Characterization of [125I]GLP-1(9-36), a novel radiolabeled analog of the major metabolite of glucagon-like peptide 1 to a receptor distinct from GLP1-R and function of the peptide in murine aorta
Kuc, Rhoda E., Maguire, Janet J., Siew, Keith, Patel, Sheena, Derksen, David R., Margaret Jackson, V., O'Shaughnessey, Kevin M., Davenport, Anthony P.
Published in Life sciences (1973) (02.05.2014)
Published in Life sciences (1973) (02.05.2014)
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A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide‑1 Receptor
Griffith, David A., Edmonds, David J., Fortin, Jean-Philippe, Kalgutkar, Amit S., Kuzmiski, J. Brent, Loria, Paula M., Saxena, Aditi R., Bagley, Scott W., Buckeridge, Clare, Curto, John M., Derksen, David R., Dias, João M., Griffor, Matthew C., Han, Seungil, Jackson, V. Margaret, Landis, Margaret S., Lettiere, Daniel, Limberakis, Chris, Liu, Yuhang, Mathiowetz, Alan M., Patel, Jayesh C., Piotrowski, David W., Price, David A., Ruggeri, Roger B., Tess, David A.
Published in Journal of medicinal chemistry (23.06.2022)
Published in Journal of medicinal chemistry (23.06.2022)
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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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Short Hydrophobic Peptides with Cyclic Constraints Are Potent Glucagon-like Peptide‑1 Receptor (GLP-1R) Agonists
Hoang, Huy N, Song, Kun, Hill, Timothy A, Derksen, David R, Edmonds, David J, Kok, W. Mei, Limberakis, Chris, Liras, Spiros, Loria, Paula M, Mascitti, Vincent, Mathiowetz, Alan M, Mitchell, Justin M, Piotrowski, David W, Price, David A, Stanton, Robert V, Suen, Jacky Y, Withka, Jane M, Griffith, David A, Fairlie, David P
Published in Journal of medicinal chemistry (14.05.2015)
Published in Journal of medicinal chemistry (14.05.2015)
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Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling
Plisson, Fabien, Hill, Timothy A., Mitchell, Justin M., Hoang, Huy N., de Araujo, Aline D., Xu, Weijun, Cotterell, Adam, Edmonds, David J., Stanton, Robert V., Derksen, David R., Loria, Paula M., Griffith, David A., Price, David A., Liras, Spiros, Fairlie, David P.
Published in European journal of medicinal chemistry (15.02.2017)
Published in European journal of medicinal chemistry (15.02.2017)
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Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists
Swedberg, Joakim E., Schroeder, Christina I., Mitchell, Justin M., Durek, Thomas, Fairlie, David P., Edmonds, David J., Griffith, David A., Ruggeri, Roger B., Derksen, David R., Loria, Paula M., Liras, Spiros, Price, David A., Craik, David J.
Published in European journal of medicinal chemistry (20.10.2015)
Published in European journal of medicinal chemistry (20.10.2015)
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Truncated Glucagon-like Peptide-1 and Exendin-4 α-Conotoxin pl14a Peptide Chimeras Maintain Potency and α-Helicity and Reveal Interactions Vital for cAMP Signaling in Vitro
Swedberg, Joakim E., Schroeder, Christina I., Mitchell, Justin M., Fairlie, David P., Edmonds, David J., Griffith, David A., Ruggeri, Roger B., Derksen, David R., Loria, Paula M., Price, David A., Liras, Spiros, Craik, David J.
Published in The Journal of biological chemistry (22.07.2016)
Published in The Journal of biological chemistry (22.07.2016)
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The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus
Pfefferkorn, Jeffrey A., Tu, Meihua, Filipski, Kevin J., Guzman-Perez, Angel, Bian, Jianwei, Aspnes, Gary E., Sammons, Matthew F., Song, Wei, Li, Jian-Cheng, Jones, Christopher S., Patel, Leena, Rasmusson, Tim, Zeng, Dongxiang, Karki, Kapil, Hamilton, Michael, Hank, Richard, Atkinson, Karen, Litchfield, John, Aiello, Robert, Baker, Levenia, Barucci, Nicole, Bourassa, Patricia, Bourbounais, Francis, D’Aquila, Theresa, Derksen, David R., MacDougall, Margit, Robertson, Alan
Published in Bioorganic & medicinal chemistry letters (01.12.2012)
Published in Bioorganic & medicinal chemistry letters (01.12.2012)
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Optimization of amide-based EP3 receptor antagonists
Lee, Esther C.Y., Futatsugi, Kentaro, Arcari, Joel T., Bahnck, Kevin, Coffey, Steven B., Derksen, David R., Kalgutkar, Amit S., Loria, Paula M., Sharma, Raman
Published in Bioorganic & medicinal chemistry letters (01.06.2016)
Published in Bioorganic & medicinal chemistry letters (01.06.2016)
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Pyrimidone-based series of glucokinase activators with alternative donor–acceptor motif
Filipski, Kevin J., Guzman-Perez, Angel, Bian, Jianwei, Perreault, Christian, Aspnes, Gary E., Didiuk, Mary T., Dow, Robert L., Hank, Richard F., Jones, Christopher S., Maguire, Robert J., Tu, Meihua, Zeng, Dongxiang, Liu, Shenping, Knafels, John D., Litchfield, John, Atkinson, Karen, Derksen, David R., Bourbonais, Francis, Gajiwala, Ketan S., Hickey, Michael, Johnson, Theodore O., Humphries, Paul S., Pfefferkorn, Jeffrey A.
Published in Bioorganic & medicinal chemistry letters (15.08.2013)
Published in Bioorganic & medicinal chemistry letters (15.08.2013)
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Journal Article
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia
Stevens, Benjamin D., Litchfield, John, Pfefferkorn, Jeffrey A., Atkinson, Karen, Perreault, Christian, Amor, Paul, Bahnck, Kevin, Berliner, Martin A., Calloway, Jessica, Carlo, Anthony, Derksen, David R., Filipski, Kevin J., Gumkowski, Mike, Jassal, Charanjeet, MacDougall, Margit, Murphy, Brendan, Nkansah, Paul, Pettersen, John, Rotter, Charles, Zhang, Yan
Published in Bioorganic & medicinal chemistry letters (15.12.2013)
Published in Bioorganic & medicinal chemistry letters (15.12.2013)
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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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Corrigendum to “The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus” [Bioorg. Med. Chem. Lett. 22 (2012) 7100–7105]
Pfefferkorn, Jeffrey A., Tu, Meihua, Filipski, Kevin J., Guzman-Perez, Angel, Bian, Jianwei, Aspnes, Gary E., Sammons, Matthew F., Song, Wei, Li, Jian-Cheng, Jones, Christopher S., Patel, Leena, Rasmusson, Tim, Zeng, Dongxiang, Karki, Kapil, Hamilton, Michael, Hank, Richard, Atkinson, Karen, Litchfield, John, Aiello, Robert, Baker, Levenia, Barucci, Nicole, Bourassa, Patricia, Bourbonais, Francis, D’Aquila, Theresa, Derksen, David R., MacDougall, Margit, Robertson, Alan
Published in Bioorganic & medicinal chemistry letters (01.09.2013)
Published in Bioorganic & medicinal chemistry letters (01.09.2013)
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Journal Article
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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Journal Article
Optimizing glucokinase activator binding kinetics to lower in vivo hypoglycemia riskElectronic supplementary information (ESI) available: SPR profiles for compounds 6 and 15, KD and EC50 correlation, comparison of human and rat off rates for select activators, synthetic protocols for compounds 3, 5, 6 and 11. See DOI: 10.1039/c4md00027g
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
Year of Publication 28.05.2014
Year of Publication 28.05.2014
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Journal Article
Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzo f uran-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 (01.01.2011)
Published in MedChemComm (01.01.2011)
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Journal Article
A small-molecule oral agonist of the human glucagon-like peptide-1 receptor
Griffith, David A, Edmonds, David J, tin, Jean-Phillipe, Kalgutkar, Amit S, Kuzmiski, J Brent, Loria, Paula M, Saxena, Aditi R, Bagley, Scott W, Buckeridge, Clare, Curto, John M, Derksen, David R, Dias, João M, Grif, Matthew C, Han, Seungil, Jackson, V Margaret, Landis, Margaret S, Lettiere, Daniel J, Limberakis, Chris, Liu, Yuhang, Mathiowetz, Alan M, Piotrowski, David W, Price, David A, Ruggeri, Roger B, Tess, David A
Published in bioRxiv (30.09.2020)
Published in bioRxiv (30.09.2020)
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