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

Yichao Kong, Caihong Jiang, Guifeng Wei, Kai Sun, Ruijie Wang, Ting Qiu

2023Molecules15 citationsDOIOpen Access PDF

Abstract

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.

Topics & Concepts

Drug discoveryComputational biologyFusion proteinSmall moleculeCarcinogenesisMechanism (biology)BiologyFusion geneCancerBioinformaticsGeneGeneticsRecombinant DNAPhilosophyEpistemologyProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysPeptidase Inhibition and Analysis
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