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Record W3207372513 · doi:10.1126/sciadv.abh3794

Computational repurposing of therapeutic small molecules from cancer to pulmonary hypertension

2021· article· en· W3207372513 on OpenAlexaff
Vinny Negi, Jimin Yang, Gil Speyer, Andrés Pulgarin, Adam Handen, Jingsi Zhao, Yi‐Yin Tai, Ying Tang, Miranda K. Culley, Qiujun Yu, Patricia A. Forsythe, Anastasia Gorelova, Annie Watson, Yassmin Al Aaraj, Taijyu Satoh, Maryam Sharifi‐Sanjani, Arun Rajaratnam, John Sembrat, Steeve Provencher, Xianglin Yin, Sara O. Vargas, Mauricio Rojas, Sébastien Bonnet, Stéphanie Torrino, Bridget K. Wagner, Stuart L. Schreiber, Mingji Dai, Thomas Bertero, Imad Al Ghouleh, Seungchan Kim, Stephen Y. Chan

Bibliographic record

VenueScience Advances · 2021
Typearticle
Languageen
FieldComputer Science
TopicComputational Drug Discovery Methods
Canadian institutionsUniversité Laval
FundersNational Center for Advancing Translational SciencesNational Cancer InstituteNational Institutes of HealthGilead SciencesNational Heart, Lung, and Blood InstituteUniversity of PittsburghAmerican Heart Association
KeywordsDrug repositioningRepurposingPulmonary hypertensionCancerMedicineDrug discoveryDependency (UML)Computer scienceDrugBioinformaticsCardiologyInternal medicinePharmacologyBiologyArtificial intelligence

Abstract

fetched live from OpenAlex

Cancer therapies are being considered for treating rare noncancerous diseases like pulmonary hypertension (PH), but effective computational screening is lacking. Via transcriptomic differential dependency analyses leveraging parallels between cancer and PH, we mapped a landscape of cancer drug functions dependent upon rewiring of PH gene clusters. Bromodomain and extra-terminal motif (BET) protein inhibitors were predicted to rely upon several gene clusters inclusive of galectin-8 (LGALS8). Correspondingly, LGALS8 was found to mediate the BET inhibitor–dependent control of endothelial apoptosis, an essential role for PH in vivo. Separately, a piperlongumine analog’s actions were predicted to depend upon the iron-sulfur biogenesis gene ISCU. Correspondingly, the analog was found to inhibit ISCU glutathionylation, rescuing oxidative metabolism, decreasing endothelial apoptosis, and improving PH. Thus, we identified crucial drug-gene axes central to endothelial dysfunction and therapeutic priorities for PH. These results establish a wide-ranging, network dependency platform to redefine cancer drugs for use in noncancerous conditions.

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)0.000
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: Methods · Consensus signal: none
Teacher disagreement score0.356
Threshold uncertainty score0.442

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.002
Science and technology studies0.0000.000
Scholarly communication0.0000.001
Open science0.0010.000
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 head0.038
GPT teacher head0.329
Teacher spread0.291 · 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
GenreMethods

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

Citations37
Published2021
Admission routes1
Has abstractyes

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