17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog (Q28546964)

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English	17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog	scientific article

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scholarly article

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17β-Hydroxysteroid Dehydrogenase Type 2 Inhibition: Discovery of Selective and Metabolically Stable Compounds Inhibiting Both the Human Enzyme and Its Murine Ortholog (English)

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Emanuele M Gargano

object named as

Emanuele M Gargano

1

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4

object named as

Angelo Carotti

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author name string

Giuseppe Allegretta

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Enrico Perspicace

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Chris Van Koppen

5

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Martin Frotscher

6

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Sandrine Marchais-Oberwinkler

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Rolf W Hartmann

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publication date

2015

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10

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7

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e0134754

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Creative Commons Attribution 4.0 International

31 July 2015

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April 2022 Public Data File from Crossref

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Medium- and short-chain dehydrogenase/reductase gene and protein families : the SDR superfamily: functional and structural diversity within a family of metabolic and regulatory enzymes

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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

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19 March 2017

17Beta-hydroxysteroid dehydrogenases in human bone cells

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19 March 2017

Expression cloning and characterization of human 17 beta-hydroxysteroid dehydrogenase type 2, a microsomal enzyme possessing 20 alpha-hydroxysteroid dehydrogenase activity

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19 March 2017

Novel N-methylsulfonamide and retro-N-methylsulfonamide derivatives as 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors with good ADME-related physicochemical parameters

1 reference

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29 September 2017

Structural optimization of 2,5-thiophene amides as highly potent and selective 17β-hydroxysteroid dehydrogenase type 2 inhibitors for the treatment of osteoporosis

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29 September 2017

Triazole ring-opening leads to the discovery of potent nonsteroidal 17β-hydroxysteroid dehydrogenase type 2 inhibitors

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

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29 September 2017

New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases

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Development of a biological screening system for the evaluation of highly active and selective 17beta-HSD1-inhibitors as potential therapeutic agents

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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

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Review of nonprimate, large animal models for osteoporosis research

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Androgens and bone

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Species differences between mouse, rat, dog, monkey and human CYP-mediated drug metabolism, inhibition and induction

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29 September 2017

4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 3. Identification of lead candidate

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29 September 2017

17Beta-hydroxysteroid dehydrogenase Type 1 and Type 2: association between mRNA expression and activity in cell lines

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Inhibition of type 2 17beta-hydroxysteroid dehydrogenase by estradiol derivatives bearing a lactone on the D-ring: structure-activity relationships

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29 September 2017

Osteoporosis prevention, diagnosis, and therapy

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29 September 2017

Inhibitors of type II 17beta-hydroxysteroid dehydrogenase

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Steroidal spiro-gamma-lactones that inhibit 17 beta-hydroxysteroid dehydrogenase activity in human placental microsomes

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Subunit identity of the dimeric 17 beta-hydroxysteroid dehydrogenase from human placenta

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4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17beta-hydroxysteroid dehydrogenase. Part 2. SAR.

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21 January 2018

Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17β-hydroxysteroid dehydrogenase type 2 inhibitors.

1 reference

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21 January 2018

Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases

1 reference

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Chemical synthesis of 16beta-propylaminoacyl derivatives of estradiol and their inhibitory potency on type 1 17beta-hydroxysteroid dehydrogenase and binding affinity on steroid receptors.

1 reference

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Crystallization and Preliminary X-ray Diffraction Analysis of the Complex of Human Placental 17β-Hydroxysteroid Dehydrogenase with NADP+

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21 January 2018

Site-directed mutagenesis of the putative active site of human 17 beta-hydroxysteroid dehydrogenase type 1.

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21 January 2018

Optimization of a higher throughput microsomal stability screening assay for profiling drug discovery candidates

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Animal models of osteoporosis--necessity and limitations.

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27 November 2018

Strategic identification of in vitro metabolites of 13-desmethyl spirolide C using liquid chromatography/high-resolution mass spectrometry

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Discovery of a new class of bicyclic substituted hydroxyphenylmethanones as 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) inhibitors for the treatment of osteoporosis

1 reference

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C16 and C17 derivatives of estradiol as inhibitors of 17 beta-hydroxysteroid dehydrogenase type 1: chemical synthesis and structure-activity relationships

1 reference

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12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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10.1371/JOURNAL.PONE.0134754

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2015PLoSO..1034754G

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