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Ligands to the integrin receptor αvβ3

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Pages 1367-1383 | Published online: 25 Feb 2005

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Janet S Kerr, Andrew M Slee & Shaker A Mousa. (2002) The αv integrin antagonists as novel anticancer agents: an update. Expert Opinion on Investigational Drugs 11:12, pages 1765-1774.
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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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Sumit Goswami. (2013) Importance of integrin receptors in the field of pharmaceutical & medical science. Advances in Biological Chemistry 03:02, pages 224-252.
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Michael D. Wendt. 2012. Protein-Protein Interactions. Protein-Protein Interactions 1 55 .
Vincent Rerat, Georges Dive, Alex A. Cordi, Gordon C. Tucker, Reine Bareille, Joëlle Amédée, Laurence Bordenave & Jacqueline Marchand-Brynaert. (2009) α v β 3 Integrin-Targeting Arg-Gly-Asp (RGD) Peptidomimetics Containing Oligoethylene Glycol (OEG) Spacers . Journal of Medicinal Chemistry 52:22, pages 7029-7043.
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Leonardo Manzoni, Laura Belvisi, Daniela Arosio, Monica Civera, Michael Pilkington-Miksa, Donatella Potenza, Andrea Caprini, Elena M. V. Araldi, Eugenia Monferini, Monica Mancino, Francesca Podestà & Carlo Scolastico. (2009) Cyclic RGD-Containing Functionalized Azabicycloalkane Peptides as Potent Integrin Antagonists for Tumor Targeting. ChemMedChem 4:4, pages 615-632.
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Daniela Arosio, Laura Belvisi, Lino Colombo, Matteo Colombo, Donatella Invernizzi, Leonardo Manzoni, Donatella Potenza, Massimo Serra, Massimo Castorina, Claudio Pisano & Carlo Scolastico. (2008) A Potent Integrin Antagonist from a Small Library of Cyclic RGD Pentapeptide Mimics Including Benzyl-Substituted Azabicycloalkane Amino Acids. ChemMedChem 3:10, pages 1589-1603.
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Werner Seitz, Hervé Geneste, Gisela Backfisch, Jürgen Delzer, Claudia Graef, Wilfried Hornberger, Andreas Kling, Thomas Subkowski & Norbert Zimmermann. (2008) Design and synthesis of novel potent and selective integrin αvβ3 antagonists—Novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates. Bioorganic & Medicinal Chemistry Letters 18:2, pages 527-531.
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Klaus Urbahns, Michael Härter, Markus Albers, Delf Schmidt, Beatrix Stelte-Ludwig, Ulf Brüggemeier, Andrea Vaupel, Jörg Keldenich, Klemens Lustig, Hideki Tsujishita & Christoph Gerdes. (2007) Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides. Bioorganic & Medicinal Chemistry Letters 17:22, pages 6151-6154.
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Min-Su Bae, Kuen Yong Lee, Yoon Jeong Park & David J. Mooney. (2007) RGD Island Spacing Controls Phenotype of Primary Human Fibroblasts Adhered to Ligand-Organized Hydrogels. Macromolecular Research 15:5, pages 469-472.
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Pierre Raboisson, Renee L. DesJarlais, Rolanda Reed, Jennifer Lattanze, Margery Chaikin, Carl L. Manthey, Bruce E. Tomczuk & Juan José Marugán. (2007) Identification of novel short chain 4-substituted indoles as potent αvβ3 antagonist using structure-based drug design. European Journal of Medicinal Chemistry 42:3, pages 334-343.
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Timo Weide, Armin Modlinger & Horst Kessler. 2007. Bioactive Conformation I. Bioactive Conformation I 1 50 .
Pierre Raboisson, Carl L. Manthey, Margery Chaikin, Jennifer Lattanze, Carl Crysler, Kristi Leonard, Wenxi Pan, Bruce E. Tomczuk & Juan José Marugán. (2006) Novel potent and selective αvβ3/αvβ5 integrin dual antagonists with reduced binding affinity for human serum albumin. European Journal of Medicinal Chemistry 41:7, pages 847-861.
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Srinivasan R. Nagarajan, Jane M. Meyer, Julie M. Miyashiro, V. Wayne Engleman, Sandra K. Freeman, David W. Griggs, Jon A. Klover & G. Alan Nickols. (2006) Discovery of Diphenylmethanepropionic and Dihydrostilbeneacetic Acids as Antagonists of the Integrin alphavbeta3. Chemical Biology <html_ent glyph="@amp;" ascii="&"/> Drug Design 67:2, pages 177-181.
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Stéphane Biltresse, Mireille Attolini & Jacqueline Marchand-Brynaert. (2005) Cell adhesive PET membranes by surface grafting of RGD peptidomimetics. Biomaterials 26:22, pages 4576-4587.
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Christopher A. Burnett, Jianwu Xie, Jade Quijano, Zhimin Shen, Finie Hunter, Monica Bur, King C.P. Li & S. Narasimhan Danthi. (2005) Synthesis, in vitro, and in vivo characterization of an integrin αvβ3-targeted molecular probe for optical imaging of tumor. Bioorganic & Medicinal Chemistry 13:11, pages 3763-3771.
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Kristi Leonard, Wenxi Pan, Beth Anaclerio, Joan M. Gushue, Zihong Guo, Renee L. DesJarlais, Marge A. Chaikin, Jennifer Lattanze, Carl Crysler, Carl L. Manthey, Bruce E. Tomczuk & Juan Jose Marugan. (2005) Non-peptidic αvβ3 antagonists containing indol-1-yl propionic acids. Bioorganic & Medicinal Chemistry Letters 15:10, pages 2679-2684.
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Amy E. Zartman, Le T. Duong, Carmen Fernandez-Metzler, George D. Hartman, Chih-Tai Leu, Thomayant Prueksaritanont, Gideon A. Rodan, Sevgi B. Rodan, Mark E. Duggan & Robert S. Meissner. (2005) Nonpeptide αvβ3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics. Bioorganic & Medicinal Chemistry Letters 15:6, pages 1647-1650.
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Shaker A Mousa & Seema Mohamed. (2005) Human αvβ3 Integrin Potency and Specificity of TA138 and Its DOTA Conjugated Form (89)Y-TA138. Journal of Cardiovascular Pharmacology 45:2, pages 109-113.
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Frederick W. Hartner, Yi Hsiao, Kan K. Eng, Nelo R. Rivera, Michael Palucki, Lushi Tan, Nobuyoshi Yasuda, David L. Hughes, Steven Weissman, Daniel Zewge, Tony King, Dave Tschaen & R. P. Volante. (2004) Methods for the Synthesis of 5,6,7,8-Tetrahydro-1,8-naphthyridine Fragments for α V β 3 Integrin Antagonists . The Journal of Organic Chemistry 69:25, pages 8723-8730.
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Bart L. De Corte, William A. Kinney, Li Liu, Shyamali Ghosh, Livia Brunner, William J. Hoekstra, Rosemary J. Santulli, Robert W. Tuman, Judith Baker, Candace Burns, Jef C. Proost, Brett A. Tounge, Bruce P. Damiano, Bruce E. Maryanoff, Dana L. Johnson & Robert A. GalemmoJr.Jr.. (2004) Piperidine-containing β-arylpropionic acids as potent antagonists of αvβ3/αvβ5 integrins. Bioorganic & Medicinal Chemistry Letters 14:20, pages 5227-5232.
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Stephane Biltresse, Mireille Attolini, Georges Dive, Alex Cordi, Gordon C. Tucker & Jacqueline Marchand-Brynaert. (2004) Novel RGD-like molecules based on the tyrosine template: design, synthesis, and biological evaluation on isolated integrins αVβ3/αIIbβ3 and in cellular adhesion tests. Bioorganic & Medicinal Chemistry 12:20, pages 5379-5393.
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David B. Whitman, Ben C. Askew, Le T. Duong, Carmen Fernandez-Metzler, Wasyl Halczenko, George D. Hartman, John H. Hutchinson, Chih-Tai Leu, Thomayant Prueksaritanont, Gideon A. Rodan, Sevgi B. Rodan & Mark E. Duggan. (2004) Nonpeptide αvβ3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone. Bioorganic & Medicinal Chemistry Letters 14:17, pages 4411-4415.
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Michael J Breslin, Mark E Duggan, Wasyl Halczenko, George D Hartman, Le T Duong, Carmen Fernandez-Metzler, Michael A Gentile, Donald B Kimmel, Chih-Tai Leu, Kara Merkle, Thomayant Prueksaritanont, Gideon A Rodan, Sevgi B Rodan & John H Hutchinson. (2004) Nonpeptide αvβ3 antagonists. Part 10: In vitro and in vivo evaluation of a potent 7-methyl substituted tetrahydro-[1,8]naphthyridine derivative. Bioorganic & Medicinal Chemistry Letters 14:17, pages 4515-4518.
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Kuen Yong Lee, Eben Alsberg, Susan Hsiong, Wendy Comisar, Jennifer Linderman, Robert Ziff & David Mooney. (2004) Nanoscale Adhesion Ligand Organization Regulates Osteoblast Proliferation and Differentiation. Nano Letters 4:8, pages 1501-1506.
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Seiji Iwama, Tomoko Kitano, Fumiyo Fukuya, Yayoi Honda, Yuji Sato, Mitsue Notake & Toshiya Morie. (2004) Discovery of a potent and selective αvβ3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model. Bioorganic & Medicinal Chemistry Letters 14:10, pages 2567-2570.
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Jiabing Wang, Michael J. Breslin, Paul J. Coleman, Mark E. Duggan, Cecilia A. Hunt, John H. Hutchinson, Chih-Tai Leu, Sevgi B. Rodan, Gideon A. Rodan, Le T. Duong & George D. Hartman. (2004) Non-peptide α v β 3 antagonists. Part 7: 3-Substituted tetrahydro- [1,8] naphthyridine derivatives. Bioorganic & Medicinal Chemistry Letters 14:4, pages 1049-1052.
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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.
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John H. Hutchinson, Wasyl Halczenko, Karen M. Brashear, Michael J. Breslin, Paul J. Coleman, Le T. Duong, Carmen Fernandez-Metzler, Michael A. Gentile, John E. Fisher, George D. Hartman, Joel R. Huff, Donald B. Kimmel, Chih-Tai Leu, Robert S. Meissner, Kara Merkle, Rose Nagy, Brenda Pennypacker, James J. Perkins, Thomayant Prueksaritanont, Gideon A. Rodan, Sandor L. Varga, Greg A. Wesolowski, Amy E. Zartman, Sevgi B. Rodan & Mark E. Duggan. (2003) Nonpeptide α v β 3 Antagonists. 8. In Vitro and in Vivo Evaluation of a Potent α v β 3 Antagonist for the Prevention and Treatment of Osteoporosis . Journal of Medicinal Chemistry 46:22, pages 4790-4798.
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Thomas D. Harris, Shirley Kalogeropoulos, Tiffany Nguyen, Shuang Liu, Judit Bartis, Charles Ellars, Scott Edwards, David Onthank, Paula Silva, Padmaja Yalamanchili, Simon Robinson, Joel Lazewatsky, John Barrett & Jeffrey Bozarth. (2003) Design, Synthesis, and Evaluation of Radiolabeled Integrin α v β 3 Receptor Antagonists for Tumor Imaging and Radiotherapy . Cancer Biotherapy and Radiopharmaceuticals 18:4, pages 627-641.
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Thomas R Gadek & Robert S McDowell. (2003) Discovery of small molecule leads in a biotechnology datastream. Drug Discovery Today 8:12, pages 545-550.
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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.
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Andreas Kling, Gisela Backfisch, Jürgen Delzer, Hervé Geneste, Claudia Graef, Wilfried Hornberger, Udo E.W Lange, Arnulf Lauterbach, Werner Seitz & Thomas Subkowski. (2003) Design and synthesis of 1,5- and 2,5-substituted tetrahydrobenzazepinones as novel potent and selective integrin α V β 3 antagonists. Bioorganic & Medicinal Chemistry 11:7, pages 1319-1341.
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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.
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Klaus Urbahns, Michael Härter, Andrea Vaupel, Markus Albers, Delf Schmidt, Ulf Brüggemeier, Beatrix Stelte-Ludwig, Christoph Gerdes & Hideki Tsujishita. (2003) Biphenyls as potent vitronectin receptor antagonists. Part 2: biphenylalanine ureas. Bioorganic & Medicinal Chemistry Letters 13:6, pages 1071-1074.
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Shaker A. Mousa. (2002) αv vitronectin receptors in vascular‐mediated disorders. Medicinal Research Reviews 23:2, pages 190-199.
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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.
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Christian Zechel, Gisela Backfisch, Jürgen Delzer, Hervé Geneste, Claudia Graef, Wilfried Hornberger, Andreas Kling, Udo E.W Lange, Arnulf Lauterbach, Werner Seitz & Thomas Subkowski. (2003) Highly potent and selective αVβ3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones. Bioorganic & Medicinal Chemistry Letters 13:2, pages 165-169.
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Audrey Kelleman, Ralph-Heiko Mattern, Michael D. Pierschbacher & Murray Goodman. (2003) Incorporation of thioether building blocks into an αvβ3-specific RGD peptide: Synthesis and biological activity. Biopolymers 71:6, pages 686-695.
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Laura Belvisi, Andrea Caporale, Matteo Colombo, Leonardo Manzoni, Donatella Potenza, Carlo Scolastico, Massimo Castorina, Matilde Cati, Giuseppe Giannini & Claudio Pisano. (2003) Cyclic RGD Peptides Containing Azabicycloalkane Reverse‐Turn Mimics. Helvetica Chimica Acta 85:12, pages 4353-4368.
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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.
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Udo E.W. Lange, Gisela Backfisch, Jürgen Delzer, Hervé Geneste, Claudia Graef, Wilfried Hornberger, Andreas Kling, Arnulf Lauterbach, Thomas Subkowski & Christian Zechel. (2002) Synthesis of highly potent and selective hetaryl ureas as integrin αVβ3-Receptor antagonists. Bioorganic & Medicinal Chemistry Letters 12:10, pages 1379-1382.
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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.
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Klaus Urbahns, Michael Härter, Markus Albers, Delf Schmidt, Beatrix Stelte-Ludwig, Ulf Brüggemeier, Andrea Vaupel & Christoph Gerdes. (2002) Biphenyls as potent vitronectin receptor antagonists. Bioorganic & Medicinal Chemistry Letters 12:2, pages 205-208.
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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.
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Laura Belvisi, Anna Bernardi, Anna Checchia, Leonardo Manzoni, Donatella Potenza, Carlo Scolastico, Massimo Castorina, Amelia Cupelli, Giuseppe Giannini, Paolo Carminati & Claudio Pisano. (2001) Potent Integrin Antagonists from a Small Library of RGD-Including Cyclic Pseudopeptides. Organic Letters 3:7, pages 1001-1004.
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