Recent clinical advances in PI3K inhibitors on colorectal cancer

被引:13
|
作者
Zhu, Mingliang [1 ]
Jin, Qiuyang [1 ]
Xin, Yizhou [1 ]
机构
[1] Shandong Univ Tradit Chinese Med, Affiliated Hosp, Dept Pharm, Jinan 250014, Peoples R China
来源
PHARMAZIE | 2021年 / 76卷 / 12期
关键词
PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR; PHASE-II TRIAL; KINASE INHIBITOR; DOSE-ESCALATION; DUAL INHIBITOR; SYNERGISTIC INHIBITION; ANTITUMOR-ACTIVITY; BUPARLISIB BKM120; PIK3CA MUTATION; PX-866;
D O I
10.1691/ph.2021.1820
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The PI3K/Akt/mTOR signaling pathway has the functions of regulating cell cycle, participating in tumor angiogenesis, affecting tumor invasion activity and metastasis, regulating apoptosis and autophagy, and participating in tumor drug resistance. Alpelisib (a PI3K inhibitor) has now been approved by the FDA for the treatment of PIK3CA mutant HR-positive/HER2-negative advanced/metastatic breast cancer in combination with fulvestrant which is the first PI3K inhibitor approved for breast cancer treatment. In some human colorectal cancer cells, the activation of this signal pathway is excessive and the negative regulation is impaired. Inhibitors targeting PI3K, a key protein in the PI3K/Akt/mTOR signaling pathway, have a positive effect on the treatment of colorectal cancer. Based on the role of PI3K/Akt/mTOR in the occurrence and development of colorectal cancer and its clinical application, this article reviews the PI3K inhibitors that have been on the market or are in clinical trials.
引用
收藏
页码:568 / 573
页数:6
相关论文
共 50 条
  • [21] PI3K Inhibitors in Breast Cancer Therapy
    Haley Ellis
    Cynthia X. Ma
    Current Oncology Reports, 2019, 21
  • [22] Research advances on selective phosphatidylinositol 3 kinase δ (PI3Kδ) inhibitors
    Sun, Jiajia
    Feng, Yifan
    Huang, Yuan
    Zhang, San-Qi
    Xin, Minhang
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2020, 30 (19)
  • [23] Design, synthesis and bioevaluation of PI3Kα-selective inhibitors as potential colorectal cancer drugs
    Zheng, Xue-Mei
    Chen, Yuan-Si
    Ban, Yu-Juan
    Wang, Yu-Jie
    Dong, Yong-Xi
    Lei, Li
    Guo, Bing
    Wang, Jian-Ta
    Tang, Lei
    Li, Hong-Liang
    Zhang, Ji-Quan
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2023, 260
  • [24] Mechanisms of acquired resistance to the PI3K inhibitors in colorectal cancer cell lines.
    Edgar, Kyle A.
    Wagle, Marie-Claire
    Yan, Yibing
    Belvin, Marcia
    Friedman, Lori
    Wallin, Jeffrey
    CANCER RESEARCH, 2013, 73 (08)
  • [25] Advances in subunits of PI3K class I in cancer
    Cui, Wenli
    Cai, Ying
    Zhou, Xiaoyan
    PATHOLOGY, 2014, 46 (03) : 169 - 176
  • [26] Targeting PI3K signaling in cancer: Challenges and advances
    De Santis, Maria Chiara
    Gulluni, Federico
    Campa, Carlo Cosimo
    Martini, Miriam
    Hirsch, Emilio
    BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER, 2019, 1871 (02): : 361 - 366
  • [27] PI3K inhibitors as new cancer therapeutics: implications for clinical trial design
    Massacesi, Cristian
    Di Tomaso, Emmanuelle
    Urban, Patrick
    Germa, Caroline
    Quadt, Cornelia
    Trandafir, Lucia
    Aimone, Paola
    Fretault, Nathalie
    Dharan, Bharani
    Tavorath, Ranjana
    Hirawat, Samit
    ONCOTARGETS AND THERAPY, 2016, 9 : 203 - 210
  • [28] Clinical development of PI3K/AKT pathway inhibitors in breast cancer.
    Derynck, Mika
    MOLECULAR CANCER RESEARCH, 2018, 16 (08) : 22 - 22
  • [29] PI3K/Akt/mTOR Pathway Inhibitors in Cancer: A Perspective on Clinical Progress
    Wu, P.
    Hu, Y-Z
    CURRENT MEDICINAL CHEMISTRY, 2010, 17 (35) : 4326 - 4341
  • [30] Biomarker evaluation in phase I clinical trials of selective PI3K and PI3k/mTOR inhibitors
    Spoerke, Jill
    Desai, Rupal
    Patel, Rajesh
    Fredrickson, Jill
    Wang, Yulei
    Levy, Gallia
    Gendreau, Steve
    Lauchle, Jennifer
    Derynck, Mika
    Raja, Rajiv
    Koeppen, Hartmut
    Hampton, Garret
    Yan, Yibing
    Lackner, Mark R.
    CANCER RESEARCH, 2013, 73 (08)