<br>JQ1 类似物的合成、SAR 及其作为 PROTAC 在癌症治疗中的应用,Bioorganic & Medicinal Chemistry

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JQ1 类似物的合成、SAR 及其作为 PROTAC 在癌症治疗中的应用
Bioorganic & Medicinal Chemistry ( IF 3.3 ) Pub Date : 2024-08-16 , DOI: 10.1016/j.bmc.2024.117875
Soumik De ₁ , Raghaba Sahu ₂ , Shubhendu Palei ₃ , Laxmi Narayan Nanda ₄

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JQ1 是一种神奇的治疗分子，可选择性抑制 BRD4 信号通路，因此广泛用于抗癌药物发现计划。由于其独特的选择性BRD4结合特性，其应用在双功能PROTAC分子的设计和合成中得到进一步扩展。这种 BRD4 靶向 PROTAC 分子通过蛋白水解选择性地降解蛋白质。迄今为止，JQ1 有多种修饰，并且学术界和工业界的多个研究小组针对致癌基因在 PROTAC 技术中的应用进行了广泛的探索。在这篇综述中，我们介绍了 JQ1 分子的发现和合成。 JQ1 类似物的 SAR 将帮助研究人员开发有效的 JQ1 化合物，并改善对恶性细胞的抑制特性。此外，我们还探讨了 JQ1 类似物在 PROTAC 技术中的潜在应用。溴结构域蛋白家族的简史以及与 PROTAC 技术相关的障碍可以帮助理解当前研究的背景，这有可能改善药物开发过程。总的来说，这篇综述全面评价了 JQ1 分子及其在 PROTAC 技术和癌症治疗中的先前实施。

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Synthesis, SAR, and application of JQ1 analogs as PROTACs for cancer therapy

JQ1 is a wonder therapeutic molecule that selectively inhibits the BRD4 signaling pathway and is thus widely used in the anticancer drug discovery program. Due to its unique selective BRD4 binding property, its applications are further extended in the design and synthesis of bi-functional PROTAC molecules. This BRD4 targeting PROTAC molecule selectively degrades the protein by proteolysis. There are several modifications of JQ1 known to date and extensively explored for their applications in PROTAC technology by several research groups in academia as well as industry for targeting oncogenic genes. In this review, we have covered the discovery and synthesis of the JQ1 molecule. The SAR of the JQ1 analogs will help researchers develop potent JQ1 compounds with improved inhibitory properties against malignant cells. Furthermore, we explored the potential application of JQ1 analogs in PROTAC technology. The brief history of the bromodomain family of proteins, as well as the obstacles connected with PROTAC technology, can help comprehend the context of the current research, which has the potential to improve the drug development process. Overall, this review comprehensively appraises JQ1 molecules and their prior implementation in PROTAC technology and cancer therapy.

更新日期：2024-08-16

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