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Please use this identifier to cite or link to this item: http://repository.li.mahidol.ac.th/dspace/handle/123456789/43401
Title: Antarlides: A New Type of Androgen Receptor (AR) Antagonist that Overcomes Resistance to AR-Targeted Therapy
Authors: Shun Saito
Takahiro Fujimaki
Watanalai Panbangred
Yasuhiro Igarashi
Masaya Imoto
Keio University
Mahidol University
Toyama Prefectural University
Keywords: Chemical Engineering;Chemistry
Issue Date: 18-Feb-2016
Citation: Angewandte Chemie - International Edition. Vol.55, No.8 (2016), 2728-2732
Abstract: © 2016 Wiley-VCH Verlag GmbH & Co. KGaA. Prostate cancer is treated with androgen receptor (AR) antagonists but most patients experience disease progression after long-term treatment with these compounds. Therefore, new AR antagonists are required for patient follow-up treatment. In the course of screening for a new AR antagonist, we isolated the novel compounds antarlides A-E (1-5) from Streptomyces sp. BB47. Antarlides are mutually isomeric with respect to the double bond and have a 22-membered-ring macrocyclic structure. The full stereostructure of 1 was established by chemical modifications, including methanolysis, the Trost method, acetonide formation, and the PGME method. 1-5 inhibited the binding of androgen to ARs in vitro. In addition, 2 inhibited the transcriptional activity of not only wild-type AR but also mutant ARs, which are seen in patients with acquired resistance to clinically used AR antagonists. Therefore, antarlides are a potent new generation of AR antagonists that overcome resistance.
URI: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84958729571&origin=inward
http://repository.li.mahidol.ac.th/dspace/handle/123456789/43401
ISSN: 15213773
14337851
Appears in Collections:Scopus 2016-2017

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