Leiden Institute of Chemistry, Leiden University , P.O. Box 9502, 2300 RA Leiden, The Netherlands.
Org Lett. 2014 May 16;16(10):2744-7. doi: 10.1021/ol501049c. Epub 2014 May 5.
A new bioorthogonal N-acylazetine tag, suitable for tetrazine mediated inverse electron-demand Diels-Alder conjugation, is developed. The tag is small and achiral. We demonstrate the usefulness of N-acylazetine-tetrazine based bioorthogonal chemistry in two-step activity-based protein profiling. The performance of the new tetrazinophile in the labeling of catalytically active proteasome subunits was comparable to that of the more sterically demanding norbornene tag.
我们开发了一种新的生物正交 N-酰基氮丙啶标记物，适用于四嗪介导的逆电子需求 Diels-Alder 共轭反应。该标记物体积小且无手性。我们在两步基于活性的蛋白质谱分析中证明了 N-酰基氮丙啶-四嗪基生物正交化学的有用性。新型四嗪亲和物在标记催化活性蛋白酶体亚基方面的性能与空间要求更高的降冰片烯标记物相当。
