Guangxitoxin-1E is a specific inhibitor of the Kv current of β-cells, can enhance the glucose-dependent intracellular calcium elevations and increases the glucose-dependent insulin secretion. It is considered as a useful tool for the investigation of type 2 diabetes.
CAT No: R0935
CAS No:1233152-82-3
Synonyms/Alias:Guangxitoxin 1E;1233152-82-3;AKOS027470252;DA-63966;PD079860;
Guangxitoxin 1E is a peptide toxin originally isolated from the venom of the Chinese tarantula, known for its potent and selective modulation of voltage-gated potassium channels. As a member of the Guangxitoxin family, it is characterized by a unique amino acid sequence and a highly conserved cystine knot motif, conferring both structural stability and specificity in channel targeting. Its ability to interact with Kv2.1 and related potassium channels has made it an important molecular probe in neurophysiological research, helping to elucidate the functional roles of these channels in neuronal excitability and signaling. The distinctive properties of Guangxitoxin 1E have positioned it as a valuable tool in the study of ion channel pharmacology and the development of innovative research methodologies.
Electrophysiological Studies: Guangxitoxin 1E is widely utilized in electrophysiological investigations to dissect the functional contributions of specific potassium channel subtypes, particularly Kv2.1 and related channels, in excitable cells. By acting as a highly selective inhibitor, it enables researchers to differentiate the currents mediated by these channels from those of other potassium channel families. This selectivity is crucial for patch-clamp studies aiming to map channel distributions, characterize gating kinetics, or assess the physiological significance of Kv2.1 in neuronal and cardiac tissues.
Ion Channel Pharmacology: In the context of ion channel pharmacology, the peptide serves as a reference ligand for evaluating the efficacy and selectivity of novel channel modulators. Its well-defined binding profile and robust inhibitory effects make it an ideal standard for benchmarking new small molecules, peptides, or biologics targeting voltage-gated potassium channels. Comparative studies employing Guangxitoxin 1E facilitate the identification of structure-activity relationships and support the rational design of next-generation channel modulators.
Neuroscience Research: The toxin plays a pivotal role in neuroscience research focused on neuronal signaling, synaptic plasticity, and excitability. By modulating the activity of Kv2.1 channels, it allows for controlled manipulation of membrane potential and action potential firing patterns in cultured neurons, brain slices, and invertebrate models. This precise modulation helps unravel the contribution of specific potassium channels to processes such as neurotransmitter release, dendritic integration, and the regulation of firing thresholds.
Peptide Structure-Function Analysis: Guangxitoxin 1E is frequently employed in structure-function studies to explore the molecular determinants of potassium channel recognition and inhibition. Through techniques such as site-directed mutagenesis, NMR spectroscopy, and computational modeling, researchers can dissect the interactions between the peptide and its channel targets at the atomic level. Insights gained from these analyses inform the broader understanding of toxin-channel specificity and support the engineering of modified peptides with tailored pharmacological profiles.
Peptide Synthesis and Modification: The unique sequence and disulfide-rich architecture of Guangxitoxin 1E make it a model system for advancing peptide synthesis methodologies, including solid-phase synthesis and oxidative folding strategies. Its use in synthetic chemistry provides a benchmark for optimizing protocols that preserve complex tertiary structures and bioactivity. Furthermore, the peptide serves as a scaffold for designing analogs with altered channel selectivity or improved stability, contributing to the expanding repertoire of research tools in ion channel biology.
In addition to being more potent than hanatoxin or stromatoxin, this peptide, Guangxitoxin-1E (GxTX-1E) had higher specificity for Kv2 channels, inhibiting Kv4.3 channels with an 8-fold lower potency and without significant effect on Kv1 or Kv3 family channels. The high selectivity of GxTX-1E for Kv2 makes it an attractive tool for studying the function of Kv2 channels in various types of neurons.
Kv2 Channel Regulation of Action Potential Repolarization and Firing Patterns in Superior Cervical Ganglion Neurons and Hippocampal CA1 Pyramidal Neurons
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