Inside Cover

Inside Cover: Design and Biological Evaluation of Novel, Balanced Dual PPARα/γ Agonists (ChemMedChem 6/2009)

  1. Uwe Grether Dr.1,
  2. Agnes Bénardeau Dr.1,
  3. Jörg Benz Dr.1,
  4. Alfred Binggeli1,
  5. Denise Blum1,
  6. Hans Hilpert Dr.1,
  7. Bernd Kuhn Dr.1,
  8. Hans Peter Märki Dr.1,
  9. Markus Meyer Dr.2,
  10. Peter Mohr Dr.1,
  11. Kurt Püntener Dr.1,
  12. Susanne Raab Dr.1,
  13. Armin Ruf Dr.1,
  14. Daniel Schlatter Dr.1

Article first published online: 28 MAY 2009

DOI: 10.1002/cmdc.200990027

Issue

ChemMedChem

ChemMedChem

Special Issue: XIX NMMC Verona 2008

Volume 4, Issue 6, page 886, June 8, 2009

Additional Information

How to Cite

Grether, U., Bénardeau, A., Benz, J., Binggeli, A., Blum, D., Hilpert, H., Kuhn, B., Märki, H. P., Meyer, M., Mohr, P., Püntener, K., Raab, S., Ruf, A. and Schlatter, D. (2009), Inside Cover: Design and Biological Evaluation of Novel, Balanced Dual PPARα/γ Agonists (ChemMedChem 6/2009). ChemMedChem, 4: 886. doi: 10.1002/cmdc.200990027

Author Information

  1. 1

    Pharma Research, F. Hoffmann-La Roche Ltd., 4070 Basel (Switzerland), Fax: (+41) 61688544

  2. 2

    Pharma Development, F. Hoffmann-La Roche Ltd., 4070 Basel (Switzerland)

Publication History

  1. Issue published online: 28 MAY 2009
  2. Article first published online: 28 MAY 2009

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Keywords:

  • aryl propionic acids;
  • drug design;
  • PPAR;
  • receptors;
  • X-ray crystal structures

Abstract

Thumbnail image of graphical abstract

The inside cover picture shows the X-ray-determined binding of an α-ethoxy-phenyl-propionic acid-derived dual PPARα/γ agonist in complex with PPARα (yellow) and PPARγ (blue). The high α-selectivity of this phenylthiazole (IC50 γ/α = 37; EC50 γ/α = 7) can be rationalized mainly by a single residue difference, Cys 275 (α) vs. Gly 284 (γ), leading to three additional interactions with the terminal p-Cl-Ph group. In addition, its binding site is highlighted in a surface representation of the PPARα protein. For more details, see the Communication by U. Grether et al. on p. 951 ff.

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