Brown Laboratories, Department of Chemistry and Biochemistry, University of Delaware, Newark, DE 19716, United States.
Curr Opin Chem Biol. 2013 Oct;17(5):753-60. doi: 10.1016/j.cbpa.2013.07.031. Epub 2013 Aug 23.
Discussed herein is the development and advancement of trans-cyclooctene as a tool for facilitating bioorthogonal labeling through reactions with s-tetrazines. While a number of strained alkenes have been shown to combine with tetrazines for applications in bioorthogonal labeling, trans-cyclooctene enables fastest reactivity at low concentration with rate constants in excess of k2=10(6) M(-1) s(-1). In the present article, we describe advances in computation and synthesis that have enabled applications in chemical biology and nuclear medicine.
本文讨论了反式环辛烯作为一种工具的发展和进步，它可以通过与 s-四嗪的反应促进生物正交标记。虽然已经证明许多应变烯烃可以与四嗪结合用于生物正交标记，但反式环辛烯在低浓度下具有超过 k2=10(6) M(-1) s(-1)的速率常数，反应最快。在本文中，我们描述了计算和合成方面的进展，这些进展使得其在化学生物学和核医学中的应用成为可能。
