THE DESIGN OF PEPTIDE ANALOGS FOR IMPROVED ABSORPTION

被引:24
作者
BARLOW, D
SATOH, T
机构
[1] Department of Pharmacy, King's College London, London, England
关键词
PEPTIDE; DRUG DESIGN; LIPOPHILICITY; ABSORPTION;
D O I
10.1016/0168-3659(94)90074-4
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of elementary analyses have been conducted with the aim of defining the basic design features for a potent, specific and absorbable peptide drug. The studies show that the required characteristics can be obtained using a peptide of just 4-6 amino acid residues, provided that it has a total surface area of around 350 Angstrom(2), and a polar surface area of less than or equal to 50 Angstrom A(2). Such a molecule is predicted to have a biological activity in the nanomolar range, and to exhibit a very respectable target specificity. A case is also presented, however, to show that the molecule will have only a very limited peptide character, with the overall conclusion that successful 'peptide' drugs will probably not qualify as peptides at all.
引用
收藏
页码:283 / 291
页数:9
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