Search Results - "FOTSCH, Christopher"

Mitigating Heterocycle Metabolism in Drug Discovery by St. Jean, David J, Fotsch, Christopher

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Systematic Study of the Glutathione Reactivity of N‑Phenylacrylamides: 2. Effects of Acrylamide Substitution by Birkholz, Adam, Kopecky, David J, Volak, Laurie P, Bartberger, Michael D, Chen, Yuping, Tegley, Christopher M, Arvedson, Tara, McCarter, John D, Fotsch, Christopher, Cee, Victor J

“…A comprehensive understanding of structure–reactivity relationships is critical to the design and optimization of cysteine-targeted covalent inhibitors…”
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Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors by Lloyd, David J., St Jean, 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

“…Two small-molecule disruptors of the glucokinase–glucokinase-regulatory-protein complex, AMG-1694 and AMG-3969, are identified that decrease blood glucose…”
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Calcium sensing receptor activators: calcimimetics by Harrington, Paul E, Fotsch, Christopher

“…The calcium sensing receptor (CaR) is a G protein-coupled receptor (GPCR) that plays a fundamental role in serum calcium homeostasis. The CaR is expressed on…”
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Facile Modulation of Antibody Fucosylation with Small Molecule Fucostatin Inhibitors and Cocrystal Structure with GDP-Mannose 4,6-Dehydratase by Allen, John G, Mujacic, Mirna, Frohn, Michael J, Pickrell, Alex J, Kodama, Paul, Bagal, Dhanashri, San Miguel, Tisha, Sickmier, E. Allen, Osgood, Steve, Swietlow, Aleksander, Li, Vivian, Jordan, John B, Kim, Ki-Won, Rousseau, Anne-Marie C, Kim, Yong-Jae, Caille, Seb, Achmatowicz, Mike, Thiel, Oliver, Fotsch, Christopher H, Reddy, Pranhitha, McCarter, John D

“…The efficacy of therapeutic antibodies that induce antibody-dependent cellular cytotoxicity can be improved by reduced fucosylation. Consequently, fucosylation…”
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Creating a more strategic small molecule biophysical hit characterization workflow by Fotsch, Christopher, Basu, Debaleena, Case, Ryan, Chen, Qing, Koneru, Pratibha C., Lo, Mei-Chu, Ngo, Rachel, Sharma, Pooja, Vaish, Amit, Yi, Xiang, Zech, Stephan G., Hodder, Peter

“…To confirm target engagement of hits from our high-throughput screening efforts, we ran biophysical assays on several hundreds of hits from 15 different…”
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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 by 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.

“…Small molecule activators of glucokinase have shown robust efficacy in both preclinical models and humans. However, overactivation of glucokinase (GK) can…”
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The optimization of aminooxadiazoles as orally active inhibitors of Cdc7 by Harrington, Paul E., Bourbeau, Matthew P., Fotsch, Christopher, Frohn, Michael, Pickrell, Alexander J., Reichelt, Andreas, Sham, Kelvin, Siegmund, Aaron C., Bailis, Julie M., Bush, Tammy, Escobar, Sonia, Hickman, Dean, Heller, Scott, Hsieh, Faye, Orf, Jessica N., Rong, Minqing, San Miguel, Tisha, Tan, Helming, Zalameda, Leeanne, Allen, John G.

“…A series of aminooxadiazoles was optimized for inhibition of Cdc7. Early lead isoquinoline 1 suffered from modest cell potency (cellular IC50=0.71μM measuring…”
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Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism by 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.

“…A series of urea based calcimimetics was optimized for potency and oral bioavailability. Crucial to this process was overcoming the poor pharmacokinetic…”
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Design of Potent, Orally Available Antagonists of the Transient Receptor Potential Vanilloid 1. Structure−Activity Relationships of 2-Piperazin-1-yl-1H-benzimidazoles by Ognyanov, Vassil I, Balan, Chenera, Bannon, Anthony W, Bo, Yunxin, Dominguez, Celia, Fotsch, Christopher, Gore, Vijay K, Klionsky, Lana, Ma, Vu V, Qian, Yi-Xin, Tamir, Rami, Wang, Xianghong, Xi, Ning, Xu, Shimin, Zhu, Dawn, Gavva, Narender R, Treanor, James J. S, Norman, Mark H

“…The vanilloid receptor-1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel that is predominantly expressed by peripheral neurons sensing painful…”
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Quinolinone-based agonists of S1P1: Use of a N-scan SAR strategy to optimize in vitro and in vivo activity by Pennington, Lewis D., Croghan, Michael D., Sham, Kelvin K.C., Pickrell, Alexander J., Harrington, Paul E., Frohn, Michael J., Lanman, Brian A., Reed, Anthony B., Lee, Matthew R., Xu, Han, McElvain, Michele, Xu, Yang, Zhang, Xuxia, Fiorino, Michael, Horner, Michelle, Morrison, Henry G., Arnett, Heather A., Fotsch, Christopher, Tasker, Andrew S., Wong, Min, Cee, Victor J.

“…We reveal how a N-scan SAR strategy (systematic substitution of each CH group with a N atom) was employed for quinolinone-based S1P1 agonist 5 to modulate…”
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Enzyme-catalyzed organic synthesis: practical routes to aza sugars and their analogs for use as glycoprocessing inhibitors by Look, Gary C, Fotsch, Christopher H, Wong, Chi Huey

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Discovery and Optimization of Substituted 1-(1-Phenyl-1H-pyrazol-3-yl)methanamines as Potent and Efficacious Type II Calcimimetics by Poon, Steve F, St. Jean, David J, Harrington, Paul E, Henley, Charles, Davis, James, Morony, Sean, Lott, Fred D, Reagan, Jeff D, Lu, Jenny Ying-Lin, Yang, Yuhua, Fotsch, Christopher

“…Our efforts to discover potent, orally bioavailable type II calcimimetic agents for the treatment of secondary hyperparathyroidism focused on the development…”
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Azole-based inhibitors of AKT/PKB for the treatment of cancer by Zeng, Qingping, Allen, John G., Bourbeau, Matthew P., Wang, Xianghong, Yao, Guomin, Tadesse, Seifu, Rider, James T., Yuan, Chester C., Hong, Fang-Tsao, Lee, Matthew R., Zhang, Shiwen, Lofgren, Julie A., Freeman, Daniel J., Yang, Suijin, Li, Chun, Tominey, Elizabeth, Huang, Xin, Hoffman, Douglas, Yamane, Harvey K., Fotsch, Christopher, Dominguez, Celia, Hungate, Randall, Zhang, Xiaoling

“…Through a combination of screening and structure-based rational design, we have discovered a series of N…”
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Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core by Xi, Ning, Hale, Clarence, Kelly, Michael G., Norman, Mark H., Stec, Markian, Xu, Shimin, Baumgartner, James W., Fotsch, Christopher

“…A novel series of piperazines appended to a succinamide backbone were synthesized and found to have a high affinity for the melanocortin-4 receptor (IC 50s…”
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Structure−Activity Relationship of (1-Aryl-2-piperazinylethyl)piperazines:  Antagonists for the AGRP/Melanocortin Receptor Binding by Arasasingham, Premilla N, Fotsch, Christopher, Ouyang, Xiaohu, Norman, Mark H, Kelly, Michael G, Stark, Kevin L, Karbon, Bill, Hale, Clarence, Baumgartner, James W, Zambrano, Martha, Cheetham, Janet, Tamayo, Nuria A

“…Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin action. In the hypothalamus, melanocortin peptide agonists act as…”
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Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH2 by FOTSCH, Christopher, SMITH, Duncan M, TAMAYO, Nuria A, NING XI, BAUMGARTNER, James W, ADAMS, Jeffrey A, CHEETHAM, Janet, CROGHAN, Michael, DOHERTY, Elizabeth M, HALE, Clarence, JAROSINSKI, Mark A, KELLY, Michael G, NORMAN, Mark H

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Systematic Study of the Glutathione (GSH) Reactivity of N‑Arylacrylamides: 1. Effects of Aryl Substitution by Cee, Victor J, Volak, Laurie P, Chen, Yuping, Bartberger, Michael D, Tegley, Chris, Arvedson, Tara, McCarter, John, Tasker, Andrew S, Fotsch, Christopher

“…Success in the design of targeted covalent inhibitors depends in part on a knowledge of the factors influencing electrophile reactivity. In an effort to…”
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Blockade of Glucocorticoid Excess at the Tissue Level: Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 as a Therapy for Type 2 Diabetes by Fotsch, Christopher, Wang, Minghan

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Emerging Targets in Osteoporosis Disease Modification by Allen, John G, Fotsch, Christopher, Babij, Philip

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