title: Getting in shape: controlling peptide bioactivity and bioavailability using conformational constraints.
abstract: 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.
authors.affiliation: Department of Chemistry, Tufts University, Medford, Massachusetts 02155, United States.
authors.forename: Jonathan E
authors.initials: JE
authors.lastname: Bock
authors.affiliation: Department of Chemistry, Tufts University, Medford, Massachusetts 02155, United States.
authors.forename: Jason
authors.initials: J
authors.lastname: Gavenonis
authors.affiliation: Department of Chemistry, Tufts University, Medford, Massachusetts 02155, United States.
authors.forename: Joshua A
authors.initials: JA
authors.lastname: Kritzer
mesh_terms: D000818:Animals; D006801:Humans; D008958:Models, Molecular; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*; D011487:Protein Conformation
chemical_list: D010455:Peptides