52772-41-5Relevant 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.
Stereospecific allyl-aryl coupling catalyzed by in situ generated palladium nanoparticles in water under ambient conditions
Zhao, Jingming,Ye, Jiang,Zhang, Yong Jian
, p. 491 - 498 (2013/05/09)
A practical process for the stereospecific cross-coupling of secondary allylic carbonates with arylboronic acids has been developed. The reaction is catalyzed by in situ generated palladium nanoparticles (PdNPs) without any ligands and additional stabilizers in water under ambient conditions and furnishes the allyl-aryl coupling products in high isolated yields with high stereospecificities as well as excellent chemo-, regio- and E/Z-selectivities. The in situ generated PdNPs showed extraordinary catalytic activity (S/C up to 5000) even for the allyl-aryl coupling reactions of easily eliminated allylic carbonates under aqueous ambient conditions. The mechanism of the process has also been investigated.
Palladium-catalyzed γ -selective and stereospecific allyl-aryl coupling between allylic acetates and arylboronic acids
Ohmiya, Hirohisa,Makida, Yusuke,Tanaka, Tatsunori,Sawamura, Masaya
supporting information; experimental part, p. 17276 - 17277 (2009/07/19)
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