Covalent Modifiers: An Orthogonal Approach to Drug Design von Potashman, Michele H, Duggan, Mark E

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Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors von Lindsley, Craig W., Zhao, Zhijian, Leister, William H., Robinson, Ronald G., Barnett, Stanley F., Defeo-Jones, Deborah, Jones, Raymond E., Hartman, George D., Huff, Joel R., Huber, Hans E., Duggan, Mark E.

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Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents von Bubser, Michael, Bridges, Thomas M, Dencker, Ditte, Gould, Robert W, Grannan, Michael, Noetzel, Meredith J, Lamsal, Atin, Niswender, Colleen M, Daniels, J. Scott, Poslusney, Michael S, Melancon, Bruce J, Tarr, James C, Byers, Frank W, Wess, Jürgen, Duggan, Mark E, Dunlop, John, Wood, Michael W, Brandon, Nicholas J, Wood, Michael R, Lindsley, Craig W, Conn, P. Jeffrey, Jones, Carrie K

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Identification of a Chrysanthemic Ester as an Apolipoprotein E Inducer in Astrocytes von Fan, Jianjia, Zareyan, Shahab, Zhao, Wenchen, Shimizu, Yoko, Pfeifer, Tom A, Tak, Jun-Hyung, Isman, Murray B, Van den Hoven, Bernard, Duggan, Mark E, Wood, Michael W, Wellington, Cheryl L, Kulic, Iva

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Challenges in the development of an M 4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs von Wood, Michael R, Noetzel, Meredith J, Poslusney, Michael S, Melancon, Bruce J, Tarr, James C, Lamsal, Atin, Chang, Sichen, Luscombe, Vincent B, Weiner, Rebecca L, Cho, Hyekyung P, Bubser, Michael, Jones, Carrie K, Niswender, Colleen M, Wood, Michael W, Engers, Darren W, Brandon, Nicholas J, Duggan, Mark E, Conn, P Jeffrey, Bridges, Thomas M, Lindsley, Craig W

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Challenges in the development of an M 4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides von Tarr, James C, Wood, Michael R, Noetzel, Meredith J, Bertron, Jeanette L, Weiner, Rebecca L, Rodriguez, Alice L, Lamsal, Atin, Byers, Frank W, Chang, Sichen, Cho, Hyekyung P, Jones, Carrie K, Niswender, Colleen M, Wood, Michael W, Brandon, Nicholas J, Duggan, Mark E, Conn, P Jeffrey, Bridges, Thomas M, Lindsley, Craig W

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Covalent modifiers: an orthogonal approach to drug design von Potashman, Michele H, Duggan, Mark E

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State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 – Relation to antipsychotic-like drug effects von Gould, Robert W., Nedelcovych, Michael T., Gong, Xuewen, Tsai, Erica, Bubser, Michael, Bridges, Thomas M., Wood, Michael R., Duggan, Mark E., Brandon, Nicholas J., Dunlop, John, Wood, Michael W., Ivarsson, Magnus, Noetzel, Meredith J., Daniels, J. Scott, Niswender, Colleen M., Lindsley, Craig W., Conn, P. Jeffrey, Jones, Carrie K.

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Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia von Wood, Michael R., Noetzel, Meredith J., Melancon, Bruce J., Poslusney, Michael S., Nance, Kellie D., Hurtado, Miguel A., Luscombe, Vincent B., Weiner, Rebecca L., Rodriguez, Alice L., Lamsal, Atin, Chang, Sichen, Bubser, Michael, Blobaum, Anna L., Engers, Darren W., Niswender, Colleen M., Jones, Carrie K., Brandon, Nicholas J., Wood, Michael W., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.

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Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members von DeFeo-Jones, Deborah, Barnett, Stanley F, Fu, Sheng, Hancock, Paula J, Haskell, Kathleen M, Leander, Karen R, McAvoy, Elizabeth, Robinson, Ronald G, Duggan, Mark E, Lindsley, Craig W, Zhao, Zhijian, Huber, Hans E, Jones, Raymond E

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Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors von Zhao, Zhijian, Leister, William H., Robinson, Ronald G., Barnett, Stanley F., Defeo-Jones, Deborah, Jones, Raymond E., Hartman, George D., Huff, Joel R., Huber, Hans E., Duggan, Mark E., Lindsley, Craig W.

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Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo von Sivakumaran, Sudhir, Cardarelli, Ross A, Maguire, Jamie, Kelley, Matt R, Silayeva, Liliya, Morrow, Danielle H, Mukherjee, Jayanta, Moore, Yvonne E, Mather, Robert J, Duggan, Mark E, Brandon, Nicholas J, Dunlop, John, Zicha, Stephen, Moss, Stephen J, Deeb, Tarek Z

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Identification of Anabolic Selective Androgen Receptor Modulators with Reduced Activities in Reproductive Tissues and Sebaceous Glands von Schmidt, Azriel, Harada, Shun-Ichi, Kimmel, Donald B., Bai, Chang, Chen, Fang, Rutledge, Su Jane, Vogel, Robert L., Scafonas, Angela, Gentile, Michael A., Nantermet, Pascale V., McElwee-Witmer, Sheila, Pennypacker, Brenda, Masarachia, Patricia, Sahoo, Soumya P., Kim, Yuntae, Meissner, Robert S., Hartman, George D., Duggan, Mark E., Rodan, Gideon A., Towler, Dwight A., Ray, William J.

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Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154 von Gould, Robert W., Grannan, Michael D., Gunter, Barak W., Ball, Jacob, Bubser, Michael, Bridges, Thomas M., Wess, Jurgen, Wood, Michael W., Brandon, Nicholas J., Duggan, Mark E., Niswender, Colleen M., Lindsley, Craig W., Conn, P. Jeffrey, Jones, Carrie K.

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The small molecule CLP257 does not modify activity of the K + -Cl - co-transporter KCC2 but does potentiate GABA A receptor activity von Cardarelli, Ross A, Jones, Karen, Pisella, Lucie I, Wobst, Heike J, McWilliams, Lisa J, Sharpe, Paul M, Burnham, Matthew P, Baker, David J, Chudotvorova, Ilona, Guyot, Justine, Silayeva, Liliya, Morrow, Danielle H, Dekker, Niek, Zicha, Stephen, Davies, Paul A, Holenz, Jörg, Duggan, Mark E, Dunlop, John, Mather, Robert J, Wang, Qi, Medina, Igor, Brandon, Nicholas J, Deeb, Tarek Z, Moss, Stephen J

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Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M 4 PAM VU0467154 von Gould, Robert W, Grannan, Michael D, Gunter, Barak W, Ball, Jacob, Bubser, Michael, Bridges, Thomas M, Wess, Jurgen, Wood, Michael W, Brandon, Nicholas J, Duggan, Mark E, Niswender, Colleen M, Lindsley, Craig W, Conn, P Jeffrey, Jones, Carrie K

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Toward β‑Secretase‑1 Inhibitors with Improved Isoform Selectivity von Johansson, Patrik, Kaspersson, Karin, Gurrell, Ian K, Bäck, Elisabeth, Eketjäll, Susanna, Scott, Clay W, Cebers, Gvido, Thorne, Philip, McKenzie, Michael J, Beaton, Haydn, Davey, Paul, Kolmodin, Karin, Holenz, Jörg, Duggan, Mark E, Budd Haeberlein, Samantha, Bürli, Roland W

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Design, Synthesis, and In Vivo Efficacy of Glycine Transporter-1 (GlyT1) Inhibitors Derived from a Series of [4-Phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl Benzamides von Lindsley, Craig W., Zhao, Zhijian, Leister, William H., O'Brien, Julie, Lemaire, Wei, Williams Jr, David L., Chen, Tsing-Bau, Chang, Raymond S. L., Burno, Maryann, Jacobson, Marlene A., Sur, Cyrille, Kinney, Gene G., Pettibone, Douglas J., Tiller, Philip R., Smith, Sheri, Tsou, Nancy N., Duggan, Mark E., Conn, P. Jeffrey, Hartman, George D.

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Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides von Tarr, James C., Wood, Michael R., Noetzel, Meredith J., Bertron, Jeanette L., Weiner, Rebecca L., Rodriguez, Alice L., Lamsal, Atin, Byers, Frank W., Chang, Sichen, Cho, Hyekyung P., Jones, Carrie K., Niswender, Colleen M., Wood, Michael W., Brandon, Nicholas J., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.

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Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides von Tarr, James C., Wood, Michael R., Noetzel, Meredith J., Melancon, Bruce J., Lamsal, Atin, Luscombe, Vincent B., Rodriguez, Alice L., Byers, Frank W., Chang, Sichen, Cho, Hyekyung P., Engers, Darren W., Jones, Carrie K., Niswender, Colleen M., Wood, Michael W., Brandon, Nicholas J., Duggan, Mark E., Conn, P. Jeffrey, Bridges, Thomas M., Lindsley, Craig W.

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