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Identification of LY3522348: A Highly Selective and Orally Efficacious Ketohexokinase Inhibitor.
Durham TB, Hao J, Spinazze P, Stack DR, Toth JL, Massey S, Mbofana CT, Johnston RD, Lineswala JP, Wrobleski A, Mínguez JM, Perez C, Smith DL, Lamar J, Leon R, Corkins C, Durbin J, Tung F, Guo S, Linder RJ, Yumibe N, Wang W, MacKrell J, Antonellis M, Mascaro B. Durham TB, et al. Among authors: durbin j. J Med Chem. 2023 Dec 14;66(23):15960-15976. doi: 10.1021/acs.jmedchem.3c01410. Epub 2023 Nov 22. J Med Chem. 2023. PMID: 37992274
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. Among authors: durbin jd. J Med Chem. 2014 Dec 26;57(24):10476-85. doi: 10.1021/jm501522n. Epub 2014 Dec 5. J Med Chem. 2014. PMID: 25415648
Defining Target Engagement Required for Efficacy In Vivo at the Retinoic Acid Receptor-Related Orphan Receptor C2 (RORγt).
Lugar CW, Clarke CA, Morphy R, Rudyk H, Sapmaz S, Stites RE, Vaught GM, Furness K, Broughton HB, Durst GL, Clawson DK, Stout SL, Guo SY, Durbin JD, Stayrook KR, Edmondson DD, Kikly K, New NE, Bina HA, Chambers MG, Shetler P, Chang WY, Chang VC, Barr R, Gough WH, Steele JP, Getman B, Patel N, Mathes BM, Richardson TI. Lugar CW, et al. J Med Chem. 2021 May 13;64(9):5470-5484. doi: 10.1021/acs.jmedchem.0c01918. Epub 2021 Apr 14. J Med Chem. 2021. PMID: 33852312
Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm.
Jadhav PK, Schiffler MA, Gavardinas K, Kim EJ, Matthews DP, Staszak MA, Coffey DS, Shaw BW, Cassidy KC, Brier RA, Zhang Y, Christie RM, Matter WF, Qing K, Durbin JD, Wang Y, Deng GG. Jadhav PK, et al. Among authors: durbin jd. ACS Med Chem Lett. 2014 Aug 27;5(10):1138-42. doi: 10.1021/ml500283g. eCollection 2014 Oct 9. ACS Med Chem Lett. 2014. PMID: 25313327 Free PMC article.
Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design.
Jones SB, Pfeifer LA, Bleisch TJ, Beauchamp TJ, Durbin JD, Klimkowski VJ, Hughes NE, Rito CJ, Dao Y, Gruber JM, Bui H, Chambers MG, Chandrasekhar S, Lin C, McCann DJ, Mudra DR, Oskins JL, Swearingen CA, Thirunavukkarasu K, Norman BH. Jones SB, et al. Among authors: durbin jd. ACS Med Chem Lett. 2016 Aug 2;7(9):857-61. doi: 10.1021/acsmedchemlett.6b00207. eCollection 2016 Sep 8. ACS Med Chem Lett. 2016. PMID: 27660691 Free PMC article.
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