Proteins > 17-beta-hydroxysteroid dehydrogenase type 1
Page last updated: 2024-08-07 13:00:07
17-beta-hydroxysteroid dehydrogenase type 1
A 17-beta-hydroxysteroid dehydrogenase type 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P14061]
Synonyms
17-beta-HSD 1;
EC 1.1.1.51;
20 alpha-hydroxysteroid dehydrogenase;
20-alpha-HSD;
E2DH;
Estradiol 17-beta-dehydrogenase 1;
1.1.1.62;
Placental 17-beta-hydroxysteroid dehydrogenase;
Short chain dehydrogenase/reductase family
Research
Bioassay Publications (13)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 9 (69.23) | 29.6817 |
| 2010's | 4 (30.77) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (17)
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| estrone | Homo sapiens (human) | Km | 4.6000 | 1 | 1 |
Synopsis of some recent tactical application of bioisosteres in drug design.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Estradiol and estrone C-16 derivatives as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: blocking of ER+ breast cancer cell proliferation induced by estrone.Bioorganic & medicinal chemistry, , Feb-15, Volume: 16, Issue:4, 2008
Design and synthesis of bisubstrate inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: overview and perspectives.European journal of medicinal chemistry, , Volume: 43, Issue:11, 2008
Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold.Bioorganic & medicinal chemistry, , Jan-15, Volume: 19, Issue:2, 2011
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.Journal of medicinal chemistry, , Jan-27, Volume: 54, Issue:2, 2011
Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseaseJournal of medicinal chemistry, , Apr-10, Volume: 51, Issue:7, 2008
Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Enables
This protein enables 14 target(s):
| Target | Category | Definition |
|---|
| catalytic activity | molecular function | Catalysis of a biochemical reaction at physiological temperatures. In biologically catalyzed reactions, the reactants are known as substrates, and the catalysts are naturally occurring macromolecular substances known as enzymes. Enzymes possess specific binding sites for substrates, and are usually composed wholly or largely of protein, but RNA that has catalytic activity (ribozyme) is often also regarded as enzymatic. [GOC:vw, ISBN:0198506732] |
| estradiol 17-beta-dehydrogenase [NAD(P)] activity | molecular function | Catalysis of the reaction: estradiol-17-beta + NAD(P)+ = estrone + NAD(P)H + H+. The activity can use NAD+ or NADP+ as the acceptor. [EC:1.1.1.62] |
| steroid binding | molecular function | Binding to a steroid, any of a large group of substances that have in common a ring system based on 1,2-cyclopentanoperhydrophenanthrene. [GOC:jl, ISBN:0198506732] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| testosterone dehydrogenase [NAD(P)] activity | molecular function | Catalysis of the reaction: testosterone + NAD(P)+ = androst-4-ene-3,17-dione + NAD(P)H + H+. [EC:1.1.1.51] |
| dihydrotestosterone 17-beta-dehydrogenase activity | molecular function | Catalysis of the reaction: 5alpha-dihydrotestosterone + NAD+ = 5alpha-androstane-3,17-dione + NADH. [GOC:ecd, http://www.brenda-enzymes.org/php/result_flat.php4?ecno=1.1.1.63, PMID:4152755] |
| small molecule binding | molecular function | Binding to a small molecule, any low molecular weight, monomeric, non-encoded molecule. [GOC:curators, GOC:pde, GOC:pm] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| testosterone dehydrogenase (NAD+) activity | molecular function | Catalysis of the reaction: testosterone + NAD+ = androst-4-ene-3,17-dione + NADH. [EC:1.1.1.239] |
| testosterone 17-beta-dehydrogenase (NADP+) activity | molecular function | Catalysis of the reaction: NADP+ + testosterone = NADPH + H+ + androst-4-ene-3,17-dione. [EC:1.1.1.64, MetaCyc:1.1.1.64-RXN] |
| NADP binding | molecular function | Binding to nicotinamide-adenine dinucleotide phosphate, a coenzyme involved in many redox and biosynthetic reactions; binding may be to either the oxidized form, NADP+, or the reduced form, NADPH. [GOC:ai] |
| NADP+ binding | molecular function | Binding to the oxidized form, NADP+, of nicotinamide-adenine dinucleotide phosphate, a coenzyme involved in many redox and biosynthetic reactions. [GOC:mah] |
| 17-beta-hydroxysteroid dehydrogenase (NADP+) activity | molecular function | Catalysis of the reaction: a 17-beta-hydroxysteroid + NADP+ = a 17-oxosteroid + NADPH + H+. [GOC:kad, PMID:17074428] |
| estradiol binding | molecular function | Binding to estradiol. [GO_REF:0000067, GOC:TermGenie, PMID:9048584] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Involved In
This protein is involved in 10 target(s):
| Target | Category | Definition |
|---|
| steroid biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of steroids, compounds with a 1,2,cyclopentanoperhydrophenanthrene nucleus; includes de novo formation and steroid interconversion by modification. [GOC:go_curators] |
| estrogen biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of estrogens, C18 steroid hormones that can stimulate the development of female sexual characteristics. Also found in plants. [ISBN:0198506732] |
| lysosome organization | biological process | A process that is carried out at the cellular level which results in the assembly, arrangement of constituent parts, or disassembly of a lysosome. A lysosome is a cytoplasmic, membrane-bounded organelle that is found in most animal cells and that contains a variety of hydrolases. [GOC:mah] |
| skeletal muscle tissue development | biological process | The developmental sequence of events leading to the formation of adult skeletal muscle tissue. The main events are: the fusion of myoblasts to form myotubes that increase in size by further fusion to them of myoblasts, the formation of myofibrils within their cytoplasm and the establishment of functional neuromuscular junctions with motor neurons. At this stage they can be regarded as mature muscle fibers. [GOC:mtg_muscle] |
| estrogen metabolic process | biological process | The chemical reactions and pathways involving estrogens, C18 steroid hormones that can stimulate the development of female sexual characteristics. Also found in plants. [ISBN:0198506732] |
| gene expression | biological process | The process in which a gene's sequence is converted into a mature gene product (protein or RNA). This includes the production of an RNA transcript and its processing, as well as translation and maturation for protein-coding genes. [GOC:txnOH-2018, PMID:25934543, PMID:31580950] |
| bone development | biological process | The process whose specific outcome is the progression of bone over time, from its formation to the mature structure. Bone is the hard skeletal connective tissue consisting of both mineral and cellular components. [GOC:dph] |
| adipose tissue development | biological process | The process whose specific outcome is the progression of adipose tissue over time, from its formation to the mature structure. Adipose tissue is specialized tissue that is used to store fat. [GOC:dph] |
| testosterone biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of testosterone, an androgen having 17beta-hydroxy and 3-oxo groups, together with unsaturation at C-4 C-5. [GOC:dph, GOC:yaf] |
| cellular response to metal ion | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a metal ion stimulus. [GOC:mah] |