| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369775 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
In the present work, conjugates of 5-isoquinolinesulfonylamides and d-arginine-rich peptides were developed into highly potent inhibitors for basophilic protein kinases. Based on Hidaka’s inhibitor H9, a generic fluorescent probe ARC-1083 was constructed possessing subnanomolar dissociation constant towards several kinases of the AGC-group. Thereafter, Hidaka’s inhibitor HA1077 or Fasudil was conjugated with oligo-d-arginine resulting in the compound ARC-3002 revealing high affinity towards ROCK-II (Kd = 20 pM) and over 160-fold selectivity compared to PKAc.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Darja Lavogina, Katrin Kalind, Jevgenia Bredihhina, Madis Hurt, Angela Vaasa, Marje Kasari, Erki Enkvist, Gerda Raidaru, Asko Uri,