Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.
Bioorg Med Chem Lett
; 17(6): 1765-8, 2007 Mar 15.
Article
em En
| MEDLINE
| ID: mdl-17239592
ABSTRACT
A series of non-covalent inhibitors of the serine protease dipeptidyl peptidase IV (DPP-IV) were found to adopt a U-shaped binding conformation in X-ray co-crystallization studies. Remarkably, Tyr547 undergoes a 70 degrees side-chain rotation to accommodate the inhibitor and allows access to a previously unexposed area of the protein backbone for hydrogen bonding.
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Bases de dados:
MEDLINE
Assunto principal:
Inibidores de Proteases
/
Inibidores da Dipeptidil Peptidase IV
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2007
Tipo de documento:
Article
País de afiliação:
Estados Unidos