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Updated: May 9, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening

Identification of Kinase-substrate Pairs Using High Throughput Screening

Published on: August 29, 2015

High-throughput screening for protein tyrosine phosphatase activity modulators.

Lutz Tautz¹, Eduard A Sergienko

¹Infectious and Inflammatory Disease Center, Sanford-Burnham Medical Research Institute, La Jolla, CA, USA.

Methods in Molecular Biology (Clifton, N.J.)

|July 18, 2013

Summary

Developing targeted therapies requires identifying modulators of protein tyrosine phosphatases (PTPs). This study outlines high-throughput screening (HTS) methods for discovering PTP activity modulators, crucial for new drug development.

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Area of Science:

Biochemistry
Molecular Biology
Pharmacology

Background:

Reversible protein phosphorylation regulates eukaryotic cell function.
Dysregulation of protein kinases and phosphatases is linked to human diseases.
Protein tyrosine phosphatases (PTPs) are a large, diverse enzyme family with therapeutic potential.

Purpose of the Study:

To describe high-throughput screening (HTS) methods for identifying modulators of protein tyrosine phosphatase (PTP) activity.
To provide guidance on optimizing PTP screening assays and validating hit compounds.

Main Methods:

Implementation of absorbance- or fluorescence-based PTP assays in 384- or 1536-well microtiter plates.
Optimization of HTS assay quality and performance for PTP screening.

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Identification of Kinase-substrate Pairs Using High Throughput Screening

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Description of hit compound confirmation, follow-up, and prioritization strategies.

Main Results:

Successful application of generic phosphatase assays for PTP HTS.
Demonstration of optimized assay conditions for robust screening.
Identification of common pitfalls and best practices in PTP HTS campaigns.

Conclusions:

HTS methods can effectively identify modulators of PTP activity.
Optimized assays and rigorous follow-up are essential for successful PTP drug discovery.
This work provides a framework for developing novel PTP-targeted therapeutics.