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Page 1
Discovery and SAR Study of Boronic Acid-Based Selective PDE3B Inhibitors from a Novel DNA-Encoded Library.
Rowley AM, Yao G, Andrews L, Bedermann A, Biddulph R, Bingham R, Brady JJ, Buxton R, Cecconie T, Cooper R, Csakai A, Gao EN, Grenier-Davies MC, Lawler M, Lian Y, Macina J, Macphee C, Marcaurelle L, Martin J, McCormick P, Pindoria R, Rauch M, Rocque W, Shen Y, Shewchuk LM, Squire M, Stebbeds W, Tear W, Wang X, Ward P, Xiao S. Rowley AM, et al. Among authors: gao en. J Med Chem. 2024 Feb 8;67(3):2049-2065. doi: 10.1021/acs.jmedchem.3c01562. Epub 2024 Jan 29. J Med Chem. 2024. PMID: 38284310
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Tian X, Suarez D, Thomson D, Li W, King EA, LaFrance L, Boehm J, Barton L, Di Marco C, Martyr C, Thalji R, Medina J, Knight S, Heerding D, Gao E, Nartey E, Cecconie T, Nixon C, Zhang G, Berrodin TJ, Phelps C, Patel A, Bai X, Lind K, Prabhu N, Messer J, Zhu Z, Shewchuk L, Reid R, Graves AP, McHugh C, Mangatt B. Tian X, et al. J Med Chem. 2022 Nov 10;65(21):14391-14408. doi: 10.1021/acs.jmedchem.2c00670. Epub 2022 Oct 27. J Med Chem. 2022. PMID: 36302181
Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening.
Machutta CA, Kollmann CS, Lind KE, Bai X, Chan PF, Huang J, Ballell L, Belyanskaya S, Besra GS, Barros-Aguirre D, Bates RH, Centrella PA, Chang SS, Chai J, Choudhry AE, Coffin A, Davie CP, Deng H, Deng J, Ding Y, Dodson JW, Fosbenner DT, Gao EN, Graham TL, Graybill TL, Ingraham K, Johnson WP, King BW, Kwiatkowski CR, Lelièvre J, Li Y, Liu X, Lu Q, Lehr R, Mendoza-Losana A, Martin J, McCloskey L, McCormick P, O'Keefe HP, O'Keeffe T, Pao C, Phelps CB, Qi H, Rafferty K, Scavello GS, Steiginga MS, Sundersingh FS, Sweitzer SM, Szewczuk LM, Taylor A, Toh MF, Wang J, Wang M, Wilkins DJ, Xia B, Yao G, Zhang J, Zhou J, Donahue CP, Messer JA, Holmes D, Arico-Muendel CC, Pope AJ, Gross JW, Evindar G. Machutta CA, et al. Among authors: gao en. Nat Commun. 2017 Jul 17;8:16081. doi: 10.1038/ncomms16081. Nat Commun. 2017. PMID: 28714473 Free PMC article.
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU, Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA, Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T, McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF. Yamashita DS, et al. J Med Chem. 2006 Mar 9;49(5):1597-612. doi: 10.1021/jm050915u. J Med Chem. 2006. PMID: 16509577
Author Correction: Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening.
Machutta CA, Kollmann CS, Lind KE, Bai X, Chan PF, Huang J, Ballell L, Belyanskaya S, Besra GS, Barros-Aguirre D, Bates RH, Centrella PA, Chang SS, Chai J, Choudhry AE, Coffin A, Davie CP, Deng H, Deng J, Ding Y, Dodson JW, Fosbenner DT, Gao EN, Graham TL, Graybill TL, Ingraham K, Johnson WP, King BW, Kwiatkowski CR, Lelièvre J, Li Y, Liu X, Lu Q, Lehr R, Mendoza-Losana A, Martin J, McCloskey L, McCormick P, O'Keefe HP, O'Keeffe T, Pao C, Phelps CB, Qi H, Rafferty K, Scavello GS, Steiginga MS, Sundersingh FS, Sweitzer SM, Szewczuk LM, Taylor A, Fern Toh M, Wang J, Wang M, Wilkins DJ, Xia B, Yao G, Zhang J, Zhou J, Donahue CP, Messer JA, Holmes D, Arico-Muendel CC, Pope AJ, Gross JW, Evindar G. Machutta CA, et al. Among authors: gao en. Nat Commun. 2018 Jul 13;9:16227. doi: 10.1038/ncomms16227. Nat Commun. 2018. PMID: 30004092 Free PMC article.
New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.
Okoye-Okafor UC, Bartholdy B, Cartier J, Gao EN, Pietrak B, Rendina AR, Rominger C, Quinn C, Smallwood A, Wiggall KJ, Reif AJ, Schmidt SJ, Qi H, Zhao H, Joberty G, Faelth-Savitski M, Bantscheff M, Drewes G, Duraiswami C, Brady P, Groy A, Narayanagari SR, Antony-Debre I, Mitchell K, Wang HR, Kao YR, Christopeit M, Carvajal L, Barreyro L, Paietta E, Makishima H, Will B, Concha N, Adams ND, Schwartz B, McCabe MT, Maciejewski J, Verma A, Steidl U. Okoye-Okafor UC, et al. Among authors: gao en. Nat Chem Biol. 2015 Nov;11(11):878-86. doi: 10.1038/nchembio.1930. Epub 2015 Oct 5. Nat Chem Biol. 2015. PMID: 26436839 Free PMC article.
27 results