Application | Comment | Organism |
---|---|---|
drug development | the enzyme is an important target for is a validated target for the development of type 2 diabetes treatments and the discovery of hypoglycaemic agents, both synthetic and natural | Oryctolagus cuniculus |
drug development | the enzyme is an important target for is a validated target for the development of type 2 diabetes treatments and the discovery of hypoglycaemic agents, both synthetic and natural | Rattus norvegicus |
Crystallization (Comment) | Organism |
---|---|
purified native muscle enzyme, soaking of crystals in a 5 mM inhibitor solution in 10 mM sodium N,N-bis(2-hydroxyethyl)-2-aminoethanesulfonate, pH 6.7, containing 0.1 mM EDTA, and 0.02% w/v sodium azide at room temperature for 2 h prior to data collection, X-ray diffraction structure determination and analysis at 1.85-2.15 A resolution | Oryctolagus cuniculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
additional information | structure-based inhibitor design targeting glycogen phosphorylase b, virtual screening, synthesis, biochemical and biological assessment of N-acyl-beta-D-glucopyranosylamines, overview. In silico screening of 1888 N-acyl-beta-D-glucopyranosylamines putative enzyme inhibitors differing only in their R groups. Docking study for ligand binding affinities of the active sites and selection of six compounds and analysis of the inhibitory potency both in vitro and ex vivo | Oryctolagus cuniculus | |
additional information | structure-based inhibitor design targeting glycogen phosphorylase b, virtual screening, synthesis, biochemical and biological assessment of N-acyl-beta-D-glucopyranosylamines, overview. Determination of the effects of the enzyme inhibitors on conversion of glycogen phosphorylase a to b | Rattus norvegicus | |
N-[(2E)-3-(5,6,7,8-tetrahydronaphthalen-2-yl)prop-2-enoyl]-beta-D-glucopyranosylamine | - |
Oryctolagus cuniculus | |
N-[(2E)-3-(naphthalen-2-yl)prop-2-enoyl]-beta-D-glucopyranosylamine | - |
Oryctolagus cuniculus | |
N-[(2E)-3-([1,1'-biphenyl]-4-yl)prop-2-enoyl]-beta-D-glucopyranosylamine | - |
Oryctolagus cuniculus | |
N-[(2E)-3-[4-(propan-2-yl)phenyl]prop-2-enoyl]-beta-D-glucopyranosylamine | - |
Oryctolagus cuniculus | |
N-[(2R)-2-methyl-3-[4-(propan-2-yl)phenyl]propanoyl]-beta-D-glucopyranosylamine | - |
Oryctolagus cuniculus | |
N-[(3S)-3-(4-ethylphenyl)butanoyl]-beta-D-glucopyranosylamine | - |
Oryctolagus cuniculus | |
N-[[([1,1'-biphenyl]-4-yl)oxy]acetyl]-beta-D-glucopyranosylamine | - |
Oryctolagus cuniculus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Oryctolagus cuniculus | P00489 | - |
- |
Rattus norvegicus | P09811 | - |
- |
Rattus norvegicus Wistar | P09811 | - |
- |
Purification (Comment) | Organism |
---|---|
native enzyme from skeletal muscle | Oryctolagus cuniculus |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
hepatocyte | - |
Rattus norvegicus | - |
skeletal muscle | - |
Oryctolagus cuniculus | - |
Synonyms | Comment | Organism |
---|---|---|
glycogen phosphorylase b | - |
Oryctolagus cuniculus |
glycogen phosphorylase b | - |
Rattus norvegicus |
GPb | - |
Oryctolagus cuniculus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0035 | - |
N-[(2E)-3-(naphthalen-2-yl)prop-2-enoyl]-beta-D-glucopyranosylamine | pH and temperature not specified in the publication | Oryctolagus cuniculus | |
0.00498 | - |
N-[(2E)-3-[4-(propan-2-yl)phenyl]prop-2-enoyl]-beta-D-glucopyranosylamine | pH and temperature not specified in the publication | Oryctolagus cuniculus | |
0.00514 | - |
N-[(2E)-3-([1,1'-biphenyl]-4-yl)prop-2-enoyl]-beta-D-glucopyranosylamine | pH and temperature not specified in the publication | Oryctolagus cuniculus | |
0.00825 | - |
N-[[([1,1'-biphenyl]-4-yl)oxy]acetyl]-beta-D-glucopyranosylamine | pH and temperature not specified in the publication | Oryctolagus cuniculus | |
0.04868 | - |
N-[(2E)-3-(5,6,7,8-tetrahydronaphthalen-2-yl)prop-2-enoyl]-beta-D-glucopyranosylamine | pH and temperature not specified in the publication | Oryctolagus cuniculus | |
0.07529 | - |
N-[(2R)-2-methyl-3-[4-(propan-2-yl)phenyl]propanoyl]-beta-D-glucopyranosylamine | pH and temperature not specified in the publication | Oryctolagus cuniculus | |
0.3769 | - |
N-[(3S)-3-(4-ethylphenyl)butanoyl]-beta-D-glucopyranosylamine | pH and temperature not specified in the publication | Oryctolagus cuniculus |
General Information | Comment | Organism |
---|---|---|
additional information | modeling of the glycogen phosphorylase b GPb receptor structure using the 2.15 A resolution GPb-N-4-phenylbenzoyl-2-N'-beta-D-glycopyrglycopyranosyl urea crystal complex, PDB ID 2QLN | Oryctolagus cuniculus |