Id: acc2249
Group: 2sens
Protein: RB1
Gene Symbol: RB1
Protein Id: P06400
Protein Name: RB_HUMAN
PTM: phosphorylation
Site: Thr356
Site Sequence: SIDSFETQRTPRKSNLDEEVN
Disease Category: Cancer
Disease: Head and Neck Cancer
Disease Subtype: HNSCC
Disease Cellline: SCC61
Disease Info:
Drug: palbociclib(CDK4/6 inhibitors)
Drug Info: "Palbociclib is a selective oral cyclin-dependent kinase 4/6 (CDK4/6) inhibitor approved for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer in combination with endocrine therapies such as aromatase inhibitors or fulvestrant. "
Effect: modulate
Effect Info: "When receiving surgery or surgery plus radiotherapy, the median survival time of tumor patients with low pT356RB1 levels is almost four times that of patients with high pT356RB1 expression."
Note:
Score: 4.0
Pubmed(PMID): 26265441
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-Thr356
Cancer Intensity
BRCA
COAD -0.816
HGSC 0.881
ccRCC
GBM -0.914
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.85

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 356 U Ovarian cancer/carcinoma Phosphorylation 28319064
T 356 U Squamous cell carcinoma Phosphorylation 26265441

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 Thr356 TLQTDSIDSFETQRT(ph)PR A549 Staursporin 6.3161 down
P06400 RB1 P Thr356 LFLDHDKTLQTDSIDSFETQRT(ph)PR A549 Staursporin 6.4743 down
P06400 RB1 P Thr356 LFLDHDKTLQTDSIDSFETQRT(ph)PR A549 Dasatinib 8.7153 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR K562 Paclitaxel 7.5238 -
P06400 RB1 P Thr356 LFLDHDKTLQTDSIDSFETQRT(ph)PR K562 Paclitaxel 8.7492 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A549 Tideglusib 7.7718 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A549 Refametinib 6.9355 -
P06400 RB1 P Thr356 LFLDHDKTLQTDSIDSFETQRT(ph)PR A549 Refametinib 8.7832 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A549 Pictilisib 5.7612 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A549 PD325901 9.0731 -
P06400 RB1 P Thr356 LFLDHDKTLQTDSIDSFETQRT(ph)PR A549 Nintedanib 5.2492 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A549 Dasatinib 5.0787 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A549 Dasatinib 7.2207 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Afatinib 8.4298 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A549 AZD8055 8.8775 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Gefitinib 6.7699 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Gefitinib 5.4291 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Gefitinib 7.5513 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Gefitinib 2 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Dasatinib 6.0442 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Dasatinib 2 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Dasatinib 5.5741 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Dasatinib 5.7699 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Afatinib 8.6577 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Afatinib 6.6511 -
P06400 RB1 P Thr356 TLQTDSIDSFETQRT(ph)PR A431 Afatinib 2 -

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: