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Impact of the structures of macrocyclic Michael acceptors on covalent proteasome inhibition.
Kitahata, S; Yakushiji, F; Ichikawa, S.
Afiliación
  • Kitahata S; Faculty of Pharmaceutical Sciences , Hokkaido University , Kita-12, Nishi-6, Kita-ku , Sapporo 060-0812 , Japan . Email: ichikawa@pharm.hokudai.ac.jp.
  • Yakushiji F; Faculty of Pharmaceutical Sciences , Hokkaido University , Kita-12, Nishi-6, Kita-ku , Sapporo 060-0812 , Japan . Email: ichikawa@pharm.hokudai.ac.jp.
  • Ichikawa S; Center for Research and Education on Drug Discovery , Hokkaido University , Kita-12, Nishi-6, Kita-ku , Sapporo 060-0812 , Japan.
Chem Sci ; 8(10): 6959-6963, 2017 Oct 01.
Article en En | MEDLINE | ID: mdl-29147522
Molecules that have a reactive functional group within a macrocycle represent a class of covalent inhibitor. The relationship between reactivity and affinity for the target is cooperative and complicated. An understanding and characterization of this class of inhibitor are vital for the development of covalent inhibitors as drug candidates. Herein, we describe a systematic analysis of structure-activity relationships using a series of syringolin analogues, which are irreversible covalent inhibitors of proteasomes. We investigate the detailed mechanistic effects of the macrocycles on affinity and reaction rate.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Chem Sci Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Chem Sci Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido