Search Results - "Felts, S"

Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu5-Negative Allosteric Modulator VU0424238 (Auglurant) by Crouch, Rachel D, Blobaum, Anna L, Felts, Andrew S, Conn, P Jeffrey, Lindsley, Craig W

“…Aldehyde oxidase (AO) and xanthine oxidase (XO) are molybdo-flavoenzymes that catalyze oxidation of aromatic azaheterocycles. Differences in AO activity have…”
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A small molecule cell-impermeant Hsp90 antagonist inhibits tumor cell motility and invasion by Tsutsumi, S, Scroggins, B, Koga, F, Lee, M-J, Trepel, J, Felts, S, Carreras, C, Neckers, L

“…Heat shock protein 90 (Hsp90) is a molecular chaperone that maintains function of numerous intracellular signaling nodes utilized by cancer cells for…”
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Design of 4‑Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2 by Felts, Andrew S, Rodriguez, Alice L, Smith, Katrina A, Engers, Julie L, Morrison, Ryan D, Byers, Frank W, Blobaum, Anna L, Locuson, Charles W, Chang, Sichen, Venable, Daryl F, Niswender, Colleen M, Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W, Emmitte, Kyle A

“…Both orthosteric and allosteric antagonists of the group II metabotropic glutamate receptors (mGlus) have been used to establish a link between mGlu2/3…”
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The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5 by Morrison, Ryan D, Blobaum, Anna L, Byers, Frank W, Santomango, Tammy S, Bridges, Thomas M, Stec, Donald, Brewer, Katrina A, Sanchez-Ponce, Raymundo, Corlew, Melany M, Rush, Roger, Felts, Andrew S, Manka, Jason, Bates, Brittney S, Venable, Daryl F, Rodriguez, Alice L, Jones, Carrie K, Niswender, Colleen M, Conn, P Jeffrey, Lindsley, Craig W, Emmitte, Kyle A, Daniels, J Scott

“…Negative allosteric modulation (NAM) of metabotropic glutamate receptor subtype 5 (mGlu₅) represents a therapeutic strategy for the treatment of childhood…”
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The hsp90-related Protein TRAP1 Is a Mitochondrial Protein with Distinct Functional Properties by Felts, Sara J., Owen, Barbara A.L., Nguyen, PhuongMai, Trepel, Jane, Donner, David B., Toft, David O.

“…The hsp90 family of molecular chaperones was expanded recently due to the cloning of TRAP1 and hsp75 by yeast two-hybrid screens. Careful analysis of the human…”
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Molecular Basis of the Time-Dependent Inhibition of Cyclooxygenases by Indomethacin by Prusakiewicz, Jeffery J, Felts, Andrew S, Mackenzie, Bonnie S, Marnett, Lawrence J

“…Cyclooxygenases (COXs) are the therapeutic targets of nonsteroidal antiinflammatory drugs. Indomethacin (INDO) was one of the first nonsteroidal…”
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Discovery of a potent M5 antagonist with improved clearance profile. Part 2: Pyrrolidine amide-based antagonists by Orsi, Douglas L., Felts, Andrew S., Rodriguez, Alice L., Vinson, Paige N., Cho, Hyekyung P., Chang, Sichen, Blobaum, Anna L., Niswender, Colleen M., Conn, P. Jeffrey, Jones, Carrie K., Lindsley, Craig W., Han, Changho

“…[Display omitted] This Letter describes our ongoing effort to improve the clearance of selective M5 antagonists. Herein, we report the replacement of the…”
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Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5‑a]pyrimidine-5-carboxamide and Thieno[3,2‑b]pyridine-5-carboxamide Cores by Childress, Elizabeth S, Wieting, Joshua M, Felts, Andrew S, Breiner, Megan M, Long, Madeline F, Luscombe, Vincent B, Rodriguez, Alice L, Cho, Hyekyung P, Blobaum, Anna L, Niswender, Colleen M, Emmitte, Kyle A, Conn, P. Jeffrey, Lindsley, Craig W

“…A scaffold hopping exercise from a monocyclic mGlu2 NAM with poor rodent PK led to two novel heterobicyclic series of mGlu2 NAMs based on either a…”
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Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors by Engers, Darren W., Bollinger, Sean R., Felts, Andrew S., Vadukoot, Anish K., Williams, Charles H., Blobaum, Anna L., Lindsley, Craig W., Hong, Charles C., Hopkins, Corey R.

“…[Display omitted] The activin-like kinases are a family of kinases that play important roles in a variety of disease states. Of this class of kinases, ALK2,…”
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Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships by Gregory, Karen J, Noetzel, Meredith J, Rook, Jerri M, Vinson, Paige N, Stauffer, Shaun R, Rodriguez, Alice L, Emmitte, Kyle A, Zhou, Ya, Chun, Aspen C, Felts, Andrew S, Chauder, Brian A, Lindsley, Craig W, Niswender, Colleen M, Conn, P Jeffrey

“…Drug discovery programs increasingly are focusing on allosteric modulators as a means to modify the activity of G protein-coupled receptor (GPCR) targets…”
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A Sterically-Encumbered, C2-Symmetric Chiral Acetal for Enhanced Asymmetric Induction in the Pauson−Khand Reaction by KRAFFT, Marie E., BOñAGA, Llorente V. R., FELTS, Andrew S., HIROSAWA, Chitaru, KERRIGAN, Sean

“…High levels of diastereoselection were achieved in the PKR of 1,6- and 1,7-cyclopropylidenynes bearing a bulky propargylic C(2)-symmetric acetal…”
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Development of VU6019650 : A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M 5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder by Garrison, Aaron T, Orsi, Douglas L, Capstick, Rory A, Whomble, David, Li, Jinming, Carter, Trever R, Felts, Andrew S, Vinson, Paige N, Rodriguez, Alice L, Han, Allie, Hajari, Krishma, Cho, Hyekyung P, Teal, Laura B, Ragland, Madeline G, Ghamari-Langroudi, Masoud, Bubser, Michael, Chang, Sichen, Schnetz-Boutaud, Nathalie C, Boutaud, Olivier, Blobaum, Anna L, Foster, Daniel J, Niswender, Colleen M, Conn, P Jeffrey, Lindsley, Craig W, Jones, Carrie K, Han, Changho

“…The muscarinic acetylcholine receptor (mAChR) subtype 5 (M ) represents a novel potential target for the treatment of multiple addictive disorders, including…”
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Discovery of (R)‑(2-Fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-Hydroxypiperidin-1-yl)methanone (ML337), An mGlu3 Selective and CNS Penetrant Negative Allosteric Modulator (NAM) by Wenthur, Cody J, Morrison, Ryan, Felts, Andrew S, Smith, Katrina A, Engers, Julie L, Byers, Frank W, Daniels, J. Scott, Emmitte, Kyle A, Conn, P. Jeffrey, Lindsley, Craig W

“…A multidimensional, iterative parallel synthesis effort identified a series of highly selective mGlu3 NAMs with submicromolar potency and good CNS penetration…”
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Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles by Rook, Jerri M, Tantawy, Mohammed N, Ansari, Mohammad S, Felts, Andrew S, Stauffer, Shaun R, Emmitte, Kyle A, Kessler, Robert M, Niswender, Colleen M, Daniels, J Scott, Jones, Carrie K, Lindsley, Craig W, Conn, P Jeffrey

“…Allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGlu5) have exciting potential as therapeutic agents for multiple brain disorders…”
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Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead by Jones, Carrie K., Sheffler, Douglas J., Williams, Richard, Jadhav, Sataya B., Felts, Andrew S., Morrison, Ryan D., Niswender, Colleen M., Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W.

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Hsp90 Chaperone Activity Requires the Full-length Protein and Interaction among Its Multiple Domains by Johnson, Brian D., Chadli, Ahmed, Felts, Sara J., Bouhouche, Ilhem, Catelli, Maria G., Toft, David O.

“…Hsp90 is an abundant and ubiquitous protein involved in a diverse array of cellular processes. Mechanistically we understand little of the apparently complex…”
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The p23 molecular chaperones act at a late step in intracellular receptor action to differentially affect ligand efficacies by Freeman, B C, Felts, S J, Toft, D O, Yamamoto, K R

“…Multiple molecular chaperones, including Hsp90 and p23, interact with members of the intracellular receptor (IR) family. To investigate p23 function, we…”
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The 2′-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX‑2 Inhibitor by Blobaum, Anna L, Uddin, Md. Jashim, Felts, Andrew S, Crews, Brenda C, Rouzer, Carol A, Marnett, Lawrence J

“…Indomethacin is a potent, time-dependent, nonselective inhibitor of the cyclooxygenase enzymes (COX-1 and COX-2). Deletion of the 2′-methyl group of…”
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Species-Specific Involvement of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of the Pyrimidine-Containing mGlu 5 -Negative Allosteric Modulator VU0424238 (Auglurant) by Crouch, Rachel D, Blobaum, Anna L, Felts, Andrew S, Conn, P Jeffrey, Lindsley, Craig W

“…Aldehyde oxidase (AO) and xanthine oxidase (XO) are molybdo-flavoenzymes that catalyze oxidation of aromatic azaheterocycles. Differences in AO activity have…”
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Design and Synthesis of mGlu2 NAMs with Improved Potency and CNS Penetration Based on a Truncated Picolinamide Core by Bollinger, Katrina A, Felts, Andrew S, Brassard, Christopher J, Engers, Julie L, Rodriguez, Alice L, Weiner, Rebecca L, Cho, Hyekyung P, Chang, Sichen, Bubser, Michael, Jones, Carrie K, Blobaum, Anna L, Niswender, Colleen M, Conn, P. Jeffrey, Emmitte, Kyle A, Lindsley, Craig W

“…Herein, we detail the optimization of the mGlu2 negative allosteric modulator (NAM), VU6001192, by a reductionist approach to afford a novel, simplified mGlu2…”
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