Id: acc1677
Group: 2sens
Protein: ERalpha
Gene Symbol: ESR1
Protein Id: P03372
Protein Name: ESR1_HUMAN
PTM: phosphorylation
Site: Ser167
Site Sequence: RQGGRERLASTNDKGSMAMES
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype:
Disease Cellline: MCF7
Disease Info:
Drug: LY294002
Drug Info: "LY294002 is a broad-spectrum PI3K inhibitor targeting PI3Kalpha/delta/beta with IC50 values of 0.5 μM, 0.57 μM, and 0.97 μM, respectively, and also inhibits casein kinase 2 (CK2) with an IC50 of 98 nM, primarily used as a research tool to block the PI3K/Akt signaling pathway and autophagosome formation. "
Effect: resist
Effect Info: "ROS can phosphorylate estrogen receptor alpha (ERalpha) at serine 118 and 167 sites, leading to ligand - independent activation or down - regulation of ERalpha, which may be associated with the occurrence of endocrine therapy resistance."
Note:
Score: 5.0
Pubmed(PMID): 18941890
Sentence Index:
Sentence:

Sequence & Structure:

MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVHMINWAKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLDKITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSNKGMEHLYSMKCKNVVPLYDLLLEMLDAHRLHAPTSRGGASVEETDQSHLATAGSTSSHSLQKYYITGEAEGFPATV

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
ESR1 TOREMIFENE CITRATE Estrogen receptor modulator 4 - breast carcinoma DailyMed
DailyMed
ESR1 FULVESTRANT Estrogen receptor antagonist 4 - breast carcinoma DailyMed
ESR1 CLOMIPHENE CITRATE Estrogen receptor alpha modulator 4 - infertility DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
ESR1 CLOMIPHENE CITRATE Estrogen receptor alpha modulator 4 Completed infertility ClinicalTrials
ClinicalTrials
ESR1 CLOMIPHENE CITRATE Estrogen receptor alpha modulator 4 Unknown status infertility ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ESR1 DIETHYLSTILBESTROL DIPHOSPHATE Estrogen receptor agonist 4 - neoplasm ATC
ESR1 POLYESTRADIOL PHOSPHATE Estrogen receptor alpha agonist 4 - neoplasm ATC
ESR1 FULVESTRANT Estrogen receptor antagonist 4 - neoplasm ATC
ESR1 ETHINYL ESTRADIOL Estrogen receptor alpha agonist 4 - neoplasm ATC
ESR1 TAMOXIFEN Estrogen receptor alpha modulator 4 - neoplasm ATC
ESR1 DIETHYLSTILBESTROL Estrogen receptor alpha agonist 4 - neoplasm ATC
ESR1 CLOMIPHENE CITRATE Estrogen receptor alpha modulator 4 - polycystic ovary syndrome DailyMed
ESR1 CLOMIPHENE CITRATE Estrogen receptor alpha modulator 4 Completed polycystic ovary syndrome ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
ESR1 CLOMIPHENE CITRATE Estrogen receptor alpha modulator 4 Terminated polycystic ovary syndrome ClinicalTrials
ESR1 CLOMIPHENE CITRATE Estrogen receptor alpha modulator 4 Unknown status polycystic ovary syndrome ClinicalTrials
ClinicalTrials
ESR1 ESTETROL Estrogen receptor agonist 4 - pregnancy FDA
ESR1 ESTROPIPATE Estrogen receptor alpha agonist 4 - osteoporosis DailyMed
ESR1 ESTROGENS, CONJUGATED Estrogen receptor agonist 4 - osteoporosis DailyMed
ESR1 FULVESTRANT Estrogen receptor antagonist 4 - breast neoplasm EMA
ESR1 FULVESTRANT Estrogen receptor antagonist 4 Terminated breast neoplasm ClinicalTrials
ESR1 ELACESTRANT HYDROCHLORIDE Estrogen receptor alpha degrader 4 - breast neoplasm FDA
ESR1 ESTRADIOL Estrogen receptor alpha agonist 4 - osteoporosis DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
DailyMed
ESR1 ESTRADIOL Estrogen receptor alpha agonist 4 - postmenopausal osteoporosis DailyMed
DailyMed
DailyMed
ESR1 LASOFOXIFENE TARTRATE Estrogen receptor modulator 4 - postmenopausal osteoporosis EMA
ESR1 ESTROGENS, CONJUGATED Estrogen receptor agonist 4 - postmenopausal osteoporosis DailyMed
DailyMed
DailyMed

Note: Only show clinically investigational or approved drugs with protein targets.

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
ESR1-Ser167
Cancer Intensity
BRCA -0.707
COAD
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.707

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 167 U Breast cancer/tumor/carcinoma Phosphorylation 19940156 ;  17157789 ;  24166501
S 167 U Breast cancer Phosphorylation 20418363 ;  19104930 ;  16168121 ;  17157789 ;  17157789 ;  16168121 ;  19104930 ;  20418363
S 167 U Endometrial cancer/carcinoma Phosphorylation 23530112

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

No data.

Function score:

source: funscoR

No data.

Cross Links: