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Literature summary for 2.4.1.1 extracted from

  • Watson, K.A.; Chrysina, E.D.; Tsitsanou, K.E.; Zographos, S.E.; Archontis, G.; Fleet, G.W.; Oikonomakos, N.G.
    Kinetic and crystallographic studies of glucopyranose spirohydantoin and glucopyranosylamine analogs inhibitors of glycogen phosphorylase (2005), Proteins, 61, 966-983.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors (2R,3R,4S,5R,6R)-3,4,5-trihydroxy-2-hydroxymethyl-7,9-diaza-1-oxa-spiro[4,5]decane-8,10-dione, (2R,3R,4S,5R,6R)-3,4,5,9-tetrahydroxy-2-hydroxymethyl-7,9-diaza-1-oxa-spiro[4,5]decane-8,10-dione, 1-deoxy-1-methoxycarbonylamino-beta-D-glucopyranose. Inhibitors bind at the active site of the enzyme and induce minor movements of the side chains of D283 and N284 that block access of the substrate glycogen to the catalytic site Oryctolagus cuniculus

Inhibitors

Inhibitors Comment Organism Structure
(2R,3R,4S,5R,6R)-3,4,5,9-tetrahydroxy-2-hydroxymethyl-7,9-diaza-1-oxa-spiro[4,5]decane-8,10-dione
-
Oryctolagus cuniculus
(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-2-hydroxymethyl-7,9-diaza-1-oxa-spiro[4,5]decane-8,10-dione
-
Oryctolagus cuniculus
1-deoxy-1-methoxycarbonylamino-beta-D-glucopyranose
-
Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus P00489
-
-

Source Tissue

Source Tissue Comment Organism Textmining
muscle
-
Oryctolagus cuniculus
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0031
-
(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-2-hydroxymethyl-7,9-diaza-1-oxa-spiro[4,5]decane-8,10-dione pH 6.8, 30°C Oryctolagus cuniculus
0.0393
-
(2R,3R,4S,5R,6R)-3,4,5,9-tetrahydroxy-2-hydroxymethyl-7,9-diaza-1-oxa-spiro[4,5]decane-8,10-dione
-
Oryctolagus cuniculus
0.086
-
1-deoxy-1-methoxycarbonylamino-beta-D-glucopyranose
-
Oryctolagus cuniculus