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Record W4389452401 · doi:10.1002/pro.4857

A naturally occurring <scp>G11S</scp> mutation in the <scp>3C</scp>‐like protease from the <scp>SARS‐CoV</scp>‐2 virus dramatically weakens the dimer interface

2023· article· en· W4389452401 on OpenAlexafffund
Guanyu Wang, Felipe A. Venegas, Andrés M. Rueda, Nuwani W. Weerasinghe, Kevin A. Uggowitzer, Christopher J. Thibodeaux, Nicolas Moitessier, Anthony Mittermaier

Bibliographic record

VenueProtein Science · 2023
Typearticle
Languageen
FieldComputer Science
TopicComputational Drug Discovery Methods
Canadian institutionsMcGill University
FundersFonds de Recherche du Québec - SantéNatural Sciences and Engineering Research Council of CanadaFonds de recherche du Québec – Nature et technologiesCanadian Institutes of Health Research
KeywordsSerine proteaseProteaseDimerMutationViral replicationSerineBiologyEnzymeSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2)ChemistryProteasesBiochemistryComputational biologyCell biologyVirusVirologyCoronavirus disease 2019 (COVID-19)Gene

Abstract

fetched live from OpenAlex

Abstract The 3C‐like protease (3CL pro ) is crucial to the replication of SARS‐CoV‐2, the causative agent of COVID‐19, and is the target of several successful drugs including Paxlovid and Xocova. Nevertheless, the emergence of viral resistance underlines the need for alternative drug strategies. 3CL pro only functions as a homodimer, making the protein–protein interface an attractive drug target. Dimerization is partly mediated by a conserved glycine at position 11. However, some naturally occurring SARS‐CoV‐2 sequences contain a serine at this position, potentially disrupting the dimer. We have used concentration‐dependent activity assays and mass spectrometry to show that indeed the G11S mutation reduces the stability of the dimer by 600‐fold. This helps to set a quantitative benchmark for the minimum potency required of any future protein–protein interaction inhibitors targeting 3CL pro and raises interesting questions regarding how coronaviruses bearing such weakly dimerizing 3CL pro enzymes are capable of replication.

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)0.010
metaresearch head score (Gemma)0.018
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesMetaresearch, Meta-epidemiology (narrow), Science and technology studies, Scholarly communication, Open science
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Simulation or modeling · Consensus signal: none
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.661
Threshold uncertainty score1.000

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0100.018
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.007
Science and technology studies0.0020.001
Scholarly communication0.0030.003
Open science0.0090.003
Research integrity0.0000.001
Insufficient payload (model declined to judge)0.0000.001

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 head0.033
GPT teacher head0.321
Teacher spread0.288 · 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.

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

Citations6
Published2023
Admission routes2
Has abstractyes

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