Toxins isolated from the venom of the spider Phoneutria nigriventer either inhibit or activate a vast number of targets, such as ion channels, with high selectivity and affinity. PhTx3-1 toxin is a selective blocker o...Toxins isolated from the venom of the spider Phoneutria nigriventer either inhibit or activate a vast number of targets, such as ion channels, with high selectivity and affinity. PhTx3-1 toxin is a selective blocker of IA currents of K^＋ channels, and PhTx3-3 and PhTx3-4 are calcium channel blockers of the P/Q-type calcium channels. The spider neurotoxin PhTx3-6 reversibly and non-specifically inhibits high-voltage-activated Ca^2＋ channels with varying potency （N 〉 R 〉 P/Q 〉 L） in heterologous and native systems. There has been a huge increase in the range of medical disorders involving ionic channels, and blockers of these channels have potential as therapeutic agents. The mechanism of action of each toxin family is different; thus, each needs to be evaluated for its therapeutic potential. This review will focus on peptide toxins purified from the venom of the spider Phoneutria nigriventer that are currently being evaluated in preclinical tests as possible drugs for the treatment of pain, cardiac arrhythmias and ischemia.展开更多
文摘Toxins isolated from the venom of the spider Phoneutria nigriventer either inhibit or activate a vast number of targets, such as ion channels, with high selectivity and affinity. PhTx3-1 toxin is a selective blocker of IA currents of K^＋ channels, and PhTx3-3 and PhTx3-4 are calcium channel blockers of the P/Q-type calcium channels. The spider neurotoxin PhTx3-6 reversibly and non-specifically inhibits high-voltage-activated Ca^2＋ channels with varying potency （N 〉 R 〉 P/Q 〉 L） in heterologous and native systems. There has been a huge increase in the range of medical disorders involving ionic channels, and blockers of these channels have potential as therapeutic agents. The mechanism of action of each toxin family is different; thus, each needs to be evaluated for its therapeutic potential. This review will focus on peptide toxins purified from the venom of the spider Phoneutria nigriventer that are currently being evaluated in preclinical tests as possible drugs for the treatment of pain, cardiac arrhythmias and ischemia.
