril, not only exhibits unique guest oxidation‐driven NIR luminescence blue‐shift and effectively enhances the quantum yield by 46‐fold to 22.2% but ...
Xinping Lu, Jianchong Chen, Jie Yu
wiley   +1 more source

Allosteric activation of the glutamate receptor mGlu2 by the serotonin receptor 5-HT2A

Nature Communications
G protein-coupled receptor (GPCR) dimers and higher-order oligomers are the subject of intense debates. The complexes formed between two or more different GPCRs enable the cell to integrate several signals.
Siyu Gai, Li Lin, Jiyong Meng, Yichen Wu, Li Xue, Chanjuan Xu, Qian Sun, Adrià Ricarte, James Dalton, Pedro Renault, Jesús Giraldo, Jean-Philippe Pin, Philippe Rondard, Jianfeng Liu   +13 more
doaj   +1 more source

Chemical structure of the dopamine D2 receptor allosteric modulator 3(R)-[(2(S)-pyrrolidinylcarbonyl) amino]-2-oxo-1-pyrrolidineacetamide (PAOPA).

, 2013
Chemical structure of the dopamine D2 receptor allosteric modulator 3(R)-[(2(S)-pyrrolidinylcarbonyl) amino]-2-oxo-1-pyrrolidineacetamide (PAOPA).
Rodney L. Johnson (442506), Ram K. Mishra (442507), Jian Ru Jiang (442504), Jayant Bhandari (442503), Patricia Hui (442505), Dipannita Basu (442501), Yuxin Tian (442502)   +6 more
core   +1 more source

Co‐activation of Selective Nicotinic Acetylcholine Receptor Subtypes Is Required for Neuroprotection against Alzheimer's Disease

Advanced Science, EarlyView.
ABSTRACT Beta‐amyloid peptide (Aβ)‐induced suppression of hippocampal GABAergic interneuron activity drives hyperexcitability, amyloid pathology, and cognitive impairment in Alzheimer's disease (AD), suggesting that enhancing hippocampal inhibition may be protective.
Rahmi Lee, Gayeon Kim, Ellison R. Black, Seonil Kim   +3 more
wiley   +1 more source

Protein allosteric site identification using machine learning and per amino acid residue reported internal protein nanoenvironment descriptors

Computational and Structural Biotechnology Journal
Allosteric regulation plays a crucial role in modulating protein functions and represents a promising strategy in drug development, offering enhanced specificity and reduced toxicity compared to traditional active site inhibition.
Folorunsho Bright Omage, José Augusto Salim, Ivan Mazoni, Inácio Henrique Yano, Luiz Borro, Jorge Enrique Hernández Gonzalez, Fabio Rogerio de Moraes, Poliana Fernanda Giachetto, Ljubica Tasic, Raghuvir Krishnaswamy Arni, Goran Neshich   +10 more
doaj   +1 more source

FBP1‐Mediated Compartmentalization of Glycolytic Enzyme Complexes Suppresses PKM2 Function to Ameliorate MASLD Progression

Advanced Science, EarlyView.
In normal hepatocytes, FBP1 forms compartmentalized complexes with PKM2, ENO1, and LDHA independent of its catalytic activity, inhibiting PKM2 activity and restricting excessive glycolysis. During MASLD progression, FBP1 downregulation markedly reduces the abundance of these complexes and releases the “hijacked” glycolytic enzymes, leading to PKM2 ...
Busong Wang, Yiping Tang, Na Li, Xuening Dai, Jing Wu, Bin Xue, Yuxin Chen, Jingzi Zhang, Lingdong Kong, Chaojun Li, Lei Fang   +10 more
wiley   +1 more source

Noncanonical Peloruside A Biosynthesis by an Uncultivated Verrucomicrobiota Symbiont

Angewandte Chemie, EarlyView.
Noncanonical biochemistry of the peloruside PKS characterized in this work, comprising double bond generation by a noncanonical tridomain (blue), acetyl‐CoA recycling (orange), and proofreading systems (purple and yellow). The Z‐double bond is installed by TEB1 through O‐acetylation and acetate elimination. The acyl ligase PelB (AL, orange) selectively
Amy E. Fraley, Michael Rust, Moritz Wagner, Ida R. Hipfinger, Paul J. N. Böhm, Cora L. Dieterich, Christopher M. Field, Michael J. Page, Jeremy G. Owen, Robert A. Keyzers, Shinichi Sunagawa, Jörn Piel   +11 more
wiley   +2 more sources