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Cover Picture: Design and Synthesis of Potent and Selective Azaindole‐Based Rho Kinase (ROCK) Inhibitors (ChemMedChem 12/2008)
Author(s) -
Schirok Hartmut,
Kast Raimund,
FigueroaPérez Santiago,
Bennabi Samir,
Gnoth Mark J.,
Feurer Achim,
Heckroth Heike,
Thutewohl Michael,
Paulsen Holger,
Knorr Andreas,
Hütter Joachim,
Lobell Mario,
Münter Klaus,
Geiß Volker,
Ehmke Heimo,
Lang Dieter,
Radtke Martin,
Mittendorf Joachim,
Stasch JohannesPeter
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200890046
Subject(s) - chemistry , rho associated protein kinase , stereochemistry , kinase , biophysics , crystallography , biochemistry , biology
The cover picture shows the 2D chemical structure of Bayer Schering's azaindole‐based Rho kinase (ROCK) inhibitor, and also its 3D tube model docked into the ATP binding site of ROCK‐1 (X‐ray crystallographic structure). The kinase protein is mostly shown as a ribbon diagram with the β‐sheet lobe on the left, the hinge region at the bottom, and the α‐helical lobe on the right. The gatekeeper methionine and some additional key residues are also shown in tube representation. The depicted inhibitor was identified as a highly selective and orally available ROCK inhibitor, which leads to sustained blood pressure reduction in vivo. For more details, see the Full Paper by H. Schirok et al. on p. 1893 ff.