Id: acc0636
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: ACHN
Disease Info:
Drug: sunitinib
Drug Info: Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor used in the treatment of gastrointestinal stromal tumors (GIST) and metastatic renal cell carcinoma (RCC) in patients who are resistant or intolerant to prior therapy.
Effect: inhibit
Effect Info: "NC886 promotes EMT by facilitating the nuclear translocation of beta-catenin mediated by Rock2 phosphorylation, thereby enhancing 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: