Id: acc3648
Group: 1sens
Protein: pRb
Gene Symbol: RB1
Protein Id: P06400
Protein Name: RB_HUMAN
PTM: phosphorylation
Site: Thr252
Site Sequence: VIPINGSPRTPRRGQNRSARI
Disease Category: Cancer
Disease: Leukemia
Disease Subtype: Myeloid Leukemia
Disease Cellline: MV4-11
Disease Info:
Drug: Transforming growth factor beta
Drug Info: "Transforming growth factor beta is a cytokine that plays a crucial role in various cellular processes such as cell growth, differentiation, and apoptosis."
Effect: no effect
Effect Info: Transforming growth factor beta dephosphorylates pRB in tumor cells.
Note: no effect
Score: 2.0
Pubmed(PMID): 11027571
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-Thr252
Cancer Intensity
BRCA
COAD -0.392
HGSC 0.883
ccRCC
GBM 0.465
HNSC 0.788
LUAD -1.849
LUSC 1.098
non_ccRCC
PDAC -0.735
UCEC -0.259

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 252 U Breast cancer/tumor/carcinoma Phosphorylation 17599043

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 Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Gefitinib 8.8586 -
P06400 RB1 P Thr252 TAVIPINGSPRT(ph)PR A549 Tideglusib 6.7698 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A549 Staursporin 7.642 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A549 PD325901 10.6071 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A549 Dasatinib 8.7717 -
P06400 RB1 P Thr252 TAVIPINGSPRT(ph)PR A549 Dasatinib 8.9576 -
P06400 RB1 P Thr252 TAVIPINGSPRT(ph)PR A549 Dactolisib 5.5441 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A549 Dactolisib 6.1766 -
P06400 RB1 P Thr252 TAVIPINGSPRT(ph)PR A549 AZD8055 7.5694 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Afatinib 7.2253 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Gefitinib 8.2497 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Gefitinib 7.9731 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Dasatinib 5.1816 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Dasatinib 7.148 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Dasatinib 6.2497 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Afatinib 7.7579 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Afatinib 7.1355 -
P06400 RB1 P Ser249;Thr252 TAVIPINGS(ph)PRT(ph)PR A431 Afatinib 8.5301 -

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: