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Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.
Qiu, Zongxing; Kuhn, Bernd; Aebi, Johannes; Lin, Xianfeng; Ding, Haiyuan; Zhou, Zheng; Xu, Zhiheng; Xu, Danqing; Han, Li; Liu, Cheng; Qiu, Hongxia; Zhang, Yuxia; Haap, Wolfgang; Riemer, Claus; Stahl, Martin; Qin, Ning; Shen, Hong C; Tang, Guozhi.
Afiliação
  • Qiu Z; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Kuhn B; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.
  • Aebi J; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.
  • Lin X; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Ding H; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Zhou Z; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Xu Z; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Xu D; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Han L; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Liu C; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Qiu H; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Zhang Y; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Haap W; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.
  • Riemer C; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.
  • Stahl M; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.
  • Qin N; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Shen HC; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
  • Tang G; Roche Pharma Research and Early Development, Therapeutic Modalities, Roche Innovation Center Shanghai , 720 Cailun Road, Shanghai 201203, China.
ACS Med Chem Lett ; 7(8): 802-6, 2016 Aug 11.
Article em En | MEDLINE | ID: mdl-27563406
ATG4B or autophagin-1 is a cysteine protease that cleaves ATG8 family proteins. ATG4B plays essential roles in the autophagosome formation and the autophagy pathway. Herein we disclose the design and structural modifications of a series of fluoromethylketone (FMK)-based peptidomimetics as highly potent ATG4B inhibitors. Their structure-activity relationship (SAR) and protease selectivity are also discussed.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2016 Tipo de documento: Article País de afiliação: China País de publicação: Estados Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2016 Tipo de documento: Article País de afiliação: China País de publicação: Estados Unidos