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Page 1
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Boga SB, Alhassan AB, Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Zhu H, Desai J, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Cooper A, Kim RM, Kozlowski JA. Boga SB, et al. Among authors: xu z. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3939-3943. doi: 10.1016/j.bmcl.2017.03.040. Epub 2017 Mar 18. Bioorg Med Chem Lett. 2017. PMID: 28720503
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: xu z. ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985298 Free PMC article.
Discovery of novel BTK inhibitors with carboxylic acids.
Gao X, Wang J, Liu J, Guiadeen D, Krikorian A, Boga SB, Alhassan AB, Selyutin O, Yu W, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Cooper A, Zhu H, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Gao X, et al. Among authors: xu z. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1471-1477. doi: 10.1016/j.bmcl.2016.11.079. Epub 2016 Nov 25. Bioorg Med Chem Lett. 2017. PMID: 28254166
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, Alhassan AB, Yu W, Selyutin O, Yu Y, Anand R, Xu J, Kelly J, Duffy JL, Liu S, Yang C, Wu H, Cai J, Bennett C, Maloney KM, Tyagarajan S, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: xu j, xu z. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127390. doi: 10.1016/j.bmcl.2020.127390. Epub 2020 Jul 11. Bioorg Med Chem Lett. 2020. PMID: 32738973
Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5).
Palte RL, Schneider SE, Altman MD, Hayes RP, Kawamura S, Lacey BM, Mansueto MS, Reutershan M, Siliphaivanh P, Sondey C, Xu H, Xu Z, Ye Y, Machacek MR. Palte RL, et al. Among authors: xu h, xu z. ACS Med Chem Lett. 2020 Aug 7;11(9):1688-1693. doi: 10.1021/acsmedchemlett.9b00525. eCollection 2020 Sep 10. ACS Med Chem Lett. 2020. PMID: 32944135 Free PMC article.
Identification of Potent Reverse Indazole Inhibitors for HPK1.
Yu EC, Methot JL, Fradera X, Lesburg CA, Lacey BM, Siliphaivanh P, Liu P, Smith DM, Xu Z, Piesvaux JA, Kawamura S, Xu H, Miller JR, Bittinger M, Pasternak A. Yu EC, et al. Among authors: xu h, xu z. ACS Med Chem Lett. 2021 Mar 1;12(3):459-466. doi: 10.1021/acsmedchemlett.0c00672. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738073 Free PMC article.
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.
Vara BA, Levi SM, Achab A, Candito DA, Fradera X, Lesburg CA, Kawamura S, Lacey BM, Lim J, Methot JL, Xu Z, Xu H, Smith DM, Piesvaux JA, Miller JR, Bittinger M, Ranganath SH, Bennett DJ, DiMauro EF, Pasternak A. Vara BA, et al. Among authors: xu h, xu z. ACS Med Chem Lett. 2021 Mar 19;12(4):653-661. doi: 10.1021/acsmedchemlett.1c00096. eCollection 2021 Apr 8. ACS Med Chem Lett. 2021. PMID: 33859804 Free PMC article.
Development of High-Throughput Assays for Evaluation of Hematopoietic Progenitor Kinase 1 Inhibitors.
Lacey BM, Xu Z, Chai X, Laskey J, Fradera X, Mittal P, Mishra S, Piesvaux J, Saradjian P, Shaffer L, Vassileva G, Gerdt C, Wang Y, Ferguson H, Smith DM, Ballard J, Wells S, Jain R, Mueller U, Addona G, Kariv I, Methot JL, Bittinger M, Ranganath S, Mcleod R, Pasternak A, Miller JR, Xu H. Lacey BM, et al. Among authors: xu h, xu z. SLAS Discov. 2021 Jan;26(1):88-99. doi: 10.1177/2472555220952071. Epub 2020 Aug 26. SLAS Discov. 2021. PMID: 32844715 Free article.
Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor.
Ma X, Sloman DL, Duggal R, Anderson KD, Ballard JE, Bharathan I, Brynczka C, Gathiaka S, Henderson TJ, Lyons TW, Miller R, Munsell EV, Orth P, Otte RD, Palani A, Rankic DA, Robinson MR, Sather AC, Solban N, Song XS, Wen X, Xu Z, Yang Y, Yang R, Day PJ, Stoeck A, Bennett DJ, Han Y. Ma X, et al. Among authors: xu z. J Med Chem. 2024 Jul 11;67(13):11024-11052. doi: 10.1021/acs.jmedchem.4c00572. Epub 2024 Jun 26. J Med Chem. 2024. PMID: 38924388 Clinical Trial.
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