1.Design and synthesis of photoaffinity biotin labelled 2'-O-propargyl-guanosine.
Lu-xin NA ; Xin LIU ; Zhuo-ming MENG ; Zhu GUAN ; Li-he ZHANG ; Zhen-jun YANG
Acta Pharmaceutica Sinica 2015;50(1):59-63
Photoaffinity labeling is widely applied to demonstrate targets of small molecule ligands. In this paper, biotin photoaffinity labeled molecule with propargyl group 1 has been designed and synthesized, followed it's labeling of N2-acetyl-2'-O-propargyl guanosine 9 by "click chemistry". This technology presents delight development potential in labeling of second messenger cyclic nucleotide, antisense oligonucleotide or siRNA.
Biotin
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chemistry
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Click Chemistry
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Guanosine
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chemical synthesis
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chemistry
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Ligands
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Photoaffinity Labels
2.The application of small molecule bioactive probes in the identification of cellular targets.
Acta Pharmaceutica Sinica 2012;47(3):299-306
Identification of the cellular targets of bioactive compounds is a major challenge and a key issue in chemical biology and drug discovery. As an important technology in functional proteomics, small molecule probes play a pivotal role in the identification of cellular targets of bioactive compounds. This review is intended to introduce the application principles and structural design philosophy of chemical probes for the purpose of mechanistic study. Recent cases of successful application were also discussed to further demonstrate the principles and significance ofbioactive small molecule-based probes.
Biotin
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metabolism
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Drug Delivery Systems
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Drug Design
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Drug Discovery
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methods
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Molecular Probe Techniques
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Molecular Probes
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chemistry
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Photoaffinity Labels
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Proteins
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metabolism
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Proteome
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chemistry
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Proteomics
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methods
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Small Molecule Libraries
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chemistry
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pharmacology