{"id":179,"date":"2013-01-30T17:04:27","date_gmt":"2013-01-30T09:04:27","guid":{"rendered":"http:\/\/www.huanglab.org.cn\/wordpress\/?p=179"},"modified":"2013-03-11T18:41:40","modified_gmt":"2013-03-11T10:41:40","slug":"a-soluble-bis-chelated-goldi-diphosphine-compound-with-strong-anticancer-activity-and-low-toxicity","status":"publish","type":"post","link":"https:\/\/www.huanglab.org.cn\/wordpress\/?p=179","title":{"rendered":"A Soluble Bis-Chelated Gold(I) Diphosphine Compound with Strong Anticancer Activity and Low Toxicity"},"content":{"rendered":"<p><a href=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2013\/03\/yanliwan.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"alignnone size-medium wp-image-178\" alt=\"yanliwan\" src=\"http:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2013\/03\/yanliwan-300x126.jpg\" width=\"300\" height=\"126\" srcset=\"https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2013\/03\/yanliwan-300x126.jpg 300w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2013\/03\/yanliwan-1024x432.jpg 1024w, https:\/\/www.huanglab.org.cn\/wordpress\/wp-content\/uploads\/2013\/03\/yanliwan.jpg 1053w\" sizes=\"auto, (max-width: 300px) 100vw, 300px\" \/><\/a><\/p>\n<p>A Soluble Bis-Chelated Gold(I) Diphosphine Compound with Strong Anticancer Activity and Low Toxicity<br \/>\nYanli Wang \u2021, Minyu Liu \u2020\u00a7, Ran Cao \u2021, Wanbin Zhang \u2020, Ming Yin \u2020, Xuhua Xiao \u00a7, Quanhai Liu *\u00a7, and Niu Huang *\u2021<br \/>\n\u2020 School of Pharmacy, Shanghai Jiao Tong University, 800 Dong Chuan Road, Shanghai 200240, China<br \/>\n\u2021 National Institute of Biological Sciences, Beijing, 7 Science Park Road, Zhongguancun Life Science Park, Beijing 102206, China<br \/>\n\u00a7 Department of Pharmacology, Shanghai Institute of Pharmaceutical Industry, 1111 Zhong Shan Bei Yi Road, Shanghai 200437, China<br \/>\nJ. Med. Chem., 2013, 56 (4), pp 1455\u20131466<br \/>\nDOI: 10.1021\/jm3009822<br \/>\nPublication Date (Web): January 30, 2013<\/p>\n<p>Abstract<\/p>\n<p>Gold-containing compounds have shown anticancer potential, but their clinical applications have been severely limited by poor stability and high toxicity in vivo. Here, we report a novel soluble bis-chelated gold(I)\u2013diphosphine compound (GC20) with strong anticancer activity and low toxicity. GC20 shows strong antiproliferation potency against a broad spectrum of cancer cell lines including cisplatin-resistant cancer cells (IC50 \u2248 0.5 \u03bcM) and significantly reduces tumor growth in several tumor xenografts in mouse models at doses as low as 2 mg\/kg. Studies of its mechanism revealed that GC20 specifically inhibits the enzymatic activity of thioredoxin reductase by binding to selenocysteine residue, without targeting other well-known selenol and thiol groups contained in biomolecules. Remarkably, in animal studies GC20 was shown to be well tolerated even at the high dose of 8 mg\/kg. Our results strongly suggest that GC20 represents a promising candidate for the development of novel anticancer drugs.<\/p>\n<p><a href=\"http:\/\/pubs.acs.org\/doi\/abs\/10.1021\/jm3009822\" name=\"tex2html5\">[Epub ahead of print]<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>A Soluble Bis-Chelated Gold(I) Diphosphine Compound with Strong Anticancer Activity and Low Toxicity Yanli Wang \u2021, Minyu Liu \u2020\u00a7, Ran Cao \u2021, Wanbin Zhang \u2020, Ming Yin \u2020, Xuhua Xiao \u00a7, Quanhai Liu *\u00a7, and Niu Huang *\u2021 \u2020 School of Pharmacy, Shanghai Jiao Tong University, 800 Dong Chuan Road, Shanghai 200240, China \u2021 National [&hellip;]<\/p>\n","protected":false},"author":1,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"ngg_post_thumbnail":0,"footnotes":""},"categories":[10],"tags":[],"class_list":["post-179","post","type-post","status-publish","format-standard","hentry","category-news"],"_links":{"self":[{"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/179","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=179"}],"version-history":[{"count":8,"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/179\/revisions"}],"predecessor-version":[{"id":187,"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=\/wp\/v2\/posts\/179\/revisions\/187"}],"wp:attachment":[{"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=179"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=179"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.huanglab.org.cn\/wordpress\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=179"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}