{"id":3255,"date":"2021-10-26T08:33:45","date_gmt":"2021-10-26T08:33:45","guid":{"rendered":"https:\/\/zobio.com\/?p=3255"},"modified":"2025-01-21T15:11:29","modified_gmt":"2025-01-21T15:11:29","slug":"remarkable-achievement-in-collaboration-with-essa-pharma","status":"publish","type":"post","link":"https:\/\/zobio.com\/online\/news\/remarkable-achievement-in-collaboration-with-essa-pharma\/","title":{"rendered":"Remarkable NMR Achievement in Collaboration with ESSA Pharma"},"content":{"rendered":"

Remarkable NMR Achievement in Collaboration with ESSA Pharma <\/h2>\n
\n\t

The androgen receptor (AR) pathway drives most metastatic, castration-resistant prostate cancers (mCRPC). Anti-androgen resistance mechanisms include AR gene amplification, C-terminal ligand-binding domain (LBD) mutations and expression of constitutively-active truncated AR splice variants lacking the LBD altogether (eg. AR-V7). Selective inhibition of the N-terminal domain (NTD) of the AR can prevent transcriptional activity even in the presence of LBD-driven resistance [1]. ESSA Pharma has developed EPI-7386, a potent and selective small molecule inhibitor that can bind to the N-terminal domain (NTD) of the androgen receptor (AR). EPI-7386 is currently in clinical trials for the treatment of patients with metastatic castration-resistant prostate cancer.<\/p>\n

At the recent AACR-NCI-EORTC Virtual International Conference (7-10 October 2021), ESSA Pharma has presented some remarkable results showing preclinical characterization of the mechanism of action of EPI-7386 on the AR-NTD. ESSA Pharma collaborated with ZoBio to use our expertise in NMR for this characterization.\u00a0 We used three different NMR approaches to unequivocally demonstrate for the first time binding of EPI-7836 to AR-NTD. We are proud to participate in this ground-breaking project.<\/p>\n

Check out the virtual poster here<\/a>!<\/p>\n

\u00a0<\/strong><\/p>\n

[1] R. Le Moigne et al., Annals of Oncology., 2019, v.30, p.189-190<\/p>\n

 <\/p>\n<\/div>\n<\/div><\/div><\/div><\/div><\/div><\/div><\/div>","protected":false},"excerpt":{"rendered":"

The androgen receptor (AR) pathway drives most metastatic, castration-resistant prostate cancers (mCRPC). Anti-androgen resistance mechanisms include AR gene amplification, C-terminal ligand-binding domain (LBD) mutations and expression of constitutively-active truncated AR splice variants lacking…<\/p>\n","protected":false},"author":3,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"gpsa_enabled":false,"gpsa_required_form_ids":[],"gpsa_require_unique_form_submission":false,"gpsa_access_behavior":"show_message","gpsa_form_redirect_path":"","gpsa_requires_access_message":"","gpsa_access":[],"gpsa_content_loading_message":"","footnotes":""},"categories":[3],"tags":[],"class_list":["post-3255","post","type-post","status-publish","format-standard","hentry","category-news"],"yoast_head":"\nRemarkable NMR Achievement in Collaboration with ESSA Pharma - ZoBio - Drug Discovery Technology<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/zobio.com\/online\/news\/remarkable-achievement-in-collaboration-with-essa-pharma\/\" \/>\n<meta property=\"og:locale\" content=\"en_GB\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Remarkable NMR Achievement in Collaboration with ESSA Pharma - ZoBio - Drug Discovery Technology\" \/>\n<meta property=\"og:description\" content=\"The androgen receptor (AR) pathway drives most metastatic, castration-resistant prostate cancers (mCRPC). 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