Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents

The current study presents the design, synthesis, and evaluation of novel cytochrome P450 17A1 (CYP17A1) ligands. CYP17A1 is a key enzyme in the steroidogenic pathway that produces androgens among other steroids, and it is implicated in prostate cancer. The obtained compounds are potent enzyme inhib...

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Autores principales: Wróbel, Tomasz M., Rogova, Oksana, Andersen, Kasper L., Yadav, Rahul, Brixius-Anderko, Simone, Scott, Emily E., Olsen, Lars, Jørgensen, Flemming Steen, Björkling, Fredrik
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7402352/
https://www.ncbi.nlm.nih.gov/pubmed/32660148
http://dx.doi.org/10.3390/ijms21144868
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author Wróbel, Tomasz M.
Rogova, Oksana
Andersen, Kasper L.
Yadav, Rahul
Brixius-Anderko, Simone
Scott, Emily E.
Olsen, Lars
Jørgensen, Flemming Steen
Björkling, Fredrik
author_facet Wróbel, Tomasz M.
Rogova, Oksana
Andersen, Kasper L.
Yadav, Rahul
Brixius-Anderko, Simone
Scott, Emily E.
Olsen, Lars
Jørgensen, Flemming Steen
Björkling, Fredrik
author_sort Wróbel, Tomasz M.
collection PubMed
description The current study presents the design, synthesis, and evaluation of novel cytochrome P450 17A1 (CYP17A1) ligands. CYP17A1 is a key enzyme in the steroidogenic pathway that produces androgens among other steroids, and it is implicated in prostate cancer. The obtained compounds are potent enzyme inhibitors (sub µM) with antiproliferative activity in prostate cancer cell lines. The binding mode of these compounds is also discussed.
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spelling pubmed-74023522020-08-11 Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents Wróbel, Tomasz M. Rogova, Oksana Andersen, Kasper L. Yadav, Rahul Brixius-Anderko, Simone Scott, Emily E. Olsen, Lars Jørgensen, Flemming Steen Björkling, Fredrik Int J Mol Sci Article The current study presents the design, synthesis, and evaluation of novel cytochrome P450 17A1 (CYP17A1) ligands. CYP17A1 is a key enzyme in the steroidogenic pathway that produces androgens among other steroids, and it is implicated in prostate cancer. The obtained compounds are potent enzyme inhibitors (sub µM) with antiproliferative activity in prostate cancer cell lines. The binding mode of these compounds is also discussed. MDPI 2020-07-09 /pmc/articles/PMC7402352/ /pubmed/32660148 http://dx.doi.org/10.3390/ijms21144868 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Wróbel, Tomasz M.
Rogova, Oksana
Andersen, Kasper L.
Yadav, Rahul
Brixius-Anderko, Simone
Scott, Emily E.
Olsen, Lars
Jørgensen, Flemming Steen
Björkling, Fredrik
Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents
title Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents
title_full Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents
title_fullStr Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents
title_full_unstemmed Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents
title_short Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents
title_sort discovery of novel non-steroidal cytochrome p450 17a1 inhibitors as potential prostate cancer agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7402352/
https://www.ncbi.nlm.nih.gov/pubmed/32660148
http://dx.doi.org/10.3390/ijms21144868
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