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翻訳と辞書　辞書検索 [ 開発暫定版 ] スポンサード リンク Anti-thrombin aptamers ： ウィキペディア英語版 Anti-thrombin aptamers Anti-thrombin aptamers are G-quadruplex-bearing oligonucleotides, which recognizes the exosites of human thrombin. The first anti-thrombin aptamer, TBA, was generated through via SELEX (Systematic Evolution of Ligands by Exponential Enrichment) technology in 1992 by L.C. Bock, J.J. Toole and colleagues.〔Bock, L. C. et al., Selection of single-stranded DNA molecules that bind and inhibit human thrombin. Nature 355, 564-566, (doi:10.1038/355564a0 ) (1992).〕 A second thrombin-binding aptamer, HD22, recognizes thrombin exosite II and was discovered in 1997 by NeXstar (now Gilead Sciences).〔Tasset, D. M. et al., Oligonucleotide inhibitors of human thrombin that bind distinct epitopes. Journal of molecular biology 272, 688-698, (doi:10.1006/jmbi.1997.1275 ) (1997).〕 These two aptamers have high affinity and good specificity and have been widely-studied and used for the development of aptamer-based therapeutics and diagnostics. == Aptamer TBA (the exosite I-binding aptamer)== The aptamer TBA (also known as G15D, HTQ, HD1 or ARC183) is a 15-mer single-stranded DNA with the sequence ''5'-GGTTGGTGTGGTTGG-3.〔 It interacts with the exosite I of human alpha-thrombin, which is the binding site of fibrinogen, so this aptamer acts as an anti-coagulant agent inhibiting the activation of fibrinogen as well as platelet aggregation. In addition, TBA shows good affinity and specificity against thrombin. The dissociation constant of TBA-thrombin has been reported in nano-molar range, and TBA does not interact with other plasma proteins or thrombin analogues (e.g., gamma-thrombin).〔Li, J. J. et al., Molecular aptamer beacons for real-time protein recognition. Biochemical and biophysical research communications 292, 31-40, (doi: 10.1006/bbrc.2002.6581 ) (2002).〕 As a result, TBA has been used as a short-term anti-coagulant designed for the application in the coronary artery bypass graft surgery, and its optimized form (NU172) is now under the phase II of clinical trial by ARCA Biopharma (NCT00808964).〔http://www.clinicaltrials.gov/ct2/show/NCT00808964?term=NU+172&rank=1〕 Also, due to its high affinity and specificity, a variety of sensors was coupled with TBA and developed for thrombosis diagnostics. 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「Anti-thrombin aptamers」の詳細全文を読む スポンサード リンク 翻訳と辞書 : 翻訳のためのインターネットリソース Copyright(C) kotoba.ne.jp 1997-2016. All Rights Reserved.