Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase von Ernst, Justin T, Thompson, Peggy A, Nilewski, Christian, Sprengeler, Paul A, Sperry, Samuel, Packard, Garrick, Michels, Theodore, Xiang, Alan, Tran, Chinh, Wegerski, Christopher J, Eam, Boreth, Young, Nathan P, Fish, Sarah, Chen, Joan, Howard, Haleigh, Staunton, Jocelyn, Molter, Jolene, Clarine, Jeff, Nevarez, Andres, Chiang, Gary G, Appleman, Jim R, Webster, Kevin R, Reich, Siegfried H

Volltext

Structure-based Design of Pyridone–Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition von Reich, Siegfried H, Sprengeler, Paul A, Chiang, Gary G, Appleman, James R, Chen, Joan, Clarine, Jeff, Eam, Boreth, Ernst, Justin T, Han, Qing, Goel, Vikas K, Han, Edward Z. R, Huang, Vera, Hung, Ivy N. J, Jemison, Adrianna, Jessen, Katti A, Molter, Jolene, Murphy, Douglas, Neal, Melissa, Parker, Gregory S, Shaghafi, Michael, Sperry, Samuel, Staunton, Jocelyn, Stumpf, Craig R, Thompson, Peggy A, Tran, Chinh, Webber, Stephen E, Wegerski, Christopher J, Zheng, Hong, Webster, Kevin R

Volltext

Discovery of Selective Irreversible Inhibitors for Bruton's Tyrosine Kinase von Pan, Zhengying, Scheerens, Heleen, Li, Shyr-Jiann, Schultz, Brian E., Sprengeler, Paul A., Burrill, L. Chuck, Mendonca, Rohan V., Sweeney, Michael D., Scott, Keana C. K., Grothaus, Paul G., Jeffery, Douglas A., Spoerke, Jill M., Honigberg, Lee A., Young, Peter R., Dalrymple, Stacie A., Palmer, James T.

Volltext

Molecular Characteristics of Repotrectinib That Enable Potent Inhibition of TRK Fusion Proteins and Resistant Mutations von Murray, Brion W, Rogers, Evan, Zhai, Dayong, Deng, Wei, Chen, Xi, Sprengeler, Paul A, Zhang, Xin, Graber, Armin, Reich, Siegfried H, Stopatschinskaja, Shanna, Solomon, Benjamin, Besse, Benjamin, Drilon, Alexander

Volltext

Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A von Thompson, Peggy A, Eam, Boreth, Young, Nathan P, Fish, Sarah, Chen, Joan, Barrera, Maria, Howard, Haleigh, Sung, Eric, Parra, Ana, Staunton, Jocelyn, Chiang, Gary G, Gerson-Gurwitz, Adina, Wegerski, Christopher J, Nevarez, Andres, Clarine, Jeff, Sperry, Samuel, Xiang, Alan, Nilewski, Christian, Packard, Garrick K, Michels, Theodore, Tran, Chinh, Sprengeler, Paul A, Ernst, Justin T, Reich, Siegfried H, Webster, Kevin R

Volltext

Expression, Crystallization, and Three-dimensional Structure of the Catalytic Domain of Human Plasma Kallikrein von Tang, Jie, Yu, Christine Luong, Williams, Steven R., Springman, Eric, Jeffery, Douglas, Sprengeler, Paul A., Estevez, Alberto, Sampang, Jun, Shrader, William, Spencer, Jeff, Young, Wendy, McGrath, Mary, Katz, Bradley A.

Volltext

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

Volltext

Strategic Diastereoselective C1 Functionalization in the Aza-Rocaglamide Scaffold toward Natural Product-Inspired eIF4A Inhibitors von Nilewski, Christian, Michels, Theodore D, Xiang, Alan X, Packard, Garrick K, Sprengeler, Paul A, Eam, Boreth, Fish, Sarah, Thompson, Peggy A, Wegerski, Christopher J, Ernst, Justin T, Reich, Siegfried H

Volltext

1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties von Nilewski, Christian, Michels, Theodore D., Packard, Garrick K., Xiang, Alan X., Sprengeler, Paul A., Eam, Boreth, Fish, Sarah, Thompson, Peggy A., Wegerski, Christopher J., Nevarez, Andres, Clarine, Jeff, Sperry, Samuel, Ernst, Justin T., Reich, Siegfried H.

Volltext

The Structure of the Extracellular Region of Human Hepsin Reveals a Serine Protease Domain and a Novel Scavenger Receptor Cysteine-Rich (SRCR) Domain von Somoza, John R, Ho, Joseph D, Luong, Christine, Ghate, Manjiri, Sprengeler, Paul A, Mortara, Kyle, Shrader, William D, Sperandio, David, Chan, Hedy, McGrath, Mary E, Katz, Bradley A

Volltext

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.

Volltext

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

Volltext

Discovery of novel heterocyclic factor VIIa inhibitors von Rai, Roopa, Kolesnikov, Aleksandr, Sprengeler, Paul A., Torkelson, Steven, Ton, Tony, Katz, Bradley A., Yu, Christine, Hendrix, John, Shrader, William D., Stephens, Robin, Cabuslay, Ronnell, Sanford, Ellen, Young, Wendy B.

Volltext

Factor VIIa inhibitors: Chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model von Young, Wendy B., Mordenti, Joyce, Torkelson, Steven, Shrader, William D., Kolesnikov, Aleksandr, Rai, Roopa, Liu, Liang, Hu, Huiyong, Leahy, Ellen M., Green, Michael J., Sprengeler, Paul A., Katz, Bradley A., Yu, Christine, Janc, James W., Elrod, Kyle C., Marzec, Ulla M., Hanson, Stephen R.

Volltext

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

Volltext

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

Volltext

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

Volltext

Stereostructure of (−)-Chloropeptin I, a Novel Inhibitor of gp120−CD4 Binding, via High- Temperature Molecular Dynamics, Monte Carlo Conformational Searching, and NMR Spectroscopy... von Gouda, Hiroaki, Matsuzaki, Keiichi, Tanaka, Haruo, Hirono, Shuichi, Ōmura, Satoshi, McCauley, John A, Sprengeler, Paul A, Furst, George T, Smith, Amos B

Volltext

Total Synthesis of (+)-Lactacystin von Nagamitsu, Tohru, Sunazuka, Toshiaki, Tanaka, Haruo, Ōmura, Satoshi, Sprengeler, Paul A, Smith, Amos B

Volltext

Potent 4-amino-5-azaindole factor VIIa inhibitors von Hu, Huiyong, Kolesnikov, Aleksandr, Riggs, Jennifer R., Wesson, Kieron E., Stephens, Robin, Leahy, Ellen M., Shrader, William D., Sprengeler, Paul A., Green, Michael J., Sanford, Ellen, Nguyen, Margaret, Gjerstad, Erik, Cabuslay, Ronnel, Young, Wendy B.

Volltext