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Page 1
Crystal structures of the two major aggrecan degrading enzymes, ADAMTS4 and ADAMTS5.
Protein Sci. 2008 Jan;17(1):16-21. doi: 10.1110/ps.073287008. Epub 2007 Nov 27.
Protein Sci. 2008.
PMID: 18042673
Free PMC article.
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.
Xiang JS, Hu Y, Rush TS, Thomason JR, Ipek M, Sum PE, Abrous L, Sabatini JJ, Georgiadis K, Reifenberg E, Majumdar M, Morris EA, Tam S.
Xiang JS, et al.
Bioorg Med Chem Lett. 2006 Jan 15;16(2):311-6. doi: 10.1016/j.bmcl.2005.10.001. Epub 2005 Nov 3.
Bioorg Med Chem Lett. 2006.
PMID: 16275085
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5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5.
Gilbert AM, Bursavich MG, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.
Gilbert AM, et al.
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1189-92. doi: 10.1016/j.bmcl.2006.12.020. Epub 2006 Dec 12.
Bioorg Med Chem Lett. 2007.
PMID: 17210252
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Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors.
Hopper DW, Vera MD, How D, Sabatini J, Xiang JS, Ipek M, Thomason J, Hu Y, Feyfant E, Wang Q, Georgiadis KE, Reifenberg E, Sheldon RT, Keohan CC, Majumdar MK, Morris EA, Skotnicki J, Sum PE.
Hopper DW, et al.
Bioorg Med Chem Lett. 2009 May 1;19(9):2487-91. doi: 10.1016/j.bmcl.2009.03.056. Epub 2009 Mar 18.
Bioorg Med Chem Lett. 2009.
PMID: 19329309
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Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2).
Bursavich MG, Gilbert AM, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.
Bursavich MG, et al.
Bioorg Med Chem Lett. 2007 Mar 1;17(5):1185-8. doi: 10.1016/j.bmcl.2006.12.027. Epub 2006 Dec 12.
Bioorg Med Chem Lett. 2007.
PMID: 17210251
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N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2).
Gilbert AM, Bursavich MG, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.
Gilbert AM, et al.
Bioorg Med Chem Lett. 2008 Dec 15;18(24):6454-7. doi: 10.1016/j.bmcl.2008.10.065. Epub 2008 Oct 18.
Bioorg Med Chem Lett. 2008.
PMID: 18974001
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5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2).
Bursavich MG, Gilbert AM, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.
Bursavich MG, et al.
Bioorg Med Chem Lett. 2007 Oct 15;17(20):5630-3. doi: 10.1016/j.bmcl.2007.07.048. Epub 2007 Aug 19.
Bioorg Med Chem Lett. 2007.
PMID: 17804234
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Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition.
Hu Y, Xing L, Thomason JR, Xiang J, Ipek M, Guler S, Li H, Sabatini J, Chockalingam P, Reifenberg E, Sheldon R, Morris EA, Georgiadis KE, Tam S.
Hu Y, et al.
Bioorg Med Chem Lett. 2011 Nov 15;21(22):6800-3. doi: 10.1016/j.bmcl.2011.09.036. Epub 2011 Sep 18.
Bioorg Med Chem Lett. 2011.
PMID: 21982494
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