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Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).
Asquith, Christopher R M; Treiber, Daniel K; Zuercher, William J.
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  • Asquith CRM; Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA; Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA. Electronic address: chris.asquith@unc.edu.
  • Treiber DK; Eurofins DiscoverX, 42501 Albrae Street, Fremont, CA 94538, USA.
  • Zuercher WJ; Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA. Electronic address: william.zuercher@unc.edu.
Bioorg Med Chem Lett ; 29(14): 1727-1731, 2019 07 15.
Article en En | MEDLINE | ID: mdl-31129055
We demonstrate an innovative approach for optimization of kinase inhibitor potency and selectivity utilising kinase mini-panels and kinome-wide panels. We present a focused case study on development of a selective inhibitor of cyclin G associated kinase (GAK) using the quin(az)oline inhibitor chemotype. These results exemplify a versatile, efficient approach to drive kinome selectivity during inhibitor development programs.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Quinolinas / Inhibidores de Proteínas Quinasas / Ciclina G Tipo de estudio: Risk_factors_studies Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Quinolinas / Inhibidores de Proteínas Quinasas / Ciclina G Tipo de estudio: Risk_factors_studies Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2019 Tipo del documento: Article