Small Molecule Drug A-769662 and AMP Synergistically Activate Naive AMPK Independent of Upstream Kinase Signaling
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- 作者：John W. Scott1 ; jscott@svi.edu.au" class="auth_mail ; Naomi Ling1 ; Samah M.A. Issa1 ; Toby A. Dite1 ; Matthew T. O&rsquo ; Brien1 ; Zhi-Ping Chen1 ; Sandra Galic1 ; Christopher G. Langendorf1 ; Gregory R. Steinberg2 ; Bruce E. Kemp1 ; Jonathan S. Oakhill1 ; joakhill@svi.edu.au" class="auth_mail
- 刊名：Chemistry & Biology
- 出版年：22 May 2014
- 年：2014
- 卷：21
- 期：5
- 页码：619-627
- 全文大小：1508 K
文摘
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尾-Ser108 phosphorylation is entirely sufficient for AMPK activation by A-769662
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Exchange of 尾-Ser108 for Glu provides an ultrasensitive construct for drug screens
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AMPK 尾-Ser108 is a cis-autophosphorylation site
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AMP and A-769662 synergistically activate fully dephosphorylated AMPK ∼1,000-fold