Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms
Calabrese, Matthew F., Rajamohan, Francis, Harris, Melissa S., Caspers, Nicole L., Magyar, Rachelle, Withka, Jane M., Wang, Hong, Borzilleri, Kris A., Sahasrabudhe, Parag V., Hoth, Lise R., Geoghegan, Kieran F., Han, Seungil, Brown, Janice, Subashi, Timothy A., Reyes, Allan R., Frisbie, Richard K., Ward, Jessica, Miller, Russell A., Landro, James A., Londregan, Allyn T., Carpino, Philip A., Cabral, Shawn, Smith, Aaron C., Conn, Edward L., Cameron, Kimberly O., Qiu, Xiayang, Kurumbail, Ravi G.
Published in Structure (London) (05.08.2014)
Published in Structure (London) (05.08.2014)
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Discovery of 2‑(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)‑yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases
Ruggeri, Roger B, Buckbinder, Leonard, Bagley, Scott W, Carpino, Philip A, Conn, Edward L, Dowling, Matthew S, Fernando, Dilinie P, Jiao, Wenhua, Kung, Daniel W, Orr, Suvi T. M, Qi, Yingmei, Rocke, Benjamin N, Smith, Aaron, Warmus, Joseph S, Zhang, Yan, Bowles, Daniel, Widlicka, Daniel W, Eng, Heather, Ryder, Tim, Sharma, Raman, Wolford, Angela, Okerberg, Carlin, Walters, Karen, Maurer, Tristan S, Zhang, Yanwei, Bonin, Paul D, Spath, Samantha N, Xing, Gang, Hepworth, David, Ahn, Kay, Kalgutkar, Amit S
Published in Journal of medicinal chemistry (12.11.2015)
Published in Journal of medicinal chemistry (12.11.2015)
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Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists
Humphries, Paul S., Benbow, John W., Bonin, Paul D., Boyer, David, Doran, Shawn D., Frisbie, Richard K., Piotrowski, David W., Balan, Gayatri, Bechle, Bruce M., Conn, Edward L., Dirico, Kenneth J., Oliver, Robert M., Soeller, Walter C., Southers, James A., Yang, Xiaojing
Published in Bioorganic & medicinal chemistry letters (01.05.2009)
Published in Bioorganic & medicinal chemistry letters (01.05.2009)
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Expedient Synthesis of α‑(2-Azaheteroaryl) Acetates via the Addition of Silyl Ketene Acetals to Azine‑N‑oxides
Londregan, Allyn T, Burford, Kristen, Conn, Edward L, Hesp, Kevin D
Published in Organic letters (20.06.2014)
Published in Organic letters (20.06.2014)
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Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy
Cameron, Kimberly O, Kung, Daniel W, Kalgutkar, Amit S, Kurumbail, Ravi G, Miller, Russell, Salatto, Christopher T, Ward, Jessica, Withka, Jane M, Bhattacharya, Samit K, Boehm, Markus, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew, Caspers, Nicole L, Cokorinos, Emily, Conn, Edward L, Dowling, Matthew S, Edmonds, David J, Eng, Heather, Fernando, Dilinie P, Frisbie, Richard, Hepworth, David, Landro, James, Mao, Yuxia, Rajamohan, Francis, Reyes, Allan R, Rose, Colin R, Ryder, Tim, Shavnya, Andre, Smith, Aaron C, Tu, Meihua, Wolford, Angela C, Xiao, Jun
Published in Journal of medicinal chemistry (08.09.2016)
Published in Journal of medicinal chemistry (08.09.2016)
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Identification of parallel medicinal chemistry protocols to expand branched amine design space
Conn, Edward L, Perry, Matthew A, Shi, Kecheng, Wang, Guotao, Hoy, Susan, Sach, Neal W, Qi, Wenying, Qu, Liqiang, Gao, Yu, Xu, Yan, Schmitt, Daniel C
Published in Organic & biomolecular chemistry (11.05.2022)
Published in Organic & biomolecular chemistry (11.05.2022)
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6-Azaspiro[2.5]octanes as small molecule agonists of the human glucagon-like peptide-1 receptor
Aspnes, Gary E., Bagley, Scott W., Coffey, Steven B., Conn, Edward L., Curto, John M., Edmonds, David J., Genovino, Julien, Griffith, David A., Ingle, Gajendra, Jiao, Wenhua, Limberakis, Chris, Mathiowetz, Alan M., Piotrowski, David W., Rose, Colin R., Ruggeri, Roger B., Wei, Liuqing
Published in Bioorganic & medicinal chemistry letters (01.10.2023)
Published in Bioorganic & medicinal chemistry letters (01.10.2023)
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Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging
Liang, Steven H., Chen, Jinshan Michael, Normandin, Marc D., Chang, Jeanne S., Chang, George C., Taylor, Christine K., Trapa, Patrick, Plummer, Mark S., Para, Kimberly S., Conn, Edward L., Lopresti-Morrow, Lori, Lanyon, Lorraine F., Cook, James M., Richter, Karl E. G., Nolan, Charlie E., Schachter, Joel B., Janat, Fouad, Che, Ye, Shanmugasundaram, Veerabahu, Lefker, Bruce A., Enerson, Bradley E., Livni, Elijahu, Wang, Lu, Guehl, Nicolas J., Patnaik, Debasis, Wagner, Florence F., Perlis, Roy, Holson, Edward B., Haggarty, Stephen J., El Fakhri, Georges, Kurumbail, Ravi G., Vasdev, Neil
Published in Angewandte Chemie (International ed.) (08.08.2016)
Published in Angewandte Chemie (International ed.) (08.08.2016)
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Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK)
Huard, Kim, Ahn, Kay, Amor, Paul, Beebe, David A, Borzilleri, Kris A, Chrunyk, Boris A, Coffey, Steven B, Cong, Yang, Conn, Edward L, Culp, Jeffrey S, Dowling, Matthew S, Gorgoglione, Matthew F, Gutierrez, Jemy A, Knafels, John D, Lachapelle, Erik A, Pandit, Jayvardhan, Parris, Kevin D, Perez, Sylvie, Pfefferkorn, Jeffrey A, Price, David A, Raymer, Brian, Ross, Trenton T, Shavnya, Andre, Smith, Aaron C, Subashi, Timothy A, Tesz, Gregory J, Thuma, Benjamin A, Tu, Meihua, Weaver, John D, Weng, Yan, Withka, Jane M, Xing, Gang, Magee, Thomas V
Published in Journal of medicinal chemistry (28.09.2017)
Published in Journal of medicinal chemistry (28.09.2017)
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Discovery of Orally Bioavailable Selective Inhibitors of the Sodium-Phosphate Cotransporter NaPi2a (SLC34A1)
Filipski, Kevin J, Sammons, Matthew F, Bhattacharya, Samit K, Panteleev, Jane, Brown, Janice A, Loria, Paula M, Boehm, Markus, Smith, Aaron C, Shavnya, Andre, Conn, Edward L, Song, Kun, Weng, Yan, Facemire, Carie, Jüppner, Harald, Clerin, Valerie
Published in ACS medicinal chemistry letters (10.05.2018)
Published in ACS medicinal chemistry letters (10.05.2018)
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Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Edmonds, David J, Kung, Daniel W, Kalgutkar, Amit S, Filipski, Kevin J, Ebner, David C, Cabral, Shawn, Smith, Aaron C, Aspnes, Gary E, Bhattacharya, Samit K, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew F, Caspers, Nicole L, Cokorinos, Emily C, Conn, Edward L, Dowling, Matthew S, Eng, Heather, Feng, Bo, Fernando, Dilinie P, Genung, Nathan E, Herr, Michael, Kurumbail, Ravi G, Lavergne, Sophie Y, Lee, Esther C.-Y, Li, Qifang, Mathialagan, Sumathy, Miller, Russell A, Panteleev, Jane, Polivkova, Jana, Rajamohan, Francis, Reyes, Allan R, Salatto, Christopher T, Shavnya, Andre, Thuma, Benjamin A, Tu, Meihua, Ward, Jessica, Withka, Jane M, Xiao, Jun, Cameron, Kimberly O
Published in Journal of medicinal chemistry (22.03.2018)
Published in Journal of medicinal chemistry (22.03.2018)
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Species Differences in the Oxidative Desulfurization of a Thiouracil-Based Irreversible Myeloperoxidase Inactivator by Flavin-Containing Monooxygenase Enzymes
Eng, Heather, Sharma, Raman, Wolford, Angela, Di, Li, Ruggeri, Roger B, Buckbinder, Leonard, Conn, Edward L, Dalvie, Deepak K, Kalgutkar, Amit S
Published in Drug metabolism and disposition (01.08.2016)
Published in Drug metabolism and disposition (01.08.2016)
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Evolution of the Synthesis of AMPK Activators for the Treatment of Diabetic Nephropathy: From Three Preclinical Candidates to the Investigational New Drug PF-06409577
Smith, Aaron C, Kung, Daniel W, Shavnya, Andre, Brandt, Thomas A, Dent, Philip D, Genung, Nathan E, Cabral, Shawn, Panteleev, Jane, Herr, Michael, Yip, Ka Ning, Aspnes, Gary E, Conn, Edward L, Dowling, Matthew S, Edmonds, David J, Edmonds, Ian D, Fernando, Dilinie P, Herrinton, Paul M, Keene, Nandell F, Lavergne, Sophie Y, Li, Qifang, Polivkova, Jana, Rose, Colin R, Thuma, Benjamin A, Vetelino, Michael G, Wang, Guoqiang, Weaver, John D, Widlicka, Daniel W, Price Wiglesworth, Kristin E, Xiao, Jun, Zahn, Todd, Zhang, Yingxin
Published in Organic process research & development (15.06.2018)
Published in Organic process research & development (15.06.2018)
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1,4-Addition of an aryllithium reagent to diethyl ketomalonate. Scalable synthesis of ethyl 1-(hydroxymethyl)-1,3-dihydroisobenzofuran-1-carboxylate
Rocke, Benjamin N., Conn, Edward L., Eisenbeis, Shane A., Ruggeri, Roger B.
Published in Tetrahedron letters (10.10.2012)
Published in Tetrahedron letters (10.10.2012)
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Journal Article
Insights into the Novel Hydrolytic Mechanism of a Diethyl 2‑Phenyl-2-(2-arylacetoxy)methyl Malonate Ester-Based Microsomal Triglyceride Transfer Protein (MTP) Inhibitor
Ryder, Tim, Walker, Gregory S, Goosen, Theunis C, Ruggeri, Roger B, Conn, Edward L, Rocke, Benjamin N, Lapham, Kimberly, Steppan, Claire M, Hepworth, David, Kalgutkar, Amit S
Published in Chemical research in toxicology (15.10.2012)
Published in Chemical research in toxicology (15.10.2012)
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A Novel Series of Non-Carboxylic Acid, Non-Hydantoin Inhibitors of Aldose Reductase with Potent Oral Activity in Diabetic Rat Models: 6-(5-Chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and Congeners
Mylari, Banavara L, Armento, Sandra J, Beebe, David A, Conn, Edward L, Coutcher, James B, Dina, Michael S, O'Gorman, Melissa T, Linhares, Michael C, Martin, William H, Oates, Peter J, Tess, David A, Withbroe, Gregory J, Zembrowski, William J
Published in Journal of medicinal chemistry (06.10.2005)
Published in Journal of medicinal chemistry (06.10.2005)
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Journal Article
A Highly Selective, Non-Hydantoin, Non-Carboxylic Acid Inhibitor of Aldose Reductase with Potent Oral Activity in Diabetic Rat Models: 6-(5-Chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one
Mylari, Banavara L, Armento, Sandra J, Beebe, David A, Conn, Edward L, Coutcher, James B, Dina, Michael S, O'Gorman, Melissa T, Linhares, Michael C, Martin, William H, Oates, Peter J, Tess, David A, Withbroe, Gregory J, Zembrowski, William J
Published in Journal of medicinal chemistry (05.06.2003)
Published in Journal of medicinal chemistry (05.06.2003)
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Journal Article
Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging
Liang, Steven H., Chen, Jinshan Michael, Normandin, Marc D., Chang, Jeanne S., Chang, George C., Taylor, Christine K., Trapa, Patrick, Plummer, Mark S., Para, Kimberly S., Conn, Edward L., Lopresti-Morrow, Lori, Lanyon, Lorraine F., Cook, James M., Richter, Karl E. G., Nolan, Charlie E., Schachter, Joel B., Janat, Fouad, Che, Ye, Shanmugasundaram, Veerabahu, Lefker, Bruce A., Enerson, Bradley E., Livni, Elijahu, Wang, Lu, Guehl, Nicolas J., Patnaik, Debasis, Wagner, Florence F., Perlis, Roy, Holson, Edward B., Haggarty, Stephen J., El Fakhri, Georges, Kurumbail, Ravi G., Vasdev, Neil
Published in Angewandte Chemie (08.08.2016)
Published in Angewandte Chemie (08.08.2016)
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GLP-1 수용체 효능제 및 그의 용도
BAGLEY SCOTT W, CURTO JOHN M, MATHIOWETZ ALAN M, PIOTROWSKI DAVID W, ASPNES GARY ERIK, EDMONDS DAVID JAMES, FUTATSUGI KENTARO, LIMBERAKIS CHRIS, CONN EDWARD L, GRIFFITH DAVID A, RUGGERI ROGER B, FLANAGAN MARK E, HUARD KIM
Year of Publication 23.02.2021
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Year of Publication 23.02.2021
Patent
Design and synthesis of a novel family of triazine-based inhibitors of sorbitol dehydrogenase with oral activity: 1-{4-[3 R,5 S-dimethyl-4-(4-methyl-[1,3,5]triazin-2-yl)-piperazin-1-yl]-[1,3,5]triazin-2-yl}-( R) ethanol
Mylari, Banavara L., Withbroe, Gregory J., Beebe, David A., Brackett, Nathaniel S., Conn, Edward L., Coutcher, James B., Oates, Peter J., Zembrowski, William J.
Published in Bioorganic & medicinal chemistry (15.09.2003)
Published in Bioorganic & medicinal chemistry (15.09.2003)
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