Pan, Sijun Jang, Se-Young Liew, Si Si Fu, Jiaqi Wang, Danyang Lee, Jun-Seok Yao, Shao Q. 2024-01-19T23:33:17Z 2024-01-19T23:33:17Z 2021-09-03 2018-01-08 1433-7851 https://pubs.kist.re.kr/handle/201004/121813 Chemical probes are powerful tools for interrogating small molecule-target interactions. With additional fluorescence Turn-ON functionality, such probes might enable direct measurements of target engagement in live mammalian cells. DNS-pE (and its terminal alkyne-containing version DNSpE2) is the first small molecule that can selectively label endogenous 3-phosphoglycerate dehydrogenase (PHGDH) from various mammalian cells. Endowed with an electrophilic vinyl sulfone moiety that possesses fluorescence-quenching properties, DNS-pE/DNS-pE2 became highly fluorescent only upon irreversible covalent modification of PHGDH. With an inhibitory property (in vitro K-i= 7.4 mm) comparable to that of known PHGDH inhibitors, our probes thus offer a promising approach to simultaneously image endogenous PHGDH activities and study its target engagement in live-cell settings. English John Wiley & Sons Ltd. FISCHER-TROPSCH SYNTHESIS SUPPORTED COBALT CO/SIO2 CATALYSTS CO HYDROGENATION STRUCTURE SENSITIVITY PORE-SIZE NANOPARTICLES HYDROCARBONS METALS SILICA A Vinyl Sulfone-Based Fluorogenic Probe Capable of Selective Labeling of PHGDH in Live Mammalian Cells Article 10.1002/anie.201710856 1 Angewandte Chemie International Edition, v.57, no.2, pp.579 - 583 Angewandte Chemie International Edition 57 2 579 583 scie scopus 000419110500037 2-s2.0-85042070329 Chemistry, Multidisciplinary Chemistry Article FISCHER-TROPSCH SYNTHESIS SUPPORTED COBALT CO/SIO2 CATALYSTS CO HYDROGENATION STRUCTURE SENSITIVITY PORE-SIZE NANOPARTICLES HYDROCARBONS METALS SILICA chemical proteomics fluorescent probes inhibitors live-cell imaging PHGDH