ArticleCell death & disease2020
I-BET726 suppresses human skin squamous cell carcinoma cell growth in vitro and in vivo.
Article in Cell death & disease, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- p53 overexpression counteracts the pro-survival effect of Bcl-2 by restoring MAMs function in cutaneous squamous cell carcinoma.Cell division · 2026Article
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- A first-in-class TIMM44 blocker inhibits bladder cancer cell growth.Cell death & disease · 2024Article
- Targeting POLRMT by a first-in-class inhibitor IMT1 inhibits osteosarcoma cell growth in vitro and in vivo.Cell death & disease · 2024Article
- Overexpressed Gαi1 exerts pro-tumorigenic activity in nasopharyngeal carcinoma.Cell death & disease · 2023Article
- Targeting SphK1/2 by SKI-178 inhibits prostate cancer cell growth.Cell death & disease · 2023Article
- A first-in-class POLRMT specific inhibitor IMT1 suppresses endometrial carcinoma cell growth.Cell death & disease · 2023Article
- Inhibition of OTUB2 suppresses colorectal cancer cell growth by regulating β-Catenin signaling.American journal of cancer research · 2023Article
- The mitochondrial RNA polymerase POLRMT promotes skin squamous cell carcinoma cell growth.Cell death discovery · 2022Article
- The anti-osteosarcoma cell activity by the sphingosine kinase 1 inhibitor SKI-V.Cell death discovery · 2022Article
- The role of protein acetylation in carcinogenesis and targeted drug discovery.Frontiers in endocrinology · 2022Review
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- GDC-0349 inhibits non-small cell lung cancer cell growth.Cell death & disease · 2020Article
- The therapeutic effect of the BRD4-degrading PROTAC A1874 in human colon cancer cells.Cell death & disease · 2020Article
- Article
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Authors and funding
7 authors.
Funding
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Abstract
Bromodomain-containing protein 4 (BRD4) is a potential therapeutic target of skin squamous cell carcinoma (SCC). I-BET726 is a novel BRD4 inhibitor. Its potential effect in skin SCC cells was tested in the present study. We show that I-BET726 potently inhibited survival, proliferation, cell cycle progression, and migration in established (A431/SCC-9/SCC-12/SCC-13 lines) and primary human skin SCC cells. I-BET726 induced significant apoptosis activation in skin SCC cells. It was more efficient in inhibiting skin SCC cells than known BRD4 inhibitors (JQ1, CPI203, and AZD5153). I-BET726 not only downregulated BRD4-regulated proteins (c-Myc, Bcl-2, and cyclin D1), but also inhibited sphingosine kinase 1 (SphK1) and Akt signalings in SCC cells. Restoring Akt activation, by a constitutively active S473D mutant Akt1 ("caAkt1"), partially inhibited I-BET726-induced cytotoxicity in A431 cells. In vivo, I-BET726 oral administration potently inhibited A431 xenograft growth in severe combined immunodeficient mice. Downregulation of BRD4-regulated proteins and inhibition of the SphK1-Akt signaling were detected in I-BET726-treated A431 xenograft tumor tissues. Together, I-BET726 inhibits skin SCC cell growth in vitro and in vivo.
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