Probing the structural requirements of non-electrophilic naphthalene-based Nrf2 activators
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- 作者：Atul D. Jaina ; Haranatha Pottetib ; 1 ; Benjamin G. Richardsona ; 1 ; Laura Kingsleyd ; Julia P. Lucianoc ; Aya F. Ryuzojic ; Hyun Leea ; Aleksej Krunica ; Andrew D. Mesecarc ; d ; Sekhar P. Reddyb ; e ; Terry W. Moorea ; e ; twmoore@uic.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：Nrf2 ; Keap1 ; Protein&ndash ; protein interaction ; Transcription factor ; Cul3 ; Keap1/Nrf2 interaction
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2015
- 出版时间：20 October 2015
- 年：2015
- 卷：103
- 期：Complete
- 页码：252-268
- 全文大小：2161 K
文摘
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Neutral substituents can replace charged carboxylate groups.
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Crystal structure of amide 12e bound to Kelch domain.
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Unsymmetrically substituted analogs can have high affinity for the Kelch domain.
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Binding site waters can be displaced without incurring a large energetic penalty.