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DGKα/ζ inhibitors combine with PD-1 checkpoint therapy to promote T cell-mediated antitumor immunity.
Wichroski M, Benci J, Liu SQ, Chupak L, Fang J, Cao C, Wang C, Onorato J, Qiu H, Shan Y, Banas D, Powles R, Locke G, Witt A, Stromko C, Qi H, Zheng X, Martin S, Ding M, Gentles R, Meanwell N, Velaparthi U, Olson R, Wee S, Tenney D, Parker CG, Cravatt BF, Lawrence M, Borzilleri R, Lees E. Wichroski M, et al. Among authors: locke g. Sci Transl Med. 2023 Oct 25;15(719):eadh1892. doi: 10.1126/scitranslmed.adh1892. Epub 2023 Oct 25. Sci Transl Med. 2023. PMID: 37878674
Enhanced antitumor immunity by a novel small molecule HPK1 inhibitor.
You D, Hillerman S, Locke G, Chaudhry C, Stromko C, Murtaza A, Fan Y, Koenitzer J, Chen Y, Briceno S, Bhadra R, Duperret E, Gullo-Brown J, Gao C, Zhao D, Feder J, Curtin J, Degnan AP, Kumi G, Wittman M, Johnson BM, Parrish KE, Gokulrangan G, Morrison J, Quigley M, Hunt JT, Salter-Cid L, Lees E, Sanjuan MA, Liu J. You D, et al. Among authors: locke g. J Immunother Cancer. 2021 Jan;9(1):e001402. doi: 10.1136/jitc-2020-001402. J Immunother Cancer. 2021. PMID: 33408094 Free PMC article.
Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1.
Degnan AP, Kumi GK, Allard CW, Araujo EV, Johnson WL, Zimmermann K, Pearce BC, Sheriff S, Futran A, Li X, Locke GA, You D, Morrison J, Parrish KE, Stromko C, Murtaza A, Liu J, Johnson BM, Vite GD, Wittman MD. Degnan AP, et al. ACS Med Chem Lett. 2021 Feb 19;12(3):443-450. doi: 10.1021/acsmedchemlett.0c00660. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33732413 Free PMC article.
Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase.
Johnson JA, Tora G, Pi Z, Phillips M, Yin X, Yang R, Zhao L, Chen AY, Taylor DS, Basso M, Rose A, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Galella M, Adam LP, Gordon D, Wexler RR, Finlay HJ. Johnson JA, et al. Among authors: locke g. ACS Med Chem Lett. 2018 Nov 21;9(12):1263-1268. doi: 10.1021/acsmedchemlett.8b00424. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613337 Free PMC article.
Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.
Kim SH, Johnson JA, Jiang J, Parkhurst B, Phillips M, Pi Z, Qiao JX, Tora G, Ye Chen A, Liu E, Yin X, Yang R, Zhao L, Taylor DS, Basso M, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Adam LP, Gordon D, Wexler RR, Finlay HJ. Kim SH, et al. Among authors: locke g. Bioorg Med Chem Lett. 2019 Aug 1;29(15):1918-1921. doi: 10.1016/j.bmcl.2019.05.048. Epub 2019 May 25. Bioorg Med Chem Lett. 2019. PMID: 31176700
Corrigendum to "Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase" [Bioorg. Med. Chem. Lett. 29 (2019) 1918-1921].
Kim SH, Johnson JA, Jiang J, Parkhurst B, Phillips M, Pi Z, Qiao JX, Tora G, Ye Chen A, Liu E, Yin X, Yang R, Zhao L, Taylor DS, Basso M, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Adam LP, Gordon D, Wexler RR, Finlay HJ. Kim SH, et al. Among authors: locke g. Bioorg Med Chem Lett. 2019 Sep 1;29(17):2525. doi: 10.1016/j.bmcl.2019.07.032. Epub 2019 Jul 25. Bioorg Med Chem Lett. 2019. PMID: 31353296 No abstract available.
Discovery and structure activity relationships of 7-benzyl triazolopyridines as stable, selective, and reversible inhibitors of myeloperoxidase.
Shaw SA, Vokits BP, Dilger AK, Viet A, Clark CG, Abell LM, Locke GA, Duke G, Kopcho LM, Dongre A, Gao J, Krishnakumar A, Jusuf S, Khan J, Spronk SA, Basso MD, Zhao L, Cantor GH, Onorato JM, Wexler RR, Duclos F, Kick EK. Shaw SA, et al. Among authors: locke ga. Bioorg Med Chem. 2020 Nov 15;28(22):115723. doi: 10.1016/j.bmc.2020.115723. Epub 2020 Sep 1. Bioorg Med Chem. 2020. PMID: 33007547
Benzothiazole-based compounds as potent endothelial lipase inhibitors.
Meng W, Adam LP, Behnia K, Zhao L, Yang R, Kopcho LM, Locke GA, Taylor DS, Yin X, Wexler RR, Finlay H. Meng W, et al. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126673. doi: 10.1016/j.bmcl.2019.126673. Epub 2019 Sep 6. Bioorg Med Chem Lett. 2019. PMID: 31519373
Discovery of Non-Nucleotide Small-Molecule STING Agonists via Chemotype Hybridization.
Cherney EC, Zhang L, Lo J, Huynh T, Wei D, Ahuja V, Quesnelle C, Schieven GL, Futran A, Locke GA, Lin Z, Monereau L, Chaudhry C, Blum J, Li S, Fereshteh M, Li-Wang B, Gangwar S, Pan C, Chong C, Zhu X, Posy SL, Sack JS, Zhang P, Ruzanov M, Harner M, Akhtar F, Schroeder GM, Vite G, Fink B. Cherney EC, et al. Among authors: locke ga. J Med Chem. 2022 Feb 24;65(4):3518-3538. doi: 10.1021/acs.jmedchem.1c01986. Epub 2022 Feb 2. J Med Chem. 2022. PMID: 35108011
314 results