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However, no PTP1B inhibitor has come into clinic application. Herein, we report mixed 3,3\u2032\u2010bisindoles as novel PTP1B inhibitors with low micromole\u2010ranged inhibitory activity. The best active compound <jats:bold>9f<\/jats:bold> inhibited PTP1B activity with an IC<jats:sub>50<\/jats:sub> of 2.79\u2009\u00b5M. Meanwhile, it had low cytotoxicity and enhanced glucose uptake <jats:italic>in vitro<\/jats:italic>. Further studies demonstrated that some of these active compounds had a specific selectivity over other PTPs. Computational analysis further showed the binding mode of compound <jats:bold>9f<\/jats:bold> with the active pocket of PTP1B. Our studies provide a novel scaffold for further development of more promising PTP1B inhibitors and potential drugs for type II diabetes and obesity.<\/jats:p><\/jats:sec>","DOI":"10.1002\/ardp.201600173","type":"journal-article","created":{"date-parts":[[2016,12,28]],"date-time":"2016-12-28T10:47:30Z","timestamp":1482922050000},"source":"Crossref","is-referenced-by-count":3,"title":["Discovery of Bisindole as a Novel Scaffold for Protein Tyrosine Phosphatase 1B Inhibitors"],"prefix":"10.1002","volume":"350","author":[{"given":"Changcheng","family":"Jing","sequence":"first","affiliation":[{"name":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development School of Chemistry and Molecular Engineering East China Normal University Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ziyan","family":"Li","sequence":"additional","affiliation":[{"name":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development School of Chemistry and Molecular Engineering East China Normal University Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kaili","family":"Jia","sequence":"additional","affiliation":[{"name":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development School of Chemistry and Molecular Engineering East China Normal University Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chen","family":"Chen","sequence":"additional","affiliation":[{"name":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development School of Chemistry and Molecular Engineering East China Normal University Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiao","family":"Liu","sequence":"additional","affiliation":[{"name":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development School of Chemistry and Molecular Engineering East China Normal University Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Beibei","family":"Wang","sequence":"additional","affiliation":[{"name":"Chinese National Center for Drug Screening State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wenhao","family":"Hu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jia","family":"Li","sequence":"additional","affiliation":[{"name":"Chinese National Center for Drug Screening State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tong","family":"Zhu","sequence":"additional","affiliation":[{"name":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development School of Chemistry and Molecular Engineering East China Normal University Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Suzhen","family":"Dong","sequence":"additional","affiliation":[{"name":"Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development School of Chemistry and Molecular Engineering East China Normal University Shanghai China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2016,12,28]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.271.33.19810"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1074\/jbc.272.3.1639"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1086\/339270"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1128\/MCB.20.15.5479-5489.2000"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.283.5407.1544"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1073\/pnas.142298199"},{"key":"e_1_2_7_8_1","first-page":"331","volume":"6","author":"Liu G.","year":"2004","journal-title":"Curr. 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