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Page 1
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: fradera x. 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 and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Zhou H, McGowan MA, Lipford K, Christopher M, Fradera X, Witter D, Lesburg CA, Li C, Methot JL, Lampe J, Achab A, Shaffer L, Goldenblatt P, Shah S, Bass A, Schroeder G, Chen D, Zeng H, Augustin MA, Katz JD. Zhou H, et al. Among authors: fradera x. Bioorg Med Chem Lett. 2020 Jan 1;30(1):126715. doi: 10.1016/j.bmcl.2019.126715. Epub 2019 Oct 18. Bioorg Med Chem Lett. 2020. PMID: 31757666
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.
Pu Q, Zhang H, Guo L, Cheng M, Doty AC, Ferguson H, Fradera X, Lesburg CA, McGowan MA, Miller JR, Geda P, Song X, Otte K, Sciammetta N, Solban N, Yu W, Sloman DL, Zhou H, Lammens A, Neumann L, Bennett DJ, Pasternak A, Han Y. Pu Q, et al. Among authors: fradera x. ACS Med Chem Lett. 2020 Jul 15;11(8):1548-1554. doi: 10.1021/acsmedchemlett.0c00195. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832022 Free PMC article.
Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors.
Methot JL, Achab A, Christopher M, Zhou H, McGowan MA, Trotter BW, Fradera X, Lesburg CA, Goldenblatt P, Hill A, Chen D, Otte KM, Augustin M, Shah S, Katz JD. Methot JL, et al. Among authors: fradera x. ACS Med Chem Lett. 2020 Nov 19;11(12):2461-2469. doi: 10.1021/acsmedchemlett.0c00441. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335668 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: fradera x. 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: fradera x. SLAS Discov. 2021 Jan;26(1):88-99. doi: 10.1177/2472555220952071. Epub 2020 Aug 26. SLAS Discov. 2021. PMID: 32844715 Free article.
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.
Methot JL, Zhou H, McGowan MA, Anthony NJ, Christopher M, Garcia Y, Achab A, Lipford K, Trotter BW, Altman MD, Fradera X, Lesburg CA, Li C, Alves S, Chappell CP, Jain R, Mangado R, Pinheiro E, Williams SMG, Goldenblatt P, Hill A, Shaffer L, Chen D, Tong V, McLeod RL, Lee HH, Yu H, Shah S, Katz JD. Methot JL, et al. Among authors: fradera x. J Med Chem. 2021 Apr 22;64(8):5137-5156. doi: 10.1021/acs.jmedchem.1c00237. Epub 2021 Apr 2. J Med Chem. 2021. PMID: 33797901
Utilization of Metabolite Identification and Structural Data to Guide Design of Low-Dose IDO1 Inhibitors.
Hopkins B, Zhang H, Bharathan I, Li D, Pu Q, Zhou H, Martinot TA, Fradera X, Lammens A, Lesburg CA, Cohen RD, Ballard J, Knemeyer I, Otte K, Vincent S, Miller JR, Solban N, Cheng M, Geda P, Smotrov N, Song X, Bennett DJ, Han Y. Hopkins B, et al. Among authors: fradera x. ACS Med Chem Lett. 2021 Aug 18;12(9):1435-1440. doi: 10.1021/acsmedchemlett.1c00265. eCollection 2021 Sep 9. ACS Med Chem Lett. 2021. PMID: 34531952 Free PMC article.
Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow.
Fradera X, Methot JL, Achab A, Christopher M, Altman MD, Zhou H, McGowan MA, Kattar SD, Wilson K, Garcia Y, Augustin MA, Lesburg CA, Shah S, Goldenblatt P, Katz JD. Fradera X, et al. Bioorg Med Chem Lett. 2019 Sep 15;29(18):2575-2580. doi: 10.1016/j.bmcl.2019.08.004. Epub 2019 Aug 5. Bioorg Med Chem Lett. 2019. PMID: 31416665
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.
Zhang H, Liu K, Pu Q, Achab A, Ardolino MJ, Cheng M, Deng Y, Doty AC, Ferguson H, Fradera X, Knemeyer I, Kurukulasuriya R, Lam YH, Lesburg CA, Martinot TA, McGowan MA, Miller JR, Otte K, Biju PJ, Sciammetta N, Solban N, Yu W, Zhou H, Wang X, Bennett DJ, Han Y. Zhang H, et al. Among authors: fradera x. ACS Med Chem Lett. 2019 Sep 18;10(11):1530-1536. doi: 10.1021/acsmedchemlett.9b00344. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749906 Free PMC article.
48 results