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Record W2045131958 · doi:10.1096/fj.14-264499

Solution NMR and calorimetric analysis of Rem2 binding to the Ca <sup>2+</sup> channel β4 subunit: a low affinity interaction is required for inhibition of Cav2.1 Ca <sup>2+</sup> currents

2015· article· en· W2045131958 on OpenAlexafffund
Xingfu Xu, Fang‐Xiong Zhang, Gerald W. Zamponi, William A. Horne

Bibliographic record

VenueThe FASEB Journal · 2015
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicIon channel regulation and function
Canadian institutionsUniversity of Calgary
FundersNational Institute of Neurological Disorders and StrokeNatural Sciences and Engineering Research Council of CanadaCanadian Institutes of Health ResearchAlberta Innovates - Health SolutionsNational Institutes of HealthNational Science Foundation
KeywordsProtein subunitMutantBinding siteChemistryBiophysicsIntracellularAllosteric regulationWild typeBiochemistryBiologyReceptorGene

Abstract

fetched live from OpenAlex

ABSTRACT Rem, Rad, Kir/Gem (RGK) proteins, including Rem2, mediate profound inhibition of high‐voltage activated Ca 2+ channels containing intracellular regulatory β subunits. All RGK proteins bind to voltage‐gated Ca 2+ channel β subunit (Cavβ) subunits in vitro , but the necessity of the interaction for current inhibition remains controversial. This study applies NMR and calorimetric techniques to map the binding site for Rem2 on human Cavβ4a and measure its binding affinity. Our experiments revealed 2 binding surfaces on the β4 guanylate kinase domain contributing to a 156 ± 18 μM K d interaction: a hydrophobic pocket lined by 4 critical residues (L173, N261, H262, and V303), mutation of any of which completely disrupted binding, and a nearby surface containing 3 residues (D206, L209, and D258) that when individually mutated decreased affinity. Voltage‐gated Ca 2+ channel α1A subunit (Cav2.1) Ca 2+ currents were completely inhibited by Rem2 when co‐expressed with wild‐type Cavβ4a, but were unaffected by Rem2 when coexpressed with a Cavβ4a site 1 (L173A/V303A) or site 2 (D258A) mutant. These results provide direct evidence for a low‐affinity Rem2/Cavβ4 interaction and show definitively that the interaction is required for Cav2.1 inhibition.—Xu, X., Zhang, F., Zamponi, G. W., Horne, W. A. Solution NMR and calorimetric analysis of Rem2 binding to the Ca 2+ channel β4 subunit: a low affinity interaction is required for inhibition of Cav2.1 Ca 2+ currents. FASEB J. 29, 1794‐1804 (2015). www.fasebj.org

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.001
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Simulation or modeling · Consensus signal: Simulation or modeling
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.052
Threshold uncertainty score0.470

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0010.001
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.047
GPT teacher head0.290
Teacher spread0.243 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designSimulation or modeling
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations8
Published2015
Admission routes2
Has abstractyes

Explore more

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