Id: acc2287
Group: 2sens
Protein: RB
Gene Symbol: RB1
Protein Id: P06400
Protein Name: RB_HUMAN
PTM: phosphorylation
Site: Ser807
Site Sequence: RIPGGNIYISPLKSPYKISEG
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype: EGFR-high/ERBB2-amplified
Disease Cellline: HCC1954
Disease Info:
Drug: erlotinib + trastuzumab
Drug Info: "Erlotinib is a first-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor used primarily in the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations, as well as pancreatic cancer in combination with chemotherapy. Trastuzumab is a humanized monoclonal antibody targeting HER2/neu receptors, approved for HER2-positive breast cancer and metastatic gastric or gastroesophageal junction adenocarcinoma."
Effect: modulate
Effect Info: "Erlotinib significantly reduces the phosphorylation levels of RPS6 and RB by inhibiting the EGFR signaling pathway, thereby suppressing the growth and proliferation of tumor cells."
Note:
Score: 4.0
Pubmed(PMID): 23552733
Sentence Index:
Sentence:

Sequence & Structure:

MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTALCQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIAAVDLDEMSFTFTELQKNIEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSSISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYKTAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFMNSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDARLFLDHDKTLQTDSIDSFETQRTPRKSNLDEEVNVIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVKDIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDNIFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEGNLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNHTAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYLRLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLKFKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMDTSNKEEK

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

No data.

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
RB1-Ser807
Cancer Intensity
BRCA
COAD -0.643
HGSC -0.466
ccRCC
GBM -0.785
HNSC -0.414
LUAD 1.544
LUSC -0.86
non_ccRCC
PDAC 1.566
UCEC 0.058

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 807 D Ovarian cancer/carcinoma Phosphorylation 28319064
S 807 D Skin cancer Phosphorylation 23888052
S 807 U Intraocular melanoma Phosphorylation 10969768 ;  10969768
S 807 U Bladder cancer Phosphorylation 22787429
S 807 U Neuroendocrine cancer/carcinoma Phosphorylation 24135281
S 807 U Melanoma Phosphorylation 15502804 ;  10969768 ;  10969768 ;  15502804 ;  15502804
S 807 U Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 23408967
S 807 U Cervical cancer Phosphorylation 33516252

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
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 Staursporin 6.5006 up
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A549 Staursporin 6.6237 up
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A549 Nintedanib 5.3381 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Gefitinib 6.2454 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Gefitinib 5.7048 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 AZD8055 7.8834 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A549 AZD8055 7.4705 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 AZD8055 6.0392 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 Dactolisib 10.8604 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 Dactolisib 10.167 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A549 Dactolisib 8.227 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 Dasatinib 10.6727 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A549 Dasatinib 9.0233 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 Dasatinib 6.7852 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 Dasatinib 6.4918 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 Dasatinib 6.2296 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 Nintedanib 8.0388 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Gefitinib 7.2253 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 Nintedanib 5.2746 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 PD325901 9.0766 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 PD325901 6.9109 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 Pictilisib 10.5849 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 Pictilisib 6.0753 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A549 Pictilisib 5.8979 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A549 Refametinib 2 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 Staursporin 11.4859 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A549 Tideglusib 10.5827 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A549 Tideglusib 9.9041 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A549 Tideglusib 4.8968 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Dasatinib 2 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Afatinib 7.2979 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Afatinib 7.0918 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Afatinib 7.4741 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Afatinib 2 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Afatinib 10.2657 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Afatinib 8.3885 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Afatinib 2 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Afatinib 7.9573 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Afatinib 7.9015 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Afatinib 7.8323 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Dasatinib 12.3408 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Dasatinib 7.2827 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Dasatinib 9.4125 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Afatinib 7.9664 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Dasatinib 8.9649 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Dasatinib 7.2151 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Dasatinib 7.104 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Dasatinib 9.0028 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Dasatinib 6.6454 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Dasatinib 2 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Gefitinib 7.7927 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Gefitinib 7.2868 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Gefitinib 2 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLK A431 Gefitinib 11.9361 -
P06400 RB1 P Ser807;Ser811 IPGGNIYIS(ph)PLKS(ph)PYK A431 Gefitinib 8.2708 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Gefitinib 2 -
P06400 RB1 P Ser807 IPGGNIYIS(ph)PLKSPYK A431 Gefitinib 6.2129 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: