Výsledky vyhledávání - "Simon M. Blake"

A highly potent inhibitor of cathepsin K (relacatib) reduces biomarkers of bone resorption both in vitro and in an acute model of elevated bone turnover in vivo in monkeys

Autor: Dennis S. Yamashita, Thaddeus A. Tomaszek, H.-J. Oh, M.W. Lark, S M Hwang, David J. Rickard, Ian E. James, Jae U. Jeong, Robert W. Marquis, George B. Stroup, M. Gowen, Shaji Kumar, Lauren Dare, Simon M. Blake, Daniel F. Veber, Janice A. Vasko-Moser

Publikováno v: Bone. 40:122-131

Cathepsin K is an osteoclast-derived cysteine protease that has been implicated as playing a major role in bone resorption. A substantial body of evidence indicates that cathepsin K is critical in osteoclast-mediated bone resorption and suggests that

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18e6d676f9661e2618786dd5a638714d
https://doi.org/10.1016/j.bone.2006.07.015

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Ultrastructural quantification of cell death after injurious compression of bovine calf articular cartilage

Autor: Ian E. James, Simon M. Blake, E. Berger, M.W. Lark, Alan J. Grodzinsky, Parth Patwari, Véronique Gaschen, Ernst B. Hunziker

Publikováno v: Osteoarthritis and Cartilage. 12:245-252

Objective: It has been suggested that chondrocyte death by apoptosis may play a role in the pathogenesis of cartilage destruction in osteoarthritis, but the results of in-vivo and in-vitro investigations have been conflicting. To investigate further

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5610c20a828af4323c05d44db2efd7b2
https://doi.org/10.1016/j.joca.2003.11.004

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Small-molecule inhibitors of NF-κB for the treatment of inflammatory joint disease

Autor: Simon M. Blake, Amy K. Roshak, James F. Callahan

Publikováno v: Current Opinion in Pharmacology. 2:316-321

Recent advances in our understanding of the role of cytokine networks in inflammatory processes have led to the development of novel biological agents for the treatment of chronic inflammatory diseases. At the present time, significant efforts are fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2139e132f35d1c532890a093f5a3de73
https://doi.org/10.1016/s1471-4892(02)00165-0

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Potent and Selective Inhibition of Human Cathepsin K Leads to Inhibition of Bone Resorption In Vivo in a Nonhuman Primate

Autor: Robert W. Marquis, Karl F. Erhard, Sandra J. Hoffman, Daniel F. Veber, Maxine Gowen, Ru Yu, Lauren Dare, Brian R. Smith, Michael W. Lark, Thadeus Tomaszek, Janice A. Vasko-Moser, Amit Bhattacharyya, Ian E. James, Simon M. Blake, George B. Stroup

Publikováno v: Journal of Bone and Mineral Research. 16:1739-1746

Cathepsin K is a cysteine protease that plays an essential role in osteoclast-mediated degradation of the organic matrix of bone. Knockout of the enzyme in mice, as well as lack of functional enzyme in the human condition pycnodysostosis, results in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1ddae3d2bf5ed626eb85a813a302b4d
https://doi.org/10.1359/jbmr.2001.16.10.1739

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Potent and Selective Cathepsin L Inhibitors Do Not Inhibit Human Osteoclast Resorption in Vitro

Autor: Maxine Gowen, Catherine J. Gress, Shing Mei Hwang, Michael W. Lark, Michael S. McQueney, Ian E. James, Robert W. Marquis, Simon M. Blake, Ru Yu, Daniel F. Veber, Hye-Ja Oh, Denise Zembryki, Thaddeus A. Tomaszek, Dennis S. Yamashita

Publikováno v: Journal of Biological Chemistry. 276:11507-11511

Cathepsins K and L are related cysteine proteases that have been proposed to play important roles in osteoclast-mediated bone resorption. To further examine the putative role of cathepsin L in bone resorption, we have evaluated selective and potent i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::892b89bfe824acabaf8fa273601f5802
https://doi.org/10.1074/jbc.m010684200

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Disease-modifying activity of SB 273005, an orally active, nonpeptide ?v?3 (vitronectin receptor) antagonist, in rat adjuvant-induced arthritis

Autor: Barbara A. Swift, Maxine Gowen, Rasesh Kapadia, Michael W. Lark, George B. Stroup, Alison M. Badger, Joshua M. Levin, Simon M. Blake, William H. Miller, S.J. Hoffman, Susanta K. Sarkar

Publikováno v: Arthritis & Rheumatism. 44:128-137

Objective To evaluate the effects of SB 273005, a potent, orally active nonpeptide antagonist of the integrin αvβ3 vitronectin receptor, on joint integrity in rats with adjuvant-induced arthritis (AIA). Methods Male Lewis rats with AIA were orally

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f0f522d5ccb562d2dc5eb737ed1ef7cc
https://doi.org/10.1002/1529-0131(200101)44:1<128::aid-anr17>3.0.co

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Disease-modifying activity of SB 242235, a selective inhibitor of p38 mitogen-activated protein kinase, in rat adjuvant-induced arthritis

Autor: Edward F. Webb, Alison M. Badger, Simon M. Blake, S.J. Hoffman, Jerry L. Adams, Jeffrey C. Boehm, David J. Rieman, Maxine Gowen, Barbara A. Swift, Don E. Griswold, Rasesh Kapadia, John C. Lee, George B. Stroup

Publikováno v: Arthritis & Rheumatism. 43:175-183

Objective To evaluate the effects of SB 242235, a potent and selective inhibitor of p38 mitogen-activated protein (MAP) kinase, on joint integrity in rats with adjuvant-induced arthritis (AIA). Methods Male Lewis rats with AIA were orally treated eit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::63a7f8607dedfc0c89f09cef22bd1e60
https://doi.org/10.1002/1529-0131(200001)43:1<175::aid-anr22>3.0.co

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Azepanone-based inhibitors of human cathepsin L

Autor: Robert W. Marquis, Dennis S. Yamashita, Thaddeus A. Tomaszek, Simon M. Blake, Priscilla H. Offen, Martha S. Head, Shing-Mei Hwang, Ren Xie, Attiq Rahman, Scott K. Thompson, Ru Yu, Jin Zeng, Ian E. James, Robert E. Lee Trout, Cummings Maxwell D, Michael A. Lark, Daniel F. Veber, Catherine J. Gress

Publikováno v: Journal of medicinal chemistry. 48(22)

The extension of a previously reported cathepsin K azepanone-based inhibitor template to the design and synthesis of potent and selective inhibitors of the homologous cysteine protease cathepsin L is detailed. Structure-activity studies examining the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c55b20e3835b8f957914448867db4290
https://pubmed.ncbi.nlm.nih.gov/16250645

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Increased osteoblastogenesis and decreased bone resorption protect against ovariectomy-induced bone loss in thrombospondin-2-null mice

Autor: Kurt D. Hankenson, Ian E. James, M.W. Lark, Xiaoguang Liang, S. Apone, George B. Stroup, Simon M. Blake, Paul Bornstein

Publikováno v: Matrix biology : journal of the International Society for Matrix Biology. 24(5)

Although bone is composed primarily of extracellular matrix (ECM), the dynamic role that the ECM plays in regulating bone remodeling secondary to estrogen loss is relatively unexplored. Previous studies have shown that mice deficient in the matricell

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da8ff0021638403ef75d03d636d8c58a
https://pubmed.ncbi.nlm.nih.gov/15979292

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