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铁糖烯酸作为Sirt5特异性抑制剂

Bin He¹, Jintang Du, Hening Lin

¹Department of Chemistry and Chemical Biology, Cornell University, Ithaca, New York 14853, USA.

Journal of the American Chemical Society

|January 24, 2012

概括

新的硫烯酸是Sirt5的强效和选择性抑制剂,Sirt5是一种依赖尼古丁胺胺氨酸二核酸的脱乙酶. 这个发现利用了Sirt5

科学领域:

生物化学生物化学
酶学是一种酶学.
药物发现药物发现药物发现

背景情况:

赛尔图因 (尼古丁胺氨酸二核酸依赖性脱乙酶) 调节关键的生物过程,如衰老,转录和新陈代谢.
人类的sirtuins (Sirt1-7) 与各种疾病有关,这使得它们成为治疗干预的关键目标.
为单个sirtuins开发选择性小分子对于药物开发和生物研究至关重要.

研究的目的:

识别和描述针对特定人体sirtuins的新型抑制剂.
为了利用sirtuins独特的酶特性进行选择性抑制剂设计.
开发Sirt5.5的强效和选择性抑制剂.

主要方法:

进行了酶抑制试验,以评估候选抑制剂的效力和选择性.
抑制剂的设计以Sirt5对马洛尼尔和基尼尔组的独特基质偏好为指导.
在不同的人类Sirtuin家族成员中对基组水解的比较分析.

主要成果:

硫糖酸被确定为Sirt5.5的强效和选择性抑制剂.
Sirt5 显示出一种独特的偏好,即在乙烯基组上对化马龙尼尔和基尼尔组进行化.
这种基偏好在7种人类基中是唯一的.

结论:

硫糖酸是Sirt5抑制剂的一个有前途的类别.
素的独特的基偏好可以被利用来开发高度选择性的抑制剂.
这种方法有助于有针对性的药物开发和对Sirtuin生物学的基础研究.

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