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PubMed · 7527015

BPTI backbone variants and implications for inhibitory activity.

C Groeger·H R Wenzel·H Tschesche
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Abstract

Structural variants of BPTI were synthesized en route an enzymatic-chemical semisynthesis. The P1-P2 amide bond of the inhibitor molecule, which, as donor, contributes a hydrogen bond towards trypsin in the enzyme-inhibitor complex, was replaced by either a ketomethylene function or an ester bond yielding molecules with inhibitory activity. The two backbone-mutated BPTI derivatives showed increased dissociation constants of their respective trypsin complexes, obviously due to the lack of a single hydrogen-bond interaction in the enzyme-inhibitor complex.

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AprotininHydrogen BondingModels, MolecularProtein ConformationStructure-Activity RelationshipTrypsinComparative StudyJournal ArticleResearch Support, Non-U.S. Gov't

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BibTeXRIS

C Groeger, H R Wenzel, H Tschesche. 1994. BPTI backbone variants and implications for inhibitory activity.. https://doi.org/10.1111/j.1399-3011.1994.tb00572.x

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