Kantner Terrence, Alkhawaja Bayan, Watts Andrew G
Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, U.K.
ACS Omega. 2017 Sep 30;2(9):5785-5791. doi: 10.1021/acsomega.7b01094. Epub 2017 Sep 14.
Trialkylphosphines tris(2-carboxy-ethyl)-phosphine and tris(3-hydroxypropyl)-phosphine are popular reagents for the reduction of cysteine residues in bioconjugation reactions using maleimides. However, it has been demonstrated that these phosphines are reactive toward maleimide, necessitating their removal before the addition of the Michael acceptor. Here, a method using water-soluble PEG-azides is reported for the quenching of trialkylphosphines in situ, which is demonstrated to improve the level of maleimide conjugation to proteins.
三烷基膦（三（2-羧基-乙基）-膦和三（3-羟丙基）-膦）是在使用马来酰亚胺的生物共轭反应中用于还原半胱氨酸残基的常用试剂。然而，已经证明这些膦对马来酰亚胺具有反应性，因此在添加迈克尔受体之前必须将其除去。在此，报道了一种使用水溶性聚乙二醇叠氮化物原位淬灭三烷基膦的方法，该方法被证明可提高马来酰亚胺与蛋白质的共轭水平。
