What question did this study set out to answer?

To identify and optimize a novel class of allosteric glucokinase activators to improve glucose regulation in type 2 diabetes.

September 9, 2013Journal of Medicinal ChemistryOpen Access

Identification of a New Class of Glucokinase Activators through Structure-Based Design

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Authors

RHRonald J. HinklinPfizer (United States)SBSteven A. BoydVenatoRx Pharmaceuticals (United States)MCMark J. ChicarelliCogent (United Kingdom)

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Implication

Preclinical study demonstrates blood glucose reduction using novel glucokinase activators in rodent models of diabetes, highlighting a potential therapeutic strategy for type 2 diabetes.

Key Points

To identify and optimize a novel class of allosteric glucokinase activators to improve glucose regulation in type 2 diabetes.
Optimized a thiazolylamino pyridine-based hit into lead compound 26 using structure-based drug design.
Characterized in vitro potency and enzyme kinetic parameters of the synthesized glucokinase activators.
Evaluated in vivo glycemic efficacy via oral glucose tolerance tests in C57BL/6J mice and high-fat fed Zucker diabetic fatty rats.
Identified compound 26 as an early lead exhibiting a balanced profile of in vitro potency and enzyme kinetics.
Demonstrated marked blood glucose reductions during oral glucose tolerance testing in both C57BL/6J mice and high-fat fed Zucker diabetic fatty rats.

Cite This Study

Hinklin et al. (2013) studied this question.

synapsesocial.com/papers/6aa8ffb59f1973992770fabc https://doi.org/10.1021/jm401116k

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Implication

Preclinical study demonstrates blood glucose reduction using novel glucokinase activators in rodent models of diabetes, highlighting a potential therapeutic strategy for type 2 diabetes.

Identification of a New Class of Glucokinase Activators through Structure-Based Design

Discussion

Member takes

Implication

Key Points

Cite This Study

Identification of a New Class of Glucokinase Activators through Structure-Based Design

Discussion

Member takes

Implication

Key Points

Cite This Study

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