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| | ==3D structures of Rho-associated protein kinase== | | ==3D structures of Rho-associated protein kinase== |
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| - | [[Rho-associated protein kinase]] | + | [[Rho-associated protein kinase 3D structures]] |
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| - | Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | |
| - | {{#tree:id=OrganizedByTopic|openlevels=0| | |
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| - | *Rho-associated protein kinase 1; domains – kinase 6-415; coiled-coil 535-700; Shroom-binding 834-914; Rho-binding 947-1015 | |
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| - | **[[4l2w]] – hROCK1 Shroom-binding domain - human<br /> | |
| - | **[[3o0z]] – hROCK1 coiled-coil domain <br /> | |
| - | **[[5wne]], [[5wnf]], [[5wng]], [[5wnh]], [[6e9w]], [[5hvu]], [[4yvc]], [[4yve]], [[5bml]], [[4w7p]], [[3twj]], [[3tv7]], [[3v8s]], [[3ncz]], [[3ndm]], [[3d9v]], [[2esm]], [[2etk]], [[2etr]], [[5uzj]], [[7jou]] – hROCK1 kinase domain + anti-cancer inhibitor <br /> | |
| - | **[[5f5p]] – hROCK1 Shroom-binding domain + Shroom2 <br /> | |
| - | **[[2v55]] – hROCK1 kinase domain + RhoE + GDP + ANP <br /> | |
| - | **[[1s1c]] – hROCK1 Rho-binding domain + RhoA + GNP<br /> | |
| - | **[[1uix]] – bROCK1 coiled-coil domain 979-1047 - bovine<br /> | |
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| - | *Rho-associated protein kinase 2 | |
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| - | **[[2f2u]] – hROCK2 kinase domain <br /> | |
| - | **[[4wot]], [[4l6q]], [[2h9v]], [[5u7q]], [[5u7r]], [[6ed6]], [[7jnt]], [[7jov]] – hROCK2 kinase domain + inhibitor <br /> | |
| - | **[[6p5m]], [[6p5p]] – hROCK2 kinase domain + anti-cancer inhibitor <br /> | |
| - | **[[2rov]] – hROCK2 split PH domain - NMR<br /> | |
| - | **[[2row]] – hROCK2 C1 domain - NMR<br /> | |
| - | }} | |
| | == References == | | == References == |
| | <references/> | | <references/> |
| | </StructureSection> | | </StructureSection> |
| | [[Category:Topic Page]] | | [[Category:Topic Page]] |
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Function
Rho-associated protein kinase (ROCK) is a Rho GTPase effector. ROCK has been shown to regulate cadherin function and thus cell-cell adhesion[1]. ROCKs phosphorylate a large number of actin-binding proteins to modulate their functions. ROCKs are kinases belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine specific protein kinases.
Disease
Aberrant ROCK expression and activation contribute to cancer development. ROCK levels are elevated in testicular, bladder and esophageal cancers[2].
Relevance
ROCK inhibitors have potential to be developed for treatment of glaucoma and other ocular diseases[3].
Structural highlights
ROCK contains several domains including (in ROCK1) a kinase domain (residues 76-338); a coiled-coil region (residues 339-1103) which contains a Rho-binding domain (residues 934-1015) and a pleckstrin homology and cysteine-rich domain (residues 1103-1320) at the C-terminal. making interactions with a [4].
3D structures of Rho-associated protein kinase
Rho-associated protein kinase 3D structures
References
- ↑ Smith AL, Dohn MR, Brown MV, Reynolds AB. Association of Rho-associated protein kinase 1 with E-cadherin complexes is mediated by p120-catenin. Mol Biol Cell. 2012 Jan;23(1):99-110. doi: 10.1091/mbc.E11-06-0497. Epub 2011 Oct, 26. PMID:22031287 doi:http://dx.doi.org/10.1091/mbc.E11-06-0497
- ↑ Schofield AV, Bernard O. Rho-associated coiled-coil kinase (ROCK) signaling and disease. Crit Rev Biochem Mol Biol. 2013 Jul-Aug;48(4):301-16. doi:, 10.3109/10409238.2013.786671. Epub 2013 Apr 19. PMID:23601011 doi:http://dx.doi.org/10.3109/10409238.2013.786671
- ↑ Honjo M, Tanihara H, Inatani M, Kido N, Sawamura T, Yue BY, Narumiya S, Honda Y. Effects of rho-associated protein kinase inhibitor Y-27632 on intraocular pressure and outflow facility. Invest Ophthalmol Vis Sci. 2001 Jan;42(1):137-44. PMID:11133858
- ↑ Green J, Cao J, Bandarage UK, Gao H, Court J, Marhefka C, Jacobs M, Taslimi P, Newsome D, Nakayama T, Shah S, Rodems S. Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors. J Med Chem. 2015 Jun 12. PMID:26039570 doi:http://dx.doi.org/10.1021/acs.jmedchem.5b00424
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