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鲁比鲁昔替尼:一种光释放的抗肿瘤 JAK 抑制剂。

RuBi-Ruxolitinib: A Photoreleasable Antitumor JAK Inhibitor.

机构信息

Departamento de Química Inorgánica, Analítica y Química Física, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, INQUIMAE, CONICET, Buenos Aires C1428EHA, Argentina.

Institute for Cancer Genetics, Columbia University, New York, New York 10032, United States.

出版信息

J Am Chem Soc. 2024 May 15;146(19):13317-13325. doi: 10.1021/jacs.4c01720. Epub 2024 May 3.

Abstract

We describe the synthesis and biological testing of ruthenium-bipyridine ruxolitinib (RuBiRuxo), a photoreleasable form of ruxolitinib, a JAK inhibitor used as an antitumoral agent in cutaneous T-cell lymphomas (CTCL). This novel caged compound is synthesized efficiently, is stable in aqueous solution at room temperature, and is photoreleased rapidly by visible light. Irradiation of RuBiRuxo reduces cell proliferation and induces apoptosis in a light- and time-dependent manner in a CTCL cell line. This effect is specific and is mediated by a decreased phosphorylation of STAT proteins. Our results demonstrate the potential of ruthenium-based photocompounds and light-based therapeutic approaches for the potential treatment of cutaneous lymphomas and other pathologies.

摘要

我们描述了钌-联吡啶鲁索替尼(RuBiRuxo)的合成和生物测试,RuBiRuxo 是鲁索替尼的光释放形式,鲁索替尼是一种用于治疗皮肤 T 细胞淋巴瘤(CTCL)的抗肿瘤药物。这种新型笼状化合物可以高效合成,在室温下的水溶液中稳定,并且可以通过可见光快速光解。RuBiRuxo 的照射以光和时间依赖的方式减少 CTCL 细胞系中的细胞增殖并诱导细胞凋亡。这种作用是特异性的,是由 STAT 蛋白磷酸化减少介导的。我们的结果表明,基于钌的光化合物和基于光的治疗方法具有治疗皮肤淋巴瘤和其他病理的潜力。

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