Ephedrannin A: A potent dual inhibitor of FAK and Src with anticancer effects

被引:0
作者
Ong, Hien Thi My [1 ,2 ]
Ates, Eda [1 ,2 ]
Kang, Min-Jung [1 ,2 ]
机构
[1] Korea Inst Sci & Technol, Ctr Adv Biomol Recognit, Seoul 02792, South Africa
[2] Univ Sci & Technol, KIST Sch, Div Biomed Sci & Technol, Seoul, South Korea
关键词
anticancer compound; colon cancer cells; ephedrannin A; inhibition of FAK and Src; natural product; SIGNALING PATHWAYS; ADHESION; PHOSPHORYLATION; RESVERATROL; ACTIVATION; EXPRESSION; CONFERONE; APOPTOSIS; MIGRATION; CURCUMIN;
D O I
暂无
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Cancer is the leading cause of death worldwide, and the development of effective treatments remains an important challenge. Here, we present ephedrannin A, a compound that exhibits strong anticancer activity against various types of cancer including lung, liver, colon, and kidney cancer. The compound has demonstrated its remarkable ability to inhibit cell proliferation and invasion similar to conferone and Y15, known focal adhesion kinase (FAK) inhibitors. Treatment with 10 mu M ephedrannin A significantly reduced the expression of FAK, and phosphorylated FAK and proto-oncogene tyrosine-protein kinase Src, two major signaling proteins involved in cancer progression in colon, kidney, and lung cancer cell lines. Furthermore, knockdown experiments targeting Src found no effect on FAK expression and phosphorylation, suggesting that FAK/Src complex inhibition is the main mechanism of action of ephedrannin A. Co-targeting of FAK and Src is a promising therapeutic strategy because these proteins play important roles in promoting cell proliferation, migration, and invasion. By disrupting these pathways, ephedrannin A could effectively inhibit the growth and metastasis of cancer cells. Further investigation is necessary to elucidate the exact molecular mechanisms underlying the anticancer effects of ephedrannin A and to explore the possibility of clinical development.
引用
收藏
页码:317 / 325
页数:9
相关论文
共 50 条
  • [21] Synthesis of dual-action parthenolide prodrugs as potent anticancer agents
    Taleghani, Akram
    Nasseri, Mohammad Ali
    Iranshahi, Mehrdad
    BIOORGANIC CHEMISTRY, 2017, 71 : 128 - 134
  • [22] Dual Targeting of CDK4 and ARK5 Using a Novel Kinase Inhibitor ON123300 Exerts Potent Anticancer Activity against Multiple Myeloma
    Perumal, Deepak
    Kuo, Pei-Yu
    Leshchenko, Violetta V.
    Jiang, Zewei
    Divakar, Sai Krishna Athaluri
    Cho, Hearn Jay
    Chari, Ajai
    Brody, Joshua
    Reddy, M. V. Ramana
    Zhang, Weijia
    Reddy, E. Premkumar
    Jagannath, Sundar
    Parekh, Samir
    CANCER RESEARCH, 2016, 76 (05) : 1225 - 1236
  • [23] Discovery of a novel Aurora B inhibitor GSK650394 with potent anticancer and anti-aspergillus fumigatus dual efficacies in vitro
    He, Yuhua
    Fu, Wei
    Du, Liyang
    Yao, Huiqiao
    Hua, Zhengkang
    Li, Jinyu
    Lin, Zhonghui
    JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2022, 37 (01) : 109 - 117
  • [24] Synthesis and Anticancer Activity of Novel Indole Derivatives as Dual EGFR/SRC Kinase Inhibitors
    Olgen, Sureyya
    Kaleli, Sevde Nur Biltekin
    Karaca, Banu Taktak
    Demirel, Ural U.
    Bristow, Hacer Karatas
    CURRENT MEDICINAL CHEMISTRY, 2024, 31 (24) : 3798 - 3817
  • [25] Improved synthesis and anticancer activity of a potent neuronal nitric oxide synthase inhibitor
    Vasu, Dhananjayan
    Reidl, Cory T.
    Wang, Eric
    Yang, Sun
    Silverman, Richard B.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2023, 90
  • [26] A Highly Potent TACC3 Inhibitor as a Novel Anticancer Drug Candidate
    Akbulut, Ozge
    Lengerli, Deniz
    Saatci, Ozge
    Duman, Elif
    Seker, Urartu O. S.
    Isik, Aynur
    Akyol, Aytekin
    Caliskan, Burcu
    Banoglu, Erden
    Sahin, Ozgur
    MOLECULAR CANCER THERAPEUTICS, 2020, 19 (06) : 1243 - 1254
  • [27] Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine
    Du, Guangyan
    Rao, Suman
    Gurbani, Deepak
    Henning, Nathaniel J.
    Jiang, Jie
    Che, Jianwei
    Yang, Annan
    Ficarro, Scott B.
    Marto, Jarrod A.
    Aguirre, Andrew J.
    Sorger, Peter K.
    Westover, Kenneth D.
    Zhang, Tinghu
    Gray, Nathanael S.
    JOURNAL OF MEDICINAL CHEMISTRY, 2020, 63 (04) : 1624 - 1641
  • [28] Antitumor Effects and Biomarkers of Activity of AZD0530, a Src Inhibitor, in Pancreatic Cancer
    Rajeshkumar, N. V.
    Tan, Aik Choon
    De Oliveira, Elizabeth
    Womack, Chris
    Wombwell, Helen
    Morgan, Shethah
    Warren, Madhuri V.
    Walker, Jill
    Green, Tim P.
    Jimeno, Antonio
    Messersmith, Wells A.
    Hidalgo, Manuel
    CLINICAL CANCER RESEARCH, 2009, 15 (12) : 4138 - 4146
  • [29] A Multitargeted Approach: Organorhodium Anticancer Agent Based on Vorinostat as a Potent Histone Deacetylase Inhibitor
    Hanif, Muhammad
    Arshad, Jahanzaib
    Astin, Jonathan W.
    Rana, Zohaib
    Zafar, Ayesha
    Movassaghi, Sanam
    Leung, Euphemia
    Patel, Kamal
    Sohnel, Tilo
    Reynisson, Johannes
    Sarojini, Vijayalekshmi
    Rosengren, Rhonda J.
    Jamieson, Stephen M. F.
    Hartinger, Christian G.
    ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2020, 59 (34) : 14609 - 14614
  • [30] Activity of the potent dual Abl/Src tyrosine kinase inhibitor FB2 against Bcr-Abl positive cell lines in vitro and in vivo
    Yuan, Xia
    Zhang, Yi
    Zhang, Haijing
    Jin, Jing
    Li, Xiangyan
    Liu, He
    Feng, Zhiqiang
    Chen, Xiaoguang
    LEUKEMIA RESEARCH, 2011, 35 (02) : 237 - 242