Recent Updates on Glucokinase Activators and Glucokinase Regulatory Protein Disrupters for the Treatment of Type 2 Diabetes Mellitus

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INTRODUCTION: The impairment of glucose metabolism leads to hyperglycemia and type-2 diabetes mellitus. Glucokinase enzyme is the key regulator of glucose homeostasis that catalyzes the conversion of glucose to glucose-6-phosphate in liver and pancreatic cells. In hepatocytes, GK controls the glucose uptake and glycogen synthesis. The action of liver GK is controlled by Glucokinase Regulatory Protein (GKRP) partially. In fasting conditions the GKRP binds with GK and inactivate it from carbohydrate metabolism and serve as new target for treatment of diabetes mellitus. However, the GK activators as potential antidiabetic agents but results in increased risks of hypoglycemia.

CONCLUSION: The allosteric inhibitors of the GK-GKRP interaction are coming as alternative agents that can mitigate the risk associated with GK activators. This review discusses the recent advances and current status of potential molecules targeted to GK activators and GK-GKRP disrupters.

Medienart:

E-Artikel

Erscheinungsjahr:

2019

Erschienen:

2019

Enthalten in:

Zur Gesamtaufnahme - volume:15

Enthalten in:

Current diabetes reviews - 15(2019), 3 vom: 15., Seite 205-212

Sprache:

Englisch

Beteiligte Personen:

Kaushik, Aditi [VerfasserIn]
Kaushik, Manish [VerfasserIn]

Links:

Volltext

Themen:

Allosteric regulators
Blood Glucose
Carrier Proteins
Glucokinase
Glucokinase activators
Glucokinase regulatory protein
Glucose concentration.
Hypoglycemic Agents
Journal Article
Review
Type 2 diabetes mellitus

Anmerkungen:

Date Completed 09.08.2019

Date Revised 09.08.2019

published: Print

Citation Status MEDLINE

doi:

10.2174/1573399814666180724100749

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM286800845