Id: acc2248
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: FaDu
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: The median survival time of tumor patients with low levels of pT356RB1 is almost four times that of patients with high pT356RB1 expression when they receive surgery or surgery plus radiotherapy.
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: