Related Experiment Video

Updated: Jun 8, 2026

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
10:27

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts

Published on: July 25, 2020

PI3K/Akt/mTOR pathway inhibitors in cancer: a perspective on clinical progress

P Wu1, Y-Z Hu

  • 1ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

Current Medicinal Chemistry
|October 14, 2010
PubMed

Insights

Targeting the PI3K/Akt/mTOR pathway with small-molecule kinase inhibitors shows therapeutic potential for cancer treatment. This review details the latest inhibitors developed for this pathway and their progression into clinical studies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • The phosphoinositide 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) pathway regulates critical cellular functions like growth and survival.
  • Dysregulation of this pathway is implicated in various cancers, making it a key therapeutic target.
  • Numerous small-molecule kinase inhibitors targeting PI3K, Akt, mTOR, and PDK-1 are under development.

Purpose of the Study:

  • To provide an up-to-date review of small-molecule kinase inhibitors targeting the PI3K/Akt/mTOR pathway.
  • To focus on inhibitors that have advanced into clinical studies for cancer treatment.

Main Methods:

  • Literature review of recent pharmacological studies.
  • Analysis of clinical trial data for PI3K/Akt/mTOR pathway inhibitors.
  • Synthesis of information on small-molecule kinase inhibitors in development.

Main Results:

  • A growing number of small-molecule kinase inhibitors targeting the PI3K/Akt/mTOR pathway are progressing through clinical development.
  • These inhibitors target key nodes including PI3K, Akt, mTOR, and PDK-1.
  • The therapeutic potential of targeting this pathway for cancer treatment is extensively validated.

Conclusions:

  • Small-molecule kinase inhibitors targeting the PI3K/Akt/mTOR pathway represent a promising area of cancer therapy development.
  • Continued research and clinical investigation are crucial for advancing these therapies.
  • The landscape of these inhibitors is rapidly evolving, with many entering clinical studies.

More Related Videos

Exploring the Pharmacological Action and Molecular Mechanism of Salidroside in Inhibiting MCF-7 Cell Proliferation and Migration11:13

Exploring the Pharmacological Action and Molecular Mechanism of Salidroside in Inhibiting MCF-7 Cell Proliferation and Migration

Published on: June 9, 2023

Related Concept Videos

mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...