期刊
METHODS
卷 43, 期 4, 页码 313-323出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.ymeth.2007.08.003
关键词
G-quadruplex DNA; binding dialysis; drug discovery; structural selectivity
资金
- NCI NIH HHS [CA35635, R01 CA035635] Funding Source: Medline
- NIGMS NIH HHS [R01 GM077422-01A1, R01 GM077422, GM077422] Funding Source: Medline
G-quadrplex DNA can exist in a rich variety of structural forms, ranging from unimolecular folded structures containing diverse types of loops and strand oreintations, to bimolecular dimeric structures, and finally to tetramolecular parallel-stranded structures. These diverse structures present numerous potential small molecule binding sites with distinctive properties. There is mounting evidence for important functional roles for G-quadruplex structures in biology. G-quadruplexes may participate in the maintenance of telomeres, in transcriptional regulation and, in mRNA, may act to modulate translation. G-quadruplexes thus represent an attractive target for new small-molecule therapeutic agents. Competition dialysis provides a useful tool for the discovery of small molecules that selectively recognize the unique structural features of G-quadruplexes. The principles and practice of the competition dialysis experiment are described here. (c) 2007 Elsevier Inc. All rights reserved.
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