Thiophene inhibitors of PDE4: crystal structures show a second binding mode at the catalytic domain of PDE4D2.
Bioorg Med Chem Lett
; 21(23): 7089-93, 2011 Dec 01.
Article
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| MEDLINE
| ID: mdl-22030030
ABSTRACT
PDE4 inhibitors have been identified as therapeutic targets for a variety of conditions, particularly inflammatory diseases. We have serendipitously identified a novel class of phosphodiesterase 4 (PDE4) inhibitor during a study to discover antagonists of the parathyroid hormone receptor. X-ray crystallographic studies of PDE4D2 complexed to four potent inhibitors reveal the atomic details of how they inhibit the enzyme and a notable contrast to another recently reported thiophene-based inhibitor.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Tiofenos
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Modelos Moleculares
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Fosfodiesterasas de Nucleótidos Cíclicos Tipo 4
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Inhibidores de Fosfodiesterasa 4
Idioma:
En
Año:
2011
Tipo del documento:
Article