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Record W3032373991 · doi:10.1371/journal.pcbi.1007926

In silico analysis of hypoxia activated prodrugs in combination with anti angiogenic therapy through nanocell delivery

2020· article· en· W3032373991 on OpenAlexafffund
Cameron Meaney, Sander Rhebergen, Mohammad Kohandel

Bibliographic record

VenuePLoS Computational Biology · 2020
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicCancer, Hypoxia, and Metabolism
Canadian institutionsUniversity of Waterloo
FundersNatural Sciences and Engineering Research Council of CanadaCanadian Institutes of Health Research
KeywordsHypoxia (environmental)ProdrugIn silicoDrugPharmacologyTirapazamineDrug deliveryCombination therapyAdverse effectMedicineComputational biologyBioinformaticsChemistryBiologyCytotoxicityIn vitro

Abstract

fetched live from OpenAlex

Tumour hypoxia is a well-studied phenomenon with implications in cancer progression, treatment resistance, and patient survival.While a clear adverse prognosticator, hypoxia is also a theoretically ideal target for guided drug delivery.This idea has lead to the development of hypoxia-activated prodrugs (HAPs): a class of chemotherapeutics which remain inactive in the body until metabolized within hypoxic regions.In theory, these drugs have the potential for increased tumour selectivity and have therefore been the focus of numerous preclinical studies.Unfortunately, HAPs have had mixed results in clinical trials, necessitating further study in order to harness their therapeutic potential.One possible avenue for the improvement of HAPs is through the selective application of anti angiogenic agents (AAs) to improve drug delivery.Such techniques have been used in combination with other conventional chemotherapeutics to great effect in many studies.A further benefit is theoretically achieved through nanocell administration of the combination, though this idea has not been the subject of any experimental or mathematical studies to date.In the following, a mathematical model is outlined and used to compare the predicted efficacies of separate vs. nanocell administration for AAs and HAPs in tumours.The model is experimentally motivated, both in mathematical form and parameter values.Preliminary results of the model are highlighted throughout which qualitatively agree with existing experimental evidence.The novel prediction of our model is an improvement in the efficacy of AA/HAP combination therapies when administered through nanocells as opposed to separately.While this study specifically models treatment on glioblastoma, similar analyses could be performed for other vascularized tumours, making the results potentially applicable to a range of tumour types. Author summaryTumour hypoxia is a well-documented phenomenon with adverse effects for the progression of the cancer.Accordingly, various therapeutic strategies have emerged in recent years to combat its effects.Herein, we present an experimentally-motivated mathematical model used to assess the feasibility of the therapeutic combination of anti angiogenic agents with hypoxia-activated prodrugs.Analysis of the combination therapy shows that

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 machine prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.001
Version: metacan-v3-hybrid-931329e0061cValidation 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 score0.006
Threshold uncertainty score0.013

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0000.001
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0010.001
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0010.000
Open science0.0000.000
Research integrity0.0010.000
Insufficient payload (model declined to judge)0.0020.000

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 head0.018
GPT teacher head0.248
Teacher spread0.230 · 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 source (direct Gemma or distilled Codex), 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

Citations18
Published2020
Admission routes2
Has abstractyes

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