Unconventional Secondary Structure Mimics: Ladder‐Rungs
Autor: | Kevin Burgess, Maritess Arancillo, Jonathan Whisenant, Chen-Ming Lin |
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Rok vydání: | 2020 |
Předmět: | |
Zdroj: | Angew Chem Int Ed Engl |
ISSN: | 1521-3773 1433-7851 |
Popis: | Secondary structures tend to be recognizable because they have repeating structural motifs, but mimicry of these does not have to follow such well-defined patterns. Bioinformatics studies to match side-chain orientations of a novel hydantoin triazole chemotype (1) to protein-protein interfaces revealed it tends to align well across parallel and antiparallel sheets, like rungs on a ladder. One set of these overlays was observed for the protein-protein interaction uPA⋅uPAR. Consequently, chemotype 1 was made with appropriate side-chains to mimic uPA at this interface. Biophysical assays indicate these compounds did in fact bind uPAR, and elicit cellular responses that affected invasion, migration, and wound healing. |
Databáze: | OpenAIRE |
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