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Title: Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (n N → σ* S–X ) Interaction for Conformational Constraint

Journal Article · · Journal of Medicinal Chemistry
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  1. Medicinal Chemistry, ‡Molecular Structure and Characterization, §Pharmacokinetics and Drug Metabolism, ∥Metabolic Disorders Research, and ⊥Pathology, Amgen, One Amgen Center Drive, Thousand Oaks, California 91320-1799, United States
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Sponsoring Organization:
USDOE
Grant/Contract Number:
AC02-05CH11231
OSTI ID:
1227324
Journal Information:
Journal of Medicinal Chemistry, Journal Name: Journal of Medicinal Chemistry Vol. 58 Journal Issue: 24; ISSN 0022-2623
Publisher:
American Chemical SocietyCopyright Statement
Country of Publication:
United States
Language:
English
Citation Metrics:
Cited by: 25 works
Citation information provided by
Web of Science

References (32)

Effects of MK-0941, a Novel Glucokinase Activator, on Glycemic Control in Insulin-Treated Patients With Type 2 Diabetes journal October 2011
Mitigating Heterocycle Metabolism in Drug Discovery journal May 2012
Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 4. Exploration of a Novel Binding Pocket journal July 2014
Creating Structural Manifolds from a Common Precursor: Basicity Gradient-Driven Isomerization of Halopyridines journal December 2002
Glucokinase and molecular aspects of liver glycogen metabolism journal July 2008
Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 1. Discovery of a Novel Tool Compound for in Vivo Proof-of-Concept journal January 2014
The mechanism by which rat liver glucokinase is inhibited by the regulatory protein journal July 1990
Glucokinase Activators for Diabetes Therapy: May 2010 status report journal April 2011
Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis journal May 2015
A Survey of the Role of Noncovalent Sulfur Interactions in Drug Design journal March 2015
Potent s-cis -Locked Bithiazole Correctors of ΔF508 Cystic Fibrosis Transmembrane Conductance Regulator Cellular Processing for Cystic Fibrosis Therapy journal September 2008
Biophysical Characterization of the Interaction between Hepatic Glucokinase and Its Regulatory Protein journal November 2008
A patent review of glucokinase activators and disruptors of the glucokinase – glucokinase regulatory protein interaction: 2011 – 2014 journal May 2014
Novel Pharmacological Approaches to the Treatment of Type 2 Diabetes journal March 2012
The Economic Costs of Type 2 Diabetes: A Global Systematic Review journal March 2015
Chiral Azole Derivatives. 4. 1 Enantiomers of Bifonazole and Related Antifungal Agents:  Synthesis, Configuration Assignment, and Biological Evaluation journal July 2000
Discovery of Small-Molecule Glucokinase Regulatory Protein Modulators That Restore Glucokinase Activity journal April 2014
Applications of Fluorine in Medicinal Chemistry journal July 2015
Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 3. Structure–Activity Relationships within the Aryl Carbinol Region of the N -Arylsulfonamido- N ′-arylpiperazine Series journal March 2014
Natural bond Orbitals and Extensions of Localized Bonding Concepts journal January 2001
Synthesis and Applications of tert -Butanesulfinamide journal June 2010
Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors journal November 2013
Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 2. Leveraging Structure-Based Drug Design to Identify Analogues with Improved Pharmacokinetic Profiles journal January 2014
Utilization of a nitrogen–sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors journal October 2010
Small molecular glucokinase activators: has another new anti-diabetic therapeutic lost favour?: Small molecular glucokinase activators journal December 2012
Synthesis and Evaluation of Dual Wavelength Fluorescent Benzo[b]thiophene Boronic Acid Derivatives for Sugar Sensing journal October 2007
The determination of the absolute configurations of chiral molecules using vibrational circular dichroism (VCD) spectroscopy journal January 2008
Torsional Barriers and Equilibrium Angle of Biphenyl: Reconciling Theory with Experiment journal July 2008
GKAs for diabetes therapy: why no clinically useful drug after two decades of trying? journal February 2013
Pancreatic beta-cell glucokinase: closing the gap between theoretical concepts and experimental realities journal March 1998
Glucokinase as Glucose Sensor and Metabolic Signal Generator in Pancreatic  -Cells and Hepatocytes journal June 1990
Cost-of-Illness Studies in Diabetes Mellitus journal January 2004

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