Literature DB >> 15109663

A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.

David W Borhani1, David J Calderwood, Michael M Friedman, Gavin C Hirst, Biqin Li, Adelaine K W Leung, Brad McRae, Sheldon Ratnofsky, Kurt Ritter, Wendy Waegell.   

Abstract

We have identified the pyrazolo[3,4-d]pyrimidine A-420983 (compound 7) as a potent inhibitor of lck. A-420983 exhibits oral efficacy in animal models of delayed-type hypersensitivity and organ transplant rejection.

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Year:  2004        PMID： 15109663     DOI： 10.1016/j.bmcl.2004.02.101

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


  6 in total

1.  Molecular pathway profiling of T lymphocyte signal transduction pathways; Th1 and Th2 genomic fingerprints are defined by TCR and CD28-mediated signaling.

Authors:  Ruben L Smeets; Wilco W M Fleuren; Xuehui He; Paul M Vink; Frank Wijnands; Monika Gorecka; Henri Klop; Sussane Bauerschmidt; Anja Garritsen; Hans J P M Koenen; Irma Joosten; Annemieke M H Boots; Wynand Alkema
Journal:  BMC Immunol       Date:  2012-03-14       Impact factor: 3.615

2.  NRF2 activator A-1396076 ameliorates inflammation in autoimmune disease models by inhibiting antigen dependent T cell activation.

Authors:  Christian Goess; Sonia Terrillon; Martha Mayo; Peter Bousquet; Craig Wallace; Michelle Hart; Suzanne Mathieu; Rachel Twomey; Diana Donnelly-Roberts; Marian Namovic; Paul Jung; Min Hu; Paul Richardson; Tim Esbenshade; Carolyn A Cuff
Journal:  J Transl Autoimmun       Date:  2020-12-23

3.  New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011-2021) focussing on structure-activity relationship (SAR) and docking insights.

Authors:  Ahmed Elkamhawy; Eslam M H Ali; Kyeong Lee
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

4.  Damnacanthal, an effective inhibitor of LIM-kinase, inhibits cell migration and invasion.

Authors:  Kazumasa Ohashi; Kaori Sampei; Mami Nakagawa; Naoto Uchiumi; Tatsuya Amanuma; Setsuya Aiba; Masato Oikawa; Kensaku Mizuno
Journal:  Mol Biol Cell       Date:  2014-01-29       Impact factor: 4.138

5.  Inhibition of lymphangiogenesis in vitro and in vivo by the multikinase inhibitor nintedanib.

Authors:  Tong Lin; Lan Gong
Journal:  Drug Des Devel Ther       Date:  2017-04-05       Impact factor: 4.162

6.  Imaging alloreactive T cells provides early warning of organ transplant rejection.

Authors:  Toshihito Hirai; Aaron T Mayer; Tomomi W Nobashi; Po-Yu Lin; Zunyu Xiao; Tomokatsu Udagawa; Kinya Seo; Federico Simonetta; Jeanette Baker; Alan G Cheng; Robert S Negrin; Sanjiv S Gambhir
Journal:  JCI Insight       Date:  2021-07-08
  6 in total

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