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]

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

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 >

Language :

Anglais

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

INSERM
Université de Lille

Collections :

• Protéomique, Réponse Inflammatoire, Spectrométrie de Masse (PRISM) - U1192

Submission date :

2022-06-15T14:00:51Z
2023-01-18T10:00:18Z