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Development of VPC-70619, a Small-Molecule N-Myc Inhibitor as a Potential Therapy for Neuroendocrine Prostate Cancer Ton, Anh-Tien; Foo, Jane; Singh, Kriti; Lee, Joseph; Kalyta, Anastasia; Morin, Helene; Perez, Carl; Ban, Fuqiang; Leblanc, Eric; Lallous, Nada; Cherkasov, Artem
Abstract
The Myc family of transcription factors are involved in the development and progression of numerous cancers, including prostate cancer (PCa). Under the pressure of androgen receptor (AR)-directed therapies resistance can occur, leading to the lethal form of PCa known as neuroendocrine prostate cancer (NEPC), characterized among other features by N-Myc overexpression. There are no clinically approved treatments for NEPC, translating into poor patient prognosis and survival. Therefore, there is a pressing need to develop novel therapeutic avenues to treat NEPC patients. In this study, we investigate the N-Myc-Max DNA binding domain (DBD) as a potential target for small molecule inhibitors and utilize computer-aided drug design (CADD) approaches to discover prospective hits. Through further exploration and optimization, a compound, VPC-70619, was identified with notable anti-N-Myc potency and strong antiproliferative activity against numerous N-Myc expressing cell lines, including those representing NEPC.
Item Metadata
| Title |
Development of VPC-70619, a Small-Molecule N-Myc Inhibitor as a Potential Therapy for Neuroendocrine Prostate Cancer
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| Creator | |
| Contributor | |
| Publisher |
Multidisciplinary Digital Publishing Institute
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| Date Issued |
2022-02-26
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| Description |
The Myc family of transcription factors are involved in the development and progression of numerous cancers, including prostate cancer (PCa). Under the pressure of androgen receptor (AR)-directed therapies resistance can occur, leading to the lethal form of PCa known as neuroendocrine prostate cancer (NEPC), characterized among other features by N-Myc overexpression. There are no clinically approved treatments for NEPC, translating into poor patient prognosis and survival. Therefore, there is a pressing need to develop novel therapeutic avenues to treat NEPC patients. In this study, we investigate the N-Myc-Max DNA binding domain (DBD) as a potential target for small molecule inhibitors and utilize computer-aided drug design (CADD) approaches to discover prospective hits. Through further exploration and optimization, a compound, VPC-70619, was identified with notable anti-N-Myc potency and strong antiproliferative activity against numerous N-Myc expressing cell lines, including those representing NEPC.
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| Subject | |
| Genre | |
| Type | |
| Language |
eng
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| Date Available |
2022-03-25
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| Provider |
Vancouver : University of British Columbia Library
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| Rights |
CC BY 4.0
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| DOI |
10.14288/1.0407324
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| URI | |
| Affiliation | |
| Citation |
International Journal of Molecular Sciences 23 (5): 2588 (2022)
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| Publisher DOI |
10.3390/ijms23052588
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| Peer Review Status |
Reviewed
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| Scholarly Level |
Faculty; Researcher; Other
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| Rights URI | |
| Aggregated Source Repository |
DSpace
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Item Citations and Data
Rights
CC BY 4.0