The Future of Peptide-based Drugs

Craik, David J., Fairlie, David P., Liras, Spiros and Price, David (2013) The Future of Peptide-based Drugs. Chemical Biology and Drug Design, 81 1: 136-147. doi:10.1111/cbdd.12055

Author Craik, David J.
Fairlie, David P.
Liras, Spiros
Price, David
Title The Future of Peptide-based Drugs
Journal name Chemical Biology and Drug Design   Check publisher's open access policy
ISSN 1747-0277
Publication date 2013-01
Year available 2012
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1111/cbdd.12055
Volume 81
Issue 1
Start page 136
End page 147
Total pages 12
Place of publication Malden, MA United States
Publisher Wiley-Blackwell Publishing
Collection year 2014
Language eng
Formatted abstract
The suite of currently used drugs can be divided into two categories - traditional 'small molecule' drugs with typical molecular weights of <500Da but with oral bioavailability, and much larger 'biologics' typically >5000Da that are not orally bioavailable and need to be delivered via injection. Due to their small size, conventional small molecule drugs may suffer from reduced target selectivity that often ultimately manifests in human side-effects, whereas protein therapeutics tend to be exquisitely specific for their targets due to many more interactions with them, but this comes at a cost of low bioavailability, poor membrane permeability, and metabolic instability. The time has now come to reinvestigate new drug leads that fit between these two molecular weight extremes, with the goal of combining advantages of small molecules (cost, conformational restriction, membrane permeability, metabolic stability, oral bioavailability) with those of proteins (natural components, target specificity, high potency). This article uses selected examples of peptides to highlight the importance of peptide drugs, some potential new opportunities for their exploitation, and some difficult challenges ahead in this field.
Keyword Conformation
Cyclic peptides
Oral Bioavailability
Peptide scaffolds
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ
Additional Notes Article first published online: 17 DEC 2012

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Official 2014 Collection
Institute for Molecular Bioscience - Publications
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