Next Article in Journal
Lipophilic Toxin Profile in Mytilus galloprovincialis during Episodes of Diarrhetic Shellfish Poisoning (DSP) in the N.E. Adriatic Sea in 2006
Next Article in Special Issue
Efficient In Vivo Selection of a Novel Tumor-Associated Peptide from a Phage Display Library
Previous Article in Journal
Enhancement of Diepoxin ζ Production by Yeast Extract and Its Fractions in Liquid Culture of Berkleasmium-Like Endophytic Fungus Dzf12 from Dioscorea zingiberensis
Previous Article in Special Issue
Phage Display: Selecting Straws Instead of a Needle from a Haystack
Article Menu

Article Versions

Export Article

Open AccessReview
Molecules 2011, 16(1), 857-887;

Peptide Phage Display as a Tool for Drug Discovery: Targeting Membrane Receptors

Department of Pharmaceutical Biology, Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, SI-1000 Ljubljana, Slovenia
Department of Biotechnology, Jozef Stefan Institute, Jamova 39, SI-1000 Ljubljana, Slovenia
Author to whom correspondence should be addressed.
Received: 7 December 2010 / Revised: 14 January 2011 / Accepted: 19 January 2011 / Published: 21 January 2011
(This article belongs to the Special Issue Phage Display of Combinatorial Libraries)
PDF [338 KB, uploaded 18 June 2014]   |  


Ligands selected from phage-displayed random peptide libraries tend to be directed to biologically relevant sites on the surface of the target protein. Consequently, peptides derived from library screenings often modulate the target protein’s activity in vitro and in vivo and can be used as lead compounds in drug design and as alternatives to antibodies for target validation in both genomics and drug discovery. This review discusses the use of phage display to identify membrane receptor modulators with agonistic or antagonistic activities. Because isolating or producing recombinant membrane proteins for use as target molecules in library screening is often impossible, innovative selection strategies such as panning against whole cells or tissues, recombinant receptor ectodomains, or neutralizing antibodies to endogenous binding partners were devised. Prominent examples from a two-decade history of peptide phage display will be presented, focusing on the design of affinity selection experiments, methods for improving the initial hits, and applications of the identified peptides.
Keywords: membrane receptors; agonists; antagonists; peptides; phage display membrane receptors; agonists; antagonists; peptides; phage display

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Share & Cite This Article

MDPI and ACS Style

Molek, P.; Strukelj, B.; Bratkovic, T. Peptide Phage Display as a Tool for Drug Discovery: Targeting Membrane Receptors. Molecules 2011, 16, 857-887.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top