Related Experiment Video

Updated: Jun 6, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
12:40

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors

Published on: December 7, 2014

Targeted inhibition of kinases in cancer therapy

Stacey J Baker1, E Premkumar Reddy

  • 1Mount Sinai School of Medicine, New York, NY, USA.

The Mount Sinai Journal of Medicine, New York
|November 25, 2010
PubMed

Insights

Cancer drug discovery now targets specific molecular changes in tumor cells, moving beyond general cell death induction. This review covers targeted therapies, including kinase inhibitors and newer agents, addressing treatment resistance.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cancer drug discovery has shifted from non-specific cell death induction to targeting specific molecular alterations in tumor cells.
  • The identification of oncogene mutations and amplifications has driven the development of targeted therapies.
  • Early successes like imatinib and trastuzumab have paved the way for novel cancer treatments.

Purpose of the Study:

  • To review key examples of targeted cancer therapies, including kinase inhibitors.
  • To highlight newer agents in development for cancer treatment.
  • To discuss second-generation kinase inhibitors designed to overcome treatment resistance.

Main Methods:

  • Literature review of targeted cancer therapies.
  • Analysis of mechanisms of action for kinase inhibitors.
  • Discussion of clinical development stages for novel agents.

Main Results:

  • Several classes of targeted therapies have emerged, focusing on specific cancer-driving proteins.
  • Newer agents targeting kinases are in various stages of clinical development.
  • Second-generation kinase inhibitors show promise in addressing acquired resistance.

Conclusions:

  • Targeted therapies represent a significant advancement in cancer treatment, offering more precise mechanisms of action.
  • Ongoing research and development are crucial for overcoming resistance and improving patient outcomes.
  • The future of cancer drug discovery lies in continued molecular understanding and targeted intervention.

More Related Videos

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Related Concept Videos

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...
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...
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include: