Synthesis and Biological Evaluation of Second-Generation Tropanol-Based Androgen Receptor Modulators

Summary, in English

To circumvent antiandrogen resistance in prostate cancer, antiandrogens effective for both the androgen receptor (AR) and AR mutants are required. The AR antagonists in this study originate from previous findings, which showed that subtle differences in substitution pattern lead to a conformational change that alters the ligand activity, rendering an agonist to an antagonist. We have identified small yet potent tropanol-based ligands possessing significant antiandrogenic activity with both wild-type AR and the two most common AR ligand binding domain (LBD) mutants.

• Författare: Henrik Sunden; Mareike C. Holland; Pekka K. Poutiainen; Tiina Jaaskelainen; Juha T. Pulkkinen; Jorma J. Palvimo; Roger Olsson
• Avdelning/ar: Kemisk biologi med inriktning mot läkemedelsutveckling; MultiPark: Multidisciplinary research focused on Parkinson´s disease
• Publiceringsår: 2015
• Språk: Engelska
• Sidor: 1569-1574
• Publikation/Tidskrift/Serie: Journal of Medicinal Chemistry
• Volym: 58
• Issue: 3
• Länkar: http://dx.doi.org/10.1021/jm501995n
• Dokumenttyp: Artikel i tidskrift
• Förlag: The American Chemical Society (ACS)
• Ämne: Medicinal Chemistry
• Status: Published
• Forskningsgrupp: Chemical Biology and Therapeutics
• ISBN/ISSN/Övrigt: ISSN: 1520-4804