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CDK9 INHIBITORS: a promising combination partner in the treatment of hematological malignancies

Most hematological malignancies are characterized by overexpression of certain cancer promoting genes, such as MYC, MCL1 and cyclin D1. Preclinical studies in animal models have shown that CDK9 inhibitors supress the transcription of these anti-apoptotic and pro-survival proteins, and suggest their...

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Detalles Bibliográficos
Autores principales: Morillo, Daniel, Vega, Gala, Moreno, Victor
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Impact Journals LLC 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10408673/
https://www.ncbi.nlm.nih.gov/pubmed/37552223
http://dx.doi.org/10.18632/oncotarget.28473
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author Morillo, Daniel
Vega, Gala
Moreno, Victor
author_facet Morillo, Daniel
Vega, Gala
Moreno, Victor
author_sort Morillo, Daniel
collection PubMed
description Most hematological malignancies are characterized by overexpression of certain cancer promoting genes, such as MYC, MCL1 and cyclin D1. Preclinical studies in animal models have shown that CDK9 inhibitors supress the transcription of these anti-apoptotic and pro-survival proteins, and suggest their potential synergism with other drugs. In its first in-human trial, enitociclib demonstrated clinical activity in a small cohort of patients with high grade B lymphoma with MYC and BCL2 and/or BCL6 rearrangements, inducing complete responses in 2 of 7 subjects (29%) in monotherapy. These data suggest CDK9 inhibitors could play a role in the treatment of hematological diseases and could be a great ally when combined with other therapeutic approaches.
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spelling pubmed-104086732023-08-09 CDK9 INHIBITORS: a promising combination partner in the treatment of hematological malignancies Morillo, Daniel Vega, Gala Moreno, Victor Oncotarget Research Perspective Most hematological malignancies are characterized by overexpression of certain cancer promoting genes, such as MYC, MCL1 and cyclin D1. Preclinical studies in animal models have shown that CDK9 inhibitors supress the transcription of these anti-apoptotic and pro-survival proteins, and suggest their potential synergism with other drugs. In its first in-human trial, enitociclib demonstrated clinical activity in a small cohort of patients with high grade B lymphoma with MYC and BCL2 and/or BCL6 rearrangements, inducing complete responses in 2 of 7 subjects (29%) in monotherapy. These data suggest CDK9 inhibitors could play a role in the treatment of hematological diseases and could be a great ally when combined with other therapeutic approaches. Impact Journals LLC 2023-08-07 /pmc/articles/PMC10408673/ /pubmed/37552223 http://dx.doi.org/10.18632/oncotarget.28473 Text en Copyright: © 2023 Morillo et al. https://creativecommons.org/licenses/by/3.0/This is an open access article distributed under the terms of the Creative Commons Attribution License (https://creativecommons.org/licenses/by/3.0/) (CC BY 3.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
spellingShingle Research Perspective
Morillo, Daniel
Vega, Gala
Moreno, Victor
CDK9 INHIBITORS: a promising combination partner in the treatment of hematological malignancies
title CDK9 INHIBITORS: a promising combination partner in the treatment of hematological malignancies
title_full CDK9 INHIBITORS: a promising combination partner in the treatment of hematological malignancies
title_fullStr CDK9 INHIBITORS: a promising combination partner in the treatment of hematological malignancies
title_full_unstemmed CDK9 INHIBITORS: a promising combination partner in the treatment of hematological malignancies
title_short CDK9 INHIBITORS: a promising combination partner in the treatment of hematological malignancies
title_sort cdk9 inhibitors: a promising combination partner in the treatment of hematological malignancies
topic Research Perspective
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10408673/
https://www.ncbi.nlm.nih.gov/pubmed/37552223
http://dx.doi.org/10.18632/oncotarget.28473
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