Acyclic cyanamide-based inhibitors of cathepsin K
Copyright policy )Acyclic cyanamide-based inhibitors of cathepsin K
Conversion of the proline-derived cyanamide lead to an acyclic cyanamide capable of forming an additional hydrogen bond with cathepsin K resulted in a large increase in inhibitory activity. An X-ray structure of a co-crystal of a cyanamide with cathepsin K confirmed the enzyme interaction. Furthermore, a representative acyclic cyanamide inhibitor 6r was able to attenuate bone resorption in the rat calvarial model.
- GlaxoSmithKline (United States) United States
- Research Triangle Park Foundation United States
Models, Molecular, Cathepsin H, Binding Sites, Molecular Structure, Cathepsin L, Cathepsin K, Hydrogen Bonding, Cysteine Proteinase Inhibitors, Crystallography, X-Ray, Cathepsins, Cathepsin B, Cysteine Endopeptidases, Disease Models, Animal, Inhibitory Concentration 50, Cyanamide, Osteogenesis, Animals, Humans, Bone Resorption, Protein Binding
Models, Molecular, Cathepsin H, Binding Sites, Molecular Structure, Cathepsin L, Cathepsin K, Hydrogen Bonding, Cysteine Proteinase Inhibitors, Crystallography, X-Ray, Cathepsins, Cathepsin B, Cysteine Endopeptidases, Disease Models, Animal, Inhibitory Concentration 50, Cyanamide, Osteogenesis, Animals, Humans, Bone Resorption, Protein Binding
selected citations These citations are derived from selected sources.This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).29 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Average influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 10%
Citations provided by BIP!Popularity provided by BIP!