An improved synthesis of a fluorophosphonate–polyethylene glycol–biotin probe and its use against competitive substrates

• Hao Xu,
• Hairat Sabit,
• Gordon L. Amidon and
• H. D. Hollis Showalter

Beilstein J. Org. Chem. 2013, 9, 89–96, doi:10.3762/bjoc.9.12

• these competition studies demonstrate a new application of FP-based probes seldom explored before. Keywords: biotin; fluorophosphonate; high turnover rate; reversible substrate; Introduction One of the goals of chemical biology is to develop small–molecule- and biomolecule-based probes to interrogate

• by the Cravatt group [21]. Kinetic study of FP probe labelling activity An incubation-time control study is the key toward successfully monitoring the competition between FP probe 1 and a reversible substrate with a high turnover rate. Hence, over a long incubation time, the substrate will be

• . Additionally, preliminary kinetic and competition studies of probe 1 with reversible substrates have been conducted, showing that FP probes can be utilized for the investigation of reversible substrate activities as long as sufficient care is taken to identify the time course of reaction. Experimental All