Evidence map›Paper›PMID 38942129›Full record

ArticleBioorganic & medicinal chemistry letters2024

Ophiobolin A derivatives with enhanced activities under tumor-relevant acidic conditions.

Vladimir A Maslivetc, Md Nabiul Hasan, Angela Boari, Arben Zejnelovski, Antonio Evidente, Dandan Sun, Alexander Kornienko

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed.

  1. Review
  2. Article
  3. Article
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors.

Vladimir A MaslivetcDepartment of Chemistry and Biochemistry, Texas State University, 601 University Dr., San Marcos, TX 78666, USA.
Md Nabiul HasanDepartment of Neurology, University of Pittsburgh, 3501 Fifth Ave, Pittsburgh, PA 15260, USA.
Angela BoariInstitute of Sciences of Food Production, National Research Council, Via Amendola 122/O, 70125 Bari, Italy.
Arben ZejnelovskiDepartment of Chemistry and Biochemistry, Texas State University, 601 University Dr., San Marcos, TX 78666, USA.
Antonio EvidenteInstitute of Biomolecular Chemistry, National Research Council, Via Campi Flegrei 34, 80078 Pozzuoli, Italy.
Dandan SunDepartment of Neurology, University of Pittsburgh, 3501 Fifth Ave, Pittsburgh, PA 15260, USA; Research Service, Veterans Affairs Pittsburgh Health Care System, Pittsburgh, PA, USA.
Alexander KornienkoDepartment of Chemistry and Biochemistry, Texas State University, 601 University Dr., San Marcos, TX 78666, USA. Electronic address: a_k76@txstate.edu.

Funding

Acid-Sensitive Glioblastoma Prodrugs Derived from Ophiobolin AR15CA227680 · NCI · TEXAS STATE UNIVERSITY · PI KORNIENKO, ALEXANDER · 2019 to 2019
$462k
BLRD Research Career Scientist Award ApplicationIK6BX005647 · VA · VETERANS HEALTH ADMINISTRATION · PI Dandan Sun · 2021 to 2026
–
BLRD VA IK6 BX005647NCI NIH HHS R15 CA227680
6 · The paper itself

Abstract

Glioblastoma (GBM) is the most common form of malignant primary brain tumor and is one of the most lethal cancers. The difficulty in treating GBM stems from its highly developed mechanisms of drug resistance. Our research team has recently identified the fungal secondary metabolite ophiobolin A (OpA) as an agent with significant activity against drug-resistant GBM cells. However, the OpA's mode of action is likely based on covalent modification of its intracellular target(s) and thus possible off-target reactivity needs to be addressed. This work involves the investigation of an acid-sensitive OpA analogue approach that exploits the elevated acidity of the GBM microenvironment to enhance the selectivity for tumor targeting. This project identified analogues that showed selectivity at killing GBM cells grown in cultures at reduced pH compared to those maintained under normal neutral conditions. These studies are expected to facilitate the development of OpA as an anti-GBM agent by investigating its potential use in an acid-sensitive analogue form with enhanced selectivity for tumor targeting.

Indexed as

Antineoplastic AgentsSesterterpenesBrain NeoplasmsCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorGlioblastomaHumansHydrogen-Ion ConcentrationMolecular StructureStructure-Activity RelationshipAntineoplastic Agentsophiobolin ASesterterpenesAcetal prodrugFungal metaboliteGlioma stem cellPaal-KnorrTumor microenvironment

Identifiers

PMID38942129
PMCPMC11646455

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.