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Back Cover: Design and Development of a Cyclic Decapeptide Scaffold with Suitable Properties for Bioavailability and Oral Exposure (ChemMedChem 10/2016)
Author(s) -
Fouché Marianne,
Schäfer Michael,
Berghausen Jörg,
Desrayaud Sandrine,
Blatter Markus,
Piéchon Philippe,
Dix Ina,
Martin Garcia Aimar,
Roth HansJörg
Publication year - 2016
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201600230
Subject(s) - chemistry , bioavailability , cyclic peptide , scaffold , solubility , combinatorial chemistry , organic chemistry , biochemistry , pharmacology , computer science , peptide , database , medicine
The back cover picture shows the preferred conformations, obtained via NMR spectroscopy, of a cyclic decapeptide in both polar and apolar environment. Based on an engineered scaffold that combines two opposite β‐turns to favor a rigid β‐hairpin conformation and a specific N‐methylation pattern, we were able to prepare cyclic decapeptides that, despite being outside of Lipinski′s rule of five, exhibit excellent permeability and pharmacokinetic properties. With bioavailability as high as 100%, low in vivo clearance, and good solubility, these cyclic decapeptides prove that drug‐like properties can be achieved with this class of compounds, opening therefore a path forward for the development of new therapeutics. More information can be found in the Full Papers by Marianne Fouché et al. on page 1048 and page 1060 in Issue 10, 2016 (DOI: 10.1002/cmdc.201600082 and DOI: 10.1002/cmdc.201600083).