HsTX1[R14A]   Click here for help

GtoPdb Ligand ID: 9582

Synonyms: KTx 6.3
Immunopharmacology Ligand
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 [1].
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Immunopharmacology Comments
HsTX1[R14A] [1] and its PEGylated analogue (PEG-HsTX1[R14A]) [2] 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 [2].