Targeting the phosphoinositide 3-kinase pathway in cancer

Related Experiment Video

Updated: Jun 21, 2026

Exploring the Pharmacological Action and Molecular Mechanism of Salidroside in Inhibiting MCF-7 Cell Proliferation and Migration
11:13

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

Published on: June 9, 2023

Pixu Liu1, Hailing Cheng, Thomas M Roberts

  • 1Department of Cancer Biology, Dana-Farber Cancer Institute, Pathology, Harvard Medical School, Boston, MA 02115, USA.

Nature Reviews. Drug Discovery
|August 1, 2009
PubMed

Insights

The phosphoinositide 3-kinase (PI3K) pathway is frequently activated in cancer, offering therapeutic opportunities. Despite ongoing clinical trials for PI3K inhibitors, significant challenges remain in developing effective cancer treatments targeting this pathway.

Area of Science:

  • Oncology
  • Molecular Biology
  • Signal Transduction

Background:

  • The phosphoinositide 3-kinase (PI3K) pathway is a critical signaling network involved in cellular functions.
  • This pathway is frequently dysregulated in human cancers, linking oncogenes and receptor signaling to tumor growth.
  • Its central role makes it a common target for cancer therapies.

Purpose of the Study:

  • To review recent advancements in understanding the PI3K pathway in cancer.
  • To discuss the therapeutic potential of targeting the PI3K pathway.
  • To identify challenges associated with developing PI3K-targeted cancer therapies.

Main Methods:

  • Literature review of recent research on the PI3K pathway.
  • Analysis of clinical trial data for PI3K, AKT, and mTOR inhibitors.
  • Discussion of molecular mechanisms and therapeutic strategies.

Main Results:

  • The PI3K pathway is a prevalent target in human cancers.
  • Inhibitors targeting PI3K, AKT, and mTOR are progressing through clinical trials.
  • Significant challenges persist in optimizing these targeted therapies.

Conclusions:

  • Targeting the PI3K pathway holds promise for cancer treatment.
  • Overcoming resistance mechanisms and improving drug specificity are key challenges.
  • Further research is needed to fully realize the therapeutic potential of PI3K pathway inhibitors.

More Related Videos

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors08:45

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors

Published on: July 17, 2020

Related Concept Videos

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...
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...
The JAK-STAT Signaling Pathway01:20

The JAK-STAT Signaling Pathway

Several cytokine receptors have tightly bound Janus kinase or JAK proteins attached at their cytosolic tail. Small signaling molecules such as cytokines, growth hormones, or prolactins bind to the cytokine receptors and initiate their dimerization. The dimerization brings the cytosolic JAKs together that trans-phosphorylate and activates each other. The activated JAKs now phosphorylate cytosolic tails of the cytokine receptors, which serve as binding sites for adaptor proteins such as  SH2...
Interactions Between Signaling Pathways01:19

Interactions Between Signaling Pathways

Signaling cascades usually lack linearity. Multiple pathways interact and regulate one another, allowing cells to integrate and respond to diverse environmental stimuli.
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...
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...