Id: acc0021
Group: 1sens
Protein: Rb
Gene Symbol: RB1
Protein Id: P06400
Protein Name: RB_HUMAN
PTM: phosphorylation
Site: Ser795
Site Sequence: PRSPYKFPSSPLRIPGGNIYI
Disease Category: Cancer
Disease: Pancreas Cancer
Disease Subtype:
Disease Cellline: CFPAC-1
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 the 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-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: