靶向 HIF-2α 和贫血:透明细胞肾细胞癌的治疗突破

IF 11.3 1区 化学 Q1 CHEMISTRY, PHYSICAL ACS Catalysis Pub Date : 2024-07-17 DOI:10.1016/j.ctrv.2024.102801
Patricia Rioja , M. Rey-Cardenas , Guillermo De Velasco
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引用次数: 0

摘要

肾细胞癌(RCC)是一种异质性疾病,其发病率在全球呈上升趋势。Von Hipple Lindau(VHP)在调节缺氧诱导因子信号通路中的作用得到了确认和理解,这为该疾病的治疗带来了革命性的变化。贝珠替凡是一种口服缺氧诱导因子(HIF)-2α抑制剂,在治疗冯-希佩尔-林道(VHL)病以及治疗PD-1/PD-L1-和血管内皮生长因子受体(VEGFR)靶向疗法后出现疾病进展的成人RCC患者方面疗效显著。该药最常见的不良反应之一是贫血,但其治疗效果并不为人所知。本综述总结了VHL-HIF通路在ccRCC中的作用,引起了靶向HIF活性的兴趣,介绍了贝珠替凡的发展历史及其与贫血的关系,并提出了一种管理算法。
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Targeting HIF-2α and anemia: A therapeutic breakthrough for clear-cell renal cell carcinoma

Renal cell carcinoma (RCC) is a heterogenous disease which the incidence is increasing worldwide. The identification and understanding of the role of the Von Hipple Lindau (VHP) in regulating the hypoxia-inducible factor signaling pathway has revolutionized the treatment of this disease. Belzutifan is an oral hypoxia-inducible factor (HIF)-2α inhibitor, which has demonstrated efficacy in treating von Hippel-Lindau (VHL) disease and for the treatment of adults with RCC who experienced disease progression after PD-1/PD-L1– and VEGFR-targeted therapies. One of the most common adverse effect of this drug is anemia; however, it is treatment is not well known. This review summarizes role of the VHL-HIF pathway in ccRCC aroused the interest of targeting HIF activity, the history of belzutifan development and their relationship to anemia as well as propose a management algorithm.

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来源期刊
ACS Catalysis
ACS Catalysis CHEMISTRY, PHYSICAL-
CiteScore
20.80
自引率
6.20%
发文量
1253
审稿时长
1.5 months
期刊介绍: ACS Catalysis is an esteemed journal that publishes original research in the fields of heterogeneous catalysis, molecular catalysis, and biocatalysis. It offers broad coverage across diverse areas such as life sciences, organometallics and synthesis, photochemistry and electrochemistry, drug discovery and synthesis, materials science, environmental protection, polymer discovery and synthesis, and energy and fuels. The scope of the journal is to showcase innovative work in various aspects of catalysis. This includes new reactions and novel synthetic approaches utilizing known catalysts, the discovery or modification of new catalysts, elucidation of catalytic mechanisms through cutting-edge investigations, practical enhancements of existing processes, as well as conceptual advances in the field. Contributions to ACS Catalysis can encompass both experimental and theoretical research focused on catalytic molecules, macromolecules, and materials that exhibit catalytic turnover.
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