Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.1.1.205 extracted from

  • Mitsuhashi, S.; Takenaka, J.; Iwamori, K.; Nakajima, N.; Ubukata, M.
    Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase and differentiation induction of K562 cells among the mycophenolic acid derivatives (2010), Bioorg. Med. Chem., 18, 8106-8111.
    View publication on PubMed
Search for more literature for 1.1.1.205

Cloned(Commentary)

Cloned (Comment) Organism
expression in Eshcerichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4E)-6-(4,6-dihydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid derivative of mycophenolic acid. IC50 value for K562 cells proliferation 8.2 microM; derivative of mycophenolic acid. IC50 value for K562 cells proliferation 8.2 microM Homo sapiens
(4E)-6-[4-(acetyloxy)-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl]-4-methylhex-4-enoic acid derivative of mycophenolic acid. IC50 value for K562 cells proliferation 0.59 microM; derivative of mycophenolic acid. IC50 value for K562 cells proliferation 0.59 microM Homo sapiens
(4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide derivative of mycophenolic acid. IC50 value for K562 cells proliferation 2.1 microM; derivative of mycophenolic acid. IC50 value for K562 cells proliferation 2.1 microM Homo sapiens
methyl (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoate derivative of mycophenolic acid. IC50 value for K562 cells proliferation 0.73 microM; derivative of mycophenolic acid. IC50 value for K562 cells proliferation 0.73 microM Homo sapiens
additional information synthesis of mycophenolic acid derivatives as inhibitors. Functional groups at C5, C7, and C6' positions in mycophenolic acid are important for inhibitory activity against IMPDH. It is difficult to improve specificity against IMPDH II by modification of 5-, 7-, and 6'-group. Demethylation of 5-OMe results in increasing hydrophilicity, and lowering cell permeability. Ester bonds of protective groups at C7 and C6' positions are hydrolyzed to give mycophenolic acid in cultures, the effects of a tubulin-specific histone deacetylase inhibitor on proliferation and differentiation are weaker than its inhibitory activity against IMPDH; synthesis of mycophenolic acid derivatives as inhibitors. Functional groups at C5, C7, and C6' positions in mycophenolic acid are important for inhibitory activity against IMPDH. It is difficult to improve specificity against IMPDH II by modification of 5-, 7-, and 6'-group. Demethylation of 5-OMe results in increasing hydrophilicity, and lowering cell permeability. Ester bonds of protective groups at C7 and C6' positions are hydrolyzed to give mycophenolic acid in cultures, the effects of a tubulin-specific histone deacetylase inhibitor on proliferation and differentiation are weaker than its inhibitory activity against IMPDH Homo sapiens
Mycophenolic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P12268 IMPDH 2
-
Homo sapiens P20839 IMPDH 1
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000012
-
 pH 7.4, 37°C Homo sapiens Mycophenolic acid
0.000019
-
 pH 7.4, 37°C Homo sapiens Mycophenolic acid
0.00015
-
 pH 7.4, 37°C Homo sapiens (4E)-6-(4,6-dihydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid
0.00017
-
 pH 7.4, 37°C Homo sapiens (4E)-6-(4,6-dihydroxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoic acid
0.00035
-
 pH 7.4, 37°C Homo sapiens (4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.00042
-
 pH 7.4, 37°C Homo sapiens (4E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.0014
-
 pH 7.4, 37°C Homo sapiens methyl (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoate
0.0015
-
 pH 7.4, 37°C Homo sapiens methyl (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enoate
0.0041
-
 pH 7.4, 37°C Homo sapiens (4E)-6-[4-(acetyloxy)-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl]-4-methylhex-4-enoic acid