Information on EC 2.4.1.1 - glycogen phosphorylase and Organism(s) Homo sapiens

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Homo sapiens


The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea


The taxonomic range for the selected organisms is: Homo sapiens

EC NUMBER
COMMENTARY hide
2.4.1.1
-
RECOMMENDED NAME
GeneOntology No.
glycogen phosphorylase
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hexosyl group transfer
-
-
-
-
PATHWAY
BRENDA Link
KEGG Link
MetaCyc Link
glycogen degradation II
-
-
starch degradation III
-
-
glycogen degradation I
-
-
starch degradation V
-
-
sucrose biosynthesis II
-
-
glycogen metabolism
-
-
Starch and sucrose metabolism
-
-
Metabolic pathways
-
-
Biosynthesis of secondary metabolites
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-
SYSTEMATIC NAME
IUBMB Comments
(1->4)-alpha-D-glucan:phosphate alpha-D-glucosyltransferase
This entry covers several enzymes from different sources that act in vivo on different forms of (1->4)-alpha-D-glucans. Some of these enzymes catalyse the first step in the degradation of large branched glycan polymers - the phosphorolytic cleavage of alpha-1,4-glucosidic bonds from the non-reducing ends of linear poly(1->4)-alpha-D-glucosyl chains within the polymers. The enzyme stops when it reaches the fourth residue away from an alpha-1,6 branching point, leaving a highly branched core known as a limit dextrin. The accepted name of the enzyme should be modified for each specific instance by substituting "glycogen" with the name of the natural substrate, e.g. maltodextrin phosphorylase, starch phosphorylase, etc.
CAS REGISTRY NUMBER
COMMENTARY hide
9035-74-9
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
-
glycogen degradation and synthesis during the diurnal cycle are mediated by changes in the activities of phosphorylase and glycogen synthase. Phosphorylase is regulated by phosphorylation of Ser14. Only the phosphorylated form of liver phosphorylase (GPa) is catalytically active. Interconversion between GPa and GPb (unphosphorylated) is dependent on the activities of phosphorylase kinase and of phosphorylase phosphatase. The latter comprises protein phosphatase-1 in conjunction with a glycogen-targeting protein (G-subunit) of the PPP1R3 family. Both GPa and phosphorylated glycogen synthase serve as substrates for the catalytic subunit of protein phosphatase-1 in association with G-subunits
physiological function
additional information
-
despite a high degree of conservation of residues between liver and muscle isoforms in the ligand binding residues at the catalytic and allosteric sites, the kinetic properties of liver phosphorylase differ from the muscle isoform
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
glycogen + phosphate
glycogen + alpha-D-glucose 1-phosphate
show the reaction diagram
-
-
-
-
r
[(1->4)-alpha-D-glucosyl]n + phosphate
[(1->4)-alpha-D-glucosyl]n-1 + alpha-D-glucose 1-phosphate
show the reaction diagram
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
[(1->4)-alpha-D-glucosyl]n + phosphate
[(1->4)-alpha-D-glucosyl]n-1 + alpha-D-glucose 1-phosphate
show the reaction diagram
-
the liver enzyme catalyzes the forward reaction
-
-
r
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
-
(2-[[(2-chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
-
(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
-
(2-[[(5-chloro-1H-pyrrolo[2,3-c]pyridin-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
-
(2-[[(5-chloro-6-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
-
(2-[[(5-chloro-7-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
-
(2-[[(5-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
-
-
(2E,2'E)-N,N'-(oxydiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
-
-
(2E,2'E)-N,N'-(thiodiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
-
-
(2E,2'E)-N,N'-butane-1,4-diylbis[3-(3,4-dichlorophenyl)-acrylamide]
-
-
(2E,2'E)-N,N'-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide]
-
crystallization data
(2R)-2-cyclohexyl-2-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]propanoic acid
-
potent in vitro inhibition, reduced inhibition of CYP2C9 and good pharmacokinetic properties
(2S)-2-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]heptanoic acid
-
-
(2S)-cyclohexyl[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]ethanoic acid
-
-
(2S)-cyclopentyl[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]ethanoic acid
-
-
1-(2-carboxyphenyl)-6-[(2-chloro-4,6-difluorophenyl)amino]-4-oxo-1,2,3,4-tetrahydroquinoline-3-carboxylic acid
-
i.e. AVE9423. Inhibitor fully exploits the volume of the binding pocket and show pronounced binding entropy
1-[(2S)-2-([(5-chloro-1H-indol-2-yl)carbonyl]amino)-3-phenylpropanoyl]azetidine-3-carboxylic acid
-
i.e. CP-403700, 50% inhibition at 0.1 microM in presence of 1 mM phosphate. In presence of 1 mM phosphate plus 8 mM glucose, 50% inhibition at 0.05 microM. Presence of endogenous inhibitors such as D-glucose, ADP, ATP, D-fructose 1-phosphate, D-glucose 6-phosphate, UDP-glucose markedly reduces the inhibitory effect
1-[2-([[(2-chloro-4,5-difluorophenyl)carbonyl]carbamoyl]amino)-4-fluorophenyl]piperidine-4-carboxylic acid
-
i.e. AVE2865. Inhibitor fully exploits the volume of the binding pocket and show pronounced binding entropy
1-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]cyclodecanecarboxylic acid
-
-
1-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]cyclooctanecarboxylic acid
-
potent in vitro inhibition, reduced inhibition of CYP2C9 and good pharmacokinetic properties
2,3-dichloro-N-(1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.002 microM
2,3-dichloro-N-(1-[3-hydroxy-2-(hydroxymethyl)propyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.038 microM
2,3-dichloro-N-[1-(2-hydroxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.007 microM
2-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)-4-methoxybutanoic acid
-
-
2-amino-3,4-dihydroxy-5-methoxybenzoic acid
-
-
2-chloro-N-((3R)-1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.040 microM
2-chloro-N-((3R)-1-[(2S)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.021 microM
2-chloro-N-((3S)-1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.027 microM
2-chloro-N-((3S)-1-[(2S)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.012 microM
2-chloro-N-(1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.029 microM
2-chloro-N-(1-[2-(methylsulfinyl)ethyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.048 microM
2-chloro-N-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.041 microM
2-chloro-N-[1-(2-hydroxybutyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.044 microM
2-chloro-N-[1-(2-hydroxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.026 microM
2-chloro-N-[1-(2-methoxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.05 microM
2-chloro-N-[1-(3-hydroxypropyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.021 microM
2-chloro-N-[1-(cyanomethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.028 microM
3-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)propanoic acid
-
-
3-methoxypterolactone
-
-
3-[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)amino]-3-oxopropanoic acid
-
-
3-[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)oxy]propanoic acid
-
-
4-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)butanoic acid
-
-
4-([[(2-chloro-4,5-difluorophenyl)carbonyl]carbamoyl]amino)-3-(trifluoromethoxy)benzoic acid
-
i.e. AVE5688, binding to enzyme is exclusively enthalpic
4-hydroxy-3-methoxybenzoic acid
-
-
4-[[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)methyl]sulfonyl]butanoic acid
-
-
5-chloro-N-(1,3,6,6-tetrafluoro-(R)-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
docking study. Hydrophobic residues, such as Phe53, Pro188, and Gly186, around the two aliphatic fluorine atoms suggest that the lipophilic contact among them is an important driver of activity increases. Hydrophobic residues Leu39 and Lys191 are close to one of the aromatic fluorine atoms
5-chloro-N-(1,6,6-trifluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
-
5-chloro-N-(1-hydroxy-2,3-dihydro-1H-inden-5-yl)-1H-indole-2-carboxamide
-
-
5-chloro-N-(1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-1H-indole-2-carboxamide
-
50% inhibition at 0.044 microM
5-chloro-N-(3,6,6-trifluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
-
5-chloro-N-(5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
-
5-chloro-N-(6,6-difluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
-
-
5-chloro-N-[1-(2-hydroxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1H-indole-2-carboxamide
-
50% inhibition at 0.017 microM
5-chloro-N-[2-chloro-4-(1,2-dihydroxyethyl)-phenyl]-1H-indole-2-carboxamide
-
-
5-chloro-N-[4-(1,2-dihydroxyethyl)-3-(trifluoromethyl)phenyl]-1H-indole-2-carboxamide
-
-
5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide
-
crystallization data
5-chloro-N-[4-(2-hydroxyethyl)phenyl]-1H-indole-2-carboxamide
-
-
5-chloro-N-[5-(1,2-dihydroxyethyl)pyrazin-2-yl]-1H-indole-2-carboxamide
-
-
5-chloro-N-[5-(1,2-dihydroxyethyl)pyridin-2-yl]-1H-indole-2-carboxamide
-
-
alpha-boswellic acid
-
-
beta-amyrin
-
-
beta-amyrone
-
-
beta-boswellic acid
-
-
beta-O-trans-caffeoyl-morolic acid
-
-
Caffeine
CP-316819
-
indole-site inhibitor, presence of endogenous inhibitors such as D-glucose, ADP, ATP, D-fructose 1-phosphate, D-glucose 6-phosphate, UDP-glucose markedly reduces the inhibitory effect
CP-320626
CP-380867
-
indole-site inhibitor, presence of endogenous inhibitors such as D-glucose, ADP, ATP, D-fructose 1-phosphate, D-glucose 6-phosphate, UDP-glucose markedly reduces the inhibitory effect
-
D-Fructose 1-phosphate
-
-
D-glucose
D-glucose 6-phosphate
-
-
DTNB
-
-
gallic acid
-
-
glucose 6-phosphate
-
inhibits the phosphorylated and unphosphorylated enzyme forms. Binding of glucose 6-phosphate to the muscle isozyme is competitive with binding of AMP, but it also stabilizes a conformation that is more tense than the native T-state enzyme. Inhibition of muscle GPa enzyme activity by G6P is additive with inhibition by glucose
methyl [3-([(2-chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino)-2-oxo-3,4-dihydroquinolin-1(2H)-yl]acetate
-
50% inhibition at 0.084 microM
N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-norleucine
-
potent in vitro inhibition, low potential for P450 inhibition, and good pharmacokinetic properties
N-[1-(2-amino-2-oxoethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-2-methyl-6H-thieno[2,3-b]pyrrole-5-carboxamide
-
50% inhibition at 0.135 microM
O-(1-methylcyclopentyl)-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-allothreonine
-
-
O-tert-butyl-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-allothreonine
-
potent in vitro inhibition, low potential for P450 inhibition, and good pharmacokinetic properties
O-tert-butyl-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-serine
-
potent in vitro inhibition, low potential for P450 inhibition, and good pharmacokinetic properties
oleanolic acid
-
-
pterolactone
-
-
riboflavin
-
inhibition of the liver enzyme, counteracted by AMP
UDP-glucose
-
-
uric acid
-
inhibition of the liver enzyme, counteracted by AMP
[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)oxy]acetic acid
-
-
[[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)methyl]sulfanyl]acetic acid
-
-
additional information
-
the more active phosphorylated form of the enzyme, glycogen phosphorylase a, is a homodimer having an inhibitory allosteric binding site at the dimer interface for which synthetic ligands
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
ATP
-
stimulation via P2Y receptor signaling, primarily through P2Y2 receptors
dithiothreitol
-
required to maintain activity
Insulin
-
Insulin promotes conversion of GPa to GPb via protein kinase B activation
-
UTP
-
stimulation via P2Y receptor signaling, primarily through P2Y2 receptors
additional information
-
the muscle isoform of phosphorylase is activated by phosphorylation (GPb to GPa conversion)
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
additional information
-
comparison of muscle phosphorylases of various animals; kinetic data
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000018 - 0.0015
(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
0.00004 - 0.0012
(2-[[(2-chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
0.000057
(2-[[(5-chloro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00026
(2-[[(5-chloro-1H-pyrrolo[2,3-c]pyridin-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000076
(2-[[(5-chloro-6-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000052
(2-[[(5-chloro-7-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00016
(2-[[(5-fluoro-1H-indol-2-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000026 - 0.00043
(2E,2'E)-N,N'-(oxydiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
0.000012 - 0.00045
(2E,2'E)-N,N'-(thiodiethane-2,1-diyl)bis[3-(3,4-dichlorophenyl)acrylamide]
0.000043 - 0.00042
(2E,2'E)-N,N'-butane-1,4-diylbis[3-(3,4-dichlorophenyl)-acrylamide]
0.000023 - 0.00026
(2E,2'E)-N,N'-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide]
0.00001
(2R)-2-cyclohexyl-2-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]propanoic acid
Homo sapiens
-
-
0.000009
(2S)-2-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]heptanoic acid
Homo sapiens
-
-
0.000006
(2S)-cyclohexyl[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]ethanoic acid
Homo sapiens
-
-
0.000014
(2S)-cyclopentyl[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]ethanoic acid
Homo sapiens
-
-
0.000014
1-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]cyclodecanecarboxylic acid
Homo sapiens
-
-
0.000005
1-[[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]amino]cyclooctanecarboxylic acid
Homo sapiens
-
-
0.000017 - 0.00017
2-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)-4-methoxybutanoic acid
0.0077
2-amino-3,4-dihydroxy-5-methoxybenzoic acid
Homo sapiens
-
-
0.000056
3-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)propanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.26
3-methoxypterolactone
Homo sapiens
-
-
0.000056
3-[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)amino]-3-oxopropanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000059
3-[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)oxy]propanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000054
4-(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.091
4-hydroxy-3-methoxybenzoic acid
Homo sapiens
-
-
0.000042
4-[[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)methyl]sulfonyl]butanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
5-chloro-N-(1,3,6,6-tetrafluoro-(R)-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
Homo sapiens
-
-
0.000048
5-chloro-N-(1,6,6-trifluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
Homo sapiens
-
-
0.00044
5-chloro-N-(1-hydroxy-2,3-dihydro-1H-inden-5-yl)-1H-indole-2-carboxamide
Homo sapiens
-
-
0.000063
5-chloro-N-(3,6,6-trifluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
Homo sapiens
-
-
0.00032
5-chloro-N-(5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
Homo sapiens
-
-
0.000068
5-chloro-N-(6,6-difluoro-5-hydroxy-5,6,7,8-tetrahydronaphthalen-2-yl)-1H-indole-2-carboxamide
Homo sapiens
-
-
0.00042
5-chloro-N-[2-chloro-4-(1,2-dihydroxyethyl)-phenyl]-1H-indole-2-carboxamide
Homo sapiens
-
pH 6.8, 22C
0.00034
5-chloro-N-[4-(1,2-dihydroxyethyl)-3-(trifluoromethyl)phenyl]-1H-indole-2-carboxamide
Homo sapiens
-
pH 6.8, 22C
0.0009
5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide
Homo sapiens
-
pH 6.8, 22C
0.0012
5-chloro-N-[4-(2-hydroxyethyl)phenyl]-1H-indole-2-carboxamide
Homo sapiens
-
pH 6.8, 22C
0.00044
5-chloro-N-[5-(1,2-dihydroxyethyl)pyrazin-2-yl]-1H-indole-2-carboxamide
Homo sapiens
-
pH 6.8, 22C
0.00025
5-chloro-N-[5-(1,2-dihydroxyethyl)pyridin-2-yl]-1H-indole-2-carboxamide
Homo sapiens
-
pH 6.8, 22C
0.037
alpha-boswellic acid
Homo sapiens
-
-
0.047
beta-amyrin
Homo sapiens
-
-
0.06
beta-amyrone
Homo sapiens
-
-
0.026
beta-boswellic acid
Homo sapiens
-
-
0.044
beta-O-trans-caffeoyl-morolic acid
Homo sapiens
-
-
0.0066
Caffeine
Homo sapiens
-
-
0.00092
CP-320626
Homo sapiens
-
pH 6.8, 22C
0.0068
gallic acid
Homo sapiens
-
-
0.000023
N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-norleucine
Homo sapiens
-
-
0.000006
O-(1-methylcyclopentyl)-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-allothreonine
Homo sapiens
-
-
0.000007
O-tert-butyl-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-allothreonine
Homo sapiens
-
-
0.000044
O-tert-butyl-N-[(3-[[(2,4,6-trimethylphenyl)carbamoyl]amino]naphthalen-2-yl)carbonyl]-L-serine
Homo sapiens
-
-
0.008
oleanolic acid
Homo sapiens
-
-
0.232
pterolactone
Homo sapiens
-
-
0.00003
[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)oxy]acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.00004
[[(2-[[(2,3-dichloro-4H-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino]-2,3-dihydro-1H-inden-1-yl)methyl]sulfanyl]acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
isoforms phosphorylase a and b
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
175000
-
phosphorylase b, sucrose density gradient centrifugation
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
homodimer
-
the more active phosphorylated form, glycogen phosphorylase a, of the enzyme is a homodimer having an inhibitory allosteric binding site at the dimer interface for which synthetic ligands
additional information
-
phosphorylase a dissociates into active dimers in the presence of high salt concentration, glucose or glycogen, human enzyme at 5 mg/ml protein concentration, the rabbit enzyme remains a tetramer even at 1 mg/ml
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
-
the muscle isoform of phosphorylase is activated by phosphorylation (GPb to GPa conversion)
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
crystallization and structure determination of liver and muscle enzymes
-
dialysis against 50 mM Tris and 40 mM 2-mercaptoethanol, pH 6.8 at 0°C
-
hanging drop method, crystal structure of liver phosphorylase bound to a glycogen targeting subunit-derived peptide. C-terminus of glycogen targeting subunit of protein phosphatase 1 binds in a hydrophobically collapsed conformation to the allosteric regulator-binding site at the phosphorylase dimer interface
-
in complex with inhibitor (2E,2'E)-N,N'-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide]. Inhibitor is bound at the dimer interface site, the 3,4-dichlorophenyl moiety interacts hydroühobically with the enzyme
-
in complex with inhibitors 4-([[(2-chloro-4,5-difluorophenyl)carbonyl]carbamoyl]amino)-3-(trifluoromethoxy)benzoic acid, 1-[2-([[(2-chloro-4,5-difluorophenyl)carbonyl]carbamoyl]amino)-4-fluorophenyl]piperidine-4-carboxylic acid, and 1-(2-carboxyphenyl)-6-[(2-chloro-4,6-difluorophenyl)amino]-4-oxo-1,2,3,4-tetrahydroquinoline-3-carboxylic acid. Binding to inhibitor 4-([[(2-chloro-4,5-difluorophenyl)carbonyl]carbamoyl]amino)-3-(trifluoromethoxy)benzoic acid is exclusively enthalpic. The inhibitors 1-[2-([[(2-chloro-4,5-difluorophenyl)carbonyl]carbamoyl]amino)-4-fluorophenyl]piperidine-4-carboxylic acid, and 1-(2-carboxyphenyl)-6-[(2-chloro-4,6-difluorophenyl)amino]-4-oxo-1,2,3,4-tetrahydroquinoline-3-carboxylic acid fully exploit the volume of the binding pocket and show pronounced binding entropy
-
in complexwith inhibitor 5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide, inhibitor binds to a solvent cavity at the dimer interface, with the two hydroxyl groups making favorable electrostatic interactions with the enzyme
-
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
45
-
crystalline, several h stable
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
dithiothreitol stabilizes
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
storage in frozen or lyophilized state, crystalline human, not rabbit, phosphorylase a or b, stable to
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
-
the enzyme is a target for inhibitor design in development of drugs for treatment of type 2 diabetes
medicine