ArticleJournal of cancer research and clinical oncology2014
Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models.
Article in Journal of cancer research and clinical oncology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It has been retracted, and should not be counted. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 44 citations in OpenAlex.
- Metabolic reprogramming-mediated therapeutic resistance in renal cell carcinoma: Mechanisms and targeted intervention strategies.iScience · 2026Review
- A network medicine framework for multi-modal data integration in therapeutic target discovery.Communications chemistry · 2026Article
- The Role of the TG2-GPR56 Complex in Cutaneous Squamous Cell Carcinoma (CSCC) Aggression and Therapeutic Resistance.International journal of molecular sciences · 2026Review
- Transglutaminase 2 exacerbates ovarian cancer survival by directly inactivating GSK3β.Cell death & disease · 2026Article
- Pharmacological transglutaminase 2 inhibition enhances temozolomide response in patient-derived glioblastoma tumorspheres.Journal of neuro-oncology · 2026Article
- Synthesis and Biological Activity of Guanidine Scaffold: A Comprehensive Review.Anti-inflammatory & anti-allergy agents in medicinal chemistry · 2026Review
- Targeting the Primordial Chaperone to Overcome Acquired Drug Resistance in Cancer: TG2-Mediated Autophagy.Biomolecules & therapeutics · 2026Review
- CTCF Is Essential for the Development and Maintenance of CALM-AF10-Induced Leukemia.Cancer science · 2025Article
- Discovery and Characterization of PROTACs Targeting Tissue Transglutaminase (TG2).Journal of medicinal chemistry · 2023Article
- The transglutaminase 2 cancer cell survival factor maintains mTOR activity to drive an aggressive cancer phenotype.Molecular carcinogenesis · 2023Article
- Transglutaminase 2 regulates terminal erythroid differentiation via cross-linking activity.Frontiers in cell and developmental biology · 2023Article
- A Multidisciplinary Approach Establishes a Link between Transglutaminase 2 and the Kv10.1 Voltage-Dependent KCancers · 2022Article
- Immune subtyping for pancreatic cancer with implication in clinical outcomes and improving immunotherapy.Cancer cell international · 2021Article
- Transglutaminase 2-Mediated p53 Depletion Promotes Angiogenesis by Increasing HIF-1α-p300 Binding in Renal Cell Carcinoma.International journal of molecular sciences · 2020Article
- Article
- A Precision Strategy to Cure Renal Cell Carcinoma by Targeting Transglutaminase 2.International journal of molecular sciences · 2020Review
- Transglutaminase 2 takes center stage as a cancer cell survival factor and therapy target.Molecular carcinogenesis · 2019Article
- Transglutaminase 2: The Maestro of the Oncogenic Mediators in Renal Cell Carcinoma.Medical sciences (Basel, Switzerland) · 2019Review
- Transglutaminase 2 Promotes Autophagy by LC3 Induction through p53 Depletion in Cancer Cell.Biomolecules & therapeutics · 2019Article
- Renal Cell Carcinoma Is Abrogated by p53 Stabilization through Transglutaminase 2 Inhibition.Cancers · 2018Article
Corrections and comments
- Reinstatement · 2015-01-01Date of Article and/or Notice Unknown · Duplication of/in Article ·
Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo test whether transglutaminase 2 (TGase 2) inhibitor GK921 alone reverses renal cell carcinoma (RCC) tumor growth. RCC is resistant to both radiation and chemotherapy, and the prognosis remains poor. Despite the recent therapeutic success of vascular endothelial growth factor inhibition in RCC, approximately one-third of RCC patients develop metastatic disease. The expression of TGase 2 is markedly increased in most RCC cell lines, as well as in clinical samples.
methodsPreviously, we introduced the quinoxaline derivative GK13 as a lead compound for TGase 2 inhibitor. The inhibitory effect of GK13 on TGase 2 was improved in GK921 (3-(phenylethynyl)-2-(2-(pyridin-2-yl)ethoxy)pyrido[3,2-b]pyrazine). GK921 efficacy was tested using sulforhodamine in vitro as well as a xenograft tumor models using ACHN and CAKI-1 RCC cells.
resultsGK921 showed cytotoxicity to RCC (average GI50 in eight RCC cell lines: 0.905 μM). A single treatment with GK921 almost completely reduced tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models.
conclusionTGase 2 inhibitor GK921 abrogates RCC growth in xenograft tumor models, suggesting the possibility of a new therapeutic approach to RCC.
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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.