白血病致癌基因Bcr-Abl的l型和d型SH2结构域的合成。

Schmidt Nina, Abendroth Frank, Vázquez Olalla, Hantschel Oliver

Institute of Physiological Chemistry, University of Marburg 35032 Marburg Germany

Faculty of Chemistry, University of Marburg 35032 Marburg Germany

RSC Chem Biol. 2022 Jul 6;3(8):1008-1012. doi: 10.1039/d2cb00108j. eCollection 2022 Aug 3.

The d- and l-versions of the Bcr-Abl SH2 domain (12.7 kDa) were synthesized. Key optimizations included pseudoproline incorporation, -terminal hydrophilic tail addition and mild -acetoxy succinimide acetylation. Their folding and activity are as for the recombinant protein. Our results will enable engineering of mirror-image monobody antagonists of the central oncoprotein Bcr-Abl.

合成了Bcr-Abl SH2结构域（12.7 kDa）的d型和l型。关键优化包括引入假脯氨酸、添加N端亲水尾以及进行温和的N-乙酰氧基琥珀酰亚胺乙酰化。它们的折叠和活性与重组蛋白相同。我们的结果将有助于构建中心癌蛋白Bcr-Abl的镜像单克隆抗体拮抗剂。