This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.


1q8w

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:1q8w.jpg|left|200px]]
+
{{Seed}}
 +
[[Image:1q8w.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_1q8w| PDB=1q8w | SCENE= }}
{{STRUCTURE_1q8w| PDB=1q8w | SCENE= }}
-
'''The Catalytic Subunit of cAMP-dependent Protein Kinase in Complex with Rho-kinase Inhibitor Fasudil (HA-1077)'''
+
===The Catalytic Subunit of cAMP-dependent Protein Kinase in Complex with Rho-kinase Inhibitor Fasudil (HA-1077)===
-
==Overview==
+
<!--
-
Protein kinases require strict inactivation to prevent spurious cellular signaling; overactivity can cause cancer or other diseases and necessitates selective inhibition for therapy. Rho-kinase is involved in such processes as tumor invasion, cell adhesion, smooth muscle contraction, and formation of focal adhesion fibers, as revealed using inhibitor Y-27632. Another Rho-kinase inhibitor, HA-1077 or Fasudil, is currently used in the treatment of cerebral vasospasm; the related nanomolar inhibitor H-1152P improves on its selectivity and potency. We have determined the crystal structures of HA-1077, H-1152P, and Y-27632 in complexes with protein kinase A (PKA) as a surrogate kinase to analyze Rho-kinase inhibitor binding properties. Features conserved between PKA and Rho-kinase are involved in the key binding interactions, while a combination of residues at the ATP binding pocket that are unique to Rho-kinase may explain the inhibitors' Rho-kinase selectivity. Further, a second H-1152P binding site potentially points toward PKA regulatory domain interaction modulators.
+
The line below this paragraph, {{ABSTRACT_PUBMED_14656443}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 14656443 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_14656443}}
==About this Structure==
==About this Structure==
Line 38: Line 42:
[[Category: Rho-kinase]]
[[Category: Rho-kinase]]
[[Category: Serine/threonine-protein kinase]]
[[Category: Serine/threonine-protein kinase]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 06:00:48 2008''
+
 
 +
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 05:16:42 2008''

Revision as of 02:16, 28 July 2008

Image:1q8w.png

Template:STRUCTURE 1q8w

The Catalytic Subunit of cAMP-dependent Protein Kinase in Complex with Rho-kinase Inhibitor Fasudil (HA-1077)

Template:ABSTRACT PUBMED 14656443

About this Structure

1Q8W is a Protein complex structure of sequences from Bos taurus. Full crystallographic information is available from OCA.

Reference

Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity., Breitenlechner C, Gassel M, Hidaka H, Kinzel V, Huber R, Engh RA, Bossemeyer D, Structure. 2003 Dec;11(12):1595-607. PMID:14656443

Page seeded by OCA on Mon Jul 28 05:16:42 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1q8w"
Personal tools