Department of Chemistry, University of Basel, St. Johanns-Ring 19, Basel 4056, Switzerland.
Chem Commun (Camb). 2020 Oct 28;56(84):12861-12864. doi: 10.1039/d0cc04337k. Epub 2020 Sep 24.
Herein, a novel and rationally designed ortho-substituted pyridine activator is reported that reacts rapidly and selectively with cysteine thiols. It forms reduction-stable conjugates and induces large pseudocontact shifts, residual dipolar couplings and paramagnetic relaxation enhancement on both ubiquitin S57C and human carbonic anhydrase II S50C constructs under physiological conditions.
本文报道了一种新颖且合理设计的邻位取代吡啶激活剂，它可与半胱氨酸巯基快速且选择性地反应。在生理条件下，它与泛素 S57C 和人碳酸酐酶 II S50C 构建体形成还原稳定的缀合物，并诱导大的赝接触位移、残馀偶极耦合和顺磁弛豫增强。
