The DOI matches its Crossref record; 62 of the 62 references it cites were found in a registry or an index.
Selection of peptides binding to the alpha 5 beta 1 integrin from phage display library.
Open accessAbstract
The alpha 5 beta 1 integrin binds fibronectin through the integrin recognition sequence Arg-Gly-Asp (RGD). We have used a 6-amino acid peptide library expressed on filamentous phage to identify peptide ligands for alpha 5 beta 1. We found that this integrin selectively binds RGD-containing peptides from the library. Of the 32 different sequences obtained, 28 had the RGD motif, 3 contained sequences related to RGD, and only 1 had a clearly different sequence. One of the RGD-containing phage encoded a potentially cyclic insert CRGDCL. The cyclic peptide GAC*RGDC*LGA (where * denotes cysteines forming a disulfide bond) was 10-fold more efficient than any of the linear RGD-containing hexapeptides in inhibiting the binding of RGD-expressing phage to alpha 5 beta 1 or the attachment of alpha 5 beta 1-expressing cells to fibronectin. This peptide also inhibited cell attachment mediated by the alpha v beta 1, alpha v beta 3, and alpha v beta 5 integrins with about 10-fold higher efficiency than linear GRGDSP. One peptide containing an RGD-related sequence, NGRAHA, was also found to inhibit phage attachment and cell adhesion, especially adhesion mediated by the alpha v beta 5 integrin. These results indicate that novel and high affinity ligands for integrins can be isolated from a random peptide library.
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Self-citationCoadministration of a Tumor-Penetrating Peptide Enhances the Efficacy of Cancer Drugs
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Metadata
- Authors
- Koivunen, E., Gay, D. A., & Ruoslahti, E.
- Affiliations
- Sanford Burnham Prebys Medical Discovery Institute (US)
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 1993-09
- Volume
- 268
- Issue
- 27
- Pages
- 20205-20210
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W1506729263
- Cited by
- 344
- References
- 62
- Citations by year
- 2026: 2 · 2025: 6 · 2024: 4 · 2023: 8 · 2022: 3 · 2021: 8 · 2020: 5 · 2019: 2 · 2018: 6 · 2017: 8 · 2016: 15 · 2015: 8 · 2014: 9 · 2013: 11 · 2012: 14
- FWCI
- 7.09
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Journal of Biological Chemistry (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (5p01ca028896-15, 5r35ca042507-07)
- National Cancer Institute (CA30199, CA 28896, CA-42507, P30CA030199)
- Topics
- Health Sciences › Medicine › Immunology and Allergy › Cell Adhesion Molecules Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Structural Characterization
- Physical Sciences › Materials Science › Surfaces, Coatings and Films › Polymer Surface Interaction Studies
- Keywords
- alpha5beta1 integrin, RGD peptide, fibronectin, integrin ligands, cyclic RGD peptide, phage display, cell adhesion, peptide library screening
- MeSH terms
- Amino Acid Sequence, Animals, Bacteriophages, Base Sequence, Binding, Competitive, Fibronectins, Cricetinae, Kinetics, Molecular Sequence Data, Oligodeoxyribonucleotides, Oligopeptides, Transfection, Gene Library, Integrins, Polymerase Chain Reaction, Databases, Factual, CHO Cells, Receptors, Fibronectin
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