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Introduction of Pro and its analogues in the conserved P 1' position of trypsin inhibitor SFTI-1 retains its inhibitory activity
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نویسنده
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łȩgowska a. ,dȩbowski d. ,łukajtis r. ,sztabkowska e. ,mizeria a. ,brzozowski k. ,wysocka m. ,lesner a. ,rolka k.
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منبع
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protein and peptide letters - 2011 - دوره : 18 - شماره : 11 - صفحه:1158 -1167
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چکیده
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A number of monocyclic sfti-1 analogues modified in the conserved inhibitor p 1 position by pro,its-l hydroxyproline (hyp) derivative as well as mimetics with different ring size were synthesized by the solid-phase method. replacement of ser6 by pro,hyp,and a four-member ring,l-azetidine-2- carboxylic acid (aze),retained trypsin or chymotrypsin inhibitory activity. the determined association equilibrium constants of these analogues with a cognate enzyme were about two orders of magnitude lower than those obtained for ones with conserved ser6. in all analogues,with the exception of one,[phe 5,aze 6]sfti-1,the p 1-p 1' reactive site remained intact. the results provide first evidence that the conserved ser in the p 1' position of bowman-birk inhibitors can be successfully replaced by an amino acid with a secondary amine group. © 2011 bentham science publishers.
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کلیدواژه
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Mimetics of Pro; Peptides; Proteinase inhibitors; SFTI-1
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آدرس
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faculty of chemistry,university of gdansk,sobieskiego 18, Poland, faculty of chemistry,university of gdansk,sobieskiego 18, Poland, faculty of chemistry,university of gdansk,sobieskiego 18, Poland, faculty of chemistry,university of gdansk,sobieskiego 18, Poland, faculty of chemistry,university of gdansk,sobieskiego 18, Poland, faculty of chemistry,university of gdansk,sobieskiego 18, Poland, faculty of chemistry,university of gdansk,sobieskiego 18, Poland, faculty of chemistry,university of gdansk,sobieskiego 18, Poland, faculty of chemistry,university of gdansk,sobieskiego 18, Poland
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Authors
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