title: Stability of peptides and therapeutic success in cancer.
abstract: BACKGROUND
  Although naturally occurring peptides have been widely used as drugs, their rapid in vivo degradation by proteolysis and their interactions at multiple receptors are part of the reason for the limitation of their clinical applications.
  
  
  METHODS
  This paper reviews peptide-metabolizing enzymes in the brain and intestinal brush-border membranes, and discusses potential strategies to improve biological activity, specificity and stability of peptides. The reader will gain, via some examples, an appreciation of the challenges involved in identifying peptides stability to improve their biological properties such as selectivity.
  
  
  CONCLUSIONS
  Due to the metabolic process, it is crucial to follow the biodistribution of a peptide drug and/or a peptidic moiety in order to improve its biological properties such as selectivity. To these purposes, pseudopeptides and peptidomimetics preserving the biological properties of native peptides have been developed to increase their resistance to degradation and elimination, bioavailability and selectivity to become good drug candidates.
authors: Centre de Recherche en Automatique de Nancy, Centre Alexis Vautrin, Nancy-University, Avenue de Bourgogne, Brabois, F 54511 Vandœuvre-lès-Nancy, France.
authors: Marlène
authors: M
authors: Pernot
authors: Régis
authors: R
authors: Vanderesse
authors: Céline
authors: C
authors: Frochot
authors: François
authors: F
authors: Guillemin
authors: Muriel
authors: M
authors: Barberi-Heyob
mesh_terms: D001682:Biological Availability; D001812:Blood-Brain Barrier / Q000378:metabolism*; D004355:Drug Stability; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism*; D008871:Microvilli / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy; D010447:Peptide Hydrolases / Q000378:metabolism; D010455:Peptides / Q000737:chemistry* / Q000493:pharmacokinetics*; D057786:Peptidomimetics / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D010455:Peptides; D057786:Peptidomimetics; D010447:Peptide Hydrolases