Exploiting Subsite S1 of Trypsin-Like Serine Proteases for Selectivity:  Potent and Selective Inhibitors of Urokinase-Type Plasminogen Activator von Mackman, Richard L, Katz, Bradley A, Breitenbucher, J. Guy, Hui, Hon C, Verner, Erik, Luong, Christine, Liu, Liang, Sprengeler, Paul A

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Modulation of Receptor and Receptor Subtype Affinities Using Diastereomeric and Enantiomeric Monosaccharide Scaffolds as a Means to Structural and Biological Diversity. A New Route... von Hirschmann, Ralph, Hynes, John, Cichy-Knight, Maria A, van Rijn, Rachel D, Sprengeler, Paul A, Spoors, P. Grant, Shakespeare, William C, Pietranico-Cole, Sherrie, Barbosa, Joseph, Liu, Josephine, Yao, Wenqing, Rohrer, Susan, Smith, Amos B

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An Orally Bioavailable Pyrrolinone Inhibitor of HIV-1 Protease:  Computational Analysis and X-ray Crystal Structure of the Enzyme Complex von Smith, Amos B, Hirschmann, Ralph, Pasternak, Alexander, Yao, Wenquing, Sprengeler, Paul A, Holloway, M. Katharine, Kuo, Lawrence C, Chen, Zhongguo, Darke, Paul L, Schleif, William A

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Development of Serine Protease Inhibitors Displaying a Multicentered Short (<2.3 Å) Hydrogen Bond Binding Mode:  Inhibitors of Urokinase-Type Plasminogen Activator and Factor Xa von Verner, Erik, Katz, Bradley A, Spencer, Jeffrey R, Allen, Darin, Hataye, Jason, Hruzewicz, Witold, Hui, Hon C, Kolesnikov, Aleksandr, Li, Yong, Luong, Christine, Martelli, Arnold, Radika, Kesavan, Rai, Roopa, She, Miles, Shrader, William, Sprengeler, Paul A, Trapp, Sean, Wang, Jing, Young, Wendy B, Mackman, Richard L

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Synthesis of Potent Cyclic Hexapeptide NK-1 Antagonists. Use of a Minilibrary in Transforming a Peptidal Somatostatin Receptor Ligand into an NK-1 Receptor Ligand via a Polyvalent... von Hirschmann, Ralph, Yao, Wenqing, Cascieri, Margaret A, Strader, Catherine D, Maechler, Laurie, Cichy-Knight, Maria A, Hynes, John, van Rijn, Rachel D, Sprengeler, Paul A, Smith, Amos B

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Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport von Smith, Amos B, Hirschmann, Ralph, Pasternak, Alexander, Akaishi, Ryouichi, Guzman, Mark C, Jones, David R, Keenan, Terence P, Sprengeler, Paul A, Darke, Paul L

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Peptide Synthesis Catalyzed by an Antibody Containing a Binding Site for Variable Amino Acids von Hirschmann, Ralph, Smith, Amos B., Taylor, Carol M., Benkovic, Patricia A., Taylor, Scott D., Yager, Kraig M., Sprengeler, Paul A., Benkovic, Stephen J.

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Design, Synthesis, and Biological Evaluation of Monopyrrolinone-Based HIV-1 Protease Inhibitors von Smith, Amos B, Cantin, Louis-David, Pasternak, Alexander, Guise-Zawacki, Lisa, Yao, Wenquin, Charnley, Adam K, Barbosa, Joseph, Sprengeler, Paul A, Hirschmann, Ralph, Munshi, Sanjeev, Olsen, David B, Schleif, William A, Kuo, Lawrence C

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A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site von Katz, Bradley A, Elrod, Kyle, Luong, Christine, Rice, Mark J, Mackman, Richard L, Sprengeler, Paul A, Spencer, Jeffrey, Hataye, Jason, Janc, James, Link, John, Litvak, Joane, Rai, Roopa, Rice, Ken, Sideris, Steve, Verner, Erik, Young, Wendy

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Structure-Guided Design of Peptide-Based Tryptase Inhibitors von McGrath, Mary E, Sprengeler, Paul A, Hirschbein, Bernard, Somoza, John R, Lehoux, Isabelle, Janc, James W, Gjerstad, Erik, Graupe, Michael, Estiarte, Angeles, Venkataramani, Chandru, Liu, Yang, Yee, Robb, Ho, Joseph D, Green, Michael J, Lee, Chang-Sun, Liu, Liang, Tai, Vincent, Spencer, Jeffrey, Sperandio, David, Katz, Bradley A

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Dissecting and Designing Inhibitor Selectivity Determinants at the S1 Site Using an Artificial Ala190 Protease (Ala190 uPA) von Katz, Bradley A., Luong, Christine, Ho, Joseph D., Somoza, John R., Gjerstad, Erik, Tang, Jie, Williams, Steven R., Verner, Erik, Mackman, Richard L., Young, Wendy B., Sprengeler, Paul A., Chan, Hedy, Mortara, Kyle, Janc, James W., McGrath, Mary E.

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Transport characteristics of peptidomimetics. Effect of the pyrrolinone bioisostere on transport across Caco-2 cell monolayers von SUDOH, M, PAULETTI, G. M, YAO, W, MOSER, W, YOKOYAMA, A, PASTERNAK, A, SPRENGELER, P. A, SMITH, A. B, HIRSCHMANN, R, BORCHARDT, R. T

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Optimization of a screening lead for factor VIIa/TF von Young, Wendy B, Kolesnikov, Aleksandr, Rai, Roopa, Sprengeler, Paul A, Leahy, Ellen M, Shrader, William D, Sangalang, Joan, Burgess-Henry, Jana, Spencer, Jeff, Elrod, Kyle, Cregar, Lynne

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Nonpeptidal peptidomimetics with .beta.-D-glucose scaffolding. A partial somatostatin agonist bearing a close structural relationship to a potent, selective substance P antagonist von Hirschmann, Ralph, Nicolaou, K. C, Pietranico, Sherrie, Salvino, Joseph, Leahy, Ellen M, Sprengeler, Paul A, Furst, George, Strader, Catherine D, Smith, Amos B

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Design, Synthesis, and Solution Structure of a Pyrrolinone-Based β-Turn Peptidomimetic von Smith, Amos B, Wang, Wenyong, Sprengeler, Paul A, Hirschmann, Ralph

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Relative and Absolute Stereochemistries and Total Synthesis of (+)-Macrosphelides A and B, Potent, Orally Bioavailable Inhibitors of Cell−Cell Adhesion von Sunazuka, Toshiaki, Hirose, Tomoyasu, Harigaya, Yoshihiro, Takamatsu, Satoshi, Hayashi, Masahiko, Komiyama, Kanki, Ōmura, Satoshi, Sprengeler, Paul A, Smith, Amos B

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Neutral inhibitors of the serine protease factor Xa von SHRADER, William D, YOUNG, Wendy B, SPRENGELER, Paul A, SANGALANG, Joan C, ELROD, Kyle, CARR, Grant

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Pyrrolinone-Based HIV Protease Inhibitors. Design, Synthesis, and Antiviral Activity: Evidence for Improved Transport von Smith, Amos B, Hirschmann, Ralph, Pasternak, Alexander, Guzman, Mark C, Yokoyama, Akihisa, Sprengeler, Paul A, Darke, Paul L, Emini, Emilio A, Schleif, William A

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The first design and synthesis of a steroidal peptidomimetic. The potential value of peptidomimetics in elucidating the bioactive conformation of peptide ligands von Hirschmann, Ralph, Sprengeler, Paul A, Kawasaki, Tomomi, Leahy, James W, Shakespeare, William C, Smith, Amos B

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Design, Synthesis, and Evaluation of a Pyrrolinone-Based Matrix Metalloprotease Inhibitor von Smith, Amos B, Nittoli, Thomas, Sprengeler, Paul A, Duan, James J.-W, Liu, Rui-Qin, Hirschmann, Ralph F

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