Results 131 to 140 of about 702,558 (291)

A three-level regulatory mechanism of the aldo-keto reductase subfamily AKR12D

Nature Communications
Modulation of protein function through allosteric regulation is central in biology, but biomacromolecular systems involving multiple subunits and ligands may exhibit complex regulatory mechanisms at different levels, which remain poorly understood. Here,
Zhihong Xiao, Jinyin Zha, Xu Yang, Tingting Huang, Shuxin Huang, Qi Liu, Xiaozheng Wang, Jie Zhong, Jianting Zheng, Rubing Liang, Zixin Deng, Jian Zhang, Shuangjun Lin, Shaobo Dai   +13 more
doaj   +1 more source

An Extracellular Pore‑Targeting Peptide Defines a Designable Allosteric Site in TRPV2

Advanced Science, EarlyView.
Structure‐guided peptide engineering yields Depiv2, a highly potent and subtype‐selective TRPV2 inhibitor that binds to the extracellular pore and remodels it into a closed, non‐conductive state. Depiv2 suppresses pathological cardiac hypertrophy, establishing the TRPV2 outer pore as a designable interface for selective peptide modulation.
Aiqin Zhu, Hongkun Wang, Jiawei Wang, Xiaolu Liu, Aerziguli Aierken, Lizhen Xu, Ping Liang, Fan Yang   +7 more
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

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

Determination of the Cannabinoid CB1 Receptor’s Positive Allosteric Modulator Binding Site through Mutagenesis Studies

Pharmaceuticals
Positive allosteric modulators (PAMs) of the cannabinoid CB1 receptor (CB1) offer potential therapeutic advantages in the treatment of neuropathic pain and addiction by avoiding the adverse effects associated with orthosteric CB1 activation.
Hayley M. Green, Daniel M. J. Fellner, David B. Finlay, Daniel P. Furkert, Michelle Glass   +4 more
doaj   +1 more source

Operational models of allosteric modulation : caution is needed

, 2021
The operational model of allosteric modulation and allosteric agonism [1-5] is being used routinely to assess the functional effects of allosteric modulators.
Giraldo, Jesús
core  

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

Propagation of the Allosteric Modulation Induced by Sodium in the δ-Opioid Receptor

, 2017
Allosteric sodium in the helix bundle of a G protein-coupled receptor (GPCR) can modulate the receptor activation on the intracellular side. This phenomenon has confounded the GPCR community for decades.
Yaoquan Tu, Giguõre, Patrick M., Patrick M. Giguère, Xianqiang Sun, Sun, Xianqiang,, Laroch, Genevieve, Hans Ågren, Gregory R. Bowman, Xu Wang, Tu, Yaoquan,, Wang, Xu,, Bowman, Gregory R., Genevieve Laroche, Ågren, Hans,   +13 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

Anxiety disorders and GABA neurotransmission: a disturbance of modulation

Neuropsychiatric Disease and Treatment, 2015
Philippe Nuss1,21Department of Psychiatry, Hôpital St Antoine, AP-HP, 2UMR 7203, INSERM ERL 1057 – Bioactive Molecules Laboratory, Pierre and Marie Curie University, Paris, FranceAbstract: Lines of evidence coming from many branches of ...
Nuss P
doaj