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Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical

Oncogenic fusion proteins, arising from chromosomal rearrangements, have emerged as prominent drivers of tumorigenesis and crucial therapeutic targets in cancer research. In recent years, the potential of small molecular inhibitors in selectively targeting fusion proteins has exhibited significant p...

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Detalles Bibliográficos
Autores principales: Kong, Yichao, Jiang, Caihong, Wei, Guifeng, Sun, Kai, Wang, Ruijie, Qiu, Ting
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10301843/
https://www.ncbi.nlm.nih.gov/pubmed/37375228
http://dx.doi.org/10.3390/molecules28124672
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author Kong, Yichao
Jiang, Caihong
Wei, Guifeng
Sun, Kai
Wang, Ruijie
Qiu, Ting
author_facet Kong, Yichao
Jiang, Caihong
Wei, Guifeng
Sun, Kai
Wang, Ruijie
Qiu, Ting
author_sort Kong, Yichao
collection PubMed
description Oncogenic fusion proteins, arising from chromosomal rearrangements, have emerged as prominent drivers of tumorigenesis and crucial therapeutic targets in cancer research. In recent years, the potential of small molecular inhibitors in selectively targeting fusion proteins has exhibited significant prospects, offering a novel approach to combat malignancies harboring these aberrant molecular entities. This review provides a comprehensive overview of the current state of small molecular inhibitors as therapeutic agents for oncogenic fusion proteins. We discuss the rationale for targeting fusion proteins, elucidate the mechanism of action of inhibitors, assess the challenges associated with their utilization, and provide a summary of the clinical progress achieved thus far. The objective is to provide the medicinal community with current and pertinent information and to expedite the drug discovery programs in this area.
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spelling pubmed-103018432023-06-29 Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical Kong, Yichao Jiang, Caihong Wei, Guifeng Sun, Kai Wang, Ruijie Qiu, Ting Molecules Review Oncogenic fusion proteins, arising from chromosomal rearrangements, have emerged as prominent drivers of tumorigenesis and crucial therapeutic targets in cancer research. In recent years, the potential of small molecular inhibitors in selectively targeting fusion proteins has exhibited significant prospects, offering a novel approach to combat malignancies harboring these aberrant molecular entities. This review provides a comprehensive overview of the current state of small molecular inhibitors as therapeutic agents for oncogenic fusion proteins. We discuss the rationale for targeting fusion proteins, elucidate the mechanism of action of inhibitors, assess the challenges associated with their utilization, and provide a summary of the clinical progress achieved thus far. The objective is to provide the medicinal community with current and pertinent information and to expedite the drug discovery programs in this area. MDPI 2023-06-09 /pmc/articles/PMC10301843/ /pubmed/37375228 http://dx.doi.org/10.3390/molecules28124672 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Kong, Yichao
Jiang, Caihong
Wei, Guifeng
Sun, Kai
Wang, Ruijie
Qiu, Ting
Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical
title Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical
title_full Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical
title_fullStr Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical
title_full_unstemmed Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical
title_short Small Molecule Inhibitors as Therapeutic Agents Targeting Oncogenic Fusion Proteins: Current Status and Clinical
title_sort small molecule inhibitors as therapeutic agents targeting oncogenic fusion proteins: current status and clinical
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10301843/
https://www.ncbi.nlm.nih.gov/pubmed/37375228
http://dx.doi.org/10.3390/molecules28124672
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