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Updated: Apr 27, 2026

A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
[Kinase inhibitors against hematological malignancies]
Abstract:
Dysregulation of protein phosphorylation, especially on tyrosine residues, plays a crucial role in development and progression of hematological malignancies. Since remarkable success in imatinib therapy of CML and Ph+ALL, extensive efforts have made to explore candidate molecular targets and next breakthrough drugs. Now that next generation ABL kinase inhibitors are available for CML, the therapeutic algorithm has been revolutionized. As for AML and lymphoid malignancies, many kinase inhibitors targeting FLT3, BTK and aurora-A are on early and late clinical trials, and a number of promising drugs including ibrutinib are picked up for further evaluation.
Insights
Protein phosphorylation is key in blood cancers. New kinase inhibitors offer improved treatments for chronic myeloid leukemia (CML) and are in trials for acute myeloid leukemia (AML) and lymphoid malignancies.
Area of Science:
- Biochemistry
- Oncology
- Pharmacology
Background:
- Protein phosphorylation, particularly on tyrosine residues, is implicated in hematological malignancies.
- The success of imatinib in treating chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ALL) has spurred research into novel molecular targets.
- Next-generation ABL kinase inhibitors have significantly altered CML treatment paradigms.
Purpose of the Study:
- To review the role of protein phosphorylation in hematological malignancies.
- To discuss the advancements in kinase inhibitor therapies for various blood cancers.
- To highlight promising drug candidates currently in clinical trials.
Main Methods:
- Literature review of studies on protein phosphorylation in hematological malignancies.
- Analysis of clinical trial data for kinase inhibitors in CML, AML, and lymphoid malignancies.
- Evaluation of the therapeutic impact of next-generation ABL kinase inhibitors.
Main Results:
- Dysregulated protein phosphorylation is a critical factor in the development and progression of blood cancers.
- Next-generation ABL kinase inhibitors have revolutionized CML treatment.
- Several kinase inhibitors targeting FLT3, BTK, and aurora-A are in various stages of clinical trials for AML and lymphoid malignancies, with drugs like ibrutinib showing promise.
Conclusions:
- Targeting protein phosphorylation pathways with kinase inhibitors represents a significant therapeutic strategy for hematological malignancies.
- Ongoing clinical trials are evaluating novel agents, offering hope for improved patient outcomes in CML, AML, and lymphoid cancers.
- The development of targeted therapies continues to advance the treatment landscape for blood cancers.
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