Linked Life Data

7498466

Source:http://linkedlifedata.com/resource/pubmed/id/7498466

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-2
pubmed:dateCreated
1996-1-17
pubmed:abstractText
Enhancing the potency of peptides is a critical and important step in the development of peptide drugs. We have proposed that proline residues flanking protein-protein interaction sites perform a structural role in enhancing their interaction [R.M. Kini and H.J. Evans, Biochem. Biophys. Res. Commun. 212 (1995) 1115-1124]. To test this theory, we incorporated proline residues on either or both sides of the interaction site of an antiplatelet peptide, IARGDMNA and determined the inhibitory potency of the peptides in whole blood aggregation. Inclusion of one proline residue, on either the amino or carboxy terminal side of the interaction site, enhances the antiplatelet activity to approximately the same extent (1.5- to 2.5-fold). Incorporation of proline residues on both sides enhances the activity by 7- to 13-fold. This enhancement of the biological activity of the peptide is probably due to a reduction in the number of possible conformations of the peptide, without introducing the rigidity that would accompany cyclization. Incorporation of proline brackets thus provides a novel approach to the design and development of more potent peptide drugs and ligands.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0014-5793
pubmed:author
pubmed:issnType
Print
pubmed:day
13
pubmed:volume
375
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
15-7
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1995
pubmed:articleTitle
A novel approach to the design of potent bioactive peptides by incorporation of proline brackets: antiplatelet effects of Arg-Gly-Asp peptides.
pubmed:affiliation
Department of Biochemistry and Molecular Biophysics, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0614, USA.
pubmed:publicationType
Journal Article, Comparative Study, In Vitro, Research Support, Non-U.S. Gov't