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( Yuyao Zhu ),( Jian Zhang ),( Xiaode Huang ),( Bin Chen ),( Hua Qian ),( Botao Zhao ) 한국미생물생명공학회(구 한국산업미생물학회) 2018 Journal of microbiology and biotechnology Vol.28 No.11
A series of pentacyclic triterpenoids similar to glycyrrhetinic acid were designed and synthesized via the combination of chemical modification and microbial catalysis. All products were screened for the glycogen phosphorylases inhibitory activities in vitro. Within this series of derivatives, compound 5 displayed good inhibitory activities with IC<sub>50</sub> value of 27.7 μM, which is better than that of the other derivatives and glycyrrhetinic acid. Structure- activity relationship (SAR) analysis of these inhibitors was also discussed.
Zhu, Jia-Ying,Li, Yuyao,Cao, Dong-Mei,Yang, Hongjuan,Oh, Eunkyoo,Bi, Yang,Zhu, Shengwei,Wang, Zhi-Yong Elsevier 2017 Molecular cell Vol.66 No.5
<P><B>Summary</B></P> <P>The glycogen synthase kinase-3 (GSK3) family kinases are central cellular regulators highly conserved in all eukaryotes. In <I>Arabidopsis</I>, the GSK3-like kinase BIN2 phosphorylates a range of proteins to control broad developmental processes, and BIN2 is degraded through unknown mechanism upon receptor kinase-mediated brassinosteroid (BR) signaling. Here we identify KIB1 as an F-box E3 ubiquitin ligase that promotes the degradation of BIN2 while blocking its substrate access. Loss-of-function mutations of KIB1 and its homologs abolished BR-induced BIN2 degradation and caused severe BR-insensitive phenotypes. KIB1 directly interacted with BIN2 in a BR-dependent manner and promoted BIN2 ubiquitination in vitro. Expression of an F-box-truncated KIB1 caused BIN2 accumulation but dephosphorylation of its substrate BZR1 and activation of BR responses because KIB1 blocked BIN2 binding to BZR1. Our study demonstrates that KIB1 plays an essential role in BR signaling by inhibiting BIN2 through dual mechanisms of blocking substrate access and promoting degradation.</P> <P><B>Highlights</B></P> <P> <UL> <LI> KIB1 is an essential positive regulator in brassinosteroid signaling </LI> <LI> KIB1 mediates BR-induced ubiquitination and degradation of GSK3 kinase BIN2 </LI> <LI> KIB1 binding to BIN2 prevents BIN2-substrate interaction and promotes BIN2 degradation </LI> </UL> </P> <P><B>Graphical Abstract</B></P> <P>[DISPLAY OMISSION]</P>
Zhu, Yuyao,Zhao, Botao,Huang, Xiaode,Chen, Bin,Qian, Hua The Korean Society for Microbiology and Biotechnol 2015 Journal of microbiology and biotechnology Vol.25 No.6
The natural crosslinking agent genipin has been applied widely in biomedicines and foods nowadays. Because of the special hemiacetal ring structure in its molecule, it can only be prepared by hydrolysis of geniposide according to biocatalysis. In this research, strategies including aqueous-organic biphasic catalysis and substrate fed-batch mode were adopted to improve the biocatalysis process of genipin. A 10 L ethyl acetate-aqueous biphasic system with geniposide fed-batch led to a satisfying genipin yield. With Fusarium solani ACCC 36223, 15.7 g/l genipin in the ethyl acetate phase was obtained, corresponding to space-time yields of 0.654 g l<sup>-1</sup> h<sup>-1</sup>.