Unconventional Secondary Structure Mimics: Ladder‐Rungs Academic Article uri icon

abstract

  • 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.

altmetric score

  • 0.75

author list (cited authors)

  • Lin, C., Arancillo, M., Whisenant, J., & Burgess, K.

citation count

  • 5

publication date

  • June 2020

publisher