Literature DB >> 11294386

The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.

S J Macdonald1, M D Dowle, L A Harrison, P Shah, M R Johnson, G G Inglis, G D Clarke, R A Smith, D Humphreys, C R Molloy, A Amour, M Dixon, G Murkitt, R E Godward, T Padfield, T Skarzynski, O M Singh, K A Kumar, G Fleetwood, S T Hodgson, G W Hardy, H Finch.   

Abstract

The discovery of a potent intracellular inhibitor of human neutrophil elastase which is orally active and has a long duration of action is described. The pharmacodynamic and pharmacokinetic properties of a trans-lactam development candidate, GW311616A, are described.

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Year:  2001        PMID： 11294386     DOI： 10.1016/s0960-894x(01)00078-6

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  15 in total

1.  Development of cell-based assays for in vitro characterization of hepatitis C virus NS3/4A protease inhibitors.

Authors:  Victoria Chung; Anthony R Carroll; Norman M Gray; Nigel R Parry; Pia A Thommes; K Claire Viner; Eric A D'Souza
Journal:  Antimicrob Agents Chemother       Date:  2005-04       Impact factor: 5.191

2.  The protective function of neutrophil elastase inhibitor in liver ischemia/reperfusion injury.

Authors:  Yoichiro Uchida; Maria Cecilia S Freitas; Danyun Zhao; Ronald W Busuttil; Jerzy W Kupiec-Weglinski
Journal:  Transplantation       Date:  2010-05-15       Impact factor: 4.939

3.  Neutrophil extracellular traps sequester circulating tumor cells and promote metastasis.

Authors:  Jonathan Cools-Lartigue; Jonathan Spicer; Braedon McDonald; Stephen Gowing; Simon Chow; Betty Giannias; France Bourdeau; Paul Kubes; Lorenzo Ferri
Journal:  J Clin Invest       Date:  2013-07-01       Impact factor: 14.808

4.  The inhibition of neutrophil elastase ameliorates mouse liver damage due to ischemia and reperfusion.

Authors:  Yoichiro Uchida; Maria Cecilia S Freitas; Danyun Zhao; Ronald W Busuttil; Jerzy W Kupiec-Weglinski
Journal:  Liver Transpl       Date:  2009-08       Impact factor: 5.799

5.  SerpinB1 Promotes Pancreatic β Cell Proliferation.

Authors:  Abdelfattah El Ouaamari; Ercument Dirice; Nicholas Gedeon; Jiang Hu; Jian-Ying Zhou; Jun Shirakawa; Lifei Hou; Jessica Goodman; Christos Karampelias; Guifeng Qiang; Jeremie Boucher; Rachael Martinez; Marina A Gritsenko; Dario F De Jesus; Sevim Kahraman; Shweta Bhatt; Richard D Smith; Hans-Dietmar Beer; Prapaporn Jungtrakoon; Yanping Gong; Allison B Goldfine; Chong Wee Liew; Alessandro Doria; Olov Andersson; Wei-Jun Qian; Eileen Remold-O'Donnell; Rohit N Kulkarni
Journal:  Cell Metab       Date:  2015-12-15       Impact factor: 27.287

6.  Imbalance between neutrophil elastase and its inhibitor α1-antitrypsin in obesity alters insulin sensitivity, inflammation, and energy expenditure.

Authors:  Virginie Mansuy-Aubert; Qiong L Zhou; Xiangyang Xie; Zhenwei Gong; Jun-Yuan Huang; Abdul R Khan; Gregory Aubert; Karla Candelaria; Shantele Thomas; Dong-Ju Shin; Sarah Booth; Shahid M Baig; Ahmed Bilal; Daehee Hwang; Hui Zhang; Robin Lovell-Badge; Steven R Smith; Fazli R Awan; Zhen Y Jiang
Journal:  Cell Metab       Date:  2013-04-02       Impact factor: 27.287

7.  Neutrophil elastase and myeloperoxidase regulate the formation of neutrophil extracellular traps.

Authors:  Venizelos Papayannopoulos; Kathleen D Metzler; Abdul Hakkim; Arturo Zychlinsky
Journal:  J Cell Biol       Date:  2010-10-25       Impact factor: 10.539

8.  Neutrophil elastase and its therapeutic effect on leukemia cells.

Authors:  Kai-Ling Jiang; Peng-Peng Ma; Xiao-Qun Yang; Liang Zhong; Hui Wang; Xin-Yu Zhu; Bei-Zhong Liu
Journal:  Mol Med Rep       Date:  2015-06-17       Impact factor: 2.952

9.  A myeloperoxidase-containing complex regulates neutrophil elastase release and actin dynamics during NETosis.

Authors:  Kathleen D Metzler; Christian Goosmann; Aleksandra Lubojemska; Arturo Zychlinsky; Venizelos Papayannopoulos
Journal:  Cell Rep       Date:  2014-07-24       Impact factor: 9.423

10.  Neutrophils mediate insulin resistance in mice fed a high-fat diet through secreted elastase.

Authors:  Saswata Talukdar; Da Young Oh; Gautam Bandyopadhyay; Dongmei Li; Jianfeng Xu; Joanne McNelis; Min Lu; Pingping Li; Qingyun Yan; Yimin Zhu; Jachelle Ofrecio; Michael Lin; Martin B Brenner; Jerrold M Olefsky
Journal:  Nat Med       Date:  2012-09       Impact factor: 53.440
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