Combining medicinal chemistry with chemogenomic and computer-aided structure-based design in development of novel kinase inhibitors

• Autorzy: Vieth M , Brooks H.B. , Hamdouchi C. , McMillen W. , Sawyer J.S. , Yingling J.M. , Zhang F.
• Języki publikacji: EN

Słowa kluczowe

EN

structure; X-ray crystallography; kinase inhibitor; protein class; genome; human genome; protein kinase

• Wydawca: -
• Czasopismo: Cellular and Molecular Biology Letters
• Rocznik: 2003
• Tom: 08
• Numer: 2A
• Opis fizyczny: p.566-567

Twórcy

autor

Vieth M

• Lilly Research Laboratories, Indianapolis, IN 46285, USA

autor

Brooks H.B.

autor

Hamdouchi C.

autor

McMillen W.

autor

Sawyer J.S.

autor

Yingling J.M.

autor

Zhang F.

Bibliografia

• 1. Manning, G., Whyte, D.B., Martinez, R., Hunter, T. and Sudarsanam, S. The protein kinase complement of the human genome. Science 298 (2002) 1912-1934.
• 2. Caron, P.R., Mullican, M.D., Mashal, R.D., Wilson, K.P. and Su, M.S. Chemogenomic approaches to drug discovery. Curr. Opin. Chem. Biol. 5 (2001) 464-470.
• 3. Hamdouchi, C., deBlas, J., del Prado, M., Gruber, J., Heinz, B.A. and Vance, L.2-Amino-3-substituted-6-[(E)-1-phenyl-2-(N-methylcarbamoyl) vinyl]imidazo[1,2-a]pyridines as a novel class of inhibitors of human rhinovirus: Stereospecific synthesis and antiviral activity. J. Med. Chem. 42 (1999) 50-59.
• 4. Vieth, M. and Cummin, D.J. DoMCoSAR: A novel approach for establishing the docking mode that is consistent with the structure-activity relationship. Application to HIV-1 protease inhibitors and VEGF receptor tyrosine kinase inhibitors. J. Med. Chem. 43 (2000) 3020-3032.
• 5. Sawyer, J.S., Anderson, B.D., Beight, D.W., Campbell, R.M. and Jones, M.L. Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-b type I receptor kinase domain. J. Med. Chem. (2003) in press.