ArticleScientific reports2015
PI3Kβ inhibitor TGX221 selectively inhibits renal cell carcinoma cells with both VHL and SETD2 mutations and links multiple pathways.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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29 citing papers in PubMed, 44 citations in OpenAlex.
- The mechanism of the PI3K-AKT-mTOR signaling pathway in renal cell carcinoma: current developments and future prospects.Frontiers in oncology · 2026Review
- Modulation of miR-146b by N6-methyladenosine modification remodels tumor-associated macrophages and enhances anti-PD-1 therapy in colorectal cancer.Cellular oncology (Dordrecht, Netherlands) · 2023Article
- RNA mis-splicing drives viral mimicry response after DNMTi therapy in SETD2-mutant kidney cancer.Cell reports · 2023Article
- Precision Medicine: An Optimal Approach to Patient Care in Renal Cell Carcinoma.Frontiers in medicine · 2022Review
- Prognostic value of antitumor drug targets prediction using integrated bioinformatic analysis for immunogenic cell death-related lncRNA model based on stomach adenocarcinoma characteristics and tumor immune microenvironment.Frontiers in pharmacology · 2022Article
- IGFBP5 is Upregulated and Associated with Poor Prognosis in Colorectal Cancer.International journal of general medicine · 2022Article
- Somatic Copy Number Alterations and Associated Genes in Clear-Cell Renal-Cell Carcinoma in Brazilian Patients.International journal of molecular sciences · 2021Article
- Multi-omics analysis reveals the genetics and immune landscape of dexamethasone responsive genes in cancer microenvironment.Annals of translational medicine · 2020Article
- Comparison of the biomarkers for targeted therapies in primary extra-mammary and mammary Paget's disease.Cancer medicine · 2020Article
- SETD2 mutation in renal clear cell carcinoma suppress autophagy via regulation of ATG12.Cell death & disease · 2020Article
- SETD2 mutation in renal clear cell carcinoma suppress autophagy via regulation of ATG12.Cell death & disease · 2020Article
- Overexpression of BHLHE41, correlated with DNA hypomethylation in 3'UTR region, promotes the growth of human clear cell renal cell carcinoma.Oncology reports · 2019Article
- Roles of SETD2 in Leukemia-Transcription, DNA-Damage, and Beyond.International journal of molecular sciences · 2019Review
- Article
- Epigenetic modifiers: activities in renal cell carcinoma.Nature reviews. Urology · 2018Review
- Knockdown of tyrosine 3-monooxygenase/tryptophan 5-monooxygenase activation protein zeta (YWHAZ) enhances tumorigenesis both in vivo and in vitro in bladder cancer.Oncology reports · 2018Article
- Nutlin-3a as a novel anticancer agent for adrenocortical carcinoma with CTNNB1 mutation.Cancer medicine · 2018Article
- EZH2 Expression is increased in BAP1-mutant renal clear cell carcinoma and is related to poor prognosis.Journal of Cancer · 2018Article
- Overexpression of HSD17B4 exerts tumor suppressive function in adrenocortical carcinoma and is not associated with hormone excess.Oncotarget · 2017Article
- Cortisol inhibits mTOR signaling in avascular necrosis of the femoral head.Journal of orthopaedic surgery and research · 2017Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We aimed to exploit novel compounds with high selectivity to clear cell renal cell carcinoma (ccRCC) with common mutations. Using the GDSC databases, we searched for compounds with high selectivity for ccRCC with VHL and/or SETD2 mutations. Clinical impact and gene interactions were analysed using TCGA database. In vitro and in vivo studies were performed to validate the inhibitory effects of the compound. We identified the selective PI3Kβ inhibitor TGX221 as a selective inhibitor for ccRCC with both VHL and SETD2 mutations. TGX221 also targeted cancer cells with CDKN2A and PTEN mutations. Changes in PTEN and CDKN2A gene sets were associated with worsened prognosis of ccRCC. TGX221 substantially and selectively inhibited the down stream products of VHL, SETD2, and PTEN in ccRCC cells with VHL and SETD2 mutations. TGX221 also exhibited significant selectivity in inhibiting cell motility and tumourigenesis of ccRCC cells with VHL and SETD2 mutations. TGX221 is a novel inhibitor with high selectivity for ccRCC with VHL and SETD2 mutations. It also targeted PTEN and CDKN2A mutations. How those genes were associated with PI3Kβ warranted further investigations.
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