Abstract:
:Rho-kinase is a main player in the regulation of cytoskeletal events and a promising drug target in the treatment of both vascular and neurological disorders. Here we report the crystal structure of the Rho-kinase catalytic domain in complex with the specific inhibitor Y-27632. Comparison with the structure of PKA bound to this inhibitor revealed a potential induced-fit binding mode that can be accommodated by the phosphate binding loop. This binding mode resembles to that observed in the Rho-kinase-fasudil complex. A structural database search indicated that a pocket underneath the phosphate-binding loop is present that favors binding to a small aromatic ring. Introduction of such a ring group might spawn a new modification scheme of pre-existing protein kinase inhibitors for improved binding capability.
journal_name
J Biochemjournal_title
Journal of biochemistryauthors
Yamaguchi H,Miwa Y,Kasa M,Kitano K,Amano M,Kaibuchi K,Hakoshima Tdoi
10.1093/jb/mvj172subject
Has Abstractpub_date
2006-09-01 00:00:00pages
305-11issue
3eissn
0021-924Xissn
1756-2651pii
mvj172journal_volume
140pub_type
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