Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy

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Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy

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作者：Sebastian George Barton Furness¹ ; ^{sebastian.furness@monash.edu" class="auth_mail" title="E-mail the corresponding author} ; Yi-Lynn Liang¹ ; Cameron James Nowell¹ ; Michelle Louise Halls¹ ; Peter John Wookey² ; Emma Dal Maso¹ ; Asuka Inoue³ ; ⁴ ; Arthur Christopoulos¹ ; Denise Wootten¹ ; Patrick Michael Sexton¹ ; ⁵ ; ^{patrick.sexton@monash.edu" class="auth_mail" title="E-mail the corresponding author}
关键词：GPCR ; efficacy ; native PAGE ; calcitonin ; calcitonin receptor ; CTR ; BRET ; TIRF ; FRET ; G protein-coupled receptor
刊名：Cell
出版年：2016
出版时间：20 October 2016
年：2016
卷：167
期：3
页码：739-749.e11
全文大小：5059 K

文摘

•: Ligands stabilize distinct calcitonin receptor conformations
•: Distinct ligand-promoted receptor complexes stabilize specific effector conformations
•: Differential effector conformation contributes to ligand efficacy

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