Results 41 to 50 of about 916,915 (144)

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

Structure-Activity Studies of Cysteine-Rich α-Conotoxins that Inhibit High Voltage-Activated Calcium Channels via GABAB Receptor Activation Reveal a Minimal Functional Motif [PDF]

, 2016
α-Conotoxins are disulfide-rich peptides that target nicotinic acetylcholine receptors. Recently we identified several α-conotoxins that also modulate voltage-gated calcium channels by acting as G protein-coupled GABA receptor (GABAR) agonists.
Daniel, JT, Carstens, Bodil B., Berecki, G, Brierley, SM, Daniel, James T., Lee, H., Stuart M. Brierley, Jackson, K., Deiteren, A, Tracy O'Donnell, Berecki, G., Craik, D., Bodil B. Carstens, David J. Adams, Han‐Shen Tae, Castro, Joel, Lee, Han Siean, Daniel, J., Joel Castro, Castro, J., O'donnell, T, Mahsa Sadeghi, Lee, HS, O'Donnell, Tracy, Tae, Han-Shen, Deiteren, Annemie, Brierley, Stuart M., Carstens, B., Tae, HS, Clark, Richard J., Deiteren, A., Richard J. Clark, Sadeghi, M., James T. Daniel, Kathryn A. V. Jackson, Sadeghi, M, O'Donnell, T., David J. Craik, Jackson, KAV, Han Siean Lee, Géza Berecki, Craik, DJ, Adams, David J., Clark, R., Adams, DJ, Tae, H., Berecki, Geza, Brierley, S., Castro, J, Sadeghi, Mahsa, Craik, David J., Annemie Deiteren, Jackson, Kathryn A. V., Clark, RJ, Adams, D., Carstens, BB   +55 more
core   +1 more source

Cancer pain: current practice and emerging targets

British Journal of Pharmacology, EarlyView.
Cancer pain (CP) arises from a complex interplay between the tumour and its microenvironment. Many patients experience a mixed pain phenotype that encompasses nociceptive, neuropathic and neuroinflammatory mechanisms, and vary across tumour type and disease stage. Despite decades of intensive research, the mainstay of cancer pain treatment is still non‐
Yi Ye, Marcin Chwistek, Zhiting Gong, Vanessa Uzonwanne, Xiaojie Shi, Arpad Szallasi   +5 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

Bioactive peptides in cancer and inflammation: Mechanisms, model systems and clinical translation

Clinical and Translational Discovery, Volume 6, Issue 5, October 2026.
Bioactive peptides (BAPs) derived from host, marine, insect, plant and synthetic sources share cationic, amphipathic structures adopting α‐helical, β‐sheet or cyclic conformations. These features underlie anti‐cancer effects, including membrane disruption, apoptosis and cell‐cycle arrest, anti‐metastatic activity, reduced invasion and migration, and ...
Najwa Doha, Richa Gill, Sergio Crovella, Haissam Abou‐Saleh, Sahar Isa Da'as   +4 more
wiley   +1 more source

Total synthesis and structural characterization of a novel protein scaffold from the snail Biomphalaria glabrata

Protein Science, Volume 35, Issue 9, September 2026.
Abstract Disulfide‐rich miniproteins constitute compact and highly stable scaffolds of growing interest for molecular and structural engineering. Schistosomins are ~80‐residue proteins conserved across gastropods that form a long‐standing orphan family whose structure and biological roles have remained unknown.
Oleg Melnyk, Stéphanie Caby, Armelle Vigouroux, Christine Demanche, Rémi Desmet, Magalie Sénéchal, Benoît Snella, Alexandra Mougel, Céline Boidin‐Wichlacz, Aurélie Parmentier, Ugo Pasco, Sonia Cantel, Solange Moréra, Jérôme Vicogne   +13 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

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

British Journal of Pharmacology, Volume 183, Issue 17, Page 5157-5189, September 2026.
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

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