Id: acc1583
Group: 2sens
Protein: ERalpha
Gene Symbol: ESR1
Protein Id: P03372
Protein Name: ESR1_HUMAN
PTM: phosphorylation
Site: Ser305
Site Sequence: LMIKRSKKNSLALSLTADQMV
Disease Category: Cancer
Disease: Breast Cancer
Disease Subtype:
Disease Cellline: MCF7
Disease Info:
Drug: PGE2
Drug Info: -
Effect: modulate
Effect Info: "PGE2 can rapidly induce the phosphorylation of ERalpha and the activation of ERK, Akt, and PKA, and induce the expression of CYP1B1, which can promote tumor growth or drug resistance. Moreover, COX - 2 inhibitors can inhibit the PGE2 - induced expression of CYP1B1."
Note:
Score: 4.0
Pubmed(PMID): 20093341
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

No intensity data of this site,
show all other sites!

ESR1-Ser167
Cancer Intensity
BRCA -0.707
COAD
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.707
ESR1-Ser294
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 305 U Breast cancer/tumor/carcinoma Phosphorylation 24166501
S 305 U Breast cancer Phosphorylation 26272591 ;  15193262 ;  20179234 ;  15193262 ;  20179234 ;  24449872 ;  26272591

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: