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Page 1
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. Among authors: eckley st. 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: eckley st. 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.
Novel second generation analogs of eribulin. Part III: Blood-brain barrier permeability and in vivo activity in a brain tumor model.
Narayan S, Carlson EM, Cheng H, Condon K, Du H, Eckley S, Hu Y, Jiang Y, Kumar V, Lewis BM, Saxton P, Schuck E, Seletsky BM, Tendyke K, Zhang H, Zheng W, Littlefield BA, Towle MJ, Yu MJ. Narayan S, et al. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1639-43. doi: 10.1016/j.bmcl.2011.01.096. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21324687
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo.
Narayan S, Carlson EM, Cheng H, Condon K, Du H, Eckley S, Hu Y, Jiang Y, Kumar V, Lewis BM, Saxton P, Schuck E, Seletsky BM, Tendyke K, Zhang H, Zheng W, Littlefield BA, Towle MJ, Yu MJ. Narayan S, et al. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1634-8. doi: 10.1016/j.bmcl.2011.01.097. Epub 2011 Jan 25. Bioorg Med Chem Lett. 2011. PMID: 21324692
Peripheral Neuropathy Induced by Microtubule-Targeted Chemotherapies: Insights into Acute Injury and Long-term Recovery.
Wozniak KM, Vornov JJ, Wu Y, Liu Y, Carozzi VA, Rodriguez-Menendez V, Ballarini E, Alberti P, Pozzi E, Semperboni S, Cook BM, Littlefield BA, Nomoto K, Condon K, Eckley S, DesJardins C, Wilson L, Jordan MA, Feinstein SC, Cavaletti G, Polydefkis M, Slusher BS. Wozniak KM, et al. Cancer Res. 2018 Feb 1;78(3):817-829. doi: 10.1158/0008-5472.CAN-17-1467. Epub 2017 Nov 30. Cancer Res. 2018. PMID: 29191802 Free PMC article.
Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer.
Puyang X, Furman C, Zheng GZ, Wu ZJ, Banka D, Aithal K, Agoulnik S, Bolduc DM, Buonamici S, Caleb B, Das S, Eckley S, Fekkes P, Hao MH, Hart A, Houtman R, Irwin S, Joshi JJ, Karr C, Kim A, Kumar N, Kumar P, Kuznetsov G, Lai WG, Larsen N, Mackenzie C, Martin LA, Melchers D, Moriarty A, Nguyen TV, Norris J, O'Shea M, Pancholi S, Prajapati S, Rajagopalan S, Reynolds DJ, Rimkunas V, Rioux N, Ribas R, Siu A, Sivakumar S, Subramanian V, Thomas M, Vaillancourt FH, Wang J, Wardell S, Wick MJ, Yao S, Yu L, Warmuth M, Smith PG, Zhu P, Korpal M. Puyang X, et al. Cancer Discov. 2018 Sep;8(9):1176-1193. doi: 10.1158/2159-8290.CD-17-1229. Epub 2018 Jul 10. Cancer Discov. 2018. PMID: 29991605
Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase.
Vinayak S, Jumani RS, Miller P, Hasan MM, McLeod BI, Tandel J, Stebbins EE, Teixeira JE, Borrel J, Gonse A, Zhang M, Yu X, Wernimont A, Walpole C, Eckley S, Love MS, McNamara CW, Sharma M, Sharma A, Scherer CA, Kato N, Schreiber SL, Melillo B, Striepen B, Huston CD, Comer E. Vinayak S, et al. Sci Transl Med. 2020 Sep 30;12(563):eaba8412. doi: 10.1126/scitranslmed.aba8412. Sci Transl Med. 2020. PMID: 32998973 Free PMC article.
Diversity-oriented synthesis yields novel multistage antimalarial inhibitors.
Kato N, Comer E, Sakata-Kato T, Sharma A, Sharma M, Maetani M, Bastien J, Brancucci NM, Bittker JA, Corey V, Clarke D, Derbyshire ER, Dornan GL, Duffy S, Eckley S, Itoe MA, Koolen KM, Lewis TA, Lui PS, Lukens AK, Lund E, March S, Meibalan E, Meier BC, McPhail JA, Mitasev B, Moss EL, Sayes M, Van Gessel Y, Wawer MJ, Yoshinaga T, Zeeman AM, Avery VM, Bhatia SN, Burke JE, Catteruccia F, Clardy JC, Clemons PA, Dechering KJ, Duvall JR, Foley MA, Gusovsky F, Kocken CH, Marti M, Morningstar ML, Munoz B, Neafsey DE, Sharma A, Winzeler EA, Wirth DF, Scherer CA, Schreiber SL. Kato N, et al. Nature. 2016 Oct 20;538(7625):344-349. doi: 10.1038/nature19804. Epub 2016 Sep 7. Nature. 2016. PMID: 27602946 Free PMC article.
Industry Perspective on Contemporary Protein-Binding Methodologies: Considerations for Regulatory Drug-Drug Interaction and Related Guidelines on Highly Bound Drugs.
Di L, Breen C, Chambers R, Eckley ST, Fricke R, Ghosh A, Harradine P, Kalvass JC, Ho S, Lee CA, Marathe P, Perkins EJ, Qian M, Tse S, Yan Z, Zamek-Gliszczynski MJ. Di L, et al. Among authors: eckley st. J Pharm Sci. 2017 Dec;106(12):3442-3452. doi: 10.1016/j.xphs.2017.09.005. Epub 2017 Sep 18. J Pharm Sci. 2017. PMID: 28927987 Review.