Id: acc0637
Group: 1sens
Protein: Rock2
Gene Symbol: ROCK2
Protein Id: O75116
Protein Name: ROCK2_HUMAN
PTM: phosphorylation
Site: Ser1366
Site Sequence: PFARSSPRTSMKIQQNQSIRR
Disease Category: Cancer
Disease: Renal Cancer
Disease Subtype:
Disease Cellline: 786-O
Disease Info:
Drug: Everolimus
Drug Info: "Everolimus is a mammalian target of rapamycin (mTOR) inhibitor developed by Novartis, indicated for the treatment of advanced renal cell carcinoma, pancreatic neuroendocrine tumors, and tuberous sclerosis complex-related conditions such as subependymal giant cell astrocytoma and renal angiomyolipoma, functioning through suppression of mTOR kinase activity to inhibit tumor cell growth and proliferation. "
Effect: inhibit
Effect Info: "nc886 promotes EMT by facilitating the nuclear translocation of beta - catenin mediated by Rock2 phosphorylation, thereby promoting the resistance of renal cancer cells to sunitinib or everolimus."
Note:
Score: 5.0
Pubmed(PMID): 34974812
Sentence Index:
Sentence:

Sequence & Structure:

MSRPPPTGKMPGAPETAPGDGAGASRQRKLEALIRDPRSPINVESLLDGLNSLVLDLDFPALRKNKNIDNFLNRYEKIVKKIRGLQMKAEDYDVVKVIGRGAFGEVQLVRHKASQKVYAMKLLSKFEMIKRSDSAFFWEERDIMAFANSPWVVQLFYAFQDDRYLYMVMEYMPGGDLVNLMSNYDVPEKWAKFYTAEVVLALDAIHSMGLIHRDVKPDNMLLDKHGHLKLADFGTCMKMDETGMVHCDTAVGTPDYISPEVLKSQGGDGFYGRECDWWSVGVFLYEMLVGDTPFYADSLVGTYSKIMDHKNSLCFPEDAEISKHAKNLICAFLTDREVRLGRNGVEEIRQHPFFKNDQWHWDNIRETAAPVVPELSSDIDSSNFDDIEDDKGDVETFPIPKAFVGNQLPFIGFTYYRENLLLSDSPSCRETDSIQSRKNEESQEIQKKLYTLEEHLSNEMQAKEELEQKCKSVNTRLEKTAKELEEEITLRKSVESALRQLEREKALLQHKNAEYQRKADHEADKKRNLENDVNSLKDQLEDLKKRNQNSQISTEKVNQLQRQLDETNALLRTESDTAARLRKTQAESSKQIQQLESNNRDLQDKNCLLETAKLKLEKEFINLQSALESERRDRTHGSEIINDLQGRICGLEEDLKNGKILLAKVELEKRQLQERFTDLEKEKSNMEIDMTYQLKVIQQSLEQEEAEHKATKARLADKNKIYESIEEAKSEAMKEMEKKLLEERTLKQKVENLLLEAEKRCSLLDCDLKQSQQKINELLKQKDVLNEDVRNLTLKIEQETQKRCLTQNDLKMQTQQVNTLKMSEKQLKQENNHLMEMKMNLEKQNAELRKERQDADGQMKELQDQLEAEQYFSTLYKTQVRELKEECEEKTKLGKELQQKKQELQDERDSLAAQLEITLTKADSEQLARSIAEEQYSDLEKEKIMKELEIKEMMARHKQELTEKDATIASLEETNRTLTSDVANLANEKEELNNKLKDVQEQLSRLKDEEISAAAIKAQFEKQLLTERTLKTQAVNKLAEIMNRKEPVKRGNDTDVRRKEKENRKLHMELKSEREKLTQQMIKYQKELNEMQAQIAEESQIRIELQMTLDSKDSDIEQLRSQLQALHIGLDSSSIGSGPGDAEADDGFPESRLEGWLSLPVRNNTKKFGWVKKYVIVSSKKILFYDSEQDKEQSNPYMVLDIDKLFHVRPVTQTDVYRADAKEIPRIFQILYANEGESKKEQEFPVEPVGEKSNYICHKGHEFIPTLYHFPTNCEACMKPLWHMFKPPPALECRRCHIKCHKDHMDKKEEIIAPCKVYYDISTAKNLLLLANSTEEQQKWVSRLVKKIPKKPPAPDPFARSSPRTSMKIQQNQSIRRPSRQLAPNKPS

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
ROCK2 BELUMOSUDIL Rho-associated protein kinase inhibitor 4 - immune system disease ATC
ROCK2 NETARSUDIL DIMESYLATE Rho-associated protein kinase inhibitor 4 - open-angle glaucoma DailyMed
DailyMed
FDA
ROCK2 NETARSUDIL DIMESYLATE Rho-associated protein kinase inhibitor 4 - ocular hypertension DailyMed
FDA
DailyMed
ROCK2 BELUMOSUDIL MESYLATE Rho-associated protein kinase inhibitor 4 - graft versus host disease FDA
ROCK2 FASUDIL Rho-associated protein kinase inhibitor 3 - cardiovascular disease ATC
ROCK2 RIPASUDIL Rho-associated protein kinase inhibitor 3 Completed corneal edema ClinicalTrials
ROCK2 NETARSUDIL Rho-associated protein kinase inhibitor 3 - glaucoma ATC
ROCK2 RIPASUDIL Rho-associated protein kinase inhibitor 3 - glaucoma ATC
ROCK2 RIPASUDIL Rho-associated protein kinase inhibitor 3 Recruiting Fuchs' endothelial dystrophy ClinicalTrials
ROCK2 BELUMOSUDIL Rho-associated protein kinase inhibitor 3 Recruiting chronic graft versus host disease ClinicalTrials
ROCK2 RIPASUDIL Rho-associated protein kinase inhibitor 3 Recruiting Fuchs endothelial corneal dystrophy ClinicalTrials
ClinicalTrials
ROCK2 NETARSUDIL Rho-associated protein kinase inhibitor 3 Completed Fuchs endothelial corneal dystrophy ClinicalTrials
ROCK2 FASUDIL Rho-associated protein kinase inhibitor 2 Completed cardiovascular disease ClinicalTrials
ROCK2 BELUMOSUDIL Rho-associated protein kinase inhibitor 2 Terminated diffuse scleroderma ClinicalTrials
ClinicalTrials
ROCK2 BELUMOSUDIL Rho-associated protein kinase inhibitor 2 Completed psoriasis ClinicalTrials
ROCK2 BELUMOSUDIL Rho-associated protein kinase inhibitor 2 Completed idiopathic pulmonary fibrosis ClinicalTrials
ROCK2 SAR-407899 Rho-associated protein kinase inhibitor 2 Terminated coronary artery disease ClinicalTrials
ROCK2 SAR-407899 Rho-associated protein kinase inhibitor 2 Terminated coronary artery disease ClinicalTrials
ROCK2 FASUDIL Rho-associated protein kinase inhibitor 2 Terminated internal carotid artery stenosis ClinicalTrials
ROCK2 SAR-407899 Rho-associated protein kinase inhibitor 2 Completed erectile dysfunction ClinicalTrials
ROCK2 AMA0076 Rho-associated protein kinase inhibitor 2 Completed eye disease ClinicalTrials
ROCK2 DE-104 Rho-associated protein kinase inhibitor 2 Completed open-angle glaucoma ClinicalTrials
ClinicalTrials
ClinicalTrials
ROCK2 SAR-407899 Rho-associated protein kinase inhibitor 2 Completed erectile dysfunction ClinicalTrials
ROCK2 AMA0076 Rho-associated protein kinase inhibitor 2 Completed low tension glaucoma ClinicalTrials
ROCK2 FASUDIL Rho-associated protein kinase inhibitor 2 Unknown status retinal vein occlusion ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC

No intensity data of this site,
show all other sites!

ROCK2-Ser1047
Cancer Intensity
BRCA
COAD -0.591
HGSC 0.942
ccRCC -1.297
GBM
HNSC 1.036
LUAD -0.09
LUSC
non_ccRCC
PDAC
UCEC
ROCK2-Ser1048
Cancer Intensity
BRCA
COAD 1.377
HGSC -0.436
ccRCC -0.881
GBM
HNSC 1.286
LUAD 0.316
LUSC
non_ccRCC
PDAC -0.8
UCEC -0.863
ROCK2-Ser1051
Cancer Intensity
BRCA
COAD 1.353
HGSC
ccRCC -0.963
GBM
HNSC 0.092
LUAD
LUSC
non_ccRCC
PDAC
UCEC -0.483
ROCK2-Ser1276
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.707
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC -0.707
ROCK2-Ser1288
Cancer Intensity
BRCA
COAD -0.176
HGSC 1.555
ccRCC
GBM
HNSC
LUAD -1.509
LUSC 0.23
non_ccRCC 0.278
PDAC -0.379
UCEC
ROCK2-Ser1293
Cancer Intensity
BRCA 1.484
COAD -0.149
HGSC
ccRCC
GBM
HNSC 0.832
LUAD -1.014
LUSC -1.018
non_ccRCC
PDAC -0.136
UCEC
ROCK2-Ser337
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM -1.188
HNSC 1.223
LUAD -0.233
LUSC
non_ccRCC
PDAC
UCEC 0.198
ROCK2-Ser339
Cancer Intensity
BRCA
COAD
HGSC -1.428
ccRCC
GBM 0.562
HNSC
LUAD 0.8
LUSC
non_ccRCC
PDAC
UCEC 0.066
ROCK2-Ser676
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.11
GBM -1.432
HNSC
LUAD 0.839
LUSC 0.483
non_ccRCC
PDAC
UCEC
ROCK2-Ser844
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD -0.707
LUSC
non_ccRCC
PDAC
UCEC 0.707
ROCK2-Thr1126
Cancer Intensity
BRCA 0.495
COAD 0.384
HGSC
ccRCC -0.385
GBM
HNSC 1.672
LUAD -0.141
LUSC -0.069
non_ccRCC -1.907
PDAC -0.05
UCEC
ROCK2-Thr992
Cancer Intensity
BRCA -0.514
COAD
HGSC
ccRCC -0.112
GBM
HNSC
LUAD
LUSC 0.136
non_ccRCC
PDAC 1.584
UCEC -1.094

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 1366 U Breast adenocarcinoma Phosphorylation 22273145
S 1366 U Melanoma Phosphorylation 35718242

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: