Id: acc1681
Group: 2sens
Protein: ERalpha
Gene Symbol: ESR1
Protein Id: P03372
Protein Name: ESR1_HUMAN
PTM: phosphorylation
Site: Ser118
Site Sequence: MLLHPPPQLSPFLQPHGQQVP
Disease Category: Endocrine and metabolic diseases
Disease: Prolactinoma
Disease Subtype:
Disease Cellline:
Disease Info:
Drug: bromocriptine
Drug Info: "Bromocriptine is a potent dopamine D2 receptor agonist used in the treatment of hyperprolactinemia, Parkinson's disease, pituitary prolactinomas, and acromegaly, as well as for suppressing lactation and managing restless legs syndrome. "
Effect: inhibit
Effect Info: "In patients or cells resistant to bromocriptine, the expression levels of ERalpha and PRLR proteins are high. PRL promotes the phosphorylation of ERalpha through the JAK2 - PI3K/Akt - MEK/ERK pathway, while estrogen upregulates PRLR through pERalpha. The ERalpha inhibitor (fulvestrant) can restore the sensitivity of adenoma cells to bromocriptine."
Note:
Score: 5.0
Pubmed(PMID): 33173437
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 118 U Breast cancer Phosphorylation 20418363 ;  19104930 ;  16168121 ;  19940281 ;  12118371 ;  12118371 ;  16168121 ;  19104930 ;  19940281 ;  20418363 ;  25531331 ;  3
S 118 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: