ReviewJournal of medicinal chemistry2019
Recent Progress in the Discovery of Allosteric Inhibitors of Kidney-Type Glutaminase.
Review in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 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
22 citing papers in PubMed, 1 synthesis or guideline pooled it, 53 citations in OpenAlex.
- An Insight into the Medicinal Chemistry Perspective of Macrocyclic Derivatives with Antitumor Activity: A Systematic Review.Molecules (Basel, Switzerland) · 2022Pooled it
- Glutamine metabolism in health and disease.Signal transduction and targeted therapy · 2026Review
- Article
- Review
- Dynamic crosstalk between amino acid metabolism and cancer drug efficacy: From mechanisms to therapeutic opportunities.iScience · 2025Review
- Glycogenesis and glyconeogenesis from glutamine, lactate and glycerol support human macrophage functions.EMBO reports · 2024Article
- Cellular metabolism: A key player in cancer ferroptosis.Cancer communications (London, England) · 2024Review
- Synthesis of 1,3,4-Thiadiazole Derivatives and Their Anticancer Evaluation.International journal of molecular sciences · 2023Article
- Biomolecular condensates in kidney physiology and disease.Nature reviews. Nephrology · 2023Review
- Kidney-type glutaminase is a biomarker for the diagnosis and prognosis of hepatocellular carcinoma: a prospective study.BMC cancer · 2023Article
- Diselenide Covalent Allosteric Inhibitors of Glutaminase with StrongACS medicinal chemistry letters · 2023Article
- The pyridazine heterocycle in molecular recognition and drug discovery.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2023Review
- Methanodibenzo[Cancers · 2023Article
- Prognostic value of glutaminase 1 in breast cancer depends on H3K27me3 expression and menopausal status.Virchows Archiv : an international journal of pathology · 2022Article
- Regulation of Ferroptosis by Amino Acid Metabolism in Cancer.International journal of biological sciences · 2022Review
- Targeting the Proline-Glutamine-Asparagine-Arginine Metabolic Axis in Amino Acid Starvation Cancer Therapy.Pharmaceuticals (Basel, Switzerland) · 2021Review
- 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
- GAC inhibitors with a 4-hydroxypiperidine spacer: Requirements for potency.Bioorganic & medicinal chemistry letters · 2019Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Kidney-type glutaminase (GLS), the first enzyme in the glutaminolysis pathway, catalyzes the hydrolysis of glutamine to glutamate. GLS was found to be upregulated in many glutamine-dependent cancer cells. Therefore, selective inhibition of GLS has gained substantial interest as a therapeutic approach targeting cancer metabolism. Bis-2-[5-(phenylacetamido)-1,3,4-thiadiazol-2-yl]ethyl sulfide (BPTES), despite its poor physicochemical properties, has served as a key molecular template in subsequent efforts to identify more potent and drug-like allosteric GLS inhibitors. This review article provides an overview of the progress made to date in the development of GLS inhibitors and highlights the remarkable transformation of the unfavorable lead into "druglike" compounds guided by systematic SAR studies.
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.