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 …

Molecular pharmacology of voltage-gated sodium channel expression in metastatic disease: clinical potential of neonatal Nav1. 5 in breast cancer

R Onkal, MBA Djamgoz - European journal of pharmacology, 2009 - Elsevier
A variety of ion channels have been detected in cancer cells. In particular, upregulation of
voltage-gated sodium channels (VGSCs) has been associated pathophysiologically with …

[HTML][HTML] Production of Recombinant Disulfide-Rich Venom Peptides for Structural and Functional Analysis via Expression in the Periplasm of E. coli

JK Klint, S Senff, NJ Saez, R Seshadri, HY Lau… - PloS one, 2013 - journals.plos.org
Disulfide-rich peptides are the dominant component of most animal venoms. These peptides
have received much attention as leads for the development of novel therapeutic agents and …

[HTML][HTML] Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain

JR Deuis, JS Wingerd, Z Winter, T Durek, Z Dekan… - Toxins, 2016 - mdpi.com
Loss-of-function mutations of NaV1. 7 lead to congenital insensitivity to pain, a rare condition
resulting in individuals who are otherwise normal except for the inability to sense pain …

The tarantula toxins ProTx-II and huwentoxin-IV differentially interact with human Nav1. 7 voltage sensors to inhibit channel activation and inactivation

Y Xiao, K Blumenthal, JO Jackson, S Liang… - Molecular …, 2010 - ASPET
The voltage-gated sodium channel Nav1. 7 plays a crucial role in pain, and drugs that inhibit
hNav1. 7 may have tremendous therapeutic potential. ProTx-II and huwentoxin-IV (HWTX …

[HTML][HTML] A Neanderthal sodium channel increases pain sensitivity in present-day humans

H Zeberg, M Dannemann, K Sahlholm, K Tsuo… - Current Biology, 2020 - cell.com
The sodium channel Nav1. 7 is crucial for impulse generation and conduction in peripheral
pain pathways [1]. In Neanderthals, the Nav1. 7 protein carried three amino acid …

Voltage-gated sodium channel in grasshopper mice defends against bark scorpion toxin

AH Rowe, Y Xiao, MP Rowe, TR Cummins, HH Zakon - Science, 2013 - science.org
Painful venoms are used to deter predators. Pain itself, however, can signal damage and
thus serves an important adaptive function. Evolution to reduce general pain responses …

Identification and characterization of ProTx-III [μ-TRTX-Tp1a], a new voltage-gated sodium channel inhibitor from venom of the tarantula Thrixopelma pruriens

FC Cardoso, Z Dekan, KJ Rosengren, A Erickson… - Molecular …, 2015 - ASPET
Spider venoms are a rich source of ion channel modulators with therapeutic potential. Given
the analgesic potential of subtype-selective inhibitors of voltage-gated sodium (NaV) …

The pharmacology of voltage-gated sodium channel activators

JR Deuis, A Mueller, MR Israel, I Vetter - Neuropharmacology, 2017 - Elsevier
Toxins and venom components that target voltage-gated sodium (Na V) channels have
evolved numerous times due to the importance of this class of ion channels in the normal …

TRPs et al.: a molecular toolkit for thermosensory adaptations

LJ Hoffstaetter, SN Bagriantsev… - Pflügers Archiv-European …, 2018 - Springer
The ability to sense temperature is crucial for the survival of an organism. Temperature
influences all biological operations, from rates of metabolic reactions to protein folding, and …