An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone (Q81469973)

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scientific article published on 14 September 2007

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English	An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone	scientific article published on 14 September 2007

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scholarly article

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9 January 2020

An indomethacin analogue, N-(4-chlorobenzoyl)-melatonin, is a selective inhibitor of aldo-keto reductase 1C3 (type 2 3alpha-HSD, type 5 17beta-HSD, and prostaglandin F synthase), a potential target for the treatment of hormone dependent and hormone independent malignancies (English)

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9 January 2020

Trevor M Penning

3

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9 January 2020

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Michael C Byrns

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9 January 2020

Stephan Steckelbroeck

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9 January 2020

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14 September 2007

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9 January 2020

Biochemical Pharmacology

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9 January 2020

75

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9 January 2020

2

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9 January 2020

484-493

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9 January 2020

Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

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Drug insight: role of the androgen receptor in the development and progression of prostate cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

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A prostaglandin J2 metabolite binds peroxisome proliferator-activated receptor gamma and promotes adipocyte differentiation

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

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Relationship of human liver dihydrodiol dehydrogenases to hepatic bile-acid-binding protein and an oxidoreductase of human colon cells

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Synthesis and use of iodinated nonsteroidal antiinflammatory drug analogs as crystallographic probes of the prostaglandin H2 synthase cyclooxygenase active site

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Prostaglandins promote and block adipogenesis through opposing effects on peroxisome proliferator-activated receptor gamma

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Expression and characterization of four recombinant human dihydrodiol dehydrogenase isoforms: oxidation of trans-7, 8-dihydroxy-7,8-dihydrobenzo[a]pyrene to the activated o-quinone metabolite benzo[a]pyrene-7,8-dione

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

cDNA cloning, expression and characterization of human prostaglandin F synthase

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

15-deoxy-delta 12,14-prostaglandin J2 inhibits multiple steps in the NF-kappa B signaling pathway.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Human 3alpha-hydroxysteroid dehydrogenase isoforms (AKR1C1-AKR1C4) of the aldo-keto reductase superfamily: functional plasticity and tissue distribution reveals roles in the inactivation and formation of male and female sex hormones

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Crystal structure of human type III 3alpha-hydroxysteroid dehydrogenase/bile acid binding protein complexed with NADP(+) and ursodeoxycholate

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Tamoxifen resistant and refractory breast cancer: the value of aromatase inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Enantiospecific, selective cyclooxygenase-2 inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Kinetics of allopregnanolone formation catalyzed by human 3 alpha-hydroxysteroid dehydrogenase type III (AKR1C2).

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The aldo-keto reductase AKR1C3 is a novel suppressor of cell differentiation that provides a plausible target for the non-cyclooxygenase-dependent antineoplastic actions of nonsteroidal anti-inflammatory drugs.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Hydroxysteroid dehydrogenases and pre-receptor regulation of steroid hormone action.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Expression, localization, and signaling of prostaglandin F2 alpha receptor in human endometrial adenocarcinoma: regulation of proliferation by activation of the epidermal growth factor receptor and mitogen-activated protein kinase signaling pathways

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Preferential expression of hPGFS in primary SCCHN and tumour cell lines derived from respiratory and digestive organs.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Crystal structures of prostaglandin D(2) 11-ketoreductase (AKR1C3) in complex with the nonsteroidal anti-inflammatory drugs flufenamic acid and indomethacin.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Evidence for nucleotide receptor modulation of cross talk between MAP kinase and NF-kappa B signaling pathways in murine RAW 264.7 macrophages

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structure-function of human 3 alpha-hydroxysteroid dehydrogenases: genes and proteins.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Synthesis of prostaglandin F ethanolamide by prostaglandin F synthase and identification of Bimatoprost as a potent inhibitor of the enzyme: new enzyme assay method using LC/ESI/MS.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The kinetic mechanism catalysed by homogeneous rat liver 3 alpha-hydroxysteroid dehydrogenase. Evidence for binary and ternary dead-end complexes containing non-steroidal anti-inflammatory drugs

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Development of affinity labeling agents based on nonsteroidal anti-inflammatory drugs: labeling of the nonsteroidal anti-inflammatory drug binding site of 3 alpha-hydroxysteroid dehydrogenase

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Differential inhibition of prostaglandin endoperoxide synthase (cyclooxygenase) isozymes by aspirin and other non-steroidal anti-inflammatory drugs.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Prostaglandin F2alpha stimulates the Raf/MEK1/mitogen-activated protein kinase signaling cascade in bovine luteal cells

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identification of a principal mRNA species for human 3alpha-hydroxysteroid dehydrogenase isoform (AKR1C3) that exhibits high prostaglandin D2 11-ketoreductase activity

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Influence of J series prostaglandins on apoptosis and tumorigenesis of breast cancer cells

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Oxidative damage-related genes AKR1C3 and OGG1 modulate risks for lung cancer due to exposure to PAH-rich coal combustion emissions.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Molecular basis of the time-dependent inhibition of cyclooxygenases by indomethacin

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Characterization of a monoclonal antibody for human aldo-keto reductase AKR1C3 (type 2 3alpha-hydroxysteroid dehydrogenase/type 5 17beta-hydroxysteroid dehydrogenase); immunohistochemical detection in breast and prostate

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Development of nonsteroidal anti-inflammatory drug analogs and steroid carboxylates selective for human aldo-keto reductase isoforms: potential antineoplastic agents that work independently of cyclooxygenase isozymes

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Alpha,beta-unsaturated ketone is a core moiety of natural ligands for covalent binding to peroxisome proliferator-activated receptor gamma.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Indolyl esters and amides related to indomethacin are selective COX-2 inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Polymorphisms in genes involved in sex hormone metabolism may increase risk of benign prostatic hyperplasia

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Prostaglandin F2alpha formation from prostaglandin H2 by prostaglandin F synthase (PGFS): crystal structure of PGFS containing bimatoprost

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Increased expression of genes converting adrenal androgens to testosterone in androgen-independent prostate cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

AKR1C1 and AKR1C3 may determine progesterone and estrogen ratios in endometrial cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Aldo-keto reductase (AKR) 1C3: role in prostate disease and the development of specific inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Increased expression of type 2 3alpha-hydroxysteroid dehydrogenase/type 5 17beta-hydroxysteroid dehydrogenase (AKR1C3) and its relationship with androgen receptor in prostate carcinoma

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Transcriptosome and serum cytokine profiling of an atypical case of myelodysplastic syndrome with progression to acute myelogenous leukemia.

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Multiple steps determine the overall rate of the reduction of 5alpha-dihydrotestosterone catalyzed by human type 3 3alpha-hydroxysteroid dehydrogenase: implications for the elimination of androgens

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structure-based inhibitor design for an enzyme that binds different steroids: a potent inhibitor for human type 5 17beta-hydroxysteroid dehydrogenase

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

15-Deoxy-delta 12, 14-prostaglandin J2 is a ligand for the adipocyte determination factor PPAR gamma

1 reference

https://pubmed.ncbi.nlm.nih.gov/17950253

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1016/J.BCP.2007.09.008

1 reference

Europe PubMed Central

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:17950253%20AND%20SRC:MED&resulttype=core&format=json

9 January 2020

PMC publication ID

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PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:17950253%20AND%20SRC:MED&resulttype=core&format=json

9 January 2020

PubMed publication ID

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:17950253%20AND%20SRC:MED&resulttype=core&format=json

9 January 2020

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