Structures of highly flexible intracellular domain of human α7 nicotinic acetylcholine receptor

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作者
Vasyl Bondarenko
Marta M. Wells
Qiang Chen
Tommy S. Tillman
Kevin Singewald
Matthew J. Lawless
Joel Caporoso
Nicole Brandon
Jonathan A. Coleman
Sunil Saxena
Erik Lindahl
Yan Xu
Pei Tang
机构
[1] University of Pittsburgh,Depatment of Anesthesiology and Perioperative Medicine
[2] University of Pittsburgh,Department of Chemistry
[3] University of Pittsburgh,Department of Structural Biology
[4] Stockholm University,Department of Biochemistry and Biophysics, Science for Life Laboratory
[5] KTH Royal Institute of Technology,Department of Applied Physics, Swedish e
[6] University of Pittsburgh,Science Research Center
[7] University of Pittsburgh,Department of Pharmacology and Chemical Biology
[8] University of Pittsburgh,Department of Physics and Astronomy
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The intracellular domain (ICD) of Cys-loop receptors mediates diverse functions. To date, no structure of a full-length ICD is available due to challenges stemming from its dynamic nature. Here, combining nuclear magnetic resonance (NMR) and electron spin resonance experiments with Rosetta computations, we determine full-length ICD structures of the human α7 nicotinic acetylcholine receptor in a resting state. We show that ~57% of the ICD residues are in highly flexible regions, primarily in a large loop (loop L) with the most mobile segment spanning ~50 Å from the central channel axis. Loop L is anchored onto the MA helix and virtually forms two smaller loops, thereby increasing its stability. Previously known motifs for cytoplasmic binding, regulation, and signaling are found in both the helices and disordered flexible regions, supporting the essential role of the ICD conformational plasticity in orchestrating a broad range of biological processes.
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