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Pharmacologic inhibition of ketohexokinase prevents fructose-induced metabolic dysfunction.
Gutierrez JA, Liu W, Perez S, Xing G, Sonnenberg G, Kou K, Blatnik M, Allen R, Weng Y, Vera NB, Chidsey K, Bergman A, Somayaji V, Crowley C, Clasquin MF, Nigam A, Fulham MA, Erion DM, Ross TT, Esler WP, Magee TV, Pfefferkorn JA, Bence KK, Birnbaum MJ, Tesz GJ. Gutierrez JA, et al. Among authors: xing g. Mol Metab. 2021 Jun;48:101196. doi: 10.1016/j.molmet.2021.101196. Epub 2021 Mar 3. Mol Metab. 2021. PMID: 33667726 Free PMC article. Clinical Trial.
Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose.
Futatsugi K, Smith AC, Tu M, Raymer B, Ahn K, Coffey SB, Dowling MS, Fernando DP, Gutierrez JA, Huard K, Jasti J, Kalgutkar AS, Knafels JD, Pandit J, Parris KD, Perez S, Pfefferkorn JA, Price DA, Ryder T, Shavnya A, Stock IA, Tsai AS, Tesz GJ, Thuma BA, Weng Y, Wisniewska HM, Xing G, Zhou J, Magee TV. Futatsugi K, et al. Among authors: xing g. J Med Chem. 2020 Nov 25;63(22):13546-13560. doi: 10.1021/acs.jmedchem.0c00944. Epub 2020 Sep 27. J Med Chem. 2020. PMID: 32910646
Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK).
Huard K, Ahn K, Amor P, Beebe DA, Borzilleri KA, Chrunyk BA, Coffey SB, Cong Y, Conn EL, Culp JS, Dowling MS, Gorgoglione MF, Gutierrez JA, Knafels JD, Lachapelle EA, Pandit J, Parris KD, Perez S, Pfefferkorn JA, Price DA, Raymer B, Ross TT, Shavnya A, Smith AC, Subashi TA, Tesz GJ, Thuma BA, Tu M, Weaver JD, Weng Y, Withka JM, Xing G, Magee TV. Huard K, et al. Among authors: xing g. J Med Chem. 2017 Sep 28;60(18):7835-7849. doi: 10.1021/acs.jmedchem.7b00947. Epub 2017 Sep 11. J Med Chem. 2017. PMID: 28853885
Serine catabolism generates liver NADPH and supports hepatic lipogenesis.
Zhang Z, TeSlaa T, Xu X, Zeng X, Yang L, Xing G, Tesz GJ, Clasquin MF, Rabinowitz JD. Zhang Z, et al. Among authors: xing g. Nat Metab. 2021 Dec;3(12):1608-1620. doi: 10.1038/s42255-021-00487-4. Epub 2021 Nov 29. Nat Metab. 2021. PMID: 34845393 Free PMC article.
BDK inhibition acts as a catabolic switch to mimic fasting and improve metabolism in mice.
Bollinger E, Peloquin M, Libera J, Albuquerque B, Pashos E, Shipstone A, Hadjipanayis A, Sun Z, Xing G, Clasquin M, Stansfield JC, Tierney B, Gernhardt S, Siddall CP, Greizer T, Geoly FJ, Vargas SR, Gao LC, Williams G, Marshall M, Rosado A, Steppan C, Filipski KJ, Zhang BB, Miller RA, Roth Flach RJ. Bollinger E, et al. Among authors: xing g. Mol Metab. 2022 Dec;66:101611. doi: 10.1016/j.molmet.2022.101611. Epub 2022 Oct 8. Mol Metab. 2022. PMID: 36220546 Free PMC article.
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS. Ruggeri RB, et al. Among authors: xing g. J Med Chem. 2015 Nov 12;58(21):8513-28. doi: 10.1021/acs.jmedchem.5b00963. Epub 2015 Oct 28. J Med Chem. 2015. PMID: 26509551
1,537 results