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Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies.
Lampe JW, Alford JS, Boriak-Sjodin PA, Brach D, Cosmopoulos K, Duncan KW, Eckley ST, Foley MA, Harvey DM, Motwani V, Munchhof MJ, Raimondi A, Riera TV, Tang C, Thomenius MJ, Totman J, Farrow NA. Lampe JW, et al. ACS Med Chem Lett. 2021 Aug 24;12(10):1539-1545. doi: 10.1021/acsmedchemlett.1c00272. eCollection 2021 Oct 14. ACS Med Chem Lett. 2021. PMID: 34671445 Free PMC article.
Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies.
Alford JS, Lampe JW, Brach D, Chesworth R, Cosmopoulos K, Duncan KW, Eckley ST, Kutok JL, Raimondi A, Riera TV, Shook B, Tang C, Totman J, Farrow NA. Alford JS, et al. Among authors: lampe jw. ACS Med Chem Lett. 2022 Jun 7;13(7):1137-1143. doi: 10.1021/acsmedchemlett.2c00167. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859865 Free PMC article.
Identification of a peptide inhibitor for the histone methyltransferase WHSC1.
Morrison MJ, Boriack-Sjodin PA, Swinger KK, Wigle TJ, Sadalge D, Kuntz KW, Scott MP, Janzen WP, Chesworth R, Duncan KW, Harvey DM, Lampe JW, Mitchell LH, Copeland RA. Morrison MJ, et al. Among authors: lampe jw. PLoS One. 2018 May 9;13(5):e0197082. doi: 10.1371/journal.pone.0197082. eCollection 2018. PLoS One. 2018. PMID: 29742153 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. 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
Synthesis and protein kinase inhibitory activity of balanol analogues with modified benzophenone subunits.
Lampe JW, Biggers CK, Defauw JM, Foglesong RJ, Hall SE, Heerding JM, Hollinshead SP, Hu H, Hughes PF, Jagdmann GE Jr, Johnson MG, Lai YS, Lowden CT, Lynch MP, Mendoza JS, Murphy MM, Wilson JW, Ballas LM, Carter K, Darges JW, Davis JE, Hubbard FR, Stamper ML. Lampe JW, et al. J Med Chem. 2002 Jun 6;45(12):2624-43. doi: 10.1021/jm020018f. J Med Chem. 2002. PMID: 12036372
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Sawyer JS, Anderson BD, Beight DW, Campbell RM, Jones ML, Herron DK, Lampe JW, McCowan JR, McMillen WT, Mort N, Parsons S, Smith EC, Vieth M, Weir LC, Yan L, Zhang F, Yingling JM. Sawyer JS, et al. Among authors: lampe jw. J Med Chem. 2003 Sep 11;46(19):3953-6. doi: 10.1021/jm0205705. J Med Chem. 2003. PMID: 12954047
370 results