(Q35816836)

English

Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships

scientific article published on 15 February 2012

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scholarly article

1 reference

Europe PubMed Central

10 August 2017

Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships (English)

1 reference

Europe PubMed Central

10 August 2017

author name string

Adegoke O Adeniji

1

1 reference

Europe PubMed Central

10 August 2017

Barry M Twenter

2

1 reference

Europe PubMed Central

10 August 2017

Michael C Byrns

3

1 reference

Europe PubMed Central

10 August 2017

Yi Jin

4

1 reference

Europe PubMed Central

10 August 2017

Mo Chen

5

1 reference

Europe PubMed Central

10 August 2017

Jeffrey D Winkler

6

1 reference

Europe PubMed Central

10 August 2017

Trevor M Penning

7

1 reference

Europe PubMed Central

10 August 2017

language of work or name

0 references

publication date

15 February 2012

1 reference

Europe PubMed Central

10 August 2017

Journal of Medicinal Chemistry

1 reference

Europe PubMed Central

10 August 2017

55

1 reference

Europe PubMed Central

10 August 2017

2311-2323

1 reference

Europe PubMed Central

10 August 2017

5

1 reference

Europe PubMed Central

10 August 2017

Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors

1 reference

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Dihydrotestosterone synthesis bypasses testosterone to drive castration-resistant prostate cancer

1 reference

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27 July 2018

Identification of chemically diverse, novel inhibitors of 17β-hydroxysteroid dehydrogenase type 3 and 5 by pharmacophore-based virtual screening.

1 reference

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Activities of aldo-keto reductase 1 enzymes on two inhaled corticosteroids: implications for the pharmacological effects of inhaled corticosteroids

1 reference

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Inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3): overview and structural insights.

1 reference

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Cancer statistics, 2010

1 reference

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Significant and sustained antitumor activity in post-docetaxel, castration-resistant prostate cancer with the CYP17 inhibitor abiraterone acetate

1 reference

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Partners in crime: deregulation of AR activity and androgen synthesis in prostate cancer

1 reference

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27 July 2018

Selective inhibition of CYP17 with abiraterone acetate is highly active in the treatment of castration-resistant prostate cancer

1 reference

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Development of a second-generation antiandrogen for treatment of advanced prostate cancer

1 reference

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Oxidation of PAH trans-dihydrodiols by human aldo-keto reductase AKR1B10.

1 reference

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Androgen levels increase by intratumoral de novo steroidogenesis during progression of castration-resistant prostate cancer

1 reference

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Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics

1 reference

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27 July 2018

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

1 reference

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27 July 2018

Hormonal impact of the 17alpha-hydroxylase/C(17,20)-lyase inhibitor abiraterone acetate (CB7630) in patients with prostate cancer

1 reference

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

1 reference

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27 July 2018

Human type 3 3alpha-hydroxysteroid dehydrogenase (aldo-keto reductase 1C2) and androgen metabolism in prostate cells.

1 reference

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Human aldose reductase and human small intestine aldose reductase are efficient retinal reductases: consequences for retinoid metabolism

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

1 reference

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Structural analysis of NSAID binding by prostaglandin H2 synthase: time-dependent and time-independent inhibitors elicit identical enzyme conformations

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Purification and characterization of the human recombinant histidine-tagged prostaglandin endoperoxide H synthases-1 and -2.

1 reference

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27 July 2018

Kinetic basis for selective inhibition of cyclo-oxygenases

1 reference

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27 July 2018

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

1 reference

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27 July 2018

Expression and characterization of recombinant type 2 3 alpha-hydroxysteroid dehydrogenase (HSD) from human prostate: demonstration of bifunctional 3 alpha/17 beta-HSD activity and cellular distribution

1 reference

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Expression purification and characterization of recombinant human inducible prostaglandin G/H synthase from baculovirus-infected insect cells

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Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system

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Inhibition of a major NAD(P)-linked oxidoreductase from rat liver cytosol by steroidal and nonsteroidal anti-inflammatory agents and by prostaglandins

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Isolation and partial characterization of a full-length cDNA clone for 3 alpha-hydroxysteroid dehydrogenase: a potential target enzyme for nonsteroidal anti-inflammatory drugs

1 reference

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Overexpression of aldo-keto reductase 1C3 (AKR1C3) in LNCaP cells diverts androgen metabolism towards testosterone resulting in resistance to the 5α-reductase inhibitor finasteride.

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Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC)

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Structure-activity study in the class of 6-(3'-hydroxyphenyl)naphthalenes leading to an optimization of a pharmacophore model for 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors

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Maintenance of intratumoral androgens in metastatic prostate cancer: a mechanism for castration-resistant tumor growth

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Human cytosolic 3alpha-hydroxysteroid dehydrogenases of the aldo-keto reductase superfamily display significant 3beta-hydroxysteroid dehydrogenase activity: implications for steroid hormone metabolism and action

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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.

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1 reference

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1 reference

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24 September 2018

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

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https://pubmed.ncbi.nlm.nih.gov/22263837

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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

1 reference

https://pubmed.ncbi.nlm.nih.gov/22263837

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold

1 reference

https://pubmed.ncbi.nlm.nih.gov/22263837

12 December 2020

based on heuristic

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Identifiers

10.1021/JM201547V

1 reference

Europe PubMed Central

10 August 2017

1 reference

Europe PubMed Central

10 August 2017

1 reference

Europe PubMed Central

10 August 2017

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