PUBLICATION

Estimating the true stability of the prehydrolytic outward-facing state in an ABC protein

Authors
Simon, M.A., Iordanov, I., Szollosi, A., Csanády, L.
ID
ZDB-PUB-231013-48
Date
2023
Source
eLIFE   12: (Journal)
Registered Authors
Keywords
D-loop, composite ATP-binding site, flickery closure, molecular biophysics, mutant cycle, structural biology, xenopus, zebrafish
MeSH Terms
  • Cystic Fibrosis Transmembrane Conductance Regulator*/metabolism
  • Catalytic Domain
  • Adenosine Triphosphate*/metabolism
  • Humans
  • Mutation
  • Ion Channel Gating
PubMed
37782012 Full text @ Elife
Abstract
CFTR, the anion channel mutated in cystic fibrosis patients, is a model ABC protein whose ATP-driven conformational cycle is observable at single-molecule level in patch-clamp recordings. Bursts of CFTR pore openings are coupled to tight dimerization of its two nucleotide-binding domains (NBDs) and in wild-type (WT) channels are mostly terminated by ATP hydrolysis. The slow rate of non-hydrolytic closure - which determines how tightly bursts and ATP hydrolysis are coupled - is unknown, as burst durations of catalytic site mutants span a range of ~200-fold. Here, we show that Walker A mutation K1250A, Walker B mutation D1370N, and catalytic glutamate mutations E1371S and E1371Q all completely disrupt ATP hydrolysis. True non-hydrolytic closing rate of WT CFTR approximates that of K1250A and E1371S. That rate is slowed ~15-fold in E1371Q by a non-native inter-NBD H-bond, and accelerated ~15-fold in D1370N. These findings uncover unique features of the NBD interface in human CFTR.
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