Recent progress in the development of protein-protein interaction inhibitors targeting androgen receptor-coactivator binding in prostate cancer

Élément Dublin CoreValeurLangue
dc.contributor.authorBiron, Éric-
dc.contributor.authorBédard, François-
dc.description.abstractThe androgen receptor (AR) is a key regulator for the growth, differentiation and survival of prostate cancer cells. Identified as a primary target for the treatment of prostate cancer, many therapeutic strategies have been developed to attenuate AR signaling in prostate cancer cells. While frontline androgen-deprivation therapies targeting either the production or action of androgens usually yield favourable responses in prostate cancer patients, a significant number acquire treatment resistance. Known as the castration-resistant prostate cancer (CRPC), the treatment options are limited for this advanced stage. It has been shown that AR signaling is restored in CRPC due to many aberrant mechanisms such as AR mutations, amplification or expression of constitutively active splice-variants. Coregulator recruitment is a crucial regulatory step in AR signaling and the direct blockade of coactivator binding to AR offers the opportunity to develop therapeutic agents that would remain effective in prostate cancer cells resistant to conventional endocrine therapies. Structural analyses of the AR have identified key surfaces involved in protein-protein interaction with coregulators that have been recently used to design and develop promising AR-coactivator binding inhibitors. In this review we will discuss the design and development of small-molecule inhibitors targeting the AR-coactivator interactions for the treatment of prostate cancer.fr_CA
dc.publisherPergamon Pressfr_CA
dc.subjectProstate cancerfr_CA
dc.subjectAndrogen receptorfr_CA
dc.subjectCoregulator recruitmentfr_CA
dc.subjectProtein-protein interactionsfr_CA
dc.subjectCoactivator binding inhibitionfr_CA
dc.titleRecent progress in the development of protein-protein interaction inhibitors targeting androgen receptor-coactivator binding in prostate cancerfr_CA
dc.typeCOAR1_1::Texte::Périodique::Revue::Contribution à un journal::Article::Article de recherche-
dcterms.bibliographicCitationThe Journal of steroid biochemistry and molecular biology, Vol. 161, 36–44 (2016)fr_CA
dc.audienceProfesseurs (Enseignement supérieur)fr_CA
dc.subject.rvmProstate -- Cancer -- Traitementfr_CA
dc.subject.rvmInteractions protéine-protéinefr_CA
dc.subject.rvmAndrogènes -- Récepteursfr_CA
dc.subject.rvmProtéines -- Fixationfr_CA
rioxxterms.versionAccepted Manuscriptfr_CA
bul.rights.periodeEmbargo12 moisfr_CA
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