title: Folding and function in α/β-peptides: targets and therapeutic applications.
abstract: Combining natural α-amino acid residues and unnatural β-amino acid residues in a single chain leads to heterogeneous-backbone oligomers called α/β-peptides. Despite their unnatural backbones, α/β-peptides can manifest a variety of folding patterns and biological functions reminiscent of natural peptides and proteins. Moreover, incorporation of β-residues can impart useful properties to the oligomer such as improved stability to degradation by protease enzymes. α/β-Peptides have been developed that engage diverse biological targets, including proteins involved in apoptotic signalling, HIV-cell fusion, hormone signalling, and angiogenesis. For some systems, promising results obtained in vitro have paved the way for demonstrated activity in vivo, where α/β-peptides show equal potency and improved duration of effect compared to α-peptide counterparts.
authors.affiliation: Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, United States.
authors.forename: Halina M
authors.initials: HM
authors.lastname: Werner
authors.affiliation: Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, United States. Electronic address: horne@pitt.edu.
authors.forename: W Seth
authors.initials: WS
authors.lastname: Horne
mesh_terms: D000595:Amino Acid Sequence; D043925:Angiogenesis Inducing Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D017209:Apoptosis / Q000187:drug effects; D055808:Drug Discovery / Q000379:methods; D006678:HIV / Q000187:drug effects / Q000378:metabolism; D015700:HIV Envelope Protein gp41 / Q000378:metabolism; D015658:HIV Infections / Q000188:drug therapy; D006801:Humans; D008958:Models, Molecular; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D017510:Protein Folding; D017433:Protein Structure, Secondary; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism
chemical_list: D043925:Angiogenesis Inducing Agents; D000998:Antiviral Agents; D015700:HIV Envelope Protein gp41; D010455:Peptides; D019253:Proto-Oncogene Proteins c-bcl-2; D043562:Receptors, G-Protein-Coupled