Results 51 to 60 of about 2,164 (171)

Design of New α-Conotoxins: From Computer Modeling to Synthesis of Potent Cholinergic Compounds

open access: yesMarine Drugs, 2011
A series of 14 new analogs of α-conotoxin PnIA Conus pennaceus was synthesized and tested for binding to the human α7 nicotinic acetylcholine receptor (nAChR) and acetylcholine-binding proteins (AChBP) Lymnaea stagnalis and Aplysia californica.
Alexey Y. Khruschov   +3 more
doaj   +1 more source

Systematic dissection of genomic features determining the vast diversity of conotoxins

open access: yesBMC Genomics, 2023
Background Conus, a highly diverse species of venomous predators, has attracted significant attention in neuroscience and new drug development due to their rich collection of neuroactive peptides called conotoxins.
Jian-Wei Zheng   +9 more
doaj   +1 more source

Discovery of Novel Conotoxin Candidates Using Machine Learning

open access: yesToxins, 2018
Cone snails (genus Conus) are venomous marine snails that inject prey with a lethal cocktail of conotoxins, small, secreted, and cysteine-rich peptides.
Qing Li   +4 more
doaj   +1 more source

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

open access: yesBritish 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   +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

open access: yesExperimental 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   +4 more
wiley   +1 more source

In Silico Conotoxin Studies: Progress and Prospects. [PDF]

open access: yesMolecules
Cone snails of the genus Conus have evolved to produce structurally distinct and functionally diverse venom peptides for defensive and predatory purposes. This nature-devised delicacy enlightened drug discovery and for decades, the bioactive cone snail venom peptides, known as conotoxins, have been widely explored for their therapeutic potential, yet ...
Li R, Hasan MM, Wang D.
europepmc   +6 more sources

α‐Synuclein oligomers slow down action potential firing and enhance dopamine release by increasing Cav2.2 currents in midbrain dopaminergic neurons

open access: yesThe Journal of Physiology, Volume 604, Issue 7, Page 3094-3113, 1 April 2026.
Abstract figure legend Left: the spontaneous quantal release of dopamine (DA) occurs at very low frequency in control conditions. Right: exogenous α‐synuclein potentiates Cav2.2 currents and DA release but drastically reduces the spontaneous firing rate of substantia nigra DA neurons.
Giulia Tomagra   +12 more
wiley   +1 more source

Orthosteric and/or Allosteric Binding of α-Conotoxins to Nicotinic Acetylcholine Receptors and Their Models

open access: yesMarine Drugs, 2018
α-Conotoxins from Conus snails are capable of distinguishing muscle and neuronal nicotinic acetylcholine receptors (nAChRs). α-Conotoxin RgIA and αO-conotoxin GeXIVA, blocking neuronal α9α10 nAChR, are potential analgesics ...
Elena V. Kryukova   +8 more
doaj   +1 more source

Unraveling the Morphological and Functional Maturation Mechanisms Underlying Human Neural Development Using iPSCs‐Derived Neuronal Model

open access: yesAdvanced Science, Volume 13, Issue 18, 27 March 2026.
Using human induced pluripotent stem cells (hiPSCs)‐derived neuronal model, Tian and colleagues reveal that voltage‐gated calcium channels Cav1.2 and Cav1.3, and their mediated calcium ion influx, are essential for early morphogenesis of human neuronal development, while ECEL1 underlies human neuronal functional developmental maturation through CALM3 ...
Yue Tian   +5 more
wiley   +1 more source

Cone Snails: A Big Store of Conotoxins for Novel Drug Discovery

open access: yesToxins, 2017
Marine drugs have developed rapidly in recent decades. Cone snails, a group of more than 700 species, have always been one of the focuses for new drug discovery.
Bingmiao Gao   +5 more
doaj   +1 more source

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