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Accepted (AM)Open Access (License Unspecified), Open
Journal article
Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer
Bioorganic & medicinal chemistry letters, v 27(10), pp 2216-2220
15 May 2017
PMID: 28385503
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
Prostate cancer is the most frequently diagnosed malignancy and the leading cause of cancer related death in men. First line therapy for disseminated disease relies on androgen deprivation, leveraging the addiction of these tumors on androgens for both growth and survival. Treatment typically involves antagonizing the androgen receptor (AR) or blocking the synthesis of androgens. Recurrence is common and within 2-3years patients develop castration resistant tumors that become unresponsive to AR-axis targeted therapies. In order to provide a more effective treatment, we are utilizing an approach that targets a key scaffolding protein, Sigma1 (also known as sigma-1 receptor), a unique 26-kilodalton integral membrane protein that is critical in stabilizing the AR. Herein we report on a new series of Sigma1 compounds for lead optimization derived from a hybrid pharmacophore approach.
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Details
- Title
- Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer
- Creators
- Joseph M Salvino - Drexel UniversityYellamelli V V Srikanth - Drexel UniversityRongliang Lou - AstaTech, Inc., Keystone Business Park, 2525 Pearl Buck Road, Bristol, PA 19007, USAHalley M Oyer - Drexel UniversityNan Chen - Drexel UniversityFelix J Kim - Department of Pharmacology and Physiology, Drexel University College of Medicine, 245 N 15th Street, Philadelphia, PA 19102-1101, USA
- Publication Details
- Bioorganic & medicinal chemistry letters, v 27(10), pp 2216-2220
- Publisher
- Elsevier
- Number of pages
- 5
- Grant note
- P30 CA010815 / NCI NIH HHS R01 CA244749 / NCI NIH HHS R43 CA206691 / NCI NIH HHS
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000401492500028
- Scopus ID
- 2-s2.0-85016634810
- Other Identifier
- 991021904614004721
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- Collaboration types
- Domestic collaboration
- Web of Science research areas
- Chemistry, Medicinal
- Chemistry, Organic