Zobrazeno 1 - 10
of 45
pro vyhledávání: '"Gregg Wesolowski"'
Autor:
Bennett Ma, Gregg Wesolowski, Bin Luo, Traci Lifsted, Keith Wessner, Gary Adamson, Helmut Glantschnig, Laura S Lubbers
Publikováno v:
Journal of Circulating Biomarkers, Vol 8 (2019)
Cathepsin K (CatK) inhibitors exhibited chondroprotective and pain-reducing effects in animal models, however, improvements were relatively modest at dose levels achieving maximal suppression of CatK biomarkers in urine. In this report, a previously
Externí odkaz:
https://doaj.org/article/c88a6d1ab14d4b28be9255d748dd81aa
Autor:
Anthony Ginnetti, Daniel Paone, Kausik Nanda, Jing Li, Marina Busuek, Scott Johnson, Jun Lu, Stephen Soisson, Ronald Robinson, john Fisher, Andrea Webber, Gregg Wesolowski, Bennett Ma, Le Duong, Steven Carroll, Christopher Burgey, Shawn Stachel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 74:128927
Cathepsin K (Cat K) is a cysteine protease involved in bone remodeling. In addition to its role in bone biology, Cat K is upregulated in osteoclasts, chondrocytes and synoviocytes in osteoarthritic (OA) disease states making it a potential therapeuti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::860363fbc57bf2f176c5b861f9f18283
https://doi.org/10.1016/j.bmcl.2022.128927
https://doi.org/10.1016/j.bmcl.2022.128927
Autor:
Le T. Duong, Helmut Glantschnig, Steven S. Carroll, Danielle H. Euler, Yangsi Ou, T. Cusick, Gregg Wesolowski, Laura S. Lubbers, Bin Luo, Bennett Ma
Publikováno v:
Naunyn-Schmiedeberg's Archives of Pharmacology. 390:435-441
The correlation of in vitro inhibition of cathepsin K (CatK) activity and in vivo suppression of collagen I biomarkers was examined with three selective CatK inhibitors to explore the potential translatability from animal species to human. These inhi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a43588a2817694abf32dc4689f4782b6
https://doi.org/10.1007/s00210-017-1356-5
https://doi.org/10.1007/s00210-017-1356-5
Autor:
W. Cameron Black, Jean-François Lévesque, Denis Riendeau, Jean-Pierre Falgueyret, Kevin P. Bateman, M. David Percival, Elise Isabel, Tammy LeRiche, Vouy Linh Truong, Jacques Yves Gauthier, Michel Therien, Robert Zamboni, Sevgi B. Rodan, Sylvie Desmarais, Christophe Mellon, Deborah A. Nicoll-Griffith, Renata Oballa, Gregg Wesolowski, Sonia Lamontagne, Carmai Seto, Nathalie Chauret, Chun Sing Li, Robert N. Young, Frédéric Massé, Wanda Cromlish, Daniel J. McKay, Le T. Duong, Cheuk K. Lau, Serge Leger, Joel Robichaud, Gideon A. Rodan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:887-892
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and exhibits long half-life in pre-clinical species. In vivo st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04ce075aa9949065722c92768a34c9f4
https://doi.org/10.1016/j.bmcl.2009.12.083
https://doi.org/10.1016/j.bmcl.2009.12.083
Autor:
Le T. Duong, Wei Wang, Robert L. Phillips, Maureen Pickarski, Tadashi Hayami, Gregg Wesolowski, John Szumiloski, Chun Cheng, James Watters, Ya Zhuo
Publikováno v:
Arthritis & Rheumatism. 56:2999-3009
Objective The biologic changes associated with osteoarthritis (OA) are incompletely understood. The aim of this study was to elucidate the molecular mechanisms underlying OA progression in an STR/Ort murine model of spontaneous disease. Methods Globa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbe3571fe124f9fae18f2683de2ddf74
https://doi.org/10.1002/art.22836
https://doi.org/10.1002/art.22836
Autor:
Robert L. Vogel, Yangsi Ou, Ming-Tain Lai, Bin Luo, Danielle H. Euler, Keith Wessner, Sharon Adamski, Stephen S. Carroll, Laura S. Lubbers, Gregg Wesolowski, Dennis Murphy, Helmut Glantschnig
Publikováno v:
Journal of the American Chemical Society. 137(35)
During drug discovery, assessment of in vivo target occupancy by therapeutic candidates is often required for predicting clinical efficacy. Current strategies for determining target occupancy include using radiolabeled or irreversible surrogates, whi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e5a051cd78527c1a5a28de8d24c4bc0
https://pubmed.ncbi.nlm.nih.gov/26301491
https://pubmed.ncbi.nlm.nih.gov/26301491
Autor:
Gregg Wesolowski, James T. Palmer, Walter Yu, Eduardo L. Setti, Harry Cheung, Shankar Venkatraman, Joel Robichaud, Xiaoming Xie
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4296-4299
The synthesis and biological profile of a novel series of potent and selective inhibitors of cysteine protease cathepsin K (Cat K) are described. Pharmacokinetic evaluation of 12 indicated that some members of this series could be suitable candidates
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::798725cf77c124f6dd6aa21b59855d38
https://doi.org/10.1016/j.bmcl.2006.05.061
https://doi.org/10.1016/j.bmcl.2006.05.061
Autor:
Serge Leger, Denis Deschenes, Chun Sing Li, Donald B. Kimmel, M. David Percival, Michel Therien, Mary E. McGrath, Robert Zamboni, Daniel J. McKay, Sevgi B. Rodan, Gregg Wesolowski, Denis Riendeau, W. Cameron Black, Jean-Pierre Falgueyret, Sylvie Desmarais, Frédéric Massé, Jacques Yves Gauthier, Vouy-Linh Truong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1985-1989
Based on our previous study with trifluoroethylamine as a P2–P3 amide isostere of cathepsin K inhibitor, further optimization led to identification of compound 22 (L-873724) as a potent and selective non-basic cathepsin K inhibitor. This compound s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2b9a7db3c203cc3793f6b7504ed555a
https://doi.org/10.1016/j.bmcl.2005.12.071
https://doi.org/10.1016/j.bmcl.2005.12.071
Publikováno v:
Bone. 38:234-243
Osteoarthritis (OA) is a chronic joint disease characterized by cartilage destruction, subchondral bone sclerosis, and osteophyte formation. Subchondral bone stiffness has been proposed to initiate and/or contribute to cartilage deterioration in OA.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b8eef6ff0d0eea2a729209024ff232c
https://doi.org/10.1016/j.bone.2005.08.007
https://doi.org/10.1016/j.bone.2005.08.007
Publikováno v:
The International Journal of Biochemistry & Cell Biology. 38:1518-1529
The macrophage colony stimulating factor receptor (cFms) and alpha(V)beta(3) integrin are both abundantly expressed and play critical roles in the differentiation, survival and migration of osteoclasts. We have previously demonstrated that cross-talk
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f98654dde57036fb2a1c896238f2c4f
https://doi.org/10.1016/j.biocel.2006.02.011
https://doi.org/10.1016/j.biocel.2006.02.011