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 添加时间:2016/05/16 发布: 管理员







Department of Chemistry, National University of Singapore, Singapore 117543


Enzymes catalyze virtually every cellular process and metabolic exchange. They not only are instrumental in sustaining life but also are required for its regulation and diversification. Diseases such as cancer can be caused by minor changes in enzyme activities. In addition, the unique enzymes of pathogenic organisms are ripe targets for combating infections. Consequently, nearly one-third of all current drug targets are enzymes. Little, however, is understood about the physiological roles, substrate specificity, and downstream targets of the vast majority of these important proteins. A key step toward the biological characterization of enzymes, as well as their adoption as drug targets, is the development of global solutions that bridge the gap in understanding these proteins and their interactions. Catalomics is an emerging field in chemical biology in which chemical and biological tools are developed, enabling large-scale studies of enzymes at the organism level.1 In this presentation, I will discuss latest progress made in my laboratory in relation to drug discovery. Specifically, I will discuss our recent results on using microarray-based technologies for discovery of potential drug candidates.2 In addition, I will describe our recent strategy on the development of small molecule chemical probes for cell-based proteome profiling of potential drug targets (on and off), and imaging applications.3,4 Finally, I will discuss our recent efforts in the development of novel drug delivery methods by using mesoporous silica nanoparticles (MSNs) capped with oligonucleotides to achieve endocytosis-independent cellular uptake and intracellular controlled release of drugs with novel theranostic properties.5



1. Uttamchandani, M.; Lu, C.H.S.; Yao, S.Q., Acc. Chem. Res. 2009, 42, 1183-1192.
2. a)  Na, Z.; Peng, B.; Ng, S.; Pan, S.; Lee, J.-S.; Shen, H.M.; Yao, S.Q., Angew. Chem. Int. Ed. 2015, 54, 2515-2519; b) Na, Z.; Pan, S.; Uttamchandani, M.; Yao, S.Q., Angew. Chem. Int. Ed. 2014, 53, 8421-8426; c) Zhang, C.; Tan, C.Y.J.; Ge, J.; Na, Z.; Chen, G.Y.J.; Uttamchandani, M.; Sun, H.; Yao, S.Q., Angew. Chem. Int. Ed. 2013, 52, 14060-14064.
3. a) Su, Y.; Ge, J.; Zhu, B.; Zheng, Y.-G.; Zhu, Q.; Yao, S. Q., Curr. Opin. Chem. Biol. 2013, 17, 768-775; b) Li, Z.; Qian, L.; Li, L.; Bernhammer, J. C.; Huynh, H. V.; Lee, J.-S.; Yao, S. Q., Angew. Chem. Int. Ed. 2016, 55, 2002-2006; c) Li, Z.; Wang, D.; Li, L.; Pan, S.; Na, Z.; Tan, C.Y.J.; Yao, S.Q., J. Am. Chem. Soc. 2014, 136, 9990-9998.
4. a) Qian, L.; Li, L.; Yao, S.Q., Acc. Chem. Res. 2016, 49, 626-634; b) Li, L.; Zhang, C.-W.; Ge, J.; Qian, L.; Chai, B-H.; Zhu, Q.; Lee, J.-S.; Lim, K.-L.; Yao, S.Q., Angew. Chem. Int. Ed. 2015, 54, 10821-10825; c) Li. L.; Zhang, C.-W.; Chen, G.Y.J.; Zhu, B.; Chai, C.; Xu, Q.-H., Tan, E.-K.; Zhu, Q.; Lim, K.-L.; Yao, S.Q., Nat. Commun. 2014, 5, 3276.
5. a) Yu, C.; Qian, L.; Uttamchandani, M.; Li, L.; Yao, S.Q., Angew. Chem. Int. Ed. 2015, 54, 10574-10578; b) Fu, J.; Yu, C.; Li, L.; Yao, S.Q., J. Am. Chem. Soc. 2015, 137, 12153-12160; (c) Yu, C.; Qian, L.; Ge, J.; Fu, J.; Yuan, P.; Yao, S. Q., Angew. Chem. Int. Ed. 2016, in press.



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