Document Detail


Novel therapeutics based on inhibiting the interaction of glycogen phosphorylase and GL-subunit of glycogen-associated protein phosphatase 1: WO2009127723.
MedLine Citation:
PMID:  20367521     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Diabetes mellitus is a major challenge for healthcare systems worldwide because it is strongly associated with several major health risk factors. Currently marketed drugs are insufficient to achieve long-term control of blood glucose levels and induce considerable side effects. The development of more effective drugs for metabolic diseases is still of urgent interest. Recently, inhibiting the interaction of hepatic glycogen-targeting subunit (G(L)) of protein phosphatase 1 and glycogen phosphorylase a (GPa) is emerging as a novel mechanism to combat diabetic hyperglycemia by dephosphorylation and activation of glycogen synthase, converting high blood glucose to liver glycogen. Patent WO2009127723 describes a variety of arylsulfonylaminomethylphosphonic acids as small molecule inhibitors of G(L)-GPa interaction and their potential use as pharmaceutical compositions to treat type 1 and type 2 diabetes mellitus. Although lacking detailed in vivo biological data, WO2009127723 represents the first evidence for the novel rationale in antidiabetic pursuit, meriting the attention of the antidiabetic community.
Authors:
Lei Zhang; Hong Liu
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  20     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2010 Jul 
Date Detail:
Created Date:  2010-06-17     Completed Date:  2010-09-22     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  969-73     Citation Subset:  IM    
Affiliation:
Drug Discovery and Design Centre, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
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MeSH Terms
Descriptor/Qualifier:
Diabetes Mellitus, Type 1 / drug therapy,  enzymology
Diabetes Mellitus, Type 2 / drug therapy,  enzymology
Drug Delivery Systems
Drug Design
Glycogen Phosphorylase / metabolism*
Humans
Hypoglycemic Agents / pharmacology*
Patents as Topic
Protein Phosphatase 1 / metabolism*
Chemical
Reg. No./Substance:
0/Hypoglycemic Agents; EC 2.4.1.-/Glycogen Phosphorylase; EC 3.1.3.16/Protein Phosphatase 1

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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