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Updated: Oct 9, 2025

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
Published on: September 19, 2018
A molecular perspective for the use of type IV tyrosine kinase inhibitors as anticancer therapeutics
Rudradip Das1, Asmita Choithramani1, Amit Shard1
1Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research-Ahmedabad, Gandhinagar, Gujarat 380054, India.
Abstract:
Tyrosine kinases are enzymes that can transfer a phosphate group from ATP to a specific protein tyrosine, serine or threonine residue within a cell, operating as a switch that can turn 'on' and 'off' causing different physiological alterations in the body. Mutated kinases have been shown to display an equilibrium shift toward the activated state. Types I-III have been studied intensively leading to drugs like imatinib (type II), cobimetinib (type III), among others. It is the same scenario for types V-VII; however, there is a lacuna in information regarding type IV inhibitors, although recently some advances have surfaced. This review aims to accumulate the knowledge gained so far about type IV inhibitors.
Insights
This review focuses on type IV kinase inhibitors, a class with limited research. It compiles recent advancements to address the knowledge gap in this specific area of tyrosine kinase research.
Area of Science:
- Biochemistry
- Enzymology
- Pharmacology
Background:
- Tyrosine kinases regulate cellular processes by transferring phosphate groups from ATP.
- Mutations in tyrosine kinases can lead to an overactive state, contributing to various diseases.
- While inhibitors for types I-III and V-VII are well-documented, type IV inhibitors remain under-explored.
Purpose of the Study:
- To consolidate current knowledge on type IV kinase inhibitors.
- To highlight recent progress in the development of type IV inhibitors.
- To address the existing gap in the literature regarding type IV kinase inhibition.
Main Methods:
- Literature review of scientific databases.
- Analysis of recent research on tyrosine kinase inhibitors.
- Synthesis of information on type IV kinase inhibitor development.
Main Results:
- Identification of emerging research trends in type IV kinase inhibition.
- Compilation of known type IV kinase inhibitors and their mechanisms.
- Overview of the challenges and opportunities in targeting type IV kinases.
Conclusions:
- Type IV kinase inhibitors represent a promising but understudied area in drug discovery.
- Further research is crucial to fully understand and exploit type IV kinase inhibitors for therapeutic purposes.
- Recent advances suggest a growing interest and potential for future development in this field.
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