Id: acc1703
Group: 2sens
Protein: pRB
Gene Symbol: RB1
Protein Id: P06400
Protein Name: RB_HUMAN
PTM: phosphorylation
Site: Ser795
Site Sequence: PRSPYKFPSSPLRIPGGNIYI
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: NSCLC
Disease Cellline: Ma-10
Disease Info:
Drug: paclitaxel
Drug Info: "Paclitaxel is a plant-derived alkaloid and potent antineoplastic agent that stabilizes microtubules to inhibit cancer cell division, primarily used in the treatment of ovarian, breast, and lung cancers. "
Effect: sensitize
Effect Info: "ERK activation and subsequent pRB phosphorylation regulate the cell cycle, making tumor cells sensitive to paclitaxel."
Note:
Score: 5.0
Pubmed(PMID): 15138593
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-Ser795
Cancer Intensity
BRCA 1
COAD
HGSC 1.314
ccRCC 0.252
GBM
HNSC -0.957
LUAD -0.782
LUSC -0.826
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 795 D Skin cancer Phosphorylation 23888052
S 795 U Melanoma Phosphorylation 15502804 15502804 15502804

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 Ser795 SPYKFPSS(ph)PLR A549 Staursporin 5.9515 up
P06400 RB1 P Ser795 FPSS(ph)PLR A549 Dasatinib 6.6663 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Gefitinib 8.5113 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Gefitinib 6.2793 -
P06400 RB1 P Ser795 SPYKFPSS(ph)PLR A431 Gefitinib 5.3028 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Gefitinib 13.2099 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Gefitinib 7.2478 -
P06400 RB1 P Ser780;Ser788;Ser795 TNILQYASTRPPTLS(ph)PIPHIPRS(ph)PYKFPSS(ph)PLR A431 Gefitinib 5.3441 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Gefitinib 7.2524 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Gefitinib 6.187 -
P06400 RB1 P Ser795 FPSS(ph)PLR A549 AZD8055 7.7331 -
P06400 RB1 P Ser795 FPSS(ph)PLR A549 Dactolisib 8.783 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A549 Dasatinib 15 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Gefitinib 2 -
P06400 RB1 P Ser795 FPSS(ph)PLR A549 Dasatinib 6.0533 -
P06400 RB1 P Ser795 FPSS(ph)PLR A549 Nintedanib 7.6768 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A549 Pictilisib 10.9236 -
P06400 RB1 P Ser795 SPYKFPSS(ph)PLR A549 Pictilisib 6.309 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A549 Refametinib 15 -
P06400 RB1 P Ser795 FPSS(ph)PLR A549 Refametinib 9.4401 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A549 Staursporin 8.3624 -
P06400 RB1 P Ser795 FPSS(ph)PLR A549 Staursporin 6.3712 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A549 Tideglusib 8.7826 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Dasatinib 12.9897 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Afatinib 6.5269 -
P06400 RB1 P Ser780;Ser788;Ser795 TNILQYASTRPPTLS(ph)PIPHIPRS(ph)PYKFPSS(ph)PLR A431 Afatinib 6.4091 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Afatinib 6.6331 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Afatinib 5.4604 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Afatinib 8.7521 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Afatinib 8.2796 -
P06400 RB1 P Ser780;Tyr790;Ser795 TNILQYASTRPPTLS(ph)PIPHIPRSPY(ph)KFPSS(ph)PLR A431 Afatinib 4.641 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Afatinib 8.7822 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Afatinib 6.2606 -
P06400 RB1 P Ser780;Ser788;Ser795 TNILQYASTRPPTLS(ph)PIPHIPRS(ph)PYKFPSS(ph)PLR A431 Afatinib 5.5726 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Afatinib 9.3058 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Dasatinib 5.4737 -
P06400 RB1 P Ser795 SPYKFPSS(ph)PLR A431 Dasatinib 9.9229 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Dasatinib 5.3155 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Dasatinib 5.2464 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Dasatinib 7.2486 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Dasatinib 5.2098 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Dasatinib 9.7313 -
P06400 RB1 P Ser788;Ser795 S(ph)PYKFPSS(ph)PLR A431 Dasatinib 9.141 -
P06400 RB1 P Ser780;Ser788;Ser795 TNILQYASTRPPTLS(ph)PIPHIPRS(ph)PYKFPSS(ph)PLR A431 Gefitinib 8.0046 -
P06400 RB1 P Ser795 FPSS(ph)PLR A431 Gefitinib 5.4001 -

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: