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Published on: September 19, 2018
Aurora kinase inhibitors as anti-cancer therapy
Warren Lok1, Rhonda Q Klein, Muhammad Wasif Saif
1Departments of Medical Oncology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA.
Abstract:
Aurora kinases are serine and threonine kinases that function as key regulators of the mitosis process. There are three distinct human aurora kinases known as Aurora A, Aurora B, and Aurora C. Aurora A and Aurora B are overexpressed in a number of human cancers including non-small cell lung cancer, glioblastomas, and upper gastrointestinal adenocarcinomas. Given their association with tumorigenesis, both Aurora A and Aurora B have been targeted for cancer therapy. Currently, a number of selective and nonselective aurora kinase inhibitors are being tested in preclinical and clinical settings as anti-tumor agents. We review the biology of human aurora kinases, followed by an overview of inhibitors undergoing current clinical investigations.
Insights
Aurora kinases (A, B, and C) regulate mitosis. Aurora A and B are overexpressed in cancers, making them targets for new therapies using novel kinase inhibitors currently in clinical trials.
Area of Science:
- Molecular Biology
- Cell Biology
- Oncology
Background:
- Aurora kinases are crucial serine/threonine kinases regulating cell division (mitosis).
- Three human aurora kinases exist: Aurora A, Aurora B, and Aurora C.
- Aurora A and B are frequently overexpressed in various cancers, including lung, brain, and gastrointestinal tumors.
Purpose of the Study:
- To review the fundamental biology of human aurora kinases.
- To provide an overview of aurora kinase inhibitors in current clinical development for cancer therapy.
Main Methods:
- Literature review of aurora kinase biology.
- Survey of preclinical and clinical data on aurora kinase inhibitors.
Main Results:
- Aurora kinases play a significant role in cell cycle regulation and are implicated in tumorigenesis.
- Numerous selective and nonselective aurora kinase inhibitors are under investigation.
Conclusions:
- Targeting aurora kinases represents a promising strategy for cancer treatment.
- Ongoing clinical investigations are evaluating the efficacy of various aurora kinase inhibitors as anti-tumor agents.
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