Results 61 to 70 of about 1,665 (158)

Characterization of Binding Site Interactions and Selectivity Principles in the α3β4 Nicotinic Acetylcholine Receptor

, 2022
Nicotinic acetylcholine receptors (nAChRs) play an important role in neurotransmission and are also involved in addiction and several disease states. There is significant interest in therapeutic targeting of nAChRs; however, achieving selectivity for one
Hailey J. Knox, Hugo Rego Campello, Knox, Hailey J, Gallagher, Timothy, Henry A. Lester, Campello, Hugo Rego, Lester, Henry A, Timothy Gallagher, Dennis A. Dougherty, Dougherty, Dennis A   +9 more
core   +1 more source

An N‐Terminally Elongated Peptide From Conus rolani Defines a New Class of Ribbon α‐Conotoxins Targeting Muscle nAChRs

The FASEB Journal, Volume 39, Issue 12, 30 June 2025.
α‐RoIA is an atypical N‐terminally elongated conotoxin discovered in Conus rolani. N‐terminal elongation delays activity in vivo; however, this elongation must be removed to block muscle nicotinic acetylcholine receptors (nAChRs). Only the truncated ribbon isoform of RoIA blocks muscle nAChRs.
Matías L. Giglio, Paula Flórez‐Salcedo, Layla Azam, Maren Watkins, Thomas Lund Koch, Erianna Basgall‐De la Rosa, Adam D. Douglass, J. Michael McIntosh, Baldomero M. Olivera, Joanna Gajewiak   +9 more
wiley   +1 more source

Cyclization of the Analgesic α‐Conotoxin Vc1.1 With a Non‐Natural Linker: Effects on Structure, Stability, and Bioactivity

Journal of Peptide Science, Volume 31, Issue 6, June 2025.
This study cyclized conotoxin Vc1.1 using polyethylene glycol (PEG) linkers of different lengths and demonstrates that linker length modulates the peptide's helicity, thereby influencing its biological activity and stability. ABSTRACT α‐Conotoxin Vc1.1 is a disulfide‐rich peptide and a promising drug candidate for treating neuropathic and chronic pain.
Yuhui Zhang, Han Shen Tae, David J. Adams, Thomas Durek, David J. Craik   +4 more
wiley   +1 more source

Mitochondrial Nicotinic Acetylcholine Receptors Support Liver Cells Viability After Partial Hepatectomy

Frontiers in Pharmacology, 2018
Nicotinic acetylcholine receptors (nAChRs) expressed on the cell plasma membrane are ligand-gated ion channels mediating fast synaptic transmission, regulating neurotransmitter and cytokine release and supporting the viability of many cell types.
Kateryna Uspenska, Olena Lykhmus, Maria Obolenskaya, Stephanie Pons, Uwe Maskos, Serhiy Komisarenko, Maryna Skok   +6 more
doaj   +1 more source

Impacts of perinatal nicotine exposure on nicotinic acetylcholine receptor expression and glutamatergic synaptic transmission in the mouse auditory brainstem

The Journal of Physiology, Volume 603, Issue 9, Page 2857-2876, 1 May 2025.
Abstract figure legend Developmental nicotine exposure is known to cause a myriad of health defects including auditory processing deficits. In human and animal studies, nicotine exposure can lead to impaired auditory temporal processing and disrupted glutamate synapse development within the auditory cortex.
Mackenna Wollet, Abram Hernandez, Kaila Nip, Brett Ginsburg, Jason R. Pugh, Jun Hee Kim   +5 more
wiley   +1 more source

Nicotinic Acetylcholine Receptor (nAChR) Dependent Chorda Tympani Taste Nerve Responses to Nicotine, Ethanol and Acetylcholine.

PLoS ONE, 2015
Nicotine elicits bitter taste by activating TRPM5-dependent and TRPM5-independent but neuronal nAChR-dependent pathways. The nAChRs represent common targets at which acetylcholine, nicotine and ethanol functionally interact in the central nervous system.
Zuo Jun Ren, Shobha Mummalaneni, Jie Qian, Clive M Baumgarten, John A DeSimone, Vijay Lyall   +5 more
doaj   +1 more source

Identification of Nicotinic Acetylcholine Receptor for N‐Acetylcysteine to Rescue Nicotine‐induced Injury Using Beating Cilia in Primary Tissue Derived Airway Organoids

Advanced Science, Volume 12, Issue 1, January 9, 2025.
Human primary tissue‐derived airway organoids can recapitulate the ciliary beating of the airway. The expression of nicotinic receptors in cilia plays a role in maintaining the ciliary beating. Nicotine decreases ciliary beating function by binding to the nicotinic receptors.
Yichao Zheng, Qinyong Tian, Haowei Yang, Yongde Cai, Jiaxin Zhang, Yifen Wu, Shuo Zhu, Zuocheng Qiu, Yimin Lin, Jiangquan Hong, Yi Zhang, David Dockrell, Shaohua Ma   +12 more
wiley   +1 more source

DSPE-PEG Modification of α-Conotoxin TxID

Marine Drugs, 2019
In order to improve stability of a peptide marine drug lead, α-conotoxin TxID, we synthesized and modified TxID at the N-terminal with DSPE-PEG-NHS by a nucleophilic substitution reaction to prepare the DSPE-PEG-TxID for the first time. The reaction
Weinan Zhao, Yang Xiong, Dongting Zhangsun, Sulan Luo   +3 more
doaj   +1 more source

Nicotine-Modulated Subunit Stoichiometry Affects Stability and Trafficking of α3β4 Nicotinic Receptor

, 2013
Heteromeric nAChRs are pentameric cation channels, composed of combinations of two or three α and three or two β subunits, which play key physiological roles in the central and peripheral nervous systems.
F. Mazzo, F. Clementi, S.F. Colombo, G. Grazioso, C. Gotti, N. Borgese, F. Pistillo   +6 more
core   +1 more source

The human‐specific nicotinic receptor subunit CHRFAM7A reduces α7 receptor function in human induced pluripotent stem cells‐derived and transgenic mouse neurons

European Journal of Neuroscience, Volume 60, Issue 5, Page 4893-4906, September 2024.
Abstract We investigated the impact of the human‐specific gene CHRFAM7A on the function of α7 nicotinic acetylcholine receptors (α7 nAChRs) in two different types of neurons: human‐induced pluripotent stem cell (hiPSC)‐derived cortical neurons, and superior cervical ganglion (SCG) neurons, taken from transgenic mice expressing CHRFAM7A. dupα7, the gene
Ilayda Görgülü, Vinita Jagannath, Stephanie Pons, Filip Koniuszewski, Matthias Groszer, Uwe Maskos, Sigismund Huck, Petra Scholze   +7 more
wiley   +1 more source