ArticleBioorganic & medicinal chemistry2016
Design and evaluation of novel glutaminase inhibitors.
Article in Bioorganic & medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers, 1 of them a synthesis that pooled 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.
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.
Who cites it
25 citing papers in PubMed, 1 synthesis or guideline pooled it, 72 citations in OpenAlex.
- Frontiers and hot topics in tumor metabolic reprogramming: a bibliometric analysis from 2014 to 2023.Frontiers in oncology · 2025Pooled it
- SUCLG2 contributes to platinum resistance in lung adenocarcinoma through enhancing succinylation of GAC and glutamine metabolism.Apoptosis : an international journal on programmed cell death · 2026Article
- Glutaminase inhibition as potential cancer therapeutics: current status and future applications.Journal of enzyme inhibition and medicinal chemistry · 2024Review
- Review
- Alone and together: current approaches to targeting glutaminase enzymes as part of anti-cancer therapies.Future drug discovery · 2023Review
- Glutaminolysis and peripheral CD4Frontiers in immunology · 2023Review
- Mechanistic Insights into Biological Activities of Polyphenolic Compounds from Rosemary Obtained by Inverse Molecular Docking.Foods (Basel, Switzerland) · 2021Article
- High-Throughput Screening Reveals New Glutaminase Inhibitor Molecules.ACS pharmacology & translational science · 2021Article
- Molecular modeling and LC-MS-based metabolomics of a glutamine-valproic acid (Gln-VPA) derivative on HeLa cells.Molecular diversity · 2021Article
- Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.Journal of medicinal chemistry · 2020Article
- Allosteric kidney-type glutaminase (GLS) inhibitors with a mercaptoethyl linker.Bioorganic & medicinal chemistry · 2020Article
- Thiadiazole derivatives as anticancer agents.Pharmacological reports : PR · 2020Review
- Pyruvate anaplerosis is a mechanism of resistance to pharmacological glutaminase inhibition in triple-receptor negative breast cancer.BMC cancer · 2020Article
- Metabolic plasticity of IDH1Cancer & metabolism · 2020Article
- GAC inhibitors with a 4-hydroxypiperidine spacer: Requirements for potency.Bioorganic & medicinal chemistry letters · 2019Article
- The 'Achilles Heel' of Metabolism in Renal Cell Carcinoma: Glutaminase Inhibition as a Rational Treatment Strategy.Kidney cancer (Clifton, Va.) · 2019Review
- Recent Progress in the Discovery of Allosteric Inhibitors of Kidney-Type Glutaminase.Journal of medicinal chemistry · 2019Review
- Targeting androgen receptor-independent pathways in therapy-resistant prostate cancer.Asian journal of urology · 2019Review
- Characterization of the interactions of potent allosteric inhibitors with glutaminase C, a key enzyme in cancer cell glutamine metabolism.The Journal of biological chemistry · 2018Article
- Endothelial Cell Metabolism.Physiological reviews · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
14 authors at 3 institutions in 1 country.
Funding
Abstract
A novel set of GAC (kidney glutaminase isoform C) inhibitors able to inhibit the enzymatic activity of GAC and the growth of the triple negative MDA-MB-231 breast cancer cells with low nanomolar potency is described. Compounds in this series have a reduced number of rotatable bonds, improved ClogPs, microsomal stability and ligand efficiency when compared to the leading GAC inhibitors BPTES and CB-839. Property improvements were achieved by the replacement of the flexible n-diethylthio or the n-butyl moiety present in the leading inhibitors by heteroatom substituted heterocycloalkanes.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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.