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Page 1
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.
Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez J, Xu C, Rhee K, Chen T, Zhang H, Palakurthi S, Jang J, Lelais G, DiDonato M, Bursulaya B, Michellys PY, Epple R, Marsilje TH, McNeill M, Lu W, Harris J, Bender S, Wong KK, Jänne PA, Eck MJ. Jia Y, et al. Among authors: epple r. Nature. 2016 Jun 2;534(7605):129-32. doi: 10.1038/nature17960. Epub 2016 May 25. Nature. 2016. PMID: 27251290 Free PMC article.
EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.
Jia Y, Juarez J, Li J, Manuia M, Niederst MJ, Tompkins C, Timple N, Vaillancourt MT, Pferdekamper AC, Lockerman EL, Li C, Anderson J, Costa C, Liao D, Murphy E, DiDonato M, Bursulaya B, Lelais G, Barretina J, McNeill M, Epple R, Marsilje TH, Pathan N, Engelman JA, Michellys PY, McNamara P, Harris J, Bender S, Kasibhatla S. Jia Y, et al. Among authors: epple r. Cancer Res. 2016 Mar 15;76(6):1591-602. doi: 10.1158/0008-5472.CAN-15-2581. Epub 2016 Jan 29. Cancer Res. 2016. PMID: 26825170
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY. Lelais G, et al. Among authors: epple r. J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. Epub 2016 Jul 19. J Med Chem. 2016. PMID: 27433829
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
Epple R, Urbina HD, Russo R, Liu H, Mason D, Bursulaya B, Tumanut C, Li J, Harris JL. Epple R, et al. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1254-9. doi: 10.1016/j.bmcl.2006.12.014. Epub 2006 Dec 9. Bioorg Med Chem Lett. 2007. PMID: 17196818
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.
Azimioara M, Alper P, Cow C, Mutnick D, Nikulin V, Lelais G, Mecom J, McNeill M, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessl T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Azimioara M, et al. Among authors: epple r. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5478-83. doi: 10.1016/j.bmcl.2014.10.010. Epub 2014 Oct 13. Bioorg Med Chem Lett. 2014. PMID: 25455488
1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.
Epple R, Azimioara M, Russo R, Bursulaya B, Tian SS, Gerken A, Iskandar M. Epple R, et al. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2969-73. doi: 10.1016/j.bmcl.2006.02.079. Epub 2006 Mar 20. Bioorg Med Chem Lett. 2006. PMID: 16546385
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Velcicky J, Mathison CJN, Nikulin V, Pflieger D, Epple R, Azimioara M, Cow C, Michellys PY, Rigollier P, Beisner DR, Bodendorf U, Guerini D, Liu B, Wen B, Zaharevitz S, Brandl T. Velcicky J, et al. Among authors: epple r. ACS Med Chem Lett. 2019 May 23;10(6):887-892. doi: 10.1021/acsmedchemlett.9b00044. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223443 Free PMC article.
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Alper P, et al. Among authors: epple r. Bioorg Med Chem Lett. 2014 May 15;24(10):2383-7. doi: 10.1016/j.bmcl.2014.03.023. Epub 2014 Mar 27. Bioorg Med Chem Lett. 2014. PMID: 24751443
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.
Tully DC, Liu H, Alper PB, Chatterjee AK, Epple R, Roberts MJ, Williams JA, Nguyen KT, Woodmansee DH, Tumanut C, Li J, Spraggon G, Chang J, Tuntland T, Harris JL, Karanewsky DS. Tully DC, et al. Among authors: epple r. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1975-80. doi: 10.1016/j.bmcl.2005.12.095. Epub 2006 Jan 30. Bioorg Med Chem Lett. 2006. PMID: 16446091
42 results