Voltage-gated sodium channels: structure, function, pharmacology, and clinical indications
M de Lera Ruiz, RL Kraus - Journal of medicinal chemistry, 2015 - ACS Publications
The tremendous therapeutic potential of voltage-gated sodium channels (Navs) has been
the subject of many studies in the past and is of intense interest today. Nav1. 7 channels in …
the subject of many studies in the past and is of intense interest today. Nav1. 7 channels in …
Constraining cyclic peptides to mimic protein structure motifs
Many proteins exert their biological activities through small exposed surface regions called
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …
Molecular basis for pore blockade of human Na+ channel Nav1.2 by the μ-conotoxin KIIIA
The voltage-gated sodium channel Nav1. 2 is responsible for the initiation and propagation
of action potentials in the central nervous system. We report the cryo–electron microscopy …
of action potentials in the central nervous system. We report the cryo–electron microscopy …
Molecular biology of insect sodium channels and pyrethroid resistance
Voltage-gated sodium channels are essential for the initiation and propagation of the action
potential in neurons and other excitable cells. Because of their critical roles in electrical …
potential in neurons and other excitable cells. Because of their critical roles in electrical …
The biology and evolution of spider venoms
Spiders are diverse, predatory arthropods that have inhabited Earth for around 400 million
years. They are well known for their complex venom systems that are used to overpower …
years. They are well known for their complex venom systems that are used to overpower …
Spider-venom peptides: structure, pharmacology, and potential for control of insect pests
Spider venoms are an incredibly rich source of disulfide-rich insecticidal peptides that have
been tuned over millions of years to target a wide range of receptors and ion channels in the …
been tuned over millions of years to target a wide range of receptors and ion channels in the …
[HTML][HTML] Toxins and drug discovery
AL Harvey - Toxicon, 2014 - Elsevier
Components from venoms have stimulated many drug discovery projects, with some notable
successes. These are briefly reviewed, from captopril to ziconotide. However, there have …
successes. These are briefly reviewed, from captopril to ziconotide. However, there have …
Structural basis of α-scorpion toxin action on Nav channels
INTRODUCTION Members of the voltage-gated sodium (Nav) channel family are critical
contributors to electrical signaling. Accordingly, they are targets of drugs, toxins, and …
contributors to electrical signaling. Accordingly, they are targets of drugs, toxins, and …
Pharmacological characterisation of the highly NaV1.7 selective spider venom peptide Pn3a
Human genetic studies have implicated the voltage-gated sodium channel NaV1. 7 as a
therapeutic target for the treatment of pain. A novel peptide, μ-theraphotoxin-Pn3a, isolated …
therapeutic target for the treatment of pain. A novel peptide, μ-theraphotoxin-Pn3a, isolated …
Discovery of a selective NaV1.7 inhibitor from centipede venom with analgesic efficacy exceeding morphine in rodent pain models
S Yang, Y **ao, D Kang, J Liu, Y Li… - Proceedings of the …, 2013 - National Acad Sciences
Loss-of-function mutations in the human voltage-gated sodium channel NaV1. 7 result in a
congenital indifference to pain. Selective inhibitors of NaV1. 7 are therefore likely to be …
congenital indifference to pain. Selective inhibitors of NaV1. 7 are therefore likely to be …