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With subsequent characterization, we successfully identified PHGDH non-NAD+-competing allosteric inhibitors that attenuate its enzyme activity, selectively inhibit de novo serine …
Jan 19, 2017 · Wang et al. identify allosteric sites on PHGDH and discover inhibitors bound to these sites. These allosteric inhibitors are specific, bind to PHGDH in cells, reduce serine …
May 5, 2021 · In 2016, a series of pyrazole-5-carboxamides were reported as PHGDH inhibitors in the patent WO2016/040449A1, with some selected structures and their full-length PHGDH …
Our study not only iden-tifies novel allosteric inhibitors for PHGDH to probe its function and potential as a therapeutic target, but also provides a general strategy for the rational design of …
Jan 19, 2017 · Our study not only identifies novel allosteric inhibitors for PHGDH to probe its function and potential as a therapeutic target, but also provides a general strategy for the …
Jan 18, 2021 · In 2016, Wang and coworkers suggested two other allosteric sites of PHGDH that were confirmed by the use of probes targeting these sites. The first, sharing at least five amino …
Abstract: 3-Phosphoglycerate Dehydrogenase (PHGDH) is primarily known for catalyzing the oxidation of 3-phosphoglycerate (3PG) to 3-phosphohydroxypyvurate (3PHP) by reducing …
±1 μM, Fig. 1c; Table 1) with reasonable in vitro ADME (Supplementary Fig. 1b). Replacing the 2-pyridine-4-trifluoromethyl substituent with a 4-pyridinyl group resulted in a soluble compound …
Apr 25, 2016 · Here we report small-molecule probes of PHGDH and dem-onstrate the utility of these compounds in studying the biological consequences of PHGDH inhibition.
Dec 29, 2016 · Our study not only identifies novel allosteric inhibitors for PHGDH to probe its function and potential as a therapeutic target, but also provides a general strategy for the …
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