A Long-Acting FGF21 Molecule, PF-05231023, Decreases Body Weight and Improves Lipid Profile in Non-human Primates and Type 2 Diabetic Subjects
Talukdar, Saswata, Zhou, Yingjiang, Li, Dongmei, Rossulek, Michelle, Dong, Jennifer, Somayaji, Veena, Weng, Yan, Clark, Ronald, Lanba, Adhiraj, Owen, Bryn M., Brenner, Martin B., Trimmer, Jeffrey K., Gropp, Kathryn E., Chabot, Jeffrey R., Erion, Derek M., Rolph, Timothy P., Goodwin, Bryan, Calle, Roberto A.
Published in Cell metabolism (08.03.2016)
Published in Cell metabolism (08.03.2016)
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Efruxifermin in non-alcoholic steatohepatitis: a randomized, double-blind, placebo-controlled, phase 2a trial
Harrison, Stephen A., Ruane, Peter J., Freilich, Bradley L., Neff, Guy, Patil, Rashmee, Behling, Cynthia A., Hu, Chen, Fong, Erica, de Temple, Brittany, Tillman, Erik J., Rolph, Timothy P., Cheng, Andrew, Yale, Kitty
Published in Nature medicine (01.07.2021)
Published in Nature medicine (01.07.2021)
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Branched-chain amino acid restriction in Zucker-fatty rats improves muscle insulin sensitivity by enhancing efficiency of fatty acid oxidation and acyl-glycine export
White, Phillip J, Lapworth, Amanda L, An, Jie, Wang, Liping, McGarrah, Robert W, Stevens, Robert D, Ilkayeva, Olga, George, Tabitha, Muehlbauer, Michael J, Bain, James R, Trimmer, Jeff K, Brosnan, M. Julia, Rolph, Timothy P, Newgard, Christopher B
Published in Molecular metabolism (Germany) (01.07.2016)
Published in Molecular metabolism (Germany) (01.07.2016)
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The Acetyl Group Buffering Action of Carnitine Acetyltransferase Offsets Macronutrient-Induced Lysine Acetylation of Mitochondrial Proteins
Davies, Michael N., Kjalarsdottir, Lilja, Thompson, J. Will, Dubois, Laura G., Stevens, Robert D., Ilkayeva, Olga R., Brosnan, M. Julia, Rolph, Timothy P., Grimsrud, Paul A., Muoio, Deborah M.
Published in Cell reports (Cambridge) (12.01.2016)
Published in Cell reports (Cambridge) (12.01.2016)
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Impact of combined resistance and aerobic exercise training on branched-chain amino acid turnover, glycine metabolism and insulin sensitivity in overweight humans
Glynn, Erin L., Piner, Lucy W., Huffman, Kim M., Slentz, Cris A., Elliot-Penry, Lorraine, AbouAssi, Hiba, White, Phillip J., Bain, James R., Muehlbauer, Michael J., Ilkayeva, Olga R., Stevens, Robert D., Porter Starr, Kathryn N., Bales, Connie W., Volpi, Elena, Brosnan, M. Julia, Trimmer, Jeff K., Rolph, Timothy P., Newgard, Christopher B., Kraus, William E.
Published in Diabetologia (01.10.2015)
Published in Diabetologia (01.10.2015)
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Muscle-Liver Trafficking of BCAA-Derived Nitrogen Underlies Obesity-Related Glycine Depletion
White, Phillip J., Lapworth, Amanda L., McGarrah, Robert W., Kwee, Lydia Coulter, Crown, Scott B., Ilkayeva, Olga, An, Jie, Carson, Matthew W., Christopher, Bridgette A., Ball, James R., Davies, Michael N., Kjalarsdottir, Lilja, George, Tabitha, Muehlbauer, Michael J., Bain, James R., Stevens, Robert D., Koves, Timothy R., Muoio, Deborah M., Brozinick, Joseph T., Gimeno, Ruth E., Brosnan, M. Julia, Rolph, Timothy P., Kraus, William E., Shah, Svati H., Newgard, Christopher B.
Published in Cell reports (Cambridge) (10.11.2020)
Published in Cell reports (Cambridge) (10.11.2020)
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The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats
Erion, Derek M, Lapworth, Amanda, Amor, Paul A, Bai, Guoyun, Vera, Nicholas B, Clark, Ronald W, Yan, Qingyun, Zhu, Yimin, Ross, Trenton T, Purkal, Julie, Gorgoglione, Matthew, Zhang, Guodong, Bonato, Vinicius, Baker, Levenia, Barucci, Nicole, D'Aquila, Theresa, Robertson, Alan, Aiello, Robert J, Yan, Jiangli, Trimmer, Jeff, Rolph, Timothy P, Pfefferkorn, Jeffrey A
Published in PloS one (23.05.2014)
Published in PloS one (23.05.2014)
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Once‐weekly administration of a long‐acting fibroblast growth factor 21 analogue modulates lipids, bone turnover markers, blood pressure and body weight differently in obese people with hypertriglyceridaemia and in non‐human primates
Kim, Albert M., Somayaji, Veena R., Dong, Jennifer Q., Rolph, Timothy P., Weng, Yan, Chabot, Jeffrey R., Gropp, Kathryn E., Talukdar, Saswata, Calle, Roberto A.
Published in Diabetes, obesity & metabolism (01.12.2017)
Published in Diabetes, obesity & metabolism (01.12.2017)
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Isocitrate-to-SENP1 signaling amplifies insulin secretion and rescues dysfunctional β cells
Ferdaoussi, Mourad, Dai, Xiaoqing, Jensen, Mette V, Wang, Runsheng, Peterson, Brett S, Huang, Chao, Ilkayeva, Olga, Smith, Nancy, Miller, Nathanael, Hajmrle, Catherine, Spigelman, Aliya F, Wright, Robert C, Plummer, Gregory, Suzuki, Kunimasa, Mackay, James P, van de Bunt, Martijn, Gloyn, Anna L, Ryan, Terence E, Norquay, Lisa D, Brosnan, M Julia, Trimmer, Jeff K, Rolph, Timothy P, Kibbey, Richard G, Manning Fox, Jocelyn E, Colmers, William F, Shirihai, Orian S, Neufer, P Darrell, Yeh, Edward T H, Newgard, Christopher B, MacDonald, Patrick E
Published in The Journal of clinical investigation (01.10.2015)
Published in The Journal of clinical investigation (01.10.2015)
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Noncompetitive immunoassay optimized for pharmacokinetic assessments of biologically active efruxifermin
Kinne, Adam S., Tillman, Erik J., Abdeen, Sanofar J., Johnson, Derrick E., Parmer, Elijah S., Hurst, Jacob P., de Temple, Brittany, Rinker, Sherri, Rolph, Timothy P., Bowsher, Ronald R.
Published in Journal of pharmaceutical and biomedical analysis (05.08.2023)
Published in Journal of pharmaceutical and biomedical analysis (05.08.2023)
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Human sebum requires de novo lipogenesis, which is increased in acne vulgaris and suppressed by acetyl-CoA carboxylase inhibition
Esler, William P, Tesz, Gregory J, Hellerstein, Marc K, Beysen, Carine, Sivamani, Raja, Turner, Scott M, Watkins, Steven M, Amor, Paul A, Carvajal-Gonzalez, Santos, Geoly, Frank J, Biddle, Kathleen E, Purkal, Julie J, Fitch, Mark, Buckeridge, Clare, Silvia, Annette M, Griffith, David A, Gorgoglione, Matthew, Hassoun, Lauren, Bosanac, Suzana S, Vera, Nicholas B, Rolph, Timothy P, Pfefferkorn, Jeffrey A, Sonnenberg, Gabriele E
Published in Science translational medicine (15.05.2019)
Published in Science translational medicine (15.05.2019)
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FGF21 does not require interscapular brown adipose tissue and improves liver metabolic profile in animal models of obesity and insulin-resistance
Bernardo, Barbara, Lu, Min, Bandyopadhyay, Gautam, Li, Pingping, Zhou, Yingjiang, Huang, Jie, Levin, Nancy, Tomas, Eva M., Calle, Roberto A., Erion, Derek M., Rolph, Timothy P., Brenner, Martin, Talukdar, Saswata
Published in Scientific reports (08.07.2015)
Published in Scientific reports (08.07.2015)
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Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism
Ahn, Kay, Boehm, Markus, Brown, Matthew F, Calloway, Jessica, Che, Ye, Chen, Jinshan, Fennell, Kimberly F, Geoghegan, Kieran F, Gilbert, Adam M, Gutierrez, Jemy A, Kalgutkar, Amit S, Lanba, Adhiraj, Limberakis, Chris, Magee, Thomas V, O’Doherty, Inish, Oliver, Robert, Pabst, Brandon, Pandit, Jayvardhan, Parris, Kevin, Pfefferkorn, Jeffrey A, Rolph, Timothy P, Patel, Rushi, Schuff, Brandon, Shanmugasundaram, Veerabahu, Starr, Jeremy T, Varghese, Alison H, Vera, Nicholas B, Vernochet, Cecile, Yan, Jiangli
Published in ACS chemical biology (16.09.2016)
Published in ACS chemical biology (16.09.2016)
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Discovery of (S)-6-(3-Cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic Acid as a Hepatoselective Glucokinase Activator Clinical Candidate for Treating Type 2 Diabetes Mellitus
Pfefferkorn, Jeffrey A, Guzman-Perez, Angel, Litchfield, John, Aiello, Robert, Treadway, Judith L, Pettersen, John, Minich, Martha L, Filipski, Kevin J, Jones, Christopher S, Tu, Meihua, Aspnes, Gary, Risley, Hud, Bian, Jianwei, Stevens, Benjamin D, Bourassa, Patricia, D’Aquila, Theresa, Baker, Levenia, Barucci, Nicole, Robertson, Alan S, Bourbonais, Francis, Derksen, David R, MacDougall, Margit, Cabrera, Over, Chen, Jing, Lapworth, Amanda Lee, Landro, James A, Zavadoski, William J, Atkinson, Karen, Haddish-Berhane, Nahor, Tan, Beijing, Yao, Lili, Kosa, Rachel E, Varma, Manthena V, Feng, Bo, Duignan, David B, El-Kattan, Ayman, Murdande, Sharad, Liu, Shenping, Ammirati, Mark, Knafels, John, DaSilva-Jardine, Paul, Sweet, Laurel, Liras, Spiros, Rolph, Timothy P
Published in Journal of medicinal chemistry (09.02.2012)
Published in Journal of medicinal chemistry (09.02.2012)
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Generation of Affinity Purified Antibody Reagents for Specific Determination of Efruxifermin in Biological Matrices
Kinne, Adam S, Abdeen, Sanofar J, Parmer, Elijah S, Thystrup, Jennifer A, Tillman, Erik J, Rolph, Timothy P, Bowsher, Ronald R
Published in Journal of the Endocrine Society (03.05.2021)
Published in Journal of the Endocrine Society (03.05.2021)
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Isocitrate-to-SENP1 signaling amplifies insulin secretion and rescues dysfunctional [Beta] cells
Ferdaoussi, Mourad, Dai, Xiaoqing, Jensen, Mette V, Wang, Runsheng, Peterson, Brett S, Huang, Chao, Ilkayeva, Olga, Smith, Nancy, Miller, Nathanael, Hajmrle, Catherine, Spigelman, Aliya F, Wright, Robert C, Plummer, Gregory, Suzuki, Kunimasa, Mackay, James P, van de Bunt, Martijn, Gloyn, Anna L, Ryan, Terence E, Norquay, Lisa D, Brosnan, M Julia, Trimmer, Jeff K, Rolph, Timothy P, Kibbey, Richard G, Fox, Jocelyn E Manning, Colmers, William F, Shirihai, Orian S, Neufer, P Darrell, Yeh, Edward T H, Newgard, Christopher B, MacDonald, Patrick E
Published in The Journal of clinical investigation (01.10.2015)
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Published in The Journal of clinical investigation (01.10.2015)
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Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus
Pfefferkorn, Jeffrey A., Guzman-Perez, Angel, Oates, Peter J., Litchfield, John, Aspnes, Gary, Basak, Arindrajit, Benbow, John, Berliner, Martin A., Bian, Jianwei, Choi, Chulho, Freeman-Cook, Kevin, Corbett, Jeffrey W., Didiuk, Mary, Dunetz, Joshua R., Filipski, Kevin J., Hungerford, William M., Jones, Christopher S., Karki, Kapil, Ling, Anthony, Li, Jian-Cheng, Patel, Leena, Perreault, Christian, Risley, Hud, Saenz, James, Song, Wei, Tu, Meihua, Aiello, Robert, Atkinson, Karen, Barucci, Nicole, Beebe, David, Bourassa, Patricia, Bourbounais, Francis, Brodeur, Anne M., Burbey, Rena, Chen, Jing, D'Aquila, Theresa, Derksen, David R., Haddish-Berhane, Nahor, Huang, Cong, Landro, James, Lee Lapworth, Amanda, MacDougall, Margit, Perregaux, David, Pettersen, John, Robertson, Alan, Tan, Beijing, Treadway, Judith L., Liu, Shenping, Qiu, Xiayang, Knafels, John, Ammirati, Mark, Song, Xi, DaSilva-Jardine, Paul, Liras, Spiros, Sweet, Laurel, Rolph, Timothy P.
Published in MedChemComm (01.09.2011)
Published in MedChemComm (01.09.2011)
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Optimizing glucokinase activator binding kinetics to lower in vivo hypoglycemia risk
Borzilleri, Kris A., Pfefferkorn, Jeffrey A., Guzman-Perez, Angel, Liu, Shenping, Qiu, Xiayang, Chrunyk, Boris A., Song, Xi, Tu, Meihua, Filipski, Kevin J., Aiello, Robert, Derksen, David R., Bourbonais, Francis J., Landro, James, Bourassa, Patricia, D'Aquila, Theresa, Baker, Levenia, Barrucci, Nicole, Litchfield, John, Atkinson, Karen, Rolph, Timothy P., Withka, Jane M.
Published in MedChemComm (2014)
Published in MedChemComm (2014)
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Journal Article
Discovery of ( S )-6-(3-Cyclopentyl-2-(4-(trifluoromethyl)-1 H -imidazol-1-yl)propanamido)nicotinic Acid as a Hepatoselective Glucokinase Activator Clinical Candidate for Treating Type 2 Diabetes Mellitus
Pfefferkorn, Jeffrey A., Guzman-Perez, Angel, Litchfield, John, Aiello, Robert, Treadway, Judith L., Pettersen, John, Minich, Martha L., Filipski, Kevin J., Jones, Christopher S., Tu, Meihua, Aspnes, Gary, Risley, Hud, Bian, Jianwei, Stevens, Benjamin D., Bourassa, Patricia, D’Aquila, Theresa, Baker, Levenia, Barucci, Nicole, Robertson, Alan S., Bourbonais, Francis, Derksen, David R., MacDougall, Margit, Cabrera, Over, Chen, Jing, Lapworth, Amanda Lee, Landro, James A., Zavadoski, William J., Atkinson, Karen, Haddish-Berhane, Nahor, Tan, Beijing, Yao, Lili, Kosa, Rachel E., Varma, Manthena V., Feng, Bo, Duignan, David B., El-Kattan, Ayman, Murdande, Sharad, Liu, Shenping, Ammirati, Mark, Knafels, John, DaSilva-Jardine, Paul, Sweet, Laurel, Liras, Spiros, Rolph, Timothy P.
Published in Journal of medicinal chemistry (09.02.2012)
Published in Journal of medicinal chemistry (09.02.2012)
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