Screening and Activity Evaluation of Novel BCR-ABL/T315I Tyrosine Kinase Inhibitors


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Abstract

Introduction:Chronic myeloid leukemia (CML) is a kind of malignant tumor formed by the clonal proliferation of bone marrow hematopoietic stem cells. BCR-ABL fusion protein, found in more than 90% of patients, is a vital target for discovering anti- CML drugs. Up to date, imatinib is the first BCR-ABL tyrosine kinase inhibitor (TKI) approved by the FDA for treating CML. However, the drug resistance problems appeared for many reasons, especially the T135I mutation, a \"gatekeeper\" of BCR-ABL. Currently, there is no long-term effective and low side effect drug in clinical.

Methods:This study intends to find novel TKIs targeting BCR-ABL with high inhibitory activity against T315I mutant protein by combining artificial intelligence technology and cell growth curve, cytotoxicity, flow cytometry and Western blot experiments.

Results:The obtained compound was found to kill leukemia cells, which had good inhibitory efficacy in BaF3/T315I cells. Compound no 4 could induce cell cycle arrest, cause autophagy and apoptosis, and inhibit the phosphorylation of BCR-ABL tyrosine kinase, STAT5 and Crkl proteins.

Conclusion:The results indicated that the screened compound could be used as a lead compound for further research to discover ideal chronic myeloid leukemia therapeutic drugs.

About the authors

Jie Su

School of Pharmacy, Lanzhou University

Email: info@benthamscience.net

Chenggong Fu

School of Pharmacy, Lanzhou University

Email: info@benthamscience.net

Shuo Wang

School of Pharmacy, Lanzhou Universit

Email: info@benthamscience.net

Xuelian Chen

School of Pharmacy, Lanzhou University

Email: info@benthamscience.net

Runan Wang

School of Pharmacy, Lanzhou University

Email: info@benthamscience.net

Huaihuai Shi

School of Pharmacy, Lanzhou University

Email: info@benthamscience.net

Jiazhong Li

School of Pharmacy, Lanzhou University

Author for correspondence.
Email: info@benthamscience.net

Xin Wang

School of Pharmacy, Lanzhou University

Author for correspondence.
Email: info@benthamscience.net

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