Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism
Wehn, Paul M., Harrington, Paul E., Carlson, Timothy J., Davis, James, Deprez, Pierre, Fotsch, Christopher H., Grillo, Mark P., Lu, Jenny Ying-Lin, Morony, Sean, Pattabiraman, Kanaka, Poon, Steve F., Reagan, Jeff D., St. Jean, David J., Temal, Taoues, Wang, Minghan, Yang, Yuhua, Henley, Charles, Lively, Sarah E.
Published in Bioorganic & medicinal chemistry letters (15.12.2013)
Published in Bioorganic & medicinal chemistry letters (15.12.2013)
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Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors
Lloyd, David J, St Jean, Jr, David J, Kurzeja, Robert J M, Wahl, Robert C, Michelsen, Klaus, Cupples, Rod, Chen, Michelle, Wu, John, Sivits, Glenn, Helmering, Joan, Komorowski, Renée, Ashton, Kate S, Pennington, Lewis D, Fotsch, Christopher, Vazir, Mukta, Chen, Kui, Chmait, Samer, Zhang, Jiandong, Liu, Longbin, Norman, Mark H, Andrews, Kristin L, Bartberger, Michael D, Van, Gwyneth, Galbreath, Elizabeth J, Vonderfecht, Steven L, Wang, Minghan, Jordan, Steven R, Véniant, Murielle M, Hale, Clarence
Published in Nature (London) (01.12.2013)
Published in Nature (London) (01.12.2013)
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Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σS–X) Interaction for Conformational Constraint
Pennington, Lewis D, Bartberger, Michael D, Croghan, Michael D, Andrews, Kristin L, Ashton, Kate S, Bourbeau, Matthew P, Chen, Jie, Chmait, Samer, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Hong, Fang-Tsao, Hungate, Randall W, Jordan, Steven R, Kong, Ke, Liu, Longbin, Michelsen, Klaus, Moyer, Carolyn, Nishimura, Nobuko, Norman, Mark H, Reichelt, Andreas, Siegmund, Aaron C, Sivits, Glenn, Tadesse, Seifu, Tegley, Christopher M, Van, Gwyneth, Yang, Kevin C, Yao, Guomin, Zhang, Jiandong, Lloyd, David J, Hale, Clarence, St. Jean, David J
Published in Journal of medicinal chemistry (24.12.2015)
Published in Journal of medicinal chemistry (24.12.2015)
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Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2
Ashton, Kate S., St. Jean, David J., Poon, Steve F., Lee, Matthew R., Allen, John G., Zhang, Shiwen, Lofgren, Julie A., Zhang, Xiaoling, Fotsch, Christopher, Hungate, Randall
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
Published in Bioorganic & medicinal chemistry letters (15.09.2011)
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Structural Characterization and Pharmacodynamic Effects of an Orally Active 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor
Hale, Clarence, Véniant, Murielle, Wang, Zhulun, Chen, Michelle, McCormick, Jocelyn, Cupples, Rod, Hickman, Dean, Min, Xiaoshan, Sudom, Athena, Xu, Haoda, Matsumoto, Guy, Fotsch, Christopher, St. Jean, David J. Jr, Wang, Minghan
Published in Chemical biology & drug design (2008)
Published in Chemical biology & drug design (2008)
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Next-generation small molecule therapies for heart failure: 2015 and beyond
Malinowski, Justin T., St. Jean, David J.
Published in Bioorganic & medicinal chemistry letters (15.05.2018)
Published in Bioorganic & medicinal chemistry letters (15.05.2018)
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From Fragment Screening to In Vivo Efficacy: Optimization of a Series of 2-Aminoquinolines as Potent Inhibitors of Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1)
Cheng, Yuan, Judd, Ted C, Bartberger, Michael D, Brown, James, Chen, Kui, Fremeau, Robert T, Hickman, Dean, Hitchcock, Stephen A, Jordan, Brad, Li, Vivian, Lopez, Patricia, Louie, Steven W, Luo, Yi, Michelsen, Klaus, Nixey, Thomas, Powers, Timothy S, Rattan, Claire, Sickmier, E. Allen, St. Jean, David J, Wahl, Robert C, Wen, Paul H, Wood, Stephen
Published in Journal of medicinal chemistry (25.08.2011)
Published in Journal of medicinal chemistry (25.08.2011)
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Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 3. Structure–Activity Relationships within the Aryl Carbinol Region of the N‑Arylsulfonamido‑N′‑arylpiperazine Series
Nishimura, Nobuko, Norman, Mark H, Liu, Longbin, Yang, Kevin C, Ashton, Kate S, Bartberger, Michael D, Chmait, Samer, Chen, Jie, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Jordan, Steven R, Kunz, Roxanne K, Pennington, Lewis D, Poon, Steve F, Siegmund, Aaron, Sivits, Glenn, Lloyd, David J, Hale, Clarence, St. Jean, David J
Published in Journal of medicinal chemistry (10.04.2014)
Published in Journal of medicinal chemistry (10.04.2014)
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ChemInform Abstract: Nonracemic Synthesis of GK-GKRP Disruptor AMG-3969
Bourbeau, Matthew P., Ashton, Kate S., Yan, Jie, St. Jean, David J. Jr
Published in ChemInform (14.10.2014)
Published in ChemInform (14.10.2014)
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Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis
Tamayo, Nuria A, Norman, Mark H, Bartberger, Michael D, Hong, Fang-Tsao, Bo, Yunxin, Liu, Longbin, Nishimura, Nobuko, Yang, Kevin C, Tadesse, Seifu, Fotsch, Christopher, Chen, Jie, Chmait, Samer, Cupples, Rod, Hale, Clarence, Jordan, Steven R, Lloyd, David J, Sivits, Glenn, Van, Gwyneth, St. Jean, David J
Published in Journal of medicinal chemistry (11.06.2015)
Published in Journal of medicinal chemistry (11.06.2015)
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Nonracemic Synthesis of GK–GKRP Disruptor AMG-3969
Bourbeau, Matthew P, Ashton, Kate S, Yan, Jie, St. Jean, David J
Published in Journal of organic chemistry (18.04.2014)
Published in Journal of organic chemistry (18.04.2014)
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Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 2. Leveraging Structure-Based Drug Design to Identify Analogues with Improved Pharmacokinetic Profiles
St. Jean, David J., Ashton, Kate S., Bartberger, Michael D., Chen, Jie, Chmait, Samer, Cupples, Rod, Galbreath, Elizabeth, Helmering, Joan, Hong, Fang-Tsao, Jordan, Steven R., Liu, Longbin, Kunz, Roxanne K., Michelsen, Klaus, Nishimura, Nobuko, Pennington, Lewis D., Poon, Steve F., Reid, Darren, Sivits, Glenn, Stec, Markian M., Tadesse, Seifu, Tamayo, Nuria, Van, Gwyneth, Yang, Kevin C., Zhang, Jiandong, Norman, Mark H., Fotsch, Christopher, Lloyd, David J., Hale, Clarence
Published in Journal of medicinal chemistry (23.01.2014)
Published in Journal of medicinal chemistry (23.01.2014)
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Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 1. Discovery of a Novel Tool Compound for in Vivo Proof-of-Concept
Ashton, Kate S., Andrews, Kristin L., Bryan, Marion C., Chen, Jie, Chen, Kui, Chen, Michelle, Chmait, Samer, Croghan, Michael, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Jordan, Steve R., Kurzeja, Robert J. M., Michelsen, Klaus, Pennington, Lewis D., Poon, Steve F., Sivits, Glenn, Van, Gwyneth, Vonderfecht, Steve L., Wahl, Robert C., Zhang, Jiandong, Lloyd, David J., Hale, Clarence, St. Jean, David J.
Published in Journal of medicinal chemistry (23.01.2014)
Published in Journal of medicinal chemistry (23.01.2014)
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Discovery of a calcimimetic with differential effects on parathyroid hormone and calcitonin secretion
Henley, 3rd, Charles, Yang, Yuhua, Davis, James, Lu, Jenny Ying Lin, Morony, Sean, Fan, Wei, Florio, Monica, Sun, Banghua, Shatzen, Edward, Pretorius, James K, Richards, William G, St Jean, Jr, David J, Fotsch, Christopher, Reagan, Jeff D
Published in The Journal of pharmacology and experimental therapeutics (01.06.2011)
Published in The Journal of pharmacology and experimental therapeutics (01.06.2011)
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Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 4. Exploration of a Novel Binding Pocket
Hong, Fang-Tsao, Norman, Mark H, Ashton, Kate S, Bartberger, Michael D, Chen, Jie, Chmait, Samer, Cupples, Rod, Fotsch, Christopher, Jordan, Steven R, Lloyd, David J, Sivits, Glenn, Tadesse, Seifu, Hale, Clarence, St. Jean, David J
Published in Journal of medicinal chemistry (24.07.2014)
Published in Journal of medicinal chemistry (24.07.2014)
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