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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MDPI AG
2020-07-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/21/14/4868 |
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doaj-34dce99125be4d5fa04c03cb349df6f32020-11-25T03:38:46ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672020-07-01214868486810.3390/ijms21144868Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer AgentsTomasz M. Wróbel0Oksana Rogova1Kasper L. Andersen2Rahul Yadav3Simone Brixius-Anderko4Emily E. Scott5Lars Olsen6Flemming Steen Jørgensen7Fredrik Björkling8Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, DenmarkDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, DenmarkBiotech Research and Innovation Centre (BRIC), University of Copenhagen, Ole Maaløes Vej 5, DK-2200 Copenhagen, DenmarkDepartment of Medicinal Chemistry, University of Michigan, 428 Church Street, Ann Arbor, Michigan, MI 48109-1065, USADepartment of Medicinal Chemistry, University of Michigan, 428 Church Street, Ann Arbor, Michigan, MI 48109-1065, USADepartment of Medicinal Chemistry, University of Michigan, 428 Church Street, Ann Arbor, Michigan, MI 48109-1065, USADepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, DenmarkDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, DenmarkDepartment of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, DenmarkThe 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.https://www.mdpi.com/1422-0067/21/14/4868cytochrome P450 17A1, CYP17A1prostate cancerenzyme inhibition |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Tomasz M. Wróbel Oksana Rogova Kasper L. Andersen Rahul Yadav Simone Brixius-Anderko Emily E. Scott Lars Olsen Flemming Steen Jørgensen Fredrik Björkling |
| spellingShingle |
Tomasz M. Wróbel Oksana Rogova Kasper L. Andersen Rahul Yadav Simone Brixius-Anderko Emily E. Scott Lars Olsen Flemming Steen Jørgensen Fredrik Björkling Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents International Journal of Molecular Sciences cytochrome P450 17A1, CYP17A1 prostate cancer enzyme inhibition |
| author_facet |
Tomasz M. Wróbel Oksana Rogova Kasper L. Andersen Rahul Yadav Simone Brixius-Anderko Emily E. Scott Lars Olsen Flemming Steen Jørgensen Fredrik Björkling |
| author_sort |
Tomasz M. Wróbel |
| title |
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_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_sort |
discovery of novel non-steroidal cytochrome p450 17a1 inhibitors as potential prostate cancer agents |
| publisher |
MDPI AG |
| series |
International Journal of Molecular Sciences |
| issn |
1661-6596 1422-0067 |
| publishDate |
2020-07-01 |
| 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. |
| topic |
cytochrome P450 17A1, CYP17A1 prostate cancer enzyme inhibition |
| url |
https://www.mdpi.com/1422-0067/21/14/4868 |
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