Chemical biologists commonly seek out correlations between the physicochemical properties of molecules and their behavior in biological systems. However, a new paradigm is emerging for peptides in which conformation is recognized as the primary determinant of bioactivity and bioavailability. This review highlights an emerging body of work that directly addresses how a peptide’s conformation controls its biological effects, cell penetration, and intestinal absorption. Based on this work, the dream of mimicking the potency and bioavailability of natural product peptides is getting closer to reality.

Published as: Bock, Jonathan E., Jason Gavenonis, and Joshua A. Kritzer. Getting in Shape: Controlling Peptide Bioactivity and Bioavailability Using Conformational Constraints. ACS Chemical Biology 8, no.3 (2013): 488-499. https://pubs.acs.org/doi/10.1021/cb300515u. This author post-print is made available on Dickinson Scholar with the permission of the publisher. For more information on the published version, visit ACS Chemical Biology. © 2012 American Chemical Society