title: Tight-binding inhibitory sequences against pp60(c-src) identified using a random 15-amino-acid peptide library.
abstract: A bacteriophage peptide library containing a random 15-amino-acid insert was screened for identification of peptide sequence(s) that bind pp60(c-src). Sequencing the random insert from more than 100 virions indicated that more than 60% of the phage virions that bound to this enzyme contained a GXXG sequence motif in which X was frequently a hydrophobic residue. The GXXG sequence was often repeated as GXXGXXG. Two nonameric peptides were synthesized to determine whether or not the peptide inhibits pp60(c-src) tyrosine kinase activity and the importance of the glycine residues within this sequence. The peptide containing glycine had a Ki of 24 microM, whereas replacing the glycines with proline increased the Ki value to 3.1 mM.
authors.affiliation: Department of Neuro-Oncology, The University of Texas, M.D. Anderson Cancer Center, Houston 77030, USA.
authors.forename: T
authors.initials: T
authors.lastname: Nishi
authors.forename: R J
authors.initials: RJ
authors.lastname: Budde
authors.forename: J S
authors.initials: JS
authors.lastname: McMurray
authors.forename: N U
authors.initials: NU
authors.lastname: Obeyesekere
authors.forename: N
authors.initials: N
authors.lastname: Safdar
authors.forename: V A
authors.initials: VA
authors.lastname: Levin
authors.forename: H
authors.initials: H
authors.lastname: Saya
mesh_terms: D000595:Amino Acid Sequence; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D016392:Proto-Oncogene Proteins pp60(c-src) / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D010455:Peptides; D016392:Proto-Oncogene Proteins pp60(c-src)