A small-molecule probe for monitoring binding to prolyl hydroxylase domain 2 by fluorescence polarisation. Issue 91 (28th October 2020)

• Record Type: Journal Article
• Authors: Li, Zhihong; Zhen, Shuai; Su, Kaijun; Tumber, Anthony; Yu, Quanwei; Dong, Ying; McDonough, Michael; Schofield, Christopher J.; Zhang, Xiaojin
• Is Part Of: Chemical communications. Volume 56:Issue 91(2020)
• Page Start: 14199
• Page End: 14202
• Publication Date: 2020-10-28
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d0cc06353c
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : A small-molecule FP probe useful for monitoring binding to PHD2 and identifying potential PHD2 inhibitors. Abstract : Inhibition of the dioxygen sensing hypoxia-inducible factor prolyl hydroxylases has potential therapeutic benefit for treatment of diseases, including anaemia. We describe the discovery of a small-molecule probe useful for monitoring binding to human prolyl hydroxylase domain 2 (PHD2) via fluorescence polarisation. The assay is suitable for high-throughput screening of PHD inhibitors with both weak and strong affinities, as shown by work with clinically used inhibitors and naturally occurring PHD inhibitors.