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Review

αvβ3 Integrin antagonists as inhibitors of bone resorption

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Pages 1281-1291 | Published online: 24 Feb 2005

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Stephan Huveneers, Hoa Truong & Erik H. J. Danen. (2007) Integrins: Signaling, disease, and therapy. International Journal of Radiation Biology 83:11-12, pages 743-751.
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T. Prueksaritanont, C. Fernandez-Metzler, Y. Meng, A. Barrish, W. Halczenko, S. B. Rodan, J. H. Hutchinson, M. E. Duggan & J. H. Lin. (2004) Disposition of a novel and potent αvβ3 antagonist in animals, and extrapolation to man. Xenobiotica 34:1, pages 103-115.
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T. Prueksaritanont, J. H. Hochman, Y. Meng, N. T. Pudvah, A. Barrish, B. Ma, M. Yamazaki, C. Fernandez-metzler & J. H. Lin. (2004) Renal elimination of a novel and potent αvβ3 integrin antagonist in animals. Xenobiotica 34:11-12, pages 1059-1074.
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T. Prueksaritanont, X. Xu, P. Deluna, M. Yamazaki & J. H. Lin. (2003) Stereoselective hepatic disposition of a diastereomeric pair of αvβ3 antagonists in rat. Xenobiotica 33:11, pages 1125-1137.
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Diane M Biskobing. (2003) Novel therapies for osteoporosis. Expert Opinion on Investigational Drugs 12:4, pages 611-621.
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Larry W Moreland & Richard J Misischia. (2002) Rheumatoid arthritis: developing pharmacological therapies. Expert Opinion on Investigational Drugs 11:7, pages 927-935.
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Thomas R Gadek & Denise A Ockey. (2002) Inhibitors of protein-protein interactions. Expert Opinion on Therapeutic Patents 12:3, pages 393-400.
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T. Prueksaritanont, Y. Meng, B. Ma, P. Leppert, J. Hochman, C. Tang, J. Perkins, M. Zrada, R. Meissner, M.E Duggan & J.H Lin. (2002) Differences in the absorption, metabolism and biliary excretion of a diastereomeric pair of α v β 3 - antagonists in rat: limited role of P-glycoprotein. Xenobiotica 32:3, pages 207-220.
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Mark E Duggan & John H Hutchinson. (2000) Ligands to the integrin receptor αvβ3. Expert Opinion on Therapeutic Patents 10:9, pages 1367-1383.
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Crossref
George D. Hartman & Robert S. Meissner. 2004. 67 78 .
James J Perkins, L.T Duong, Carmen Fernandez-Metzler, George D Hartman, Donald B Kimmel, Chih-Tai Leu, Joseph J Lynch, Thomayant Prueksaritanont, Gideon A Rodan, Sevgi B Rodan, Mark E Duggan & Robert S Meissner. (2003) Non-peptide α v β 3 antagonists: Identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint. Bioorganic & Medicinal Chemistry Letters 13:24, pages 4285-4288.
Crossref
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Crossref
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Crossref
Michael A. Horton, Helen M. Massey, Nurit Rosenberg, Brian Nicholls, Uri Seligsohn & Adrienne M. Flanagan. (2003) Upregulation of osteoclast α2β1 integrin compensates for lack of αvβ3 vitronectin receptor in Iraqi-Jewish-type Glanzmann thrombasthenia. British Journal of Haematology 122:6, pages 950-957.
Crossref
Michael J Breslin, Mark E Duggan, Wasyl Halczenko, Carmen Fernandez-Metzler, Cecilia A Hunt, Chih-Tai Leu, Kara M Merkle, Adel M Naylor-Olsen, Thomayant Prueksaritanont, Gary Stump, Audrey Wallace, Sevgi B Rodan & John H Hutchinson. (2003) Non-Peptide αvβ3 antagonists. Part 6: Design and synthesis of αvβ3 antagonists containing a pyridone or pyrazinone central scaffold. Bioorganic & Medicinal Chemistry Letters 13:10, pages 1809-1812.
Crossref
William H Miller, Peter J Manley, Russell D Cousins, Karl F Erhard, Dirk A Heerding, Chet Kwon, Stephen T Ross, James M Samanen, Dennis T Takata, Irene N Uzinskas, Catherine C.K Yuan, R.Curtis Haltiwanger, Catherine J Gress, Michael W Lark, Shing-Mei Hwang, Ian E James, David J Rieman, Robert N Willette, Tian-Li Yue, Leonard M Azzarano, Kevin L Salyers, Brian R Smith, Keith W Ward, Kyung O Johanson & William F Huffman. (2003) Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin αvβ3) antagonists. Bioorganic & Medicinal Chemistry Letters 13:8, pages 1483-1486.
Crossref
Karen Meerovitch, Fr?d?ric Bergeron, Lorraine Leblond, Brigitte Grouix, Cathy Poirier, Monica Bubenik, Laval Chan, Henriette Gourdeau, Terry Bowlin & Giorgio Attardo. (2003) A novel RGD antagonist that targets both ?v?3 and ?5?1 induces apoptosis of angiogenic endothelial cells on type I collagen. Vascular Pharmacology 40:2, pages 77-89.
Crossref
Monica Bubenik, Karen Meerovitch, Frédéric Bergeron, Giorgio Attardo & Laval Chan. (2003) Thiophene-based vitronectin receptor antagonists. Bioorganic & Medicinal Chemistry Letters 13:3, pages 503-506.
Crossref
Françoise Perron-Sierra, Dominique Saint Dizier, Marc Bertrand, Annie Genton, Gordon C Tucker & Patrick Casara. (2002) Substituted benzocyloheptenes as potent and selective αv integrin antagonists. Bioorganic & Medicinal Chemistry Letters 12:22, pages 3291-3296.
Crossref
Paul J. Coleman, Ben C. Askew, John H. Hutchinson, David B. Whitman, James J. Perkins, George D. Hartman, Gideon A. Rodan, Chih-Tai Leu, Thomayant Prueksaritanont, Carmen Fernandez-Metzler, Kara M. Merkle, Robert Lynch, Joseph J. Lynch, Sevgi B. Rodan & Mark E. Duggan. (2002) Non-Peptide αvβ3 Antagonists. Part 4: Potent and Orally Bioavailable Chain-Shortened RGD Mimetics. Bioorganic & Medicinal Chemistry Letters 12:17, pages 2463-2465.
Crossref
Paul J Hippenmeyer, Peter G Ruminski, Joseph G Rico, H.S.Sharon Lu & David W Griggs. (2002) Adenovirus inhibition by peptidomimetic integrin antagonists. Antiviral Research 55:1, pages 169-178.
Crossref
Andreas Kling, Gisela Backfisch, Jürgen Delzer, Hervé Geneste, Claudia Graef, Uta Holzenkamp, Wilfried Hornberger, Udo E.W Lange, Arnulf Lauterbach, Helmut Mack, Werner Seitz & Thomas Subkowski. (2002) Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective αVβ3 antagonists. Bioorganic & Medicinal Chemistry Letters 12:3, pages 441-446.
Crossref
Michael A. Horton, Stephen A. Nesbitt, Jon H. Bennett & Gudrun Stenbeck. 2002. Principles of Bone Biology. Principles of Bone Biology 265 XX .
Le T. Duong, Archana Sanjay, William Horne, Roland Baron & Gideon A. Rodan. 2002. Principles of Bone Biology. Principles of Bone Biology 141 VII .
Anusch Peyman, Karl-Heinz Scheunemann, David W. Will, Jochen Knolle, Volkmar Wehner, Gerhard Breipohl, Hans Ulrich Stilz, Denis Carniato, Jean-Marie Ruxer, Jean-Francois Gourvest, Marielle Auberval, Bernard Doucet, Roland Baron, Martine Gaillard, Thomas R. Gadek & Sarah Bodary. (2001) αvβ3 Antagonists Based on a Central Thiophene Scaffold. Bioorganic & Medicinal Chemistry Letters 11:15, pages 2011-2015.
Crossref

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