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Page 1
Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.
Sheppard GS, Wang L, Fidanze SD, Hasvold LA, Liu D, Pratt JK, Park CH, Longenecker K, Qiu W, Torrent M, Kovar PJ, Bui M, Faivre E, Huang X, Lin X, Wilcox D, Zhang L, Shen Y, Albert DH, Magoc TJ, Rajaraman G, Kati WM, McDaniel KF. Sheppard GS, et al. Among authors: qiu w. J Med Chem. 2020 May 28;63(10):5585-5623. doi: 10.1021/acs.jmedchem.0c00628. Epub 2020 May 7. J Med Chem. 2020. PMID: 32324999
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Lasko LM, Jakob CG, Edalji RP, Qiu W, Montgomery D, Digiammarino EL, Hansen TM, Risi RM, Frey R, Manaves V, Shaw B, Algire M, Hessler P, Lam LT, Uziel T, Faivre E, Ferguson D, Buchanan FG, Martin RL, Torrent M, Chiang GG, Karukurichi K, Langston JW, Weinert BT, Choudhary C, de Vries P, Van Drie JH, McElligott D, Kesicki E, Marmorstein R, Sun C, Cole PA, Rosenberg SH, Michaelides MR, Lai A, Bromberg KD. Lasko LM, et al. Among authors: qiu w. Nature. 2017 Oct 5;550(7674):128-132. doi: 10.1038/nature24028. Epub 2017 Sep 27. Nature. 2017. PMID: 28953875 Free PMC article.
Author Correction: Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Lasko LM, Jakob CG, Edalji RP, Qiu W, Montgomery D, Digiammarino EL, Hansen TM, Risi RM, Frey R, Manaves V, Shaw B, Algire M, Hessler P, Lam LT, Uziel T, Faivre E, Ferguson D, Buchanan FG, Martin RL, Torrent M, Chiang GG, Karukurichi K, Langston JW, Weinert BT, Choudhary C, de Vries P, Kluge AF, Patane MA, Van Drie JH, Wang C, McElligott D, Kesicki EA, Marmorstein R, Sun C, Cole PA, Rosenberg SH, Michaelides MR, Lai A, Bromberg KD. Lasko LM, et al. Among authors: qiu w. Nature. 2018 Jun;558(7710):E1. doi: 10.1038/s41586-018-0111-5. Nature. 2018. PMID: 29769713
Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 (IDH1): Direct Covalent Modification of His315.
Jakob CG, Upadhyay AK, Donner PL, Nicholl E, Addo SN, Qiu W, Ling C, Gopalakrishnan SM, Torrent M, Cepa SP, Shanley J, Shoemaker AR, Sun CC, Vasudevan A, Woller KR, Shotwell JB, Shaw B, Bian Z, Hutti JE. Jakob CG, et al. Among authors: qiu w. J Med Chem. 2018 Aug 9;61(15):6647-6657. doi: 10.1021/acs.jmedchem.8b00305. Epub 2018 Jul 30. J Med Chem. 2018. PMID: 30004704
Fragment-Based Discovery of an Apolipoprotein E4 (apoE4) Stabilizer.
Petros AM, Korepanova A, Jakob CG, Qiu W, Panchal SC, Wang J, Dietrich JD, Brewer JT, Pohlki F, Kling A, Wilcox K, Lakics V, Bahnassawy L, Reinhardt P, Partha SK, Bodelle PM, Lake M, Charych EI, Stoll VS, Sun C, Mohler EG. Petros AM, et al. Among authors: qiu w. J Med Chem. 2019 Apr 25;62(8):4120-4130. doi: 10.1021/acs.jmedchem.9b00178. Epub 2019 Apr 12. J Med Chem. 2019. PMID: 30933499
Discovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases.
Ji Z, Clark RF, Bhat V, Matthew Hansen T, Lasko LM, Bromberg KD, Manaves V, Algire M, Martin R, Qiu W, Torrent M, Jakob CG, Liu H, Cole PA, Marmorstein R, Kesicki EA, Lai A, Michaelides MR. Ji Z, et al. Among authors: qiu w. Bioorg Med Chem Lett. 2021 May 1;39:127854. doi: 10.1016/j.bmcl.2021.127854. Epub 2021 Feb 23. Bioorg Med Chem Lett. 2021. PMID: 33631370 Free PMC article.
Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors.
Tong Y, Florjancic AS, Clark RF, Lai C, Mastracchio A, Zhu GD, Smith ML, Kovar PJ, Shaw B, Albert DH, Qiu W, Longenecker KL, Liu X, Olson AM, Osterling DJ, Tahir SK, Phillips DC, Leverson JD, Souers AJ, Penning TD. Tong Y, et al. Among authors: qiu w. ACS Med Chem Lett. 2021 Jun 22;12(7):1108-1115. doi: 10.1021/acsmedchemlett.1c00161. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267880 Free PMC article.
The HPK1 Inhibitor A-745 Verifies the Potential of Modulating T Cell Kinase Signaling for Immunotherapy.
Malchow S, Korepanova A, Panchal SC, McClure RA, Longenecker KL, Qiu W, Zhao H, Cheng M, Guo J, Klinge KL, Trusk P, Pratt SD, Li T, Kurnick MD, Duan L, Shoemaker AR, Gopalakrishnan SM, Warder SE, Shotwell JB, Lai A, Sun C, Osuma AT, Pappano WN. Malchow S, et al. Among authors: qiu w. ACS Chem Biol. 2022 Mar 18;17(3):556-566. doi: 10.1021/acschembio.1c00819. Epub 2022 Feb 21. ACS Chem Biol. 2022. PMID: 35188729
Targeting the Tyrosine Kinase 2 (TYK2) Pseudokinase Domain: Discovery of the Selective TYK2 Inhibitor ABBV-712.
Breinlinger E, Van Epps S, Friedman M, Argiriadi M, Chien E, Chhor G, Cowart M, Dunstan T, Graff C, Hardee D, Herold JM, Little A, McCarthy R, Parmentier J, Perham M, Qiu W, Schrimpf M, Vargo T, Webster MP, Wu F, Bennett D, Edmunds J. Breinlinger E, et al. Among authors: qiu w. J Med Chem. 2023 Oct 26;66(20):14335-14356. doi: 10.1021/acs.jmedchem.3c01373. Epub 2023 Oct 12. J Med Chem. 2023. PMID: 37823891
An anti-TNF-glucocorticoid receptor modulator antibody-drug conjugate is efficacious against immune-mediated inflammatory diseases.
McPherson MJ, Hobson AD, Hernandez A Jr, Marvin CC, Waegell W, Goess C, Oh JZ, Shi D, Hayes ME, Wang L, Wang L, Schmidt D, Wang Z, Pitney V, McCarthy K, Jia Y, Wang C, Kang BN, Bryant S, Mathieu S, Ruzek M, Parmentier J, D'Cunha RR, Pang Y, Phillips L, Brown NJ, Xu J, Graff C, Tian Y, Longenecker KL, Qiu W, Zhu H, Liu W, Zheng P, Bi Y, Stoffel R. McPherson MJ, et al. Among authors: qiu w. Sci Transl Med. 2024 Mar 20;16(739):eadd8936. doi: 10.1126/scitranslmed.add8936. Epub 2024 Mar 20. Sci Transl Med. 2024. PMID: 38507467
4,483 results