G
Gary Erik Aspnes
Researcher at Pfizer
Publications - 51
Citations - 1073
Gary Erik Aspnes is an academic researcher from Pfizer. The author has contributed to research in topics: Glucokinase & In vivo. The author has an hindex of 18, co-authored 49 publications receiving 951 citations.
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Journal ArticleDOI
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.
Jeffrey A. Pfefferkorn,Angel Guzman-Perez,John Litchfield,Robert J. Aiello,Judith L. Treadway,John C. Pettersen,Martha L. Minich,Kevin J. Filipski,Christopher S. Jones,Meihua Tu,Gary Erik Aspnes,Hud Lawrence Risley,Jianwei Bian,Benjamin D. Stevens,Patricia Bourassa,Theresa D’Aquila,Levenia Baker,Nicole Barucci,Alan Robertson,Francis Bourbonais,David R. Derksen,Margit MacDougall,Over Cabrera,Jing Chen,Amanda L. Lapworth,James A. Landro,William J. Zavadoski,Karen Atkinson,Nahor Haddish-Berhane,Beijing Tan,Lili Yao,Rachel E. Kosa,Manthena V.S. Varma,Bo Feng,David B. Duignan,Ayman El-Kattan,Sharad B. Murdande,Shenping Liu,Mark Ammirati,John D. Knafels,Paul DaSilva-Jardine,Laurel Sweet,Spiros Liras,Timothy P. Rolph +43 more
TL;DR: 19 is identified as a potent glucokinase activator with a greater than 50-fold liver-to-pancreas ratio of tissue distribution in rodent and non-rodent species, leading to its selection as a clinical development candidate for treating type 2 diabetes.
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Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design
Seungil Han,Anil Mistry,Jeanne S. Chang,David Cunningham,Matt Griffor,Peter C. Bonnette,Hong Wang,Boris A. Chrunyk,Gary Erik Aspnes,Daniel P. Walker,Brosius Arthur Douglas,Leonard Buckbinder +11 more
TL;DR: Structural, biophysical, and pharmacological studies suggest that the unique features of the DFG motif, including Leu-504 hinge-loop variability, can be exploited for the development of selective protein kinase inhibitors.
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Regioselective Synthesis of 2H-Indazoles Using a Mild, One-Pot Condensation–Cadogan Reductive Cyclization
TL;DR: An operationally simple and efficient one-pot synthesis of 2H-indazoles from commercially available reagents is reported.
Journal ArticleDOI
A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification
Whitney M. Nolte,Jean-Philippe Fortin,Benjamin D. Stevens,Gary Erik Aspnes,David A. Griffith,Lise R. Hoth,Roger B. Ruggeri,Alan M. Mathiowetz,Chris Limberakis,David Hepworth,Philip A. Carpino +10 more
TL;DR: It is shown that substitution of cysteine for phenylalanine 345 in the glucagon receptor is sufficient to confer sensitivity to BETP and covalently modifies cysteines 347 and 438 in GLP-1R.
Journal ArticleDOI
Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2)
Kentaro Futatsugi,Daniel W. Kung,Suvi T. M. Orr,Shawn Cabral,David Hepworth,Gary Erik Aspnes,Scott Bader,Jianwei Bian,Markus Boehm,Philip A. Carpino,Steven B. Coffey,Matthew S. Dowling,Michael Herr,Wenhua Jiao,Sophie Y. Lavergne,Qifang Li,Ronald W. Clark,Derek M. Erion,Kou Kou,Kyuha Lee,Brandon Pabst,Sylvie Perez,Julie Purkal,Csilla C. Jorgensen,Theunis C. Goosen,James R. Gosset,Mark Niosi,John C. Pettersen,Jeffrey A. Pfefferkorn,Kay Ahn,Bryan Goodwin +30 more
TL;DR: The medicinal chemistry and preclinical biology of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2) is described and the preclinical candidate 9 (PF-06424439) demonstrated excellent ADMET properties and decreased circulating and hepatic lipids when orally administered to dyslipidemic rodent models.