- Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type i 1/2 kinase inhibitors
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Structure-based methods were used to design a potent and highly selective group II p21-activated kinase (PAK) inhibitor with a novel binding mode, compound 17. Hydrophobic interactions within a lipophilic pocket past the methionine gatekeeper of group II
- Staben, Steven T.,Feng, Jianwen A.,Lyle, Karen,Belvin, Marcia,Boggs, Jason,Burch, Jason D.,Chua, Ching-Ching,Cui, Haifeng,Dipasquale, Antonio G.,Friedman, Lori S.,Heise, Christopher,Koeppen, Hartmut,Kotey, Adrian,Mintzer, Robert,Oh, Angela,Roberts, David Allen,Rouge, Lionel,Rudolph, Joachim,Tam, Christine,Wang, Weiru,Xiao, Yisong,Young, Amy,Zhang, Yamin,Hoeflich, Klaus P.
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p. 1033 - 1045
(2014/03/21)
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- 6,5-HETEROCYCLIC PROPARGYLIC ALCOHOL COMPOUNDS AND USES THEREFOR
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The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
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