Communication

Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase

  1. Zhengying Pan Dr.1,
  2. Heleen Scheerens Dr.2,
  3. Shyr-Jiann Li Dr.2,
  4. Brian E. Schultz Dr.2,
  5. Paul A. Sprengeler Dr.1,
  6. L. Chuck Burrill1,
  7. Rohan V. Mendonca1,
  8. Michael D. Sweeney2,
  9. Keana C. K. Scott3,
  10. Paul G. Grothaus Dr.1,
  11. Douglas A. Jeffery Dr.2,
  12. Jill M. Spoerke Dr.2,
  13. Lee A. Honigberg Dr.2,4,
  14. Peter R. Young Dr.2,
  15. Stacie A. Dalrymple Dr.2,
  16. James T. Palmer Dr.1

Article first published online: 12 DEC 2006

DOI: 10.1002/cmdc.200600221

Issue

ChemMedChem

ChemMedChem

Volume 2, Issue 1, pages 58–61, January 15, 2007

Additional Information

How to Cite

Pan, Z., Scheerens, H., Li, S.-J., Schultz, Brian E., Sprengeler, Paul A., Burrill, L. Chuck., Mendonca, Rohan V., Sweeney, Michael D., Scott, Keana C. K., Grothaus, Paul G., Jeffery, Douglas A., Spoerke, Jill M., Honigberg, Lee A., Young, Peter R., Dalrymple, Stacie A. and Palmer, James T. (2007), Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase. ChemMedChem, 2: 58–61. doi: 10.1002/cmdc.200600221

Author Information

  1. 1

    Department of Medicinal Chemistry, Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA, Fax: (+1) 650-578-9680

  2. 2

    Department of Biology, Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA

  3. 3

    Informatics, Computational Science Group, Celera Genomics, 45 West Gude Drive, Rockville, MD 20850, USA

  4. 4

    Current Address: Pharmacyclics Inc. 995 E. Arques Ave., Sunnyvale, CA 94085, USA

Publication History

  1. Issue published online: 27 DEC 2006
  2. Article first published online: 12 DEC 2006
  3. Manuscript Received: 8 SEP 2006

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Keywords:

  • biological activity;
  • drug design;
  • enzymes;
  • medicinal chemistry;
  • structural bioinformatics
Thumbnail image of graphical abstract

A series of highly selective irreversible inhibitors for Bruton's tyrosine kinase (Btk) was developed using a structural bioinformatics approach. Their capabilities to modulate Btk's activity were characterized both in vitro and in vivo. Oral treatment with once-a-day dosing of compound 4 greatly inhibited disease development in a rodent rheumatoid arthritis (RA) model.

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