Exploring the Anti-cancer Potential of the New BRD4 Inhibitor, OPT-0139, in Human Hepatic Carcinoma

• 발행기관: 셀메드 세포교정의약학회
• 저자명: Bong-Keun Jang Ala Aiob Dong Hoon Suh Kidong Kim Jae Hong No Hye-Yeoun Kang Sun-Young Park Yong Beom Kim
• 간행물 정보: 『셀메드』Volume 15 Issue 10, 18~27쪽, 전체 10쪽
• 주제분류: 의약학 > 의학일반
• 파일형태: PDF
• 발행일자: 2025.08.30

국문 초록

Objective: Bromodomain-containing protein 4 (BRD4) is integral to the regulation of cell growth and differentiation. Inhibition of BRD4 can impede the expression of its associated genes, thereby suppressing cancer cell growth. This study investigates the potential anti-cancer properties of OPT-0139, a novel inhibitor targeting BRD4. Method: Human hepatic carcinoma cell lines (SK-Hep1 and Huh-7) were employed to explore the impact of OPT-0139 treatment, both singly and in combination with Sorafenib. Cell viability, proliferation, cell cycle arrest, and apoptotic cell death were assessed using MTT and ATP assays, flow cytometry, Annexin V assay, and caspase-3 activity assay. The expression of BRD4 and apoptosis-related molecules was evaluated via RT-PCR and Western blot. An in vivo experiment utilizing a mouse xenograft model analyzed tumor growth, weight, and mRNA levels. Results: OPT-0139 significantly reduces cell viability and proliferation, inducing cell cycle arrest and apoptotic cell death. The mouse xenograft model demonstrates significant alterations in tumor growth and the expression of BRD4 and apoptosis-related proteins. Combined treatment with Sorafenib synergistically enhances apoptotic cell death and suppresses tumor growth, both in vitro and in vivo. Conclusion: This investigation validates OPT-0139's efficacy and mechanism in human hepatic carcinoma cell lines. The study underscores OPT-0139's potential as a promising therapeutic agent for human hepatocellular carcinoma.

목차

INTRODUCTION

MATERIALS AND METHODS

RESULTS

DISCUSSION

ACKNOWLEDGEMENT

RESEARCH FUNDING

CONFLICT OF INTEREST

REFERENCES

키워드

BRD4 inhibitor hepatocellular carcinoma OPT-0139 anti-cancer potential