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Literature summary for 1.1.1.62 extracted from

  • Qiu, W.; Campbell, R.L.; Gangloff, A.; Dupuis, P.; Boivin, R.P.; Tremblay, M.R.; Poirier, D.; Lin, S.X.
    A concerted, rational design of type 1 17beta-hydroxysteroid dehydrogenase inhibitors: estradiol-adenosine hybrids with high affinity (2002), FASEB J., 16, 1829-1831.
    View publication on PubMed

Application

Application Comment Organism
medicine target for suppression of estrogen synthesis in breast cancer Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapor diffusion method Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
EM-1745 strong competitive inhibitor, inhibition reversible, 50% inhibition at 52 nM Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
estrone + NADPH + H+ Homo sapiens final step in the synthesis of active estrogens estradiol-17beta + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P14061 isotype 1, 17beta-HSD type 1
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
placenta
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5-androstene-3beta-ol-17-one + NADPH
-
Homo sapiens 5-androstene-3beta,17beta-diol + NADP+
-
?
estrone + NADPH + H+
-
Homo sapiens estradiol-17beta + NADP+
-
?
estrone + NADPH + H+ final step in the synthesis of active estrogens Homo sapiens estradiol-17beta + NADP+
-
?

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000003
-
EM-1745 pH 7.5, 37°C Homo sapiens