Free for academic non-profit institutions. Other users need a Commercial license
This gene encodes a protein serine/threonine kinase that is activated when bound to the GTP-bound form of Rho. The small GTPase Rho regulates formation of focal adhesions and stress fibers of fibroblasts, as well as adhesion and aggregation of platelets and lymphocytes by shuttling between the inactive GDP-bound form and the active GTP-bound form. Rho is also essential in cytokinesis and plays a role in transcriptional activation by serum response factor. This protein, a downstream effector of Rho, phosphorylates and activates LIM kinase, which in turn, phosphorylates cofilin, inhibiting its actin-depolymerizing activity. A pseudogene, related to this gene, is also located on chromosome 18. [provided by RefSeq, Aug 2015]
ROCK1 (Rho Associated Coiled-Coil Containing Protein Kinase 1) is a Protein Coding gene. Diseases associated with ROCK1 include Pediatric Osteosarcoma and Hutchinson-Gilford Progeria Syndrome. Among its related pathways are NGF Pathway and Development Slit-Robo signaling. Gene Ontology (GO) annotations related to this gene include transferase activity, transferring phosphorus-containing groups and protein tyrosine kinase activity. An important paralog of this gene is ROCK2.
Rho-kinases (aka Rho-associated coiled-coil kinases or ROCKs) are serine/threonine kinases activated by RhoA GTPases. They are modulators of processes involving cytoskeletal rearrangement such as focal adhesion formation, cell motility and tumor cell invasion.
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0000166 | nucleotide binding | IEA | -- |
GO:0004672 | protein kinase activity | IEA,TAS | 8798490 |
GO:0004674 | protein serine/threonine kinase activity | IEA,TAS | -- |
GO:0005515 | protein binding | IPI | 10652353 |
GO:0005524 | ATP binding | IEA | -- |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0000139 | Golgi membrane | IEA | -- |
GO:0001726 | ruffle | ISS | -- |
GO:0005576 | extracellular region | TAS | -- |
GO:0005737 | cytoplasm | IBA | 21873635 |
GO:0005794 | Golgi apparatus | IEA | -- |
SuperPathway | Contained pathways | ||
---|---|---|---|
1 | Blood-Brain Barrier and Immune Cell Transmigration: VCAM-1/CD106 Signaling | ||
2 | Activation of cAMP-Dependent PKA |
Activation of cAMP-Dependent PKA
.77
cAMP Pathway
.77
|
Activation of PKA through GPCR
.71
PKA Signaling
.56
|
3 | Apoptotic execution phase |
.31
|
|
4 | EPH-Ephrin signaling |
Cytoskeleton remodeling Fibronectin-binding integrins in cell motility
.35
|
|
5 | Semaphorin interactions |
GO ID | Qualified GO term | Evidence | PubMed IDs |
---|---|---|---|
GO:0000281 | mitotic cytokinesis | IBA | 21873635 |
GO:0003180 | aortic valve morphogenesis | ISS | -- |
GO:0003383 | apical constriction | IEA | -- |
GO:0006468 | protein phosphorylation | IEA,IDA | 23093407 |
GO:0006915 | apoptotic process | IEA | -- |
Name | Status | Disease Links | Group | Role | Mechanism of Action | Clinical Trials |
---|---|---|---|---|---|---|
Netarsudil | Approved | Pharma | Target, inhibitor | 0 | ||
Hydroxyfasudil | Experimental | Pharma | Target, inhibitor | Rho-kinase inhibitor and vasodilator | 0 | |
Y-27632 | Experimental | Pharma | Target | ROCK inhibitor,potent and selective | 0 | |
(S)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLINE)SULFONYL]-HOMOPIPERAZINE | Experimental | Pharma | Target | 0 | ||
Ripasudil | Experimental | Pharma | Target, inhibitor | 0 |
Name | Synonyms | Role | CAS Number | PubChem IDs | PubMed IDs | |
---|---|---|---|---|---|---|
ADP |
|
Agonist, Full agonist, Partial agonist, Gating inhibitor, Antagonist | 58-64-0 | |||
Diglycerides Group A |
|
|
||||
Diglycerides Group B |
|
|
||||
Diglycerides Group C |
|
|
||||
Diglycerides Group D |
|
|
Compound | Action | Cas Number |
---|---|---|
Fasudil hydrochloride | Inhibitor of cyclic nucleotide dependent- and Rho-kinases | 105628-07-7 |
Glycyl-H 1152 dihydrochloride | Selective Rho-kinase (ROCK) inhibitor. More selective analog of H 1152 dihydrochloride (Cat. No. 2414) | 913844-45-8 |
H 1152 dihydrochloride | Selective Rho-kinase (ROCK) inhibitor | 871543-07-6 |
HA 1100 hydrochloride | Cell-permeable, selective Rho-kinase inhibitor | 155558-32-0 |
Y-27632 dihydrochloride | Selective p160ROCK inhibitor | 129830-38-2 |
Compound | Action | Cas Number |
---|---|---|
AS 1892802 | ROCK inhibitor,potent and ATP-competitive | 928320-12-1 |
Fasudil | calcium antagonist | 103745-39-7 |
Fasudil (HA-1077) HCl | Protein kinase inhibitor | 105628-07-7 |
GSK269962A | ROCK inhibitor | 850664-21-0 |
GSK429286A | Selective ROCK1/ROCK2 inhibitor | 864082-47-3 |
Hydroxyfasudil | Rho-kinase inhibitor and vasodilator | 105628-72-6 |
Hydroxyfasudil hydrochloride | Rho-kinase inhibitor and vasodilator | 155558-32-0 |
K-115 | 887375-67-9 | |
LX7101 HCL | Dual LIM-kinase and ROCK inhibitor | 1192189-69-7 |
Narciclasine | Modulates the Rho/ROCK/LIM kinase/cofilin pathway | 29477-83-6 |
RKI-1447 | Potent ROCK1/ROCK2 inhibitor | 1342278-01-6 |
SB 772077B dihydrochloride | 607373-46-6 | |
SLx-2119 | Selective ROCK2 inhibitor | 911417-87-3 |
Thiazovivin | ROCK inhibitor | 1226056-71-8 |
Y-27632 | ROCK inhibitor,potent and selective | 146986-50-7 |
Y-27632 dihydrochloride | ROCK1 inhibitor | 146986-50-7, 129830-38-2 |
Y-39983 dihydrochloride | ROCK family inhibitor | 173897-44-4 |
This gene was present in the common ancestor of animals and fungi.
Organism | Taxonomy | Gene | Similarity | Type | Details |
---|---|---|---|---|---|
Chimpanzee (Pan troglodytes) |
Mammalia | ROCK1 30 31 |
|
OneToOne | |
Platypus (Ornithorhynchus anatinus) |
Mammalia | ROCK1 31 |
|
OneToOne | |
Dog (Canis familiaris) |
Mammalia | ROCK1 30 31 |
|
OneToOne | |
Cow (Bos Taurus) |
Mammalia | ROCK1 30 31 |
|
OneToOne | |
Mouse (Mus musculus) |
Mammalia | Rock1 30 17 31 |
|
OneToOne | |
Oppossum (Monodelphis domestica) |
Mammalia | ROCK1 31 |
|
OneToOne | |
Rat (Rattus norvegicus) |
Mammalia | Rock1 30 |
|
||
Chicken (Gallus gallus) |
Aves | ROCK1 30 31 |
|
OneToOne | |
Lizard (Anolis carolinensis) |
Reptilia | ROCK1 31 |
|
OneToOne | |
Tropical Clawed Frog (Silurana tropicalis) |
Amphibia | rock1 30 |
|
||
Zebrafish (Danio rerio) |
Actinopterygii | rock1 30 31 |
|
OneToOne | |
Fruit Fly (Drosophila melanogaster) |
Insecta | rok 32 |
|
|
|
Worm (Caenorhabditis elegans) |
Secernentea | let-502 32 |
|
|
|
Baker's yeast (Saccharomyces cerevisiae) |
Saccharomycetes | CBK1 31 |
|
OneToMany | |
Sea Vase (Ciona intestinalis) |
Ascidiacea | Cin.501 30 |
|
SNP ID | Clinical significance and condition | Chr 18 pos | Variation | AA Info | Type |
---|---|---|---|---|---|
711996 | Benign: not provided | 21,006,451(-) | A/C | SYNONYMOUS_VARIANT | |
727646 | Likely Benign: not provided | 21,042,653(-) | T/C | SYNONYMOUS_VARIANT | |
769935 | Benign: not provided | 20,970,392(-) | T/G | SYNONYMOUS_VARIANT | |
777282 | Benign: not provided | 20,970,516(-) | G/A | INTRON_VARIANT | |
777895 | Benign: not provided | 20,984,522(-) | G/C | MISSENSE_VARIANT |
Variant ID | Type | Subtype | PubMed ID |
---|---|---|---|
dgv3324n100 | CNV | gain | 25217958 |
esv3306568 | CNV | mobile element insertion | 20981092 |
esv3308855 | CNV | mobile element insertion | 20981092 |
esv3327515 | CNV | insertion | 20981092 |
esv3433136 | CNV | insertion | 20981092 |
esv3437603 | CNV | insertion | 20981092 |
esv3573920 | CNV | gain | 25503493 |
esv3641928 | CNV | gain | 21293372 |
esv3641929 | CNV | gain | 21293372 |
esv3641931 | CNV | loss | 21293372 |
nsv833594 | CNV | gain+loss | 17160897 |
nsv960269 | CNV | duplication | 23825009 |
nsv960270 | CNV | duplication | 23825009 |
Disorder | Aliases | PubMed IDs |
---|---|---|
pediatric osteosarcoma |
|
|
hutchinson-gilford progeria syndrome |
|
|
corticobasal degeneration |
|
|
ocular hyperemia |
|
|
lung cancer |
|
|