Karen Atkinson

发表

Structural attributes influencing unbound tissue distribution.

Christopher E. Keefer, A. Kalgutkar, D. Scott, 2019, European journal of medicinal chemistry.

Evaluation of Fraction Unbound Across Seven Tissues of Five Species.

L. Di, G. Chang, D. Tess, 2019, Journal of pharmaceutical sciences.

Novel Method to Predict In Vivo Liver-to-Plasma Kpuu for OATP Substrates Using Suspension Hepatocytes

L. Di, J. Litchfield, Jian Lin, 2017, Drug Metabolism and Disposition.

A Novel Unified Approach to Predict Human Hepatic Clearance for Both Enzyme- and Transporter-Mediated Mechanisms Using Suspended Human Hepatocytes

L. Di, D. Tess, Jian Lin, 2019, Drug Metabolism and Disposition.

The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.

Michael D. Hamilton, J. Pfefferkorn, N. Barucci, 2012, Bioorganic & medicinal chemistry letters.

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

M. Ammirati, J. Treadway, S. Liras, 2011 .

Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.

A. Carlo, J. Pfefferkorn, J. Litchfield, 2013, Bioorganic & medicinal chemistry letters.

Optimizing glucokinase activator binding kinetics to lower in vivo hypoglycemia risk

T. Rolph, J. Pfefferkorn, K. Borzilleri, 2014 .

Metabolites in Safety Testing Assessment in Early Clinical Development: A Case Study with a Glucokinase Activator

W. S. Denney, A. Kalgutkar, J. Pfefferkorn, 2014, Drug Metabolism and Disposition.

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.

J. Treadway, J. Pfefferkorn, W. Zavadoski, 2013, Bioorganic & medicinal chemistry letters.

Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats.

S. Wright, A. Kalgutkar, J. Pfefferkorn, 2010, Bioorganic & medicinal chemistry letters.

Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis.

Jeffrey R. Chabot, P. Loria, C. Halldin, 2017, Angewandte Chemie.

A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.

S. Wright, J. Pfefferkorn, J. Litchfield, 2012, Bioorganic & medicinal chemistry letters.

Efficient Liver Targeting by Polyvalent Display of a Compact Ligand for the Asialoglycoprotein Receptor.

M. Ammirati, David A. Price, S. Liras, 2017, Journal of the American Chemical Society.

Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: a bench-to-bedside case study on tissue selective drug distribution.

Bo Feng, David B Duignan, Bruce Auerbach, 2011, Bioorganic & medicinal chemistry letters.

N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors.

C. Steppan, J. Litchfield, R. Trilles, 2011, Bioorganic & medicinal chemistry letters.

A Novel Relay Method for Determining Low-Clearance Values

Li Di, R Scott Obach, Yurong Lai, 2012, Drug Metabolism and Disposition.

Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.

David A. Price, A. Kalgutkar, K. Beaumont, 2018, Journal of medicinal chemistry.

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.

Jing Chen, David B Duignan, Robert Aiello, 2012, Journal of medicinal chemistry.

Novel Cytochrome P450 Reaction Phenotyping for Low-Clearance Compounds Using the Hepatocyte Relay Method

Li Di, L. Di, Karen Atkinson, 2016, Drug Metabolism and Disposition.

Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif.

K. Gajiwala, M. Hickey, J. Pfefferkorn, 2013, Bioorganic & medicinal chemistry letters.

Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators.

A. Mathiowetz, David A. Price, A. Kalgutkar, 2017, Journal of medicinal chemistry.

Identification of a novel conformationally constrained glucagon receptor antagonist.

S. Wright, A. Kalgutkar, J. Pfefferkorn, 2014, Bioorganic & medicinal chemistry letters.

In Vitro–In Vivo Correlation for Low-Clearance Compounds Using Hepatocyte Relay Method

Li Di, Jian Lin, R Scott Obach, 2013, Drug Metabolism and Disposition.

Comparison of the Circulating Metabolite Profile of PF-04991532, a Hepatoselective Glucokinase Activator, Across Preclinical Species and Humans: Potential Implications in Metabolites in Safety Testing Assessment

A. Kalgutkar, J. Pfefferkorn, L. Di, 2015, Drug Metabolism and Disposition.

In Vitro-In Vivo Extrapolation of Intestinal Availability for Carboxylesterase Substrates Using Portal Vein-Cannulated Monkey.

T. Maurer, D. Scott, K. Beaumont, 2017, Journal of pharmaceutical sciences.

Metabolism and excretion of (S)-6-(3-cyclopentyl-2-(4-trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid (PF-04991532), a hepatoselective glucokinase activator, in humans: confirmation of the MIST potential noted in first-in-Human metabolite scouting studies

A. Kalgutkar, D. Kazierad, A. Bergman, 2019, Xenobiotica; the fate of foreign compounds in biological systems.

In Vitro–In Vivo Correlation for Low-Clearance Compounds Using Hepatocyte Relay Method

L. Di, Jian Lin, Karen Atkinson, 2013, Drug Metabolism and Disposition.

Novel Cytochrome P450 Reaction Phenotyping for Low-Clearance Compounds Using the Hepatocyte Relay Method

L. Di, Karen Atkinson, Xin Yang, 2016, Drug Metabolism and Disposition.