| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371537 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
Abstract
A novel class of selective inhibitors of ROCK1 and ROCK2 has been identified by structural based drug design. PK/PD experiments using a set of highly selective Rho kinase inhibitors suggest that systemic Rho kinase inhibition is linked to a reversible reduction in lymphocyte counts. These results led to the consideration of topical delivery of these molecules, and to the identification of a lead molecule 7 which shows promising PK and PD in a murine model of pulmonary hypertension after intra-tracheal dosing.
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Related Topics
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Chemistry
Organic Chemistry
Authors
Duncan Shaw, Greg Hollingworth, Nicolas Soldermann, Elizabeth Sprague, Walter Schuler, Eric Vangrevelinghe, Nicholas Duggan, Matthew Thomas, Takatoshi Kosaka, Nigel Waters, Maurice J. van Eis,