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Page 1
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.
Durham TB, Klimkowski VJ, Rito CJ, Marimuthu J, Toth JL, Liu C, Durbin JD, Stout SL, Adams L, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR. Durham TB, et al. J Med Chem. 2014 Dec 26;57(24):10476-85. doi: 10.1021/jm501522n. Epub 2014 Dec 5. J Med Chem. 2014. PMID: 25415648
A short-term pharmacodynamic model for monitoring aggrecanase activity: injection of monosodium iodoacetate (MIA) in rats and assessment of aggrecan neoepitope release in synovial fluid using novel ELISAs.
Swearingen CA, Chambers MG, Lin C, Marimuthu J, Rito CJ, Carter QL, Dotzlaf J, Liu C, Chandrasekhar S, Duffin KL, Mitchell PG, Durham TB, Wiley MR, Thirunavukkarasu K. Swearingen CA, et al. Among authors: durham tb. Osteoarthritis Cartilage. 2010 Sep;18(9):1159-66. doi: 10.1016/j.joca.2010.02.019. Epub 2010 Jul 13. Osteoarthritis Cartilage. 2010. PMID: 20633676 Free article.
Development of a novel clinical biomarker assay to detect and quantify aggrecanase-generated aggrecan fragments in human synovial fluid, serum and urine.
Swearingen CA, Carpenter JW, Siegel R, Brittain IJ, Dotzlaf J, Durham TB, Toth JL, Laska DA, Marimuthu J, Liu C, Brown DP, Carter QL, Wiley MR, Duffin KL, Mitchell PG, Thirunavukkarasu K. Swearingen CA, et al. Among authors: durham tb. Osteoarthritis Cartilage. 2010 Sep;18(9):1150-8. doi: 10.1016/j.joca.2010.06.011. Epub 2010 Jul 13. Osteoarthritis Cartilage. 2010. PMID: 20633682 Free article.
Dual Exosite-binding Inhibitors of Insulin-degrading Enzyme Challenge Its Role as the Primary Mediator of Insulin Clearance in Vivo.
Durham TB, Toth JL, Klimkowski VJ, Cao JX, Siesky AM, Alexander-Chacko J, Wu GY, Dixon JT, McGee JE, Wang Y, Guo SY, Cavitt RN, Schindler J, Thibodeaux SJ, Calvert NA, Coghlan MJ, Sindelar DK, Christe M, Kiselyov VV, Michael MD, Sloop KW. Durham TB, et al. J Biol Chem. 2015 Aug 14;290(33):20044-59. doi: 10.1074/jbc.M115.638205. Epub 2015 Jun 17. J Biol Chem. 2015. PMID: 26085101 Free PMC article.
Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors.
Wiley MR, Durham TB, Adams LA, Chambers MG, Lin C, Liu C, Marimuthu J, Mitchell PG, Mudra DR, Swearingen CA, Toth JL, Weller JM, Thirunavukkarasu K. Wiley MR, et al. Among authors: durham tb. J Med Chem. 2016 Jun 23;59(12):5810-22. doi: 10.1021/acs.jmedchem.6b00398. Epub 2016 Jun 9. J Med Chem. 2016. PMID: 27194201
Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model.
Fales KR, Njoroge FG, Brooks HB, Thibodeaux S, Torrado A, Si C, Toth JL, Mc Cowan JR, Roth KD, Thrasher KJ, Frimpong K, Lee MR, Dally RD, Shepherd TA, Durham TB, Margolis BJ, Wu Z, Wang Y, Atwell S, Wang J, Hui YH, Meier TI, Konicek SA, Geeganage S. Fales KR, et al. Among authors: durham tb. J Med Chem. 2017 Dec 14;60(23):9599-9616. doi: 10.1021/acs.jmedchem.7b01046. Epub 2017 Nov 9. J Med Chem. 2017. PMID: 29072452
Optimization of Hydroxyethylamine Transition State Isosteres as Aspartic Protease Inhibitors by Exploiting Conformational Preferences.
Bueno AB, Agejas J, Broughton H, Dally R, Durham TB, Espinosa JF, González R, Hahn PJ, Marcos A, Rodríguez R, Sanz G, Soriano JF, Timm D, Vidal P, Yang HC, McCarthy JR. Bueno AB, et al. Among authors: durham tb. J Med Chem. 2017 Dec 14;60(23):9807-9820. doi: 10.1021/acs.jmedchem.7b01304. Epub 2017 Nov 28. J Med Chem. 2017. PMID: 29088532
Characterization of a novel AICARFT inhibitor which potently elevates ZMP and has anti-tumor activity in murine models.
Brooks HB, Meier TI, Geeganage S, Fales KR, Thrasher KJ, Konicek SA, Spencer CD, Thibodeaux S, Foreman RT, Hui YH, Roth KD, Qian YW, Wang T, Luo S, Torrado A, Si C, Toth JL, Mc Cowan JR, Frimpong K, Lee MR, Dally RD, Shepherd TA, Durham TB, Wang Y, Wu Z, Iversen PW, Njoroge FG. Brooks HB, et al. Among authors: durham tb. Sci Rep. 2018 Oct 18;8(1):15458. doi: 10.1038/s41598-018-33453-4. Sci Rep. 2018. PMID: 30337562 Free PMC article.
23 results