Xu Hua, Hett Erik C, Gopalsamy Ariamala, Parikh Mihir D, Geoghegan Kieran F, Kyne Robert E, Menard Carol A, Narayanan Arjun, Robinson Ralph P, Johnson Douglas S, Tones Michael A, Jones Lyn H
Worldwide Medicinal Chemistry, Pfizer Inc., 610 Main Street, Cambridge, MA 02139, USA.
Mol Biosyst. 2015 Oct;11(10):2709-12. doi: 10.1039/c5mb00288e.
Despite its diverse applications, such as identification of the protein binding partners of small molecules and investigation of intracellular drug-target engagement, photoaffinity labelling (PAL) is intrinsically challenging, primarily due to the difficulty in discovering functionally active photoaffinity probes. Here we describe the creation of a chemoproteomic library to discover a novel photoaffinity probe for DcpS, an mRNA decapping enzyme that is a putative target for Spinal Muscular Atrophy. This library approach expedites the discovery of photoaffinity probes and expands the chemical biology toolbox to include RNA cap-binding proteins.
尽管光亲和标记(PAL)有多种应用,如鉴定小分子的蛋白质结合伙伴以及研究细胞内药物与靶点的结合情况,但它本质上具有挑战性,主要是因为难以发现具有功能活性的光亲和探针。在这里,我们描述了一个化学蛋白质组学文库的构建,以发现一种针对DcpS的新型光亲和探针,DcpS是一种mRNA去帽酶,被认为是脊髓性肌萎缩症的一个潜在靶点。这种文库方法加快了光亲和探针的发现,并扩展了化学生物学工具箱,使其包括RNA帽结合蛋白。