http://jcps.bjmu.edu.cn

中国药学(英文版) ›› 2017, Vol. 26 ›› Issue (9): 621-634.DOI: 10.5246/jcps.2017.09.070

• 【综 述】 •    下一篇

PI3K signaling pathway targeting by using different molecular approaches to treat cancer

Mohammad Rashid1*, Shahid Karim1, Babar Ali1, Shamshir Khan1, Makhmur Ahmad1, Asif Husain2, Ravinesh Mishra3   

  1. 1. Department of Pharmaceutical Chemistry and Pharmacognosy, College of Pharmacy and Dentistry, Buraydah Colleges, Al-Qassim 31717, Kingdom of Saudi Arabia
    2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi-110062, India
    3. Institute of Pharmacy & Emerging Sciences, Baddi University of Emerging Science & Technology, Makhnumajra, Baddi, Solan-173205, Himachal Pradesh, India
  • 收稿日期:2017-04-23 修回日期:2017-06-19 出版日期:2017-09-30 发布日期:2017-08-25
  • 通讯作者: Tel.: +966-577148790, E-mail: rashidpharm2008@gmail.com

PI3K signaling pathway targeting by using different molecular approaches to treat cancer

Mohammad Rashid1*, Shahid Karim1, Babar Ali1, Shamshir Khan1, Makhmur Ahmad1, Asif Husain2, Ravinesh Mishra3   

  1. 1. Department of Pharmaceutical Chemistry and Pharmacognosy, College of Pharmacy and Dentistry, Buraydah Colleges, Al-Qassim 31717, Kingdom of Saudi Arabia
    2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi-110062, India
    3. Institute of Pharmacy & Emerging Sciences, Baddi University of Emerging Science & Technology, Makhnumajra, Baddi, Solan-173205, Himachal Pradesh, India
  • Received:2017-04-23 Revised:2017-06-19 Online:2017-09-30 Published:2017-08-25
  • Contact: Tel.: +966-577148790, E-mail: rashidpharm2008@gmail.com

摘要:

Recent evidence of research has been proposed that the phosphoinositide 3-kinase (PI3K) pathway is noticeable target for searching novel anticancer agents. The phosphoinositide 3-kinase (PI3K) is accountable for harmonizing a diverse range of cell functions, such as transcription, proliferation, cell survival, cell growth, degranulation, vesicular trafficking and cell migration, which are mostly involved in carcinogenesis. Particularly, PI3K-mediated signaling molecules and its effects on gene expression contribute to tumorigenesis. PI3Ks generally are grouped into three distinct classes: I, II and III according to their structure and function. The class IA of PI3K includes an alpha, beta or delta p110 catalytic subunit (p110α, p110β, or p110γ), which are associatedwith the activation of RTKs. Mutations in PIK3CA, the gene encoding the p110α catalytic subunit of PI3K, have just been recognizedas novel mechanisms of inducing oncogenic PI3K signaling. Therefore, the class IA PI3K is the only one of most evidently implicated in cancer. The PI3K pathway is mostly mutated in more cancer patients compared with normal person, making it an eye-catching molecular target for analyses based on inhibitor molecule. In this article, we highlighted the signaling effects and regulation pathway of PI3K involved in the development and survival of tumor cells. The consequence and intricacy of PI3K pathway made it an essential beneficial target for cancer treatment.

关键词: PI3K, AKT, mTOR, PDK-1, Tumor suppressor PTEN, Signal pathway

Abstract:

Recent evidence of research has been proposed that the phosphoinositide 3-kinase (PI3K) pathway is noticeable target for searching novel anticancer agents. The phosphoinositide 3-kinase (PI3K) is accountable for harmonizing a diverse range of cell functions, such as transcription, proliferation, cell survival, cell growth, degranulation, vesicular trafficking and cell migration, which are mostly involved in carcinogenesis. Particularly, PI3K-mediated signaling molecules and its effects on gene expression contribute to tumorigenesis. PI3Ks generally are grouped into three distinct classes: I, II and III according to their structure and function. The class IA of PI3K includes an alpha, beta or delta p110 catalytic subunit (p110α, p110β, or p110γ), which are associatedwith the activation of RTKs. Mutations in PIK3CA, the gene encoding the p110α catalytic subunit of PI3K, have just been recognizedas novel mechanisms of inducing oncogenic PI3K signaling. Therefore, the class IA PI3K is the only one of most evidently implicated in cancer. The PI3K pathway is mostly mutated in more cancer patients compared with normal person, making it an eye-catching molecular target for analyses based on inhibitor molecule. In this article, we highlighted the signaling effects and regulation pathway of PI3K involved in the development and survival of tumor cells. The consequence and intricacy of PI3K pathway made it an essential beneficial target for cancer treatment.

Key words: PI3K, AKT, mTOR, PDK-1, Tumor suppressor PTEN, Signal pathway

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