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Literature summary for 1.14.14.1 extracted from

  • Wright, A.T.; Song, J.D.; Cravatt, B.F.
    A suite of activity-based probes for human cytochrome P450 enzymes (2009), J. Am. Chem. Soc., 131, 10692-10700.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
anastrozole increases labeling of P450 1A2 by probe 3 up to 175% of control values Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
recombinant cDNA P450s coexpressed with cytochrome P450 reductase in insect cell microsomes Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
17alpha-ethynylestradiol reactive intermediates of 17alpha-ethynylestradiol inactivate P450s in a NADPH-dependent mechanism-based manner by a combination of heme alkylation and apoprotein modification Homo sapiens
8-methoxypsoralen
-
Homo sapiens
anastrozole profiling inhibition of probe 1 labeling of P450 19A1, inhibits labeling of P450 2C9 by probe 5 Homo sapiens
formestane profiling inhibition of probe 1 labeling of P450 19A1, decreases probe 5 labeling of P450 2C19 and 1 labeling of P450 3A4 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information reacts with activity-based proteins of varying chemical composition, quite distinct from their natural substrates Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
aromatase
-
Homo sapiens
P450 19A1
-
Homo sapiens
P450 1A1
-
Homo sapiens
P450 1A2
-
Homo sapiens
P450 1B1
-
Homo sapiens
P450 2A6
-
Homo sapiens
P450 2B6
-
Homo sapiens
P450 2C19
-
Homo sapiens
P450 2C9
-
Homo sapiens
P450 2D6
-
Homo sapiens
P450 2E1
-
Homo sapiens
P450 2J2
-
Homo sapiens
P450 3A4
-
Homo sapiens
P450 4A11
-
Homo sapiens
P450 4F2
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00043
-
P450 19A1 Homo sapiens formestane
0.001
-
P450 19A1 Homo sapiens anastrozole

General Information

General Information Comment Organism
physiological function P450 1B1 is able to activate a broad spectrum of chemical carcinogens, including polycyclic hydrocarbons and heterocyclic and aromatic amines Homo sapiens