Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
ACS Med Chem Lett
; 6(1): 25-30, 2015 Jan 08.
Article
em En
| MEDLINE
| ID: mdl-25589925
ABSTRACT
Fragment-based drug design was successfully applied to maternal embryonic leucine zipper kinase (MELK). A low affinity (160 µM) fragment hit was identified, which bound to the hinge region with an atypical binding mode, and this was optimized using structure-based design into a low-nanomolar and cell-penetrant inhibitor, with a good selectivity profile, suitable for use as a chemical probe for elucidation of MELK biology.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Ano de publicação:
2015
Tipo de documento:
Article