Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors

Nature ◽  
2013 ◽  
Vol 504 (7480) ◽  
pp. 437-440 ◽  
Author(s):  
David J. Lloyd ◽  
David J. St Jean ◽  
Robert J. M. Kurzeja ◽  
Robert C. Wahl ◽  
Klaus Michelsen ◽  
...  
Keyword(s):  
Small Molecule ◽  
Regulatory Protein ◽  
Glucokinase Regulatory Protein ◽  
Antidiabetic Effects

Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 4. Exploration of a Novel Binding Pocket

2014 ◽  
Vol 57 (14) ◽  
pp. 5949-5964 ◽  
Author(s):  
Fang-Tsao Hong ◽  
Mark H. Norman ◽  
Kate S. Ashton ◽  
Michael D. Bartberger ◽  
Jie Chen ◽  
...  
Keyword(s):  
Small Molecule ◽  
Protein Interaction ◽  
Regulatory Protein ◽  
Binding Pocket ◽  
Glucokinase Regulatory Protein

Glucokinase regulatory protein may interact with glucokinase in the hepatocyte nucleus

Diabetes ◽  
1997 ◽  
Vol 46 (2) ◽  
pp. 179-186 ◽  
Author(s):  
K. S. Brown ◽  
S. S. Kalinowski ◽  
J. R. Megill ◽  
S. K. Durham ◽  
K. A. Mookhtiar
Keyword(s):  
Regulatory Protein ◽  
Glucokinase Regulatory Protein ◽  
Hepatocyte Nucleus

Anomeric Specificity of Human Liver and B-cell Glucokinase: Modulation by the Glucokinase Regulatory Protein

2000 ◽  
Vol 373 (1) ◽  
pp. 126-134 ◽  
Author(s):  
Philippe Courtois ◽  
Frédéric Bource ◽  
Abdullah Sener ◽  
Willy J. Malaisse
Keyword(s):  
B Cell ◽  
Human Liver ◽  
Regulatory Protein ◽  
Glucokinase Regulatory Protein ◽  
Anomeric Specificity

scholarly journals BRD4 inhibition for the treatment of pathological organ fibrosis

F1000Research ◽  
2017 ◽  
Vol 6 ◽  
pp. 1015 ◽  
Author(s):  
Matthew S. Stratton ◽  
Saptarsi M. Haldar ◽  
Timothy A. McKinsey
Keyword(s):  
Extracellular Matrix ◽  
Pulmonary Fibrosis ◽  
Small Molecule ◽  
Regulatory Protein ◽  
Medical Need ◽  
Fibrotic Diseases ◽  
Brd4 Inhibition ◽  
Developed World ◽  
Organ Fibrosis

Fibrosis is defined as excess deposition of extracellular matrix, resulting in tissue scarring and organ dysfunction. It is estimated that 45% of deaths in the developed world are due to fibrosis-induced organ failure. Despite the well-accepted role of fibrosis in the pathogenesis of numerous diseases, there are only two US Food and Drug Administration–approved anti-fibrotic therapies, both of which are currently restricted to the treatment of pulmonary fibrosis. Thus, organ fibrosis represents a massive unmet medical need. Here, we review recent findings suggesting that an epigenetic regulatory protein, BRD4, is a nodal effector of organ fibrosis, and we highlight the potential of small-molecule BRD4 inhibitors for the treatment of diverse fibrotic diseases.

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