Mutation in the Unrearranged PML Allele Confers Resistance to Arsenic Trioxide in Acute Promyelocytic Leukemia

Arsenic trioxide (ATO) is able to selectively target and degrade the disease-causing PML::RARα (P/R) oncoprotein in acute promyelocytic leukemia (APL) for curing the disease. However, some relapsed patients develop resistance to ATO due to mutations in the promyelocytic leukemia (PML) part of the PM...

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Main Authors: Pei-Han Yu, Chen-Ying Zhu, Yuan-Yuan Kang, Hua Naranmandura, Chang Yang
Format: Article
Language:English
Published: American Association for the Advancement of Science (AAAS) 2025-01-01
Series:Research
Online Access:https://spj.science.org/doi/10.34133/research.0696
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author Pei-Han Yu
Chen-Ying Zhu
Yuan-Yuan Kang
Hua Naranmandura
Chang Yang
author_facet Pei-Han Yu
Chen-Ying Zhu
Yuan-Yuan Kang
Hua Naranmandura
Chang Yang
author_sort Pei-Han Yu
collection DOAJ
description Arsenic trioxide (ATO) is able to selectively target and degrade the disease-causing PML::RARα (P/R) oncoprotein in acute promyelocytic leukemia (APL) for curing the disease. However, some relapsed patients develop resistance to ATO due to mutations in the promyelocytic leukemia (PML) part of the PML::RARα fusion gene. A relapsed APL patient had shown resistance to ATO and chemotherapy and was identified to harbor a point mutation (A216V) in the unrearranged PML allele rather than the PML::RARα fusion gene. Here, we report that mutations in the unrearranged PML allele impede the ATO-induced destabilization and degradation of the wild-type P/R oncoprotein. Deletion of the coiled-coil domain in a PML mutant completely reversed wild-type P/R protein resistance to ATO by abolishing the interaction between PML and P/R proteins. Collectively, our findings reveal that a point mutation in the unrearranged PML allele can confer ATO resistance through a protein–protein interaction. Therefore, the unrearranged PML allele should also be screened for drug-resistant mutations in relapsed APL patients.
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spelling doaj-art-9ef740125a1f49d0a13b2a7272ef268c2025-08-20T03:11:48ZengAmerican Association for the Advancement of Science (AAAS)Research2639-52742025-01-01810.34133/research.0696Mutation in the Unrearranged PML Allele Confers Resistance to Arsenic Trioxide in Acute Promyelocytic LeukemiaPei-Han Yu0Chen-Ying Zhu1Yuan-Yuan Kang2Hua Naranmandura3Chang Yang4Department of Hematology of First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310058, China.Department of Hematology of First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310058, China.Department of Hematology of First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310058, China.Department of Hematology of First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310058, China.Department of Hematology of First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310058, China.Arsenic trioxide (ATO) is able to selectively target and degrade the disease-causing PML::RARα (P/R) oncoprotein in acute promyelocytic leukemia (APL) for curing the disease. However, some relapsed patients develop resistance to ATO due to mutations in the promyelocytic leukemia (PML) part of the PML::RARα fusion gene. A relapsed APL patient had shown resistance to ATO and chemotherapy and was identified to harbor a point mutation (A216V) in the unrearranged PML allele rather than the PML::RARα fusion gene. Here, we report that mutations in the unrearranged PML allele impede the ATO-induced destabilization and degradation of the wild-type P/R oncoprotein. Deletion of the coiled-coil domain in a PML mutant completely reversed wild-type P/R protein resistance to ATO by abolishing the interaction between PML and P/R proteins. Collectively, our findings reveal that a point mutation in the unrearranged PML allele can confer ATO resistance through a protein–protein interaction. Therefore, the unrearranged PML allele should also be screened for drug-resistant mutations in relapsed APL patients.https://spj.science.org/doi/10.34133/research.0696
spellingShingle Pei-Han Yu
Chen-Ying Zhu
Yuan-Yuan Kang
Hua Naranmandura
Chang Yang
Mutation in the Unrearranged PML Allele Confers Resistance to Arsenic Trioxide in Acute Promyelocytic Leukemia
Research
title Mutation in the Unrearranged PML Allele Confers Resistance to Arsenic Trioxide in Acute Promyelocytic Leukemia
title_full Mutation in the Unrearranged PML Allele Confers Resistance to Arsenic Trioxide in Acute Promyelocytic Leukemia
title_fullStr Mutation in the Unrearranged PML Allele Confers Resistance to Arsenic Trioxide in Acute Promyelocytic Leukemia
title_full_unstemmed Mutation in the Unrearranged PML Allele Confers Resistance to Arsenic Trioxide in Acute Promyelocytic Leukemia
title_short Mutation in the Unrearranged PML Allele Confers Resistance to Arsenic Trioxide in Acute Promyelocytic Leukemia
title_sort mutation in the unrearranged pml allele confers resistance to arsenic trioxide in acute promyelocytic leukemia
url https://spj.science.org/doi/10.34133/research.0696
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