Development of vpc-70619, a small-molecule ...
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Article dans une revue scientifique: Article original
DOI :
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Title :
Development of vpc-70619, a small-molecule n-myc inhibitor as a potential therapy for neuroendocrine prostate cancer
Author(s) :
Ton, Anh-Tien [Auteur]
University of British Columbia [Vancouver]
Foo, Jane [Auteur]
University of British Columbia [Vancouver]
Singh, Priyanka [Auteur]
Protéomique, Réponse Inflammatoire, Spectrométrie de Masse (PRISM) - U1192
Lee, Joseph [Auteur]
University of British Columbia [Vancouver]
Kalyta, Anastasia [Auteur]
University of British Columbia [Vancouver]
Morin, Helene [Auteur]
University of British Columbia [Vancouver]
Perez, Carl F. [Auteur]
University of British Columbia [Vancouver]
Ban, Fuqiang [Auteur]
University of British Columbia [Vancouver]
Leblanc, Eric [Auteur]
Protéomique, Réponse Inflammatoire, Spectrométrie de Masse (PRISM) - U1192
Lallous, Nada [Auteur]
University of British Columbia [Vancouver]
Cherkasov, Artem [Auteur]
University of British Columbia [Vancouver]
University of British Columbia [Vancouver]
Foo, Jane [Auteur]
University of British Columbia [Vancouver]
Singh, Priyanka [Auteur]
Protéomique, Réponse Inflammatoire, Spectrométrie de Masse (PRISM) - U1192
Lee, Joseph [Auteur]
University of British Columbia [Vancouver]
Kalyta, Anastasia [Auteur]
University of British Columbia [Vancouver]
Morin, Helene [Auteur]
University of British Columbia [Vancouver]
Perez, Carl F. [Auteur]
University of British Columbia [Vancouver]
Ban, Fuqiang [Auteur]
University of British Columbia [Vancouver]
Leblanc, Eric [Auteur]

Protéomique, Réponse Inflammatoire, Spectrométrie de Masse (PRISM) - U1192
Lallous, Nada [Auteur]
University of British Columbia [Vancouver]
Cherkasov, Artem [Auteur]
University of British Columbia [Vancouver]
Journal title :
International Journal of Molecular Sciences
Abbreviated title :
Int J Mol Sci
Volume number :
23
Pages :
2588
Publisher :
MDPI
Publication date :
2022-02-26
ISSN :
1422-0067
Keyword(s) :
drug discovery
Myc
computer-aided drug design
therapeutic target
prostate cancer
Myc
computer-aided drug design
therapeutic target
prostate cancer
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
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 ...
Show more >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.Show less >
Show more >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.Show less >
Language :
Anglais
Audience :
Internationale
Popular science :
Non
Administrative institution(s) :
INSERM
Université de Lille
Université de Lille
Submission date :
2022-06-15T14:00:51Z
2023-01-18T10:00:18Z
2023-01-18T10:00:18Z
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