Cheminformatics driven development of novel ...
Document type :
Article dans une revue scientifique: Article original
DOI :
PMID :
Permalink :
Title :
Cheminformatics driven development of novel therapies for drug resistant prostate cancer
Author(s) :
Ban, Fuqiang [Auteur]
Dalal, Kush [Auteur]
Leblanc, Eric [Auteur]
Morin, Helene [Auteur]
Rennie, Paul S. [Auteur]
Cherkasov, Artem [Auteur]
Dalal, Kush [Auteur]
Leblanc, Eric [Auteur]

Morin, Helene [Auteur]
Rennie, Paul S. [Auteur]
Cherkasov, Artem [Auteur]
Journal title :
Molecular informatics
Abbreviated title :
Mol Inform
Publication date :
2018-05-07
ISSN :
1868-1751
Keyword(s) :
drug resistance
prostate cancer
Androgen receptor
cheminformatics
antiandrogen
prostate cancer
Androgen receptor
cheminformatics
antiandrogen
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
Androgen receptor (AR) is a master regulator of prostate cancer (PCa), and therefore is a pivotal drug target for the treatment of PCa including its castration-resistance form (CRPC). The development of acquired resistance ...
Show more >Androgen receptor (AR) is a master regulator of prostate cancer (PCa), and therefore is a pivotal drug target for the treatment of PCa including its castration-resistance form (CRPC). The development of acquired resistance is a major challenge in the use of the current antiandrogens. The recent advancements in inhibiting AR activity with small molecules specifically designed to target areas distinct from the receptor's androgen binding site are carefully discussed. Our new classes of AR inhibitors of AF2 and BF3 functional sites and DBD domains designed using cheminformatics techniques are promising to circumvent various AR-dependent resistance mechanisms.Show less >
Show more >Androgen receptor (AR) is a master regulator of prostate cancer (PCa), and therefore is a pivotal drug target for the treatment of PCa including its castration-resistance form (CRPC). The development of acquired resistance is a major challenge in the use of the current antiandrogens. The recent advancements in inhibiting AR activity with small molecules specifically designed to target areas distinct from the receptor's androgen binding site are carefully discussed. Our new classes of AR inhibitors of AF2 and BF3 functional sites and DBD domains designed using cheminformatics techniques are promising to circumvent various AR-dependent resistance mechanisms.Show less >
Language :
Anglais
Audience :
Internationale
Popular science :
Non
Administrative institution(s) :
INSERM
Université de Lille
Université de Lille
Submission date :
2022-06-15T13:58:38Z