Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
44
|
| pubmed:dateCreated |
1998-11-30
|
| pubmed:abstractText |
We describe the first potent and selective blocker of the class E Ca2+channel. SNX-482, a novel 41 amino acid peptide present in the venom of the African tarantula, Hysterocrates gigas, was identified through its ability to inhibit human class E Ca2+ channels stably expressed in a mammalian cell line. An IC50 of 15-30 nM was obtained for block of the class E Ca2+ channel, using either patch clamp electrophysiology or K+-evoked Ca2+ flux. At low nanomolar concentrations, SNX-482 also blocked a native resistant or R-type Ca2+ current in rat neurohypophyseal nerve terminals, but concentrations of 200-500 nM had no effect on R-type Ca2+ currents in several types of rat central neurons. The peptide has the sequence GVDKAGCRYMFGGCSVNDDCCPRLGCHSLFSYCAWDLTFSD-OH and is homologous to the spider peptides grammatoxin S1A and hanatoxin, both peptides with very different ion channel blocking selectivities. No effect of SNX-482 was observed on the following ion channel activities: Na+ or K+ currents in several cultured cell types (up to 500 nM); K+ current through cloned potassium channels Kv1.1 and Kv1. 4 expressed in Xenopus oocytes (up to 140 nM); Ca2+ flux through L- and T-type Ca2+ channels in an anterior pituitary cell line (GH3, up to 500 nM); and Ba2+ current through class A Ca2+ channels expressed in Xenopus oocytes (up to 280 nM). A weak effect was noted on Ca2+ current through cloned and stably expressed class B Ca2+ channels (IC50 > 500 nM). The unique selectivity of SNX-482 suggests its usefulness in studying the diversity, function, and pharmacology of class E and/or R-type Ca2+ channels.
|
| pubmed:grant | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium Channels,
http://linkedlifedata.com/resource/pubmed/chemical/Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Spider Venoms
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Nov
|
| pubmed:issn |
0006-2960
|
| pubmed:author |
pubmed-author:ChenX hX,
pubmed-author:ConeTT,
pubmed-author:DooleyD JDJ,
pubmed-author:HopkinsWW,
pubmed-author:LemonAA,
pubmed-author:LouJ KJK,
pubmed-author:MiljanichGG,
pubmed-author:MillerJJ,
pubmed-author:NadasdiLL,
pubmed-author:NewcombRR,
pubmed-author:PalmaAA,
pubmed-author:SzokeBB,
pubmed-author:Tarczy-HornochKK,
pubmed-author:TsienR WRW,
pubmed-author:UrgeLL,
pubmed-author:WangGG
|
| pubmed:issnType |
Print
|
| pubmed:day |
3
|
| pubmed:volume |
37
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
15353-62
|
| pubmed:dateRevised |
2007-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:9799496-Amino Acid Sequence,
pubmed-meshheading:9799496-Animals,
pubmed-meshheading:9799496-Calcium Channel Blockers,
pubmed-meshheading:9799496-Calcium Channels,
pubmed-meshheading:9799496-Cell Line,
pubmed-meshheading:9799496-Humans,
pubmed-meshheading:9799496-Male,
pubmed-meshheading:9799496-Molecular Sequence Data,
pubmed-meshheading:9799496-Oocytes,
pubmed-meshheading:9799496-Patch-Clamp Techniques,
pubmed-meshheading:9799496-Peptides,
pubmed-meshheading:9799496-Potassium Channel Blockers,
pubmed-meshheading:9799496-Rats,
pubmed-meshheading:9799496-Rats, Sprague-Dawley,
pubmed-meshheading:9799496-Sodium Channel Blockers,
pubmed-meshheading:9799496-Spider Venoms,
pubmed-meshheading:9799496-Transfection,
pubmed-meshheading:9799496-Tumor Cells, Cultured,
pubmed-meshheading:9799496-Xenopus
|
| pubmed:year |
1998
|
| pubmed:articleTitle |
Selective peptide antagonist of the class E calcium channel from the venom of the tarantula Hysterocrates gigas.
|
| pubmed:affiliation |
Elan Pharmaceuticals Inc., Menlo Park, California 94025, USA.
|
| pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
|