Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Katy E. Georgiadis"'
Autor:
Shilpi Arora, Anna Kohlmann, Christopher D. Hupp, Julie Liu, Christelle Huguet, Allison Olszewski, Moritz von Rechenberg, John W. Cuozzo, Ying Zhang, Katy E Georgiadis, Matthew A. Clark, Esther C.Y. Lee, Charles J. Eyermann, Andrew J. McRiner, Paolo A. Centrella, Michael I Monteiro, Anthony D. Keefe, Benjamin Levin, Andrew D. Ferguson, Zooey Wang, Yanbin Liu
Publikováno v:
Journal of Medicinal Chemistry. 64:6730-6744
Inhibition of hydroxy acid oxidase 1 (HAO1) is a strategy to mitigate the accumulation of toxic oxalate that results from reduced activity of alanine-glyoxylate aminotransferase (AGXT) in primary hyperoxaluria 1 (PH1) patients. DNA-Encoded Chemical L
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ecd410b881fad4a6d7e1db049c6ba5c
https://doi.org/10.1021/acs.jmedchem.0c02271
https://doi.org/10.1021/acs.jmedchem.0c02271
Autor:
Yonghan Hu, Jennifer R. Thomason, Steve Tam, Priya S. Chockalingam, Erica Reifenberg, Manus Ipek, Jason Shaoyun Xiang, Huan-Qiu Li, Richard Sheldon, Li Xing, Elisabeth A. Morris, Joshua James Sabatini, Katy E. Georgiadis, Satenig Guler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6800-6803
Design, synthesis and structure–activity relationship of a series of biphenylsulfonamido-3-methylbutanoic acid based aggrecanase-1 inhibitors are described. In addition to robust aggrecanase-1 inhibition, these compounds also exhibit potent MMP-13
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f06996759f6d930ba801380ed1352ce5
https://doi.org/10.1016/j.bmcl.2011.09.036
https://doi.org/10.1016/j.bmcl.2011.09.036
Autor:
Darrin William Hopper, Elisabeth A. Morris, David Brian How, Manus Ipek, Erica Reifenberg, Phaik-Eng Sum, Matthew D. Vera, Eric Feyfant, Katy E. Georgiadis, Jerauld S. Skotnicki, Manas K. Majumdar, Jennifer R. Thomason, Qin Wang, Joshua James Sabatini, Cristin C. Keohan, Richard Sheldon, Jason Shaoyun Xiang, Yonghan Hu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2487-2491
The prevention of aggrecan (a key component of cartilage) cleavage via the inhibition of aggrecanase-1 may provide a unique opportunity to stop the progression of cartilage degradation in osteoarthritis. The evaluation of a series of biphenylsulfonam
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bfdd5fb1dbd1d63aa8e94dff08e3143
https://doi.org/10.1016/j.bmcl.2009.03.056
https://doi.org/10.1016/j.bmcl.2009.03.056
Autor:
Thomas McDonagh, Kristine Svenson, Laura Lin, Lidia Mosyak, Tracy Hebert, Stephane Olland, Erica Reifenberg, Christopher John Corcoran, Phaik-Eng Sum, Tania Shane, Mackie Stewart Andrews, Lisa A. Collins-Racie, Katy E. Georgiadis, Matthew Vera, Mark Stahl, Bethany A. Freeman, William S. Somers, Xiaotian Zhong, Tod H. Marvell, Richard Zollner, Ronald W. Kriz, Edward R. Lavallie
Publikováno v:
Protein Science. 17:16-21
Aggrecanases are now believed to be the principal proteinases responsible for aggrecan degradation in osteoarthritis. Given their potential as a drug target, we solved crystal structures of the two most active human aggrecanase isoforms, ADAMTS4 and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab66fe97cf1a8d878682e32ba1090ac3
https://doi.org/10.1110/ps.073287008
https://doi.org/10.1110/ps.073287008
Autor:
Katy E. Georgiadis, Sabrina Lombardi, Adam M. Gilbert, Matthew Gregory Bursavich, Erica Reifenberg, Carl R. Flannery, Elisabeth A. Morris
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5630-5633
5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. Selected compounds 23, 33-35 show sub-micromolar ADAMTS-5 potency and strong SAR trend
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d00a6d663d24e6e58cb6bcd68c992939
https://doi.org/10.1016/j.bmcl.2007.07.048
https://doi.org/10.1016/j.bmcl.2007.07.048
Autor:
Carl R. Flannery, Erica Reifenberg, Adam M. Gilbert, Katy E. Georgiadis, Elisabeth A. Morris, Matthew Gregory Bursavich, Sabrina Lombardi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1185-1188
5-Benzylidene-2-thioxo-thiazolidin-4-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. The identified compounds show micromolar ADAMTS-5 potency and demonstrate SAR trends for both the aryl g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c9e90cce9c8492ac54d5cdbd9169372
https://doi.org/10.1016/j.bmcl.2006.12.027
https://doi.org/10.1016/j.bmcl.2006.12.027
Autor:
Jennifer R. Thomason, Phaik-Eng Sum, Elisabeth A. Morris, Erica Reifenberg, Tam Steve Yik-Kai, Yonghan Hu, Manas K. Majumdar, Thomas S. Rush, Katy E. Georgiadis, Leila Abrous, Jason Shaoyun Xiang, Manus Ipek, Joshua James Sabatini
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:311-316
Aggrecanases are recently discovered enzymes that cleave aggrecan, a key component of cartilage. Aggrecanase inhibitors may provide a unique means to halt the progression of cartilage destruction in osteoarthritis. The synthesis and evaluation of bip
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09e990d97f59210a9bc14ea6a6dd2edb
https://doi.org/10.1016/j.bmcl.2005.10.001
https://doi.org/10.1016/j.bmcl.2005.10.001
Publikováno v:
Biochemistry. 36:554-565
The reaction between bovine heart cytochrome oxidase and dioxygen was investigated at room temperature following photolysis of the fully reduced CO-bound enzyme. Time-resolved optical absorption difference spectra were collected by a gated multichann
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f018c8ab5c16c8a54c00fe44fe252254
https://doi.org/10.1021/bi962422k
https://doi.org/10.1021/bi962422k
Publikováno v:
HSS journal : the musculoskeletal journal of Hospital for Special Surgery. 8(1)
Developing therapies for chondroprotection offers the potential to prevent debilitating osteoarthritis and associated joint replacement following acute joint trauma. Although many significant challenges must be overcome, in comparison to expensive an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::abb4f89744dd9372b21f33b37523dc51
https://pubmed.ncbi.nlm.nih.gov/23372541
https://pubmed.ncbi.nlm.nih.gov/23372541
Autor:
M.A. Rivera-Bermudez, Katy E. Georgiadis, L. Savary, S.S. Glasson, J. Tejada, S. Soucy, T.J. Blanchet, Carl R. Flannery
Publikováno v:
Osteoarthritis and Cartilage. 18
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8f352081418a09a39bce6926b562db6