52343-38-1Relevant articles and documents
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes
Wang, Congcong,Zhang, Yu-Fang,Guo, Shimeng,Zhao, Quan,Zeng, Yanping,Xie, Zhicheng,Xie, Xin,Lu, Boxun,Hu, Youhong
, p. 941 - 957 (2020/11/30)
GPR52 is an orphan G protein-coupled receptor (GPCR) that has been recently implicated as a potential drug target of Huntington's disease (HD), an incurable monogenic neurodegenerative disorder. In this research, we found that striatal knockdown of GPR52 reduces mHTT levels in adult HdhQ140 mice, validating GPR52 as an HD target. In addition, we discovered a highly potent and specific GPR52 antagonist Comp-43 with an IC50 value of 0.63 μM by a structure-activity relationship (SAR) study. Further studies showed that Comp-43 reduces mHTT levels by targeting GPR52 and promotes survival of mouse primary striatal neurons. Moreover, in vivo study showed that Comp-43 not only reduces mHTT levels but also rescues HD-related phenotypes in HdhQ140 mice. Taken together, our study confirms that inhibition of GPR52 is a promising strategy for HD therapy, and the GPR52 antagonist Comp-43 might serve as a lead compound for further investigation.
Diastereo- and enantioselective asymmetric hydrogenation of α-amido-β-keto phosphonates via dynamic kinetic resolution
Tao, Xiaoming,Li, Wanfang,Li, Xiaoming,Xie, Xiaomin,Zhang, Zhaoguo
supporting information, p. 72 - 75 (2013/03/28)
Dynamic kinetic resolution of various α-amido-β-keto phosphonates via asymmetric hydrogenation proceeded efficiently to give the corresponding β-hydroxy-α-amido phosphonates in high diastereo- and enantioselectivities (up to 99:1 syn/anti, 99.8% ee). The addition of catalytic amounts of CeCl3 3 7H2O is necessary to achieve both good selectivity and catalytic efficiency under mild reaction conditions.
Highly enantioselective epoxidation of α,β-unsaturated ketones catalyzed by primary-secondary diamines
Lu, Yingpeng,Zheng, Changwu,Yang, Yingquan,Zhao, Gang,Zou, Gang
supporting information; experimental part, p. 3129 - 3133 (2012/01/03)
The asymmetric epoxidation of α,β-unsaturated ketones has been achieved by using functional and readily accessible primary-secondary diamines as the catalysts, giving the useful alkyl epoxy products with good yields and high enantioselectivities (up to 99% ee). Copyright