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

BRENDA support

Literature summary extracted from

  • Vispe, S.; Vandenberghe, I.; Robin, M.; Annereau, J.P.; Creancier, L.; Pique, V.; Galy, J.P.; Kruczynski, A.; Barret, J.M.; Bailly, C.
    Novel tetra-acridine derivatives as dual inhibitors of topoisomerase II and the human proteasome (2007), Biochem. Pharmacol., 73, 1863-1872.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.6.2.2 aclacinomycin A
-
 Homo sapiens
5.6.2.2 bis(acridin-4-ylmethyl)cyanamide comparison with inhibition of calpain, chymotrypsin, cathepsin B, trypsin Homo sapiens
5.6.2.2 Mitoxantrone
-
 Homo sapiens
5.6.2.2 N,N,N',N'-tetrakis(acridin-4-ylmethyl)butane-1,4-diamine compound shows in addition in vitro proteasome inhibition properties. Comparison with inhibition of calpain, chymotrypsin, cathepsin B, trypsin Homo sapiens
5.6.2.2 N,N,N',N'-tetrakis(acridin-4-ylmethyl)ethane-1,2-diamine comparison with inhibition of calpain, chymotrypsin, cathepsin B, trypsin Homo sapiens
5.6.2.2 N,N,N',N'-tetrakis[(7-bromo-9-chloroacridin-4-yl)methyl]butane-1,4-diamine comparison with inhibition of calpain, chymotrypsin, cathepsin B, trypsin Homo sapiens
5.6.2.2 N,N,N',N'-tetrakis[(9-aminoacridin-4-yl)methyl]ethane-1,2-diamine compound shows in addition in vitro proteasome inhibition properties. Comparison with inhibition of calpain, chymotrypsin, cathepsin B, trypsin Homo sapiens
5.6.2.2 N-(acridin-1-ylmethyl)-N,N',N'-tris(acridin-2-ylmethyl)octane-1,8-diamine comparison with inhibition of calpain, chymotrypsin, cathepsin B, trypsin Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
5.6.2.2 Homo sapiens
-
 recombinant enzyme
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.6.2.2 HL-60 cell sensitive to topoisomerase II inhibitors Homo sapiens
-
5.6.2.2 HL60/MX2 cell resitant to topoisomerase II inhibitors Homo sapiens
-

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.6.2.2 0.0002
-
 pH 8.0 Homo sapiens N,N,N',N'-tetrakis[(7-bromo-9-chloroacridin-4-yl)methyl]butane-1,4-diamine
5.6.2.2 0.0004
-
 pH 8.0 Homo sapiens N-(acridin-1-ylmethyl)-N,N',N'-tris(acridin-2-ylmethyl)octane-1,8-diamine
5.6.2.2 0.0009
-
 pH 8.0 Homo sapiens N,N,N',N'-tetrakis[(9-aminoacridin-4-yl)methyl]ethane-1,2-diamine
5.6.2.2 0.002
-
-
 Homo sapiens Mitoxantrone
5.6.2.2 0.002
-
-
 Homo sapiens aclacinomycin A
5.6.2.2 0.0043
-
 pH 8.0 Homo sapiens N,N,N',N'-tetrakis(acridin-4-ylmethyl)butane-1,4-diamine
5.6.2.2 0.0057
-
 pH 8.0 Homo sapiens N,N,N',N'-tetrakis(acridin-4-ylmethyl)ethane-1,2-diamine
5.6.2.2 0.0065
-
 pH 8.0 Homo sapiens bis(acridin-4-ylmethyl)cyanamide