Preclinical efficacy of targeting epigenetic mechanisms in AML with 3q26 lesions and EVI1 overexpression.


Journal

Leukemia
ISSN: 1476-5551
Titre abrégé: Leukemia
Pays: England
ID NLM: 8704895

Informations de publication

Date de publication:
12 Dec 2023
Historique:
received: 18 06 2023
accepted: 29 11 2023
revised: 27 11 2023
medline: 13 12 2023
pubmed: 13 12 2023
entrez: 12 12 2023
Statut: aheadofprint

Résumé

AML with chromosomal alterations involving 3q26 overexpresses the transcription factor (TF) EVI1, associated with therapy refractoriness and inferior overall survival in AML. Consistent with a CRISPR screen highlighting BRD4 dependency, treatment with BET inhibitor (BETi) repressed EVI1, LEF1, c-Myc, c-Myb, CDK4/6, and MCL1, and induced apoptosis of AML cells with 3q26 lesions. Tegavivint (TV, BC-2059), known to disrupt the binding of nuclear β-catenin and TCF7L2/LEF1 with TBL1, also inhibited co-localization of EVI1 with TBL1 and dose-dependently induced apoptosis in AML cell lines and patient-derived (PD) AML cells with 3q26.2 lesions. TV treatment repressed EVI1, attenuated enhancer activity at ERG, TCF7L2, GATA2 and MECOM loci, abolished interactions between MYC enhancers, repressing AML stemness while upregulating mRNA gene-sets of interferon/inflammatory response, TGF-β signaling and apoptosis-regulation. Co-treatment with TV and BETi or venetoclax induced synergistic in vitro lethality and reduced AML burden, improving survival of NSG mice harboring xenografts of AML with 3q26.2 lesions.

Identifiants

pubmed: 38086946
doi: 10.1038/s41375-023-02108-3
pii: 10.1038/s41375-023-02108-3
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Informations de copyright

© 2023. The Author(s), under exclusive licence to Springer Nature Limited.

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Auteurs

Christine E Birdwell (CE)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Warren Fiskus (W)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Tapan M Kadia (TM)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Christopher P Mill (CP)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Koji Sasaki (K)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Naval Daver (N)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Courtney D DiNardo (CD)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Naveen Pemmaraju (N)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Gautam Borthakur (G)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

John A Davis (JA)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Kaberi Das (K)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Sunil Sharma (S)

TGen, Phoenix, AZ, 85004, USA.

Stephen Horrigan (S)

Iterion Therapeutics, Houston, TX, 77021, USA.

Xinjia Ruan (X)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Xiaoping Su (X)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Joseph D Khoury (JD)

University of Nebraska Medical Center, Omaha, NE, 68198, USA.

Hagop Kantarjian (H)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA.

Kapil N Bhalla (KN)

M.D. Anderson Cancer Center, The University of Texas, Houston, TX, 77030, USA. kbhalla@mdanderson.org.

Classifications MeSH