Li Ming-Hua, Zhang Nai-Xia, Chen Xue-Qin, Wu Gong, Wu Houming, Hu Guo-Yuan
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zu-Chong-Zhi Road, Shanghai 201203, China.
Toxicon. 2004 Jun 15;43(8):895-900. doi: 10.1016/j.toxicon.2003.11.028.
BmKK2 (alpha-KTx 14.2) is one of the novel short-chain peptides found in molecular cloning of a venom gland cDNA library from Asian scorpion Buthus martensi Karsch. Based upon its amino acid sequence, the peptide was proposed to adopt a classical alpha/beta-scaffold for alpha-KTxs. In the present study, we purified BmKK2 from the venom of B. martensi Karsch, and investigated its action on voltage-dependent K+ currents in dissociated hippocampal neurons from neonatal rats. BmKK2 (10-100 microM) selectively inhibited the delayed rectifier K+ current, but did not affect the fast transient K+ current. The inhibition of BmKK2 on the delayed rectifier K+ current was reversible and voltage-independent. The peptide did not affect the steady-state activation of the current, but caused a depolarizing shift (about 9 mV) of its steady-state inactivation curve. The results demonstrate that BmKK2 is a novel K+ channel-blocking scorpion peptide.
BmKK2(α-KTx 14.2)是在对亚洲蝎子东亚钳蝎毒腺cDNA文库进行分子克隆时发现的新型短链肽之一。根据其氨基酸序列,该肽被认为采用了α-KTxs的经典α/β支架结构。在本研究中,我们从东亚钳蝎毒液中纯化了BmKK2,并研究了其对新生大鼠离体海马神经元中电压依赖性钾电流的作用。BmKK2(10 - 100微摩尔)选择性抑制延迟整流钾电流,但不影响快速瞬时钾电流。BmKK2对延迟整流钾电流的抑制是可逆的且不依赖电压。该肽不影响电流的稳态激活,但导致其稳态失活曲线发生去极化偏移(约9毫伏)。结果表明,BmKK2是一种新型的钾通道阻断蝎肽。