Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
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SHR Neuro Krebs Kardio Lipid Stoffw Microb
Kubista, H; Mafra, RA; Chong, Y; Nicholson, GM; Beirao, PSL; Cruz, JS; Boehm, S; NentWig, W; Kuhn-Nentwig, L.
CSTX-1, a toxin from the venom of the hunting spider Cupiennius salei, is a selective blocker of L-type calcium channels in mammalian neurons
NEUROPHARMACOLOGY. 2007; 52(8): 1650-1662.
Doi: 10.1016/j.neuropharm.2007.03.012
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- Co-Autor*innen der Med Uni Graz
- Böhm Stefan
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- Abstract:
- The inhibitor cystine-knot motif identified in the structure of CSTX-1 from Cupiennius salei venom suggests that this toxin may act as a blocker of ion channels. Whole-cell patch-clamp experiments performed on cockroach neurons revealed that CSTX-1 produced a slow voltage-independent block of both mid/low- (M-LVA) and high-voltage-activated (HVA) insect Ca-v channels. Since C. salei venom affects both insect as well as rodent species, we investigated whether Ca-v channel currents of rat neurons are also inhibited by CSTX-1. CSTX-1 blocked rat neuronal L-type, but no other types of HVA Ca-v channels, and failed to modulate LVA Ca-v channel currents. Using neuroendocrine GH3 and GH4 cells, CSTX-1 produced a rapid voltage-independent block of L-type Cav channel currents. The concentration-response curve was biphasic in GH4 neurons and the subnanomolar IC50 values were at least 1000-fold lower than in GH3 cells. L-type Ca-v channel currents of skeletal muscle myoballs and other voltage-gated ion currents of rat neurons, such as I-Na(v) or I-K(v) were not affected by CSTX-1. The high potency and selectivity of CSTX-1 for a subset of L-type Ca-v channels in mammalian neurons may enable the toxin to be used as a molecular tool for the investigation of this family of Cav channels. (c) 2007 Elsevier Ltd. All rights reserved.
- Find related publications in this database (Keywords)
- Cupiennius salei venom
- CSTX-1
- voltage-gated calcium channels
- DUM neurons
- rat neurons