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1iva

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STRUCTURE-ACTIVITY RELATIONSHIPS FOR P-TYPE CALCIUM CHANNEL SELECTIVE OMEGA-AGATOXINS

Structural highlights

1iva is a 1 chain structure with sequence from Agelenopsis aperta. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	Solution NMR, 16 models
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

TX23A_AGEAP Omega-agatoxins inhibit neuronal voltage-gated calcium channels. This toxin acts by modifying the gating of the high voltage activated P-type Cav2.1/CACNA1A channel. Is a potent blocker in both insect and mammalian central neurons.^[1] ^[2] ^[3] ^[4] ^[5] ^[6] ^[7]

References

↑ Winterfield JR, Swartz KJ. A hot spot for the interaction of gating modifier toxins with voltage-dependent ion channels. J Gen Physiol. 2000 Nov;116(5):637-44. PMID:11055992
↑ Wang XH, Connor M, Wilson D, Wilson HI, Nicholson GM, Smith R, Shaw D, Mackay JP, Alewood PF, Christie MJ, King GF. Discovery and structure of a potent and highly specific blocker of insect calcium channels. J Biol Chem. 2001 Oct 26;276(43):40306-12. Epub 2001 Aug 24. PMID:11522785 doi:http://dx.doi.org/10.1074/jbc.M105206200
↑ Mintz IM, Venema VJ, Swiderek KM, Lee TD, Bean BP, Adams ME. P-type calcium channels blocked by the spider toxin omega-Aga-IVA. Nature. 1992 Feb 27;355(6363):827-9. PMID:1311418 doi:http://dx.doi.org/10.1038/355827a0
↑ Bickmeyer U, Rossler W, Wiegand H. Omega AGA toxin IVA blocks high-voltage-activated calcium channel currents in cultured pars intercerebralis neurosecretory cells of adult locusta migratoria. Neurosci Lett. 1994 Nov 7;181(1-2):113-6. PMID:7898748
↑ Nishio H, Kumagaye KY, Kubo S, Chen YN, Momiyama A, Takahashi T, Kimura T, Sakakibara S. Synthesis of omega-agatoxin IVA and its related peptides. Biochem Biophys Res Commun. 1993 Nov 15;196(3):1447-53. PMID:8250902 doi:http://dx.doi.org/10.1006/bbrc.1993.2414
↑ Wicher D, Penzlin H. Ca2+ currents in central insect neurons: electrophysiological and pharmacological properties. J Neurophysiol. 1997 Jan;77(1):186-99. PMID:9120560
↑ McDonough SI, Mintz IM, Bean BP. Alteration of P-type calcium channel gating by the spider toxin omega-Aga-IVA. Biophys J. 1997 May;72(5):2117-28. PMID:9129813 doi:http://dx.doi.org/10.1016/S0006-3495(97)78854-4