title: Peptide arrays for development of PDGFRβ Affine molecules.
abstract: OBJECTIVE
  Peptide arrays represent an attractive method for identification of amino acid motifs that bind to target structures. Spotting derivatives of the linear peptide platelet-derived growth factor receptor (PDGFR)-P1, which has been identified to bind the extracellular domain of the platelet-derived growth factor receptor beta, allows the synchronous investigation of the target affinity of numerous ligands.
  
  
  METHODS
  A peptide array randomizing PDGFR-P1 was constructed by replacement of each amino acid by all 20 natural amino acids. Incubation of the array with PDGFRβ and fibroblast growth factor receptor as negative control target was performed. Selected derivatives and fragments of PDGFR-P1 were chemically synthesized, radiolabeled, and evaluated in cell-based assays, using human pancreatic carcinoma BxPC3 and human breast cancer MCF7 cells.
  
  
  RESULTS
  Binding capacity was increased for the derivate yG2 by exchange of 7S to 7R. Competition experiments demonstrated a binding decrease with increasing competitor concentration. Serum stability of yG2 was improved compared to the native ligand.
  
  
  CONCLUSIONS
  Peptide arrays were successfully applied for the improvement of the PDGFRβ binding peptide PDGFR-P1.
authors: Department of Nuclear Medicine, University of Heidelberg, Heidelberg, Germany.
authors: Annabell
authors: A
authors: Marr
authors: Felix
authors: F
authors: Nissen
authors: Daniel
authors: D
authors: Maisch
authors: Annette
authors: A
authors: Altmann
authors: Shoaib
authors: S
authors: Rana
authors: Jürgen
authors: J
authors: Debus
authors: Peter E
authors: PE
authors: Huber
authors: Uwe
authors: U
authors: Haberkorn
authors: Vasileios
authors: V
authors: Askoxylakis
mesh_terms: D000595:Amino Acid Sequence; D045744:Cell Line, Tumor; D004705:Endocytosis; D006801:Humans; D020128:Inhibitory Concentration 50; D007457:Iodine Radioisotopes; D007700:Kinetics; D008024:Ligands; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry; D040081:Protein Array Analysis / Q000379:methods*; D011485:Protein Binding; D055550:Protein Stability; D020797:Receptor, Platelet-Derived Growth Factor beta / Q000378:metabolism*
chemical_list: D007457:Iodine Radioisotopes; D008024:Ligands; D010455:Peptides; D020797:Receptor, Platelet-Derived Growth Factor beta
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