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

BRENDA support

Literature summary extracted from

  • Powis, G.; Wipf, P.; Lynch, S.M.; Birmingham, A.; Kirkpatrick, D.L.
    Molecular pharmacology and antitumor activity of palmarumycin-based inhibitors of thioredoxin reductase (2006), Mol. Cancer Ther., 5, 630-636.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
1.8.1.9 medicine development of novel anticancer agents Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.9 palmarumycin CP1 0.001 mM, the naphthoquinone spiroketal fungal metabolite palmarumycin CP1 is a potent inhibitor of thioredoxin reductase-1, IC50: 0.00035 mM Homo sapiens
1.8.1.9 PX-911 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, IC50: 0.0032 mM Homo sapiens
1.8.1.9 PX-916 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, potent inhibitor of purified human thioredoxin reductase-1, IC50: 0.00028 mM Homo sapiens
1.8.1.9 PX-960 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, IC50: 0.00027 mM Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.8.1.9 cytosol
-
Homo sapiens 5829
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.8.1.9 selenium 0.001 mM, 5fold increase of activity after 7 days Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.9 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.8.1.9 breast cancer cell
-
Homo sapiens
-
1.8.1.9 MCF-7 cell
-
Homo sapiens
-
1.8.1.9 rhabdomyosarcoma cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.8.1.9 5,5'-dithiobis(2-nitrobenzoic acid) + NADPH
-
Homo sapiens 2-nitro-5-thiobenzoate + NADP+
-
?

Synonyms

EC Number Synonyms Comment Organism
1.8.1.9 NADPH-dependent thioredoxin reductase-1
-
Homo sapiens
1.8.1.9 thioredoxin reductase
-
Homo sapiens
1.8.1.9 TrxR
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.8.1.9 0.00027
-
0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, IC50: 0.00027 mM Homo sapiens PX-960
1.8.1.9 0.00028
-
0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, potent inhibitor of purified human thioredoxin reductase-1, IC50: 0.00028 mM Homo sapiens PX-916
1.8.1.9 0.00035
-
0.001 mM, the naphthoquinone spiroketal fungal metabolite palmarumycin CP1 is a potent inhibitor of thioredoxin reductase-1, IC50: 0.00035 mM Homo sapiens palmarumycin CP1
1.8.1.9 0.0032
-
0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, IC50: 0.0032 mM Homo sapiens PX-911