A new class of glycogen phosphorylase inhibitors

A new class of diacid analogues that binds at the AMP site not only are very potent but have ∼10-fold selectivity in liver versus muscle glycogen phosphorylase (GP) in the in vitro assay. The synthesis, structure, and in vitro and in vivo biological evaluation of these liver selective glycogen phosp...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (22), p.4125-4128
Main Authors: Lu, Zhijian, Bohn, Joann, Bergeron, Raynald, Deng, Qiaolin, Ellsworth, Kenneth P., Geissler, Wayne M., Harris, Georgianna, McCann, Peggy E., McKeever, Brian, Myers, Robert W., Saperstein, Richard, Willoughby, Christopher A., Yao, Jun, Chapman, Kevin
Format: Article
Language:English
Subjects:
Adenosine Triphosphate - metabolism
Amino Acid Sequence
Animals
Binding Sites
Biological and medical sciences
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - pharmacology
General and cellular metabolism. Vitamins
Glycogen Phosphorylase - antagonists & inhibitors
Glycogen Phosphorylase - chemistry
Kinetics
Liver - enzymology
Medical sciences
Mice
Models, Molecular
Molecular Conformation
Naphthols - chemical synthesis
Naphthols - pharmacology
Pharmacology. Drug treatments
Protein Conformation
Rats
Structure-Activity Relationship
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Summary:A new class of diacid analogues that binds at the AMP site not only are very potent but have ∼10-fold selectivity in liver versus muscle glycogen phosphorylase (GP) in the in vitro assay. The synthesis, structure, and in vitro and in vivo biological evaluation of these liver selective glycogen phosphorylase inhibitors are discussed. A new class of diacid analogues that binds at the AMP site not only are very potent but have ∼10-fold selectivity liver versus muscle glycogen phosphorylase (GP) in the in vitro assay. The synthesis, structure, and in vitro and in vivo biological evaluation of these liver selective glycogen phosphorylase inhibitors are discussed.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.08.046