Linked Life Data

7969037

Source:http://linkedlifedata.com/resource/pubmed/id/7969037

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1994-12-6
pubmed:abstractText
omega-Agatoxin-TK (omega-Aga-TK), a 48-amino-acid peptide isolated from the venom of the funnel web spider (Agelenopsis aperta), is a selective and potent inhibitor of P-type calcium channels in the nervous system. We have synthesized a peptide that has the amino acid sequence identified for native omega-Aga-TK. The synthetic omega-Aga-TK, however, showed 80-90-fold less potent inhibition of P-type calcium channels, compared with native omega-Aga-TK. Enantiomer analysis of native omega-Aga-TK revealed D-serine at position 46, and synthetic omega-[D-Ser46]Aga-TK had the same potency as native omega-Aga-TK for blocking P-type calcium channels in cultured cerebellar Purkinje neurons. Two peptide fragments of omega-Aga-TK, namely omega-Aga-TK(1-43) and the carboxyl-terminal peptide fragment omega-Aga-TK(44-48), did not produce any significant inhibition of P-type calcium channels or interfere with the blockade of the channels elicited by native omega-Aga-TK. Molecular dynamics calculations showed that the carboxyl-terminal, six-amino-acid peptide of omega-Aga-TK containing D-Ser46 assumes a different conformation than does the peptide containing L-Ser46. These results suggest that the specific conformation of the carboxyl-terminal region of omega-Aga-TK, particularly the configuration of Ser46, together with a beta-sheet structure formed by four disulfide bonds, might be essential for blockade of P-type calcium channels.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0026-895X
pubmed:author
pubmed:issnType
Print
pubmed:volume
46
pubmed:owner
NLM
pubmed:authorsComplete
N
pubmed:pagination
587-93
pubmed:dateRevised
2011-11-17
pubmed:meshHeading
pubmed:year
1994
pubmed:articleTitle
Omega-agatoxin-TK containing D-serine at position 46, but not synthetic omega-[L-Ser46]agatoxin-TK, exerts blockade of P-type calcium channels in cerebellar Purkinje neurons.
pubmed:affiliation
Eisai Tsukuba Research Laboratory, Ibaraki, Japan.
pubmed:publicationType
Journal Article