A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification
Nolte, Whitney M, Fortin, Jean-Philippe, Stevens, Benjamin D, Aspnes, Gary E, Griffith, David A, Hoth, Lise R, Ruggeri, Roger B, Mathiowetz, Alan M, Limberakis, Chris, Hepworth, David, Carpino, Philip A
Published in Nature chemical biology (01.08.2014)
Published in Nature chemical biology (01.08.2014)
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Journal Article
Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design
Han, Seungil, Mistry, Anil, Chang, Jeanne S., Cunningham, David, Griffor, Matt, Bonnette, Peter C., Wang, Hong, Chrunyk, Boris A., Aspnes, Gary E., Walker, Daniel P., Brosius, Arthur D., Buckbinder, Leonard
Published in The Journal of biological chemistry (08.05.2009)
Published in The Journal of biological chemistry (08.05.2009)
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Journal Article
Small molecule inhibitors of the Pyk2 and FAK kinases modulate chemoattractant-induced migration, adhesion and Akt activation in follicular and marginal zone B cells
Tse, Kathy W.K., Lin, Kevin B.L., Dang-Lawson, May, Guzman-Perez, Angel, Aspnes, Gary E., Buckbinder, Leonard, Gold, Michael R.
Published in Cellular immunology (01.01.2012)
Published in Cellular immunology (01.01.2012)
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Journal Article
Discovery of a Novel Potent and Selective HSD17B13 Inhibitor, BI‑3231, a Well-Characterized Chemical Probe Available for Open Science
Thamm, Sven, Willwacher, Marina K., Aspnes, Gary E., Bretschneider, Tom, Brown, Nicholas F., Buschbom-Helmke, Silke, Fox, Thomas, Gargano, Emanuele M., Grabowski, Daniel, Hoenke, Christoph, Matera, Damian, Mueck, Katja, Peters, Stefan, Reindl, Sophia, Riether, Doris, Schmid, Matthias, Tautermann, Christofer S., Teitelbaum, Aaron M., Trünkle, Cornelius, Veser, Thomas, Winter, Martin, Wortmann, Lars
Published in Journal of medicinal chemistry (23.02.2023)
Published in Journal of medicinal chemistry (23.02.2023)
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Journal Article
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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Journal Article
Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups
Aspnes, Gary E., Coffey, Steven B., Darout, Etzer, Dechert-Schmitt, Anne-Marie, Dullea, Robert G., Kamlet, Adam S., Limberakis, Chris, Londregan, Allyn T., McClure, Kim F., Menhaji-Klotz, Elnaz, Piotrowski, David W., Polivkova, Jana, Raymer, Brian, Ruggeri, Roger B., Salatto, Christopher T., Tu, Meihua, Wei, Liuqing, Xiao, Jun
Published in Bioorganic & medicinal chemistry letters (15.08.2023)
Published in Bioorganic & medicinal chemistry letters (15.08.2023)
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Journal Article
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents
Londregan, Allyn T, Wei, Liuqing, Xiao, Jun, Lintner, Nathanael G, Petersen, Donna, Dullea, Robert G, McClure, Kim F, Bolt, Michael W, Warmus, Joseph S, Coffey, Steven B, Limberakis, Chris, Genovino, Julien, Thuma, Benjamin A, Hesp, Kevin D, Aspnes, Gary E, Reidich, Benjamin, Salatto, Christopher T, Chabot, Jeffrey R, Cate, Jamie H. D, Liras, Spiros, Piotrowski, David W
Published in Journal of medicinal chemistry (12.07.2018)
Published in Journal of medicinal chemistry (12.07.2018)
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Journal Article
Discovery and evaluation of non-basic small molecule modulators of the atypical chemokine receptor CXCR7
Aspnes, Gary E., Menhaji-Klotz, Elnaz, Boehm, Markus, Londregan, Allyn T., Lee, Esther C.Y., Limberakis, Chris, Coffey, Steven B., Brown, Janice A., Jones, Rhys M., Hesp, Kevin D.
Published in Bioorganic & medicinal chemistry letters (15.10.2021)
Published in Bioorganic & medicinal chemistry letters (15.10.2021)
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Journal Article
Route Selection and Optimization in the Synthesis of Two Imidazopyridine Inhibitors of DGAT‑2
Bader, Scott J, Herr, Michael, Aspnes, Gary E, Cabral, Shawn, Li, Qifang, Bian, Jianwei, Coffey, Steven B, Dowling, Matthew S, Fernando, Dilinie P, Jiao, Wenhua, Lavergne, Sophie Y, Kung, Daniel W
Published in Organic process research & development (16.03.2018)
Published in Organic process research & development (16.03.2018)
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Journal Article
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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Journal Article
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus
Guzman-Perez, Angel, Pfefferkorn, Jeffrey A., Lee, Esther C.Y., Stevens, Benjamin D., Aspnes, Gary E., Bian, Jianwei, Didiuk, Mary T., Filipski, Kevin J., Moore, Dianna, Perreault, Christian, Sammons, Matthew F., Tu, Meihua, Brown, Janice, Atkinson, Karen, Litchfield, John, Tan, Beijing, Samas, Brian, Zavadoski, William J., Salatto, Christopher T., Treadway, Judith
Published in Bioorganic & medicinal chemistry letters (15.05.2013)
Published in Bioorganic & medicinal chemistry letters (15.05.2013)
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Journal Article
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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Journal Article
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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Journal Article
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
Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3- d]pyrimidine core
Dow, Robert L., Andrews, Melissa, Aspnes, Gary E., Balan, Gayatri, Michael Gibbs, E., Guzman-Perez, Angel, Karki, Kapil, LaPerle, Jennifer L., Li, Jian-Cheng, Litchfield, John, Munchhof, Michael J., Perreault, Christian, Patel, Leena
Published in Bioorganic & medicinal chemistry letters (15.10.2011)
Published in Bioorganic & medicinal chemistry letters (15.10.2011)
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Journal Article
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2) : Structure-activity relationships and strategies for the elimination of reactive metabolite formation
WALKER, Daniel P, BI, F. Christopher, MCGLYNN, Molly A, OLIVER, Robert, DUNN, Matthew, LI, Jian-Cheng, RICHTER, Daniel T, COOPER, Beth A, KATH, John C, HULFORD, Catherine A, AUTRY, Christopher L, LUZZIO, Michael J, KALGUTKAR, Amit S, UNG, Ethan J, ROBERTS, W. Gregory, BONNETTE, Peter C, BUCKBINDER, Leonard, MISTRY, Anil, GRIFFOR, Matthew C, HAN, Seungil, GUZMAN-PEREZ, Angel, BAUMAN, Jonathan N, ZHAO, Sabrina X, SOGLIA, John R, ASPNES, Gary E, KUNG, Daniel W, KLUG-MCLEOD, Jacquelyn, ZAWISTOSKI, Michael P
Published in Bioorganic & medicinal chemistry (01.12.2008)
Published in Bioorganic & medicinal chemistry (01.12.2008)
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Journal Article
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors
Bhattacharya, Samit K., Aspnes, Gary E., Bagley, Scott W., Boehm, Markus, Brosius, Arthur D., Buckbinder, Leonard, Chang, Jeanne S., Dibrino, Joseph, Eng, Heather, Frederick, Kosea S., Griffith, David A., Griffor, Matthew C., Guimarães, Cristiano R.W., Guzman-Perez, Angel, Han, Seungil, Kalgutkar, Amit S., Klug-McLeod, Jacquelyn, Garcia-Irizarry, Carmen, Li, Jianke, Lippa, Blaise, Price, David A., Southers, James A., Walker, Daniel P., Wei, Liuqing, Xiao, Jun, Zawistoski, Michael P., Zhao, Xumiao
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
Published in Bioorganic & medicinal chemistry letters (15.12.2012)
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Differences in CYP3A4 catalyzed bioactivation of 5-aminooxindole and 5-aminobenzsultam scaffolds in proline-rich tyrosine kinase 2 (PYK2) inhibitors: Retrospective analysis by CYP3A4 molecular docking, quantum chemical calculations and glutathione adduct detection using linear ion trap/orbitrap mass spectrometry
Sun, Hao, Sharma, Raman, Bauman, Jonathan, Walker, Daniel P., Aspnes, Gary E., Zawistoski, Michael P., Kalgutkar, Amit S.
Published in Bioorganic & medicinal chemistry letters (15.06.2009)
Published in Bioorganic & medicinal chemistry letters (15.06.2009)
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Journal Article
Efficient Synthesis of 4-Amino-2-methoxy-7,8-dihydropyrido[4,3-d]pyrimidin-5-ones: Practical Access to a Novel Chemotype in the Development of DGAT-1 Inhibitors
Bahnck, Kevin B., Shavnya, Andrei, Tao, Yong, Lilley, Susan C., Andrews, Melissa P., Aspnes, Gary E., Bernhardson, David J., Bill, David R., Bundesmann, Mark W., Dow, Robert L., Karki, Kapil, Le, Tung, Li, Qifang, Munchhof, Michael J., Nematalla, Asaad, Nihlawi, Mohammed, Patel, Leena, Perreault, Christian, Waldo, Michael
Published in Synthesis (Stuttgart) (18.10.2012)
Published in Synthesis (Stuttgart) (18.10.2012)
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