- Guide to PHARMACOLOGY
Synonyms: KTx 6.3
Compound class: Peptide or derivative
Comment: HsTX1[R14A] is a modified version of the scorpion toxin HsTX1 (also known as α-KTx 6.3; wild type peptide sequence ASCRTPKDCADPCRKETGCPYGKCMNRKCKCNRC). HsTX1 and this modified version are potent blockers of the Kv1.3 potassium channel. The R14A modification confers selectivity for Kv1.3 .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|HsTX1[R14A]  and its PEGylated analogue (PEG-HsTX1[R14A])  are valuable leads in the development of therapeutics for autoimmune diseases, based on the participation of Kv1.3 in the activation of effector memory T (TEM) cells in humans, and the role played by TEM cells in driving autoimmune diseases. PEG-HsTX1[R14A] has an enhanced circulating half-life compared to HsTX1[R14A], with a slightly reduced affinity, but fully retained selectivity. PEG-HsTX1[R14A] is effective in rodent models of rheumatoid arthritis .|