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Literature summary for 3.4.22.1 extracted from

  • Abu Ajaj, K.; Graeser, R.; Fichtner, I.; Kratz, F.
    In vitro and in vivo study of an albumin-binding prodrug of doxorubicin that is cleaved by cathepsin B (2009), Cancer Chemother. Pharmacol., 64, 413-418.
    View publication on PubMed

Application

Application Comment Organism
pharmacology the cathepsin B cleavable spacer Phe-Lys-4-aminobenzyloxycarbonyl, incorporated in an albumin-binding prodrug, is an effective way to increase the therapeutic index of doxorubicin Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1S,3S)-3,5,12-trihydroxy-3-(hydroxyacetyl)-10-methoxy-6,11-dioxo-1,2,3,4,6,11-hexahydrotetracen-1-yl 2,3,6-trideoxy-3-[([[4-([N-[6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanoyl]-L-phenylalanyl-L-lysyl]amino)benzyl]oxy]carbonyl)amino]-a-L-lyxo-hexopyranoside a Phe-Lys-para-aminobenzyloxycarbonyl-doxorubicin prodrug-albumin Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Phe-Lys-4-aminobenzyloxycarbonyl-doxorubicin prodrug-albumin + H2O Homo sapiens albumin-binding prodrug of doxorubicin, which incorporates a maleimide moiety and a 4-aminobenzyloxycarbonyl spacer coupled to the dipeptide Phe-Lys, is cleaved by cathepsin B and in tumor homogenates of MDA-MB 435 tumor cells from in vitro culture transplanted subcutaneously into the left flank region of mice, overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
carcinoma cell
-
Homo sapiens
-
MDA-MB-435 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Phe-Lys-4-aminobenzyloxycarbonyl-doxorubicin prodrug-albumin + H2O albumin-binding prodrug of doxorubicin, which incorporates a maleimide moiety and a 4-aminobenzyloxycarbonyl spacer coupled to the dipeptide Phe-Lys, is cleaved by cathepsin B and in tumor homogenates of MDA-MB 435 tumor cells from in vitro culture transplanted subcutaneously into the left flank region of mice, overview Homo sapiens ?
-
?
Phe-Lys-4-aminobenzyloxycarbonyl-doxorubicin prodrug-albumin + H2O albumin-binding prodrug of doxorubicin, which incorporates a maleimide moiety and a 4-aminobenzyloxycarbonyl spacer coupled to the dipeptide Phe-Lys, is cleaved by cathepsin B Homo sapiens ?
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5
-
assay at Homo sapiens