Related Experiment Video

Updated: May 13, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening
11:13

Identification of Kinase-substrate Pairs Using High Throughput Screening

Published on: August 29, 2015

Non-ATP-competitive kinase inhibitors - enhancing selectivity through new inhibition strategies

Stephen Harrison1, Kanad Das, Felix Karim

  • 1Vice President of Research KAI Pharmaceutical, Inc., 270 Littlefield Ave., South San Francisco, California 94080, USA +1 650 244 1166 ; +1 650 244 1199 ; steve.harrison@kaipharma.com.

Expert Opinion on Drug Discovery
|March 19, 2013
PubMed
Abstract

Insights

Developing selective kinase inhibitors is crucial for treating chronic diseases. New strategies, particularly small peptide therapeutics, show promise in overcoming challenges associated with ATP-competitive drugs and offer greater specificity.

Area of Science:

  • Drug Discovery
  • Medicinal Chemistry
  • Pharmacology

Background:

  • ATP-competitive kinase inhibitors are effective for cancer but lack specificity due to similar ATP binding sites.
  • Low specificity kinase inhibitors raise concerns about undesired toxicities, slowing drug development for chronic conditions.

Purpose of the Study:

  • To review alternative strategies for developing non-ATP-competitive kinase inhibitors.
  • To summarize approaches aimed at achieving greater selectivity in kinase inhibitor design.

Main Methods:

  • Comprehensive review of scientific and patent literature.
  • Analysis of emerging strategies for kinase inhibitor development.

Main Results:

  • Several novel approaches are being explored to enhance kinase inhibitor selectivity.
  • Small peptide therapeutics represent a particularly promising avenue for selective kinase inhibition.

Conclusions:

  • Non-ATP-competitive strategies offer a path to greater selectivity in kinase inhibitor development.
  • Small peptide therapeutics are demonstrating clinical promise and represent a significant advancement.

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

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries08:49

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries

Published on: January 22, 2019

Related Concept Videos

Enzyme Inhibition01:30

Enzyme Inhibition

Inhibitors are molecules that reduce enzyme activity by binding to the enzyme. In a normally functioning cell, enzymes are regulated by a variety of inhibitors. Drugs and other toxins can also inhibit enzymes. Some inhibitors bind to the enzyme’s active site, while others inhibit enzymatic activity by binding to other sites on the protein structure.
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...
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...
Enzymes02:34

Enzymes

Inside living organisms, enzymes act as catalysts for many biochemical reactions involved in cellular metabolism. The role of enzymes is to reduce the activation energies of biochemical reactions by forming complexes with its substrates. The lowering of activation energies favor an increase in the rates of biochemical reactions.
Enzyme deficiencies can often translate into life-threatening diseases. For example, a genetic abnormality resulting in the deficiency of the enzyme G6PD...
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...