Id: acc0016
Group: 1sens
Protein: Rb
Gene Symbol: RB1
Protein Id: P06400
Protein Name: RB_HUMAN
PTM: phosphorylation
Site: Ser807
Site Sequence: RIPGGNIYISPLKSPYKISEG
Disease Category: Cancer
Disease: Pancreas Cancer
Disease Subtype:
Disease Cellline: CAPAN1
Disease Info:
Drug: temozolomide(TMZ)
Drug Info: "Temozolomide (TMZ) is an alkylating chemotherapeutic agent primarily used in the treatment of glioblastoma multiforme, functioning by inhibiting DNA synthesis in cancer cells through methylation of guanine residues, and is often administered in combination with radiotherapy."
Effect: inhibit
Effect Info: "Methionine stress enhances the sensitivity of pancreatic tumor cells to DNA alkylating drugs, 5-fluorouracil, and radiation. Moreover, under methionine stress conditions, the sensitivity of cells to temozolomide increases."
Note:
Score: 5.0
Pubmed(PMID): 16170025
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: