ChemMedChem · 2012 · 71 citations · 11 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoveryEnzymologyEnzyme InhibitionMacrocyclic Drug DesignPeptide Drug DiscoveryPeptidomimetic DesignProteolytic EnzymesBicyclic Peptide DesignMacrocyclic InhibitorsMacrocyclic Peptide LibrariesMacrocyclic PeptidesMacrocyclic PeptidomimeticsPeptide MacrocyclizationPeptidomimetic MacrocyclesRing Size Effects
Picky push-bikes! Bicyclic peptides with low to sub-nanomolar inhibitory activities towards the serine protease plasma kallikrein were developed. By modulating the size of the macrocyclic rings, inhibitors with the desired specificity profile could be generated.
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Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists
Beili Wu, Ellen Y. T. Chien, Clifford D. Mol et al. · Science · 2010 · 1.8K citations