Department of Genetics, University of Delhi South Campus, Benito Juarez Road, New Delhi, 110 021, India.
Department of Genetics, University of Delhi South Campus, Benito Juarez Road, New Delhi, 110 021, India.
Biochem Biophys Res Commun. 2023 Feb 19;645:88-96. doi: 10.1016/j.bbrc.2023.01.022. Epub 2023 Jan 13.
Increasing reports suggest insulin signalling pathway as a putative drug target against polyglutamine [poly(Q)] disorders, such as Huntington's disease (HD), Spinocerebellar ataxias (SCA) 1, 2, 3 etc. However, studies on drug-based stimulation of insulin signalling cascade to mitigate poly(Q) pathogenesis are lacking. In our study, we adopted an evidence-based approach to examine if some established insulin stimulating drug can be utilized to restrict poly(Q) aetiology in Drosophila disease models. For the first time, we report that glipizide, an FDA approved anti-diabetic drug upregulates insulin signalling in poly(Q) expressing tissues and restricts formation of inclusion bodies and neurodegeneration. Moreover, it reinstates the chromatin architecture by improving histone acetylation, which is otherwise abrogated due to poly(Q) toxicity. In view of the functional conservation of insulin signalling pathway in Drosophila and humans, our finding strongly suggests that glipizide can be repurposed as an effective treatment strategy against the neurodegenerative poly(Q) disorders. Also, with appropriate validation studies in mammalian disease models, glipizide could be subsequently considered for the clinical trials in human patients.
越来越多的报告表明,胰岛素信号通路是治疗多聚谷氨酰胺[poly(Q)]疾病的潜在药物靶点,如亨廷顿病(HD)、脊髓小脑共济失调(SCA)1、2、3 等。然而,关于基于药物的刺激胰岛素信号级联以减轻 poly(Q)发病机制的研究还很缺乏。在我们的研究中,我们采用了循证方法来研究一些已被证实的胰岛素刺激药物是否可以用于限制果蝇疾病模型中的 poly(Q)发病机制。我们首次报道了 FDA 批准的抗糖尿病药物格列吡嗪可以上调 poly(Q)表达组织中的胰岛素信号,限制包涵体的形成和神经退行性变。此外,它通过改善组蛋白乙酰化来恢复染色质结构,否则由于 poly(Q)毒性而被破坏。鉴于胰岛素信号通路在果蝇和人类中的功能保守性,我们的发现强烈表明格列吡嗪可以被重新用作治疗神经退行性多聚谷氨酰胺疾病的有效治疗策略。此外,在哺乳动物疾病模型中进行适当的验证研究后,格列吡嗪可以随后考虑在人类患者中进行临床试验。