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

BRENDA support

Literature summary for 1.1.1.62 extracted from

  • Poirier, D.; Boivin, R.P.; Tremblay, M.R.; Berube, M.; Qiu, W.; Lin, S.X.
    Estradiol-adenosine hybrid compounds designed to inhibit type 1 17beta-hydroxysteroid dehydrogenase (2005), J. Med. Chem., 48, 8134-8147.
    View publication on PubMed
Search for more literature for 1.1.1.62

Inhibitors

Inhibitors Comment Organism Structure
5'-O-(10-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-decanoyl)adenosine IC50: 140 nM Homo sapiens
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-undecanoyl) adenosine IC50: 310 nM Homo sapiens
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-undecanoyl)adenosine IC50: 90 nM Homo sapiens
5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'beta-yl]-undecanoyl)adenosine IC50: 120 nM Homo sapiens
5'-O-(12-[3',17'beta-(dihydroxy)-1',3',5'(10')-estratrien-16'alpha-yl]-dodecanoyl)adenosine IC50: 1000 nM Homo sapiens
5'-O-(6-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-hexanoyl)adenosine IC50: 6900 nM Homo sapiens
5'-O-(7-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-heptanoyl)adenosine IC50: 430 nM Homo sapiens
5'-O-(8-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-octanoyl)adenosine IC50: 93 nM Homo sapiens
5'-O-(9-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-nonanoyl)adenosine IC50: 52 nM Homo sapiens
estrone IC50: 600-810 nM, depending on assay method Homo sapiens

Organism

Organism UniProt Comment Textmining
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.
estrone + NADH + H+
-
 Homo sapiens estradiol-17beta + NAD+
-
 ?

Synonyms

Synonyms Comment Organism
type 1 17beta-HSD
-
 Homo sapiens
type 1 17beta-hydroxysteroid dehydrogenase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000052
-
 IC50: 52 nM Homo sapiens 5'-O-(9-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-nonanoyl)adenosine
0.00009
-
 IC50: 90 nM Homo sapiens 5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-undecanoyl)adenosine
0.000093
-
 IC50: 93 nM Homo sapiens 5'-O-(8-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-octanoyl)adenosine
0.00012
-
 IC50: 120 nM Homo sapiens 5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'beta-yl]-undecanoyl)adenosine
0.00014
-
 IC50: 140 nM Homo sapiens 5'-O-(10-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-decanoyl)adenosine
0.00031
-
 IC50: 310 nM Homo sapiens 5'-O-(11-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-undecanoyl) adenosine
0.00043
-
 IC50: 430 nM Homo sapiens 5'-O-(7-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha-yl]-heptanoyl)adenosine
0.0006 0.00081 IC50: 600-810 nM, depending on assay method Homo sapiens estrone
0.001
-
 IC50: 1000 nM Homo sapiens 5'-O-(12-[3',17'beta-(dihydroxy)-1',3',5'(10')-estratrien-16'alpha-yl]-dodecanoyl)adenosine
0.0069
-
 IC50: 6900 nM Homo sapiens 5'-O-(6-[3',17'beta-dihydroxy-1',3',5'(10')-estratrien-16'alpha/beta-yl]-hexanoyl)adenosine