Results 31 to 40 of about 1,350 (124)

Interactions of the α3β2 Nicotinic Acetylcholine Receptor Interfaces with α-Conotoxin LsIA and its Carboxylated C-terminus Analogue: Molecular Dynamics Simulations

Marine Drugs, 2020
Notably, α-conotoxins with carboxy-terminal (C-terminal) amidation are inhibitors of the pentameric nicotinic acetylcholine receptors (nAChRs), which are therapeutic targets for neurological diseases and disorders.
Jierong Wen, David J. Adams, Andrew Hung
doaj   +1 more source

Natural Compounds Interacting with Nicotinic Acetylcholine Receptors: From Low-Molecular Weight Ones to Peptides and Proteins

Toxins, 2015
Nicotinic acetylcholine receptors (nAChRs) fulfill a variety of functions making identification and analysis of nAChR subtypes a challenging task. Traditional instruments for nAChR research are d-tubocurarine, snake venom protein α-bungarotoxin (α-Bgt ...
Denis Kudryavtsev, Irina Shelukhina, Catherine Vulfius, Tatyana Makarieva, Valentin Stonik, Maxim Zhmak, Igor Ivanov, Igor Kasheverov, Yuri Utkin, Victor Tsetlin   +9 more
doaj   +1 more source

Peripheral κ opioid receptor in pain and inflammation: From molecular signalling and gene expression to drug discovery

British Journal of Pharmacology, EarlyView.
The κ opioid receptor (κ receptor, KOR) is a G protein‐coupled receptor with well established roles in analgesia and immune modulation. Although historically studied primarily in the central nervous system (CNS), growing evidence indicates that κ signalling in peripheral tissues plays an important role in regulating pain, inflammation and immune ...
Rumsha Khan, Elena C. A. Becker, Boglarka B. Bata, Christian W. Gruber   +3 more
wiley   +1 more source

From Crystal Structures of RgIA4 in Complex with Ac-AChBP to Molecular Determinants of Its High Potency of α9α10 nAChR

Marine Drugs, 2021
α9-containing nicotinic acetylcholine receptors (nAChRs) have been shown to play critical roles in neuropathic pain. The α-conotoxin (α-CTx) RgIA and its analog RgIA4 were identified as the most selective inhibitor of α9α10 nAChR.
Si Pan, Yingxu Fan, Xiaopeng Zhu, Yi Xue, Sulan Luo, Xinquan Wang   +5 more
doaj   +1 more source

Chronic Pain: Epidemiology, Pathophysiology, and Clinical Management

MedComm, Volume 7, Issue 5, May 2026.
The multidimensional nature of chronic pain is illustrated through four interconnected domains. (Left) Epidemiology and Global Burden: Chronic pain affects approximately one in five individuals globally, contributing to a rising trend in disability‐adjusted life years (YLDs) and a significant socioeconomic impact.
Zhihao Shang, Zijiao Tian, Zhaoquan Wang, Zerui Yang, Ziyao Wang, Zikang Wang, Ziqing Wang, Xingyuan He, Yu Yan, Yuanfeng Gong, Siyuan Xu, Xinyi Li, Guihua Tian   +12 more
wiley   +1 more source

A Structure‐Informed Atlas of Venom‐Derived Peptides Reveals the Organization of Chemical Space

Molecular Informatics, Volume 45, Issue 5, May 2026.
A structure‐informed atlas integrating sequence and AlphaFold‐derived features across 3,423 venom peptides reveals that chemical space is organized by disulfide‐stabilized compactness and electrostatic–hydrophobic balance, with functional classes clearly separated and convergent design principles overriding taxonomic origin.
Thaís Caroline Gonçalves, Eduardo Henrique Toral Cortez, Danilo T. Amaral   +2 more
wiley   +1 more source

RgIA4 Potently Blocks Mouse α9α10 nAChRs and Provides Long Lasting Protection against Oxaliplatin-Induced Cold Allodynia

Frontiers in Cellular Neuroscience, 2017
Transcripts for α9 and α10 nicotinic acetylcholine receptor (nAChR) subunits are found in diverse tissues. The function of α9α10 nAChRs is best known in mechanosensory cochlear hair cells, but elsewhere their roles are less well-understood.
Sean B. Christensen, Arik J. Hone, Isabelle Roux, Julie Kniazeff, Jean-Philippe Pin, Grégory Upert, Denis Servent, Elisabeth Glowatzki, Elisabeth Glowatzki, J. Michael McIntosh, J. Michael McIntosh, J. Michael McIntosh   +11 more
doaj   +1 more source

Loop2 Size Modification Reveals Significant Impacts on the Potency of α-Conotoxin TxID

Marine Drugs, 2023
α4/6-conotoxin TxID, which was identified from Conus textile, simultaneously blocks rat (r) α3β4 and rα6/α3β4 nicotinic acetylcholine receptors (nAChRs) with IC50 values of 3.6 nM and 33.9 nM, respectively.
Jianying Dong, Panpan Zhang, Junjie Xie, Ting Xie, Xiaopeng Zhu, Dongting Zhangsun, Jinpeng Yu, Sulan Luo   +7 more
doaj   +1 more source

Molecular basis for a pore block of Tentonin 3 expressed in HEK293 cells by a conopeptide, NMB‐1

British Journal of Pharmacology, Volume 183, Issue 9, Page 1845-1859, May 2026.
Background and Purpose Tentonin 3 (TTN3/TMEM150C) is a mechanosensitive ion channel that plays critical roles in mechanotransduction processes. TTN3 forms a tetramer with a predicted rectangular shape and a central pore. A conotoxin ρ‐TIA and its synthetic analog, noxious mechanosensation blocker 1 (NMB‐1), were initially developed to inhibit slowly ...
Sujin Lim, Junhyuk Woo, Sungmin Pak, Joonho Paik, Gyu‐Sang Hong, Ji Hun Wi, Sanghee Lee, Cristina Fenollar‐Ferrer, Kyungreem Han, Young Kee Shin, Uhtaek Oh   +10 more
wiley   +1 more source

GABAB receptor‐mediated modulation of sensory neuron excitability: Roles of CaV2.2, G‐protein‐coupled inwardly rectifying potassium (GIRK) channels, and hyperpolarisation‐activated cyclic nucleotide‐gated (HCN) channels in human and mouse nociception

Experimental Physiology, Volume 111, Issue 4, Page 2026-2043, 1 April 2026.
Abstract Chronic visceral pain is a key symptom of irritable bowel syndrome. Modulation of voltage‐gated calcium and potassium channels by G protein‐coupled receptors plays a key role in dampening nociceptive transmission. Both baclofen and the analgesic peptide α‐conotoxin Vc1.1 activate GABAB receptors (GABABR), resulting in inhibition of CaV2.2 and ...
Mariana Brizuela, Anuja R. Bony, Sonia Garcia‐Caraballo, David J. Adams, Stuart M. Brierley   +4 more
wiley   +1 more source