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ASK1 contributes to fibrosis and dysfunction in models of kidney disease.
Liles JT, Corkey BK, Notte GT, Budas GR, Lansdon EB, Hinojosa-Kirschenbaum F, Badal SS, Lee M, Schultz BE, Wise S, Pendem S, Graupe M, Castonguay L, Koch KA, Wong MH, Papalia GA, French DM, Sullivan T, Huntzicker EG, Ma FY, Nikolic-Paterson DJ, Altuhaifi T, Yang H, Fogo AB, Breckenridge DG. Liles JT, et al. Among authors: lansdon eb. J Clin Invest. 2018 Oct 1;128(10):4485-4500. doi: 10.1172/JCI99768. Epub 2018 Jul 19. J Clin Invest. 2018. PMID: 30024858 Free PMC article.
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Sperandio D, Aktoudianakis V, Babaoglu K, Chen X, Elbel K, Chin G, Corkey B, Du J, Jiang B, Kobayashi T, Mackman R, Martinez R, Yang H, Zablocki J, Kusam S, Jordan K, Webb H, Bates JG, Lad L, Mish M, Niedziela-Majka A, Metobo S, Sapre A, Hung M, Jin D, Fung W, Kan E, Eisenberg G, Larson N, Newby ZER, Lansdon E, Tay C, Neve RM, Shevick SL, Breckenridge DG. Sperandio D, et al. Bioorg Med Chem. 2019 Feb 1;27(3):457-469. doi: 10.1016/j.bmc.2018.11.020. Epub 2018 Nov 15. Bioorg Med Chem. 2019. PMID: 30606676
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.
Farand J, Kropf JE, Blomgren P, Xu J, Schmitt AC, Newby ZE, Wang T, Murakami E, Barauskas O, Sudhamsu J, Feng JY, Niedziela-Majka A, Schultz BE, Schwartz K, Viatchenko-Karpinski S, Kornyeyev D, Kashishian A, Fan P, Chen X, Lansdon EB, Ports MO, Currie KS, Watkins WJ, Notte GT. Farand J, et al. Among authors: lansdon eb. ACS Med Chem Lett. 2019 Nov 19;11(3):358-364. doi: 10.1021/acsmedchemlett.9b00420. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184970 Free PMC article.
Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability.
Mulato A, Lansdon E, Aoyama R, Voigt J, Lee M, Liclican A, Lee G, Singer E, Stafford B, Gong R, Murray B, Chan J, Lee J, Xu Y, Ahmadyar S, Gonzalez A, Cho A, Stepan GJ, Schmitz U, Schultz B, Marchand B, Brumshtein B, Wang R, Yu H, Cihlar T, Xu L, Yant SR. Mulato A, et al. Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0137323. doi: 10.1128/aac.01373-23. Epub 2024 Feb 21. Antimicrob Agents Chemother. 2024. PMID: 38380945 Free PMC article.
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.
Blomgren P, Chandrasekhar J, Di Paolo JA, Fung W, Geng G, Ip C, Jones R, Kropf JE, Lansdon EB, Lee S, Lo JR, Mitchell SA, Murray B, Pohlmeyer C, Schmitt A, Suekawa-Pirrone K, Wise S, Xiong JM, Xu J, Yu H, Zhao Z, Currie KS. Blomgren P, et al. Among authors: lansdon eb. ACS Med Chem Lett. 2020 Feb 12;11(4):506-513. doi: 10.1021/acsmedchemlett.9b00621. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292557 Free PMC article.
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Currie KS, Kropf JE, Lee T, Blomgren P, Xu J, Zhao Z, Gallion S, Whitney JA, Maclin D, Lansdon EB, Maciejewski P, Rossi AM, Rong H, Macaluso J, Barbosa J, Di Paolo JA, Mitchell SA. Currie KS, et al. Among authors: lansdon eb. J Med Chem. 2014 May 8;57(9):3856-73. doi: 10.1021/jm500228a. Epub 2014 Apr 29. J Med Chem. 2014. PMID: 24779514
RNase H active site inhibitors of human immunodeficiency virus type 1 reverse transcriptase: design, biochemical activity, and structural information.
Kirschberg TA, Balakrishnan M, Squires NH, Barnes T, Brendza KM, Chen X, Eisenberg EJ, Jin W, Kutty N, Leavitt S, Liclican A, Liu Q, Liu X, Mak J, Perry JK, Wang M, Watkins WJ, Lansdon EB. Kirschberg TA, et al. Among authors: lansdon eb. J Med Chem. 2009 Oct 8;52(19):5781-4. doi: 10.1021/jm900597q. J Med Chem. 2009. PMID: 19791799
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