Bromodomain and extra-terminal (BET) inhibitors in treating myeloid neoplasms.

Szczegóły
Abstrakt

Tytuł:: Bromodomain and extra-terminal (BET) inhibitors in treating myeloid neoplasms.
Autorzy:: Chen NC; Department of Internal Medicine, The University of Texas School of Health Sciences at Houston, Houston, TX, USA.
Borthakur G; Department of Leukemia, The University of Texas MD Anderson Cancer Center, Houston, TX, USA.
Pemmaraju N; Department of Leukemia, The University of Texas MD Anderson Cancer Center, Houston, TX, USA.
Źródło:: Leukemia & lymphoma [Leuk Lymphoma] 2021 Mar; Vol. 62 (3), pp. 528-537. Date of Electronic Publication: 2020 Nov 08.
Typ publikacji:: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't
Język:: English
Imprint Name(s):: Publication: [Philadelphia, PA] : Taylor & Francis
Original Publication: Chur ; New York : London, UK : Harwood Academic Publishers ; Distributed by STBS, 1989-
MeSH Terms:: Antineoplastic Agents*/pharmacology
Antineoplastic Agents*/therapeutic use
Hematologic Neoplasms*/drug therapy
Hematologic Neoplasms*/genetics
Leukemia, Myeloid, Acute*/drug therapy
Leukemia, Myeloid, Acute*/genetics
Myeloproliferative Disorders*/drug therapy
Myeloproliferative Disorders*/genetics
Humans ; Protein Domains
Grant Information:: P30 CA016672 United States CA NCI NIH HHS
Contributed Indexing:: Keywords: BET inhibitors; Cancer; epigenetics; myeloid neoplasm
Substance Nomenclature:: 0 (Antineoplastic Agents)
Entry Date(s):: Date Created: 20201109 Date Completed: 20210427 Latest Revision: 20210427
Update Code:: 20240105
DOI:: 10.1080/10428194.2020.1842399
PMID:: 33161793
: Czasopismo naukowe

Pełny tekst

With improved understanding of the epigenetic alterations underlying cancer development, numerous novel agents targeting pathways involved in epigenetic modifications and transcription including bromodomain inhibitors are under active investigation. We aim to discuss epigenetic modulation with a focus on bromodomain extra-terminal inhibitors (BETi) in the treatment of myeloid neoplasms. Since the first proof-of-concept description of BETi synthesis and its antineoplastic effect, approximately 20 BETi have been generated and many of them are studied in the context of cancer treatment. Emerging pre-clinical and early clinical studies suggest that BETi may have activity in the management of many hematological malignancies including acute myeloid leukemia (AML), blastic plasmacytoid dendritic cell neoplasm (BPDCN), myeloproliferative neoplasm (MPNs), and lymphoma. We comprehensively reviewed and summarized preclinical and clinical data on BETi in treating myeloid neoplasms.

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