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Abstract PO-068: Efforts to define biochemical and pharmacologic pathways potentially beneficial to both cancer and COVID-19 patients

2020· article· en· W3091465868 on OpenAlexaff
Ugo Rovigatti, Amedeo Vannacci, Simone Del Corto, Ignacio Martín‐Loeches, Andrea Piccin, Nizar Naji, Carmel Mothersill

Bibliographic record

VenueClinical Cancer Research · 2020
Typearticle
Languageen
FieldMedicine
TopicPARP inhibition in cancer therapy
Canadian institutionsMcMaster UniversityUniversity of Windsor
Fundersnot available
KeywordsCancerMedicineOncogeneHydroxychloroquineDrug repositioningPharmacologyCoronavirus disease 2019 (COVID-19)DrugBioinformaticsBiologyCell cycleInternal medicineDisease

Abstract

fetched live from OpenAlex

Abstract Since COVID-19 infections have been frequently diagnosed in cancer patients, often associated with worst prognosis (1), an effort was conducted in order to identify biomolecular pathways and repurposable drugs, which could benefit patients for COVID-19 and cancer at the same time. Starting from over 3265 PubMed references, we have screened approximately 650 abstracts in order to identify the two most interesting pathways. Abstract were independently read and selected by UR and AV and then discussed in video conferences. Final decision on biochemical pathways or particular drugs was agreed only after identification of potential underlying molecular mechanism(s) for both COVID-19 and specific cancer types. Both impinge on the basic structure of 4-aminoquinoline, which is the alkaloid backbone of several important compounds effective in parasitology, rheumatology and cancer treatment. Their pharmacologic utilization was initiated with the discovery of quinine from the bark of the cinchona tree (1630) with further synthetic drugs developments such as chloroquine (CQ) and hydroxychloroquine (HCQ) in 1949-50, all variants of the 4-aminoquinoline family (2). 1. One pathway targets the PNP enzymes (purine nucleoside phosphorylases), dysregulation of which is often associated with apoptosis in cancer cells. PNP has been considered an oncogene, which is downregulated by tumor suppressors in PCa (miR-I; miR-133) (3). PNP inhibition has been demonstrated by strong binding of the aminoquinoline quinine through several MS technologies (4). We are investigating whether this is also true for COVID-19. 2. A second pathway is associated with HCQ usage. We have recently reviewed how HCQ at higher dosage could benefit COVID-19 patients, if they are treated in the earlier (or prophylactic) phases of the disease (5). Despite the wide publicity of HCQ negative effects, the results of Mehra et al. in Lancet have been recently questioned in an open letter on several scientific and ethical grounds and the paper has been finally retracted. Furthermore, there are still few and small RCTs testing this drug in the early disease phases. HCQ behaves as a weak base that is typically trapped inside the acidic environment of phagocytic organelle—such as lysosomes—thus raising their pH (2). Therefore, in the presence of lysosomotropic HCQ: 1. SARS-CoV-2 appears to be blocked inside lysosomes and devoid of the proteolytic cleavage required for infection (6) and 2. in cancer cells, the important mechanism of autophagy is strongly inhibited, causing tumor shrinkage or apoptosis (also in association with chemotherapy) (7). We are presently investigating HCQ effects in patients’ tumors explants or surrogate tissues. Our efforts in identifying molecular/pharmacologic pathways that could benefit patients for both COVID-19 and cancer led to the identification of at least two pathways, PNP and autophagy—both associated to 4-aminoquinoline derivatives—which are now being studied in experimental models. Citation Format: Ugo Rovigatti, Amedeo Vannacci, Simone Del Corto, Ignacio Martin-Loeches, Andrea Piccin, Nizar Naji, Carmel Mothersill. Efforts to define biochemical and pharmacologic pathways potentially beneficial to both cancer and COVID-19 patients [abstract]. In: Proceedings of the AACR Virtual Meeting: COVID-19 and Cancer; 2020 Jul 20-22. Philadelphia (PA): AACR; Clin Cancer Res 2020;26(18_Suppl):Abstract nr PO-068.

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)0.003
metaresearch head score (Gemma)0.007
Version: metacan-v3-hybrid-931329e0061cValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Not applicable · Consensus signal: none
GenreCandidate signal: Other · Consensus signal: none
Teacher disagreement score0.041
Threshold uncertainty score0.137

Distilled classifier scores by category (both heads)

CategoryCodexGemma
Metaresearch0.0030.007
Meta-epidemiology (narrow)0.0010.000
Meta-epidemiology (broad)0.0010.002
Bibliometrics0.0050.004
Science and technology studies0.0010.000
Scholarly communication0.0030.003
Open science0.0010.001
Research integrity0.0010.001
Insufficient payload (model declined to judge)0.0410.007

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 head0.327
GPT teacher head0.540
Teacher spread0.213 · 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 designNot applicable
Domainnot available
GenreOther

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

Citations1
Published2020
Admission routes1
Has abstractyes

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