D. Derksen

发表

A small-molecule oral agonist of the human glucagon-like peptide-1 receptor

Margaret S. Landis, A. Mathiowetz, P. Loria, 2020, bioRxiv.

Title: A small-molecule oral agonist of the human glucagon-like peptide-1 1 receptor 2

Margaret S. Landis, A. Mathiowetz, P. Loria, 2020 .

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.

A. Davenport, J. Maguire, R. Kuc, 2014, Life sciences.

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 .

Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists.

D. Craik, P. Loria, David A. Price, 2015, European journal of medicinal chemistry.

Protein kinase CK2 catalyzes tyrosine phosphorylation in mammalian cells.

James S. Duncan, S. Li, G. Lajoie, 2008, Cellular signalling.

The anti-epileptic drug lacosamide (Vimpat) has anxiolytic property in rodents.

G. Higgins, E. Undzys, M. Isaac, 2009, European journal of pharmacology.

Comparative study of five antiepileptic drugs on a translational cognitive measure in the rat: relationship to antiepileptic property

A. Depaulis, G. Higgins, W. Burnham, 2009, Psychopharmacology.

Short Hydrophobic Peptides with Cyclic Constraints Are Potent Glucagon-like Peptide-1 Receptor (GLP-1R) Agonists.

A. Mathiowetz, P. Loria, David A. Price, 2015, Journal of medicinal chemistry.

Evidence for Regulation of Mitotic Progression through Temporal Phosphorylation and Dephosphorylation of CK2α

D. Litchfield, D. Derksen, N. St-Denis, 2009, Molecular and Cellular Biology.

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.

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

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

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*

D. Craik, P. Loria, David A. Price, 2016, The Journal of Biological Chemistry.

A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor

A. Mathiowetz, P. Loria, A. Kalgutkar, 2022, Journal of medicinal chemistry.

Title: A small-molecule oral agonist of the human glucagon-like peptide-1 1 receptor 2

Margaret S. Landis, A. Mathiowetz, P. Loria, 2020 .

Helixconstraints and amino acid substitution in GLP-1 increase cAMP and insulin secretion but not beta-arrestin 2 signaling.

P. Loria, David A. Price, S. Liras, 2017, European journal of medicinal chemistry.