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In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement.
Wigle TJ, Blackwell DJ, Schenkel LB, Ren Y, Church WD, Desai HJ, Swinger KK, Santospago AG, Majer CR, Lu AZ, Niepel M, Perl NR, Vasbinder MM, Keilhack H, Kuntz KW. Wigle TJ, et al. Among authors: majer cr. Cell Chem Biol. 2020 Jul 16;27(7):877-887.e14. doi: 10.1016/j.chembiol.2020.06.009. Cell Chem Biol. 2020. PMID: 32679093 Free article.
Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes.
Wigle TJ, Church WD, Majer CR, Swinger KK, Aybar D, Schenkel LB, Vasbinder MM, Brendes A, Beck C, Prahm M, Wegener D, Chang P, Kuntz KW. Wigle TJ, et al. Among authors: majer cr. SLAS Discov. 2020 Mar;25(3):241-252. doi: 10.1177/2472555219883623. Epub 2019 Dec 19. SLAS Discov. 2020. PMID: 31855104 Free PMC article.
A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants.
Schenkel LB, Molina JR, Swinger KK, Abo R, Blackwell DJ, Lu AZ, Cheung AE, Church WD, Kunii K, Kuplast-Barr KG, Majer CR, Minissale E, Mo JR, Niepel M, Reik C, Ren Y, Vasbinder MM, Wigle TJ, Richon VM, Keilhack H, Kuntz KW. Schenkel LB, et al. Among authors: majer cr. Cell Chem Biol. 2021 Aug 19;28(8):1158-1168.e13. doi: 10.1016/j.chembiol.2021.02.010. Epub 2021 Mar 10. Cell Chem Biol. 2021. PMID: 33705687 Free article.
Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule.
Wigle TJ, Ren Y, Molina JR, Blackwell DJ, Schenkel LB, Swinger KK, Kuplast-Barr K, Majer CR, Church WD, Lu AZ, Mo J, Abo R, Cheung A, Dorsey BW, Niepel M, Perl NR, Vasbinder MM, Keilhack H, Kuntz KW. Wigle TJ, et al. Among authors: majer cr. Chembiochem. 2021 Jun 15;22(12):2107-2110. doi: 10.1002/cbic.202100047. Epub 2021 May 4. Chembiochem. 2021. PMID: 33838082
PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity.
Gozgit JM, Vasbinder MM, Abo RP, Kunii K, Kuplast-Barr KG, Gui B, Lu AZ, Molina JR, Minissale E, Swinger KK, Wigle TJ, Blackwell DJ, Majer CR, Ren Y, Niepel M, Varsamis ZA, Nayak SP, Bamberg E, Mo JR, Church WD, Mady ASA, Song J, Utley L, Rao PE, Mitchison TJ, Kuntz KW, Richon VM, Keilhack H. Gozgit JM, et al. Among authors: majer cr. Cancer Cell. 2021 Sep 13;39(9):1214-1226.e10. doi: 10.1016/j.ccell.2021.06.018. Epub 2021 Jul 22. Cancer Cell. 2021. PMID: 34375612 Free article.
A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.
Knutson SK, Wigle TJ, Warholic NM, Sneeringer CJ, Allain CJ, Klaus CR, Sacks JD, Raimondi A, Majer CR, Song J, Scott MP, Jin L, Smith JJ, Olhava EJ, Chesworth R, Moyer MP, Richon VM, Copeland RA, Keilhack H, Pollock RM, Kuntz KW. Knutson SK, et al. Among authors: majer cr. Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30. Nat Chem Biol. 2012. PMID: 23023262
A687V EZH2 is a gain-of-function mutation found in lymphoma patients.
Majer CR, Jin L, Scott MP, Knutson SK, Kuntz KW, Keilhack H, Smith JJ, Moyer MP, Richon VM, Copeland RA, Wigle TJ. Majer CR, et al. FEBS Lett. 2012 Sep 21;586(19):3448-51. doi: 10.1016/j.febslet.2012.07.066. Epub 2012 Jul 28. FEBS Lett. 2012. PMID: 22850114 Free article.
A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models.
Chan-Penebre E, Kuplast KG, Majer CR, Boriack-Sjodin PA, Wigle TJ, Johnston LD, Rioux N, Munchhof MJ, Jin L, Jacques SL, West KA, Lingaraj T, Stickland K, Ribich SA, Raimondi A, Scott MP, Waters NJ, Pollock RM, Smith JJ, Barbash O, Pappalardi M, Ho TF, Nurse K, Oza KP, Gallagher KT, Kruger R, Moyer MP, Copeland RA, Chesworth R, Duncan KW. Chan-Penebre E, et al. Among authors: majer cr. Nat Chem Biol. 2015 Jun;11(6):432-7. doi: 10.1038/nchembio.1810. Epub 2015 Apr 27. Nat Chem Biol. 2015. PMID: 25915199
17 results