Id: | acc3295 |
Group: | 2sens |
Protein: | ERRgamma |
Gene Symbol: | ESRRG |
Protein Id: | P62508 |
Protein Name: | ERR3_HUMAN |
PTM: | phosphorylation |
Site: | Ser57 |
Site Sequence: | SLTDSVNHHSPGGSSDASGSY |
Disease Category: | Cancer |
Disease: | Breast Cancer |
Disease Subtype: | ER+ |
Disease Cellline: | MCF-7 |
Disease Info: | |
Drug: | tamoxifen (TAM) |
Drug Info: | Tamoxifen (TAM) is a well - known drug often used in the treatment of breast cancer. It works by interfering with the effects of estrogen in the breast tissue. |
Effect: | inhibit |
Effect Info: | "The RK/MAPK signaling pathway promotes the tamoxifen - resistant phenotype mediated by ERRγ by phosphorylating ERRγ to enhance its protein stability and transcriptional activity. Mutating the ERK target site weakens the activity of ERRγ and tamoxifen resistance, suggesting that ERRγ phosphorylation plays a key regulatory role in the development of breast cancer resistance. " |
Note: | |
Score: | 5.0 |
Pubmed(PMID): | 24684682 |
Sentence Index: | 24684682_3-4 |
Sentence: | "The resistant phenotype is usually not driven by loss or mutation of the estrogen receptor; instead, changes in multiple proliferative and/or survival pathways over-ride the inhibitory effects of TAM. Estrogen-related receptor gamma (ERRgamma) is an orphan member of the nuclear receptor superfamily that promotes TAM resistance in ER+ breast cancer cells." |
Sequence & Structure:
MDSVELCLPESFSLHYEEELLCRMSNKDRHIDSSCSSFIKTEPSSPASLTDSVNHHSPGGSSDASGSYSSTMNGHQNGLDSPPLYPSAPILGGSGPVRKLYDDCSSTIVEDPQTKCEYMLNSMPKRLCLVCGDIASGYHYGVASCEACKAFFKRTIQGNIEYSCPATNECEITKRRRKSCQACRFMKCLKVGMLKEGVRLDRVRGGRQKYKRRIDAENSPYLNPQLVQPAKKPYNKIVSHLLVAEPEKIYAMPDPTVPDSDIKALTTLCDLADRELVVIIGWAKHIPGFSTLSLADQMSLLQSAWMEILILGVVYRSLSFEDELVYADDYIMDEDQSKLAGLLDLNNAILQLVKKYKSMKLEKEEFVTLKAIALANSDSMHIEDVEAVQKLQDVLHEALQDYEAGQHMEDPRRAGKMLMTLPLLRQTSTKAVQHFYNIKLEGKVPMHKLFLEMLEAKV
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
ESRRG | AFIMOXIFENE | Estrogen-related receptor gamma antagonist | 2 | Completed | breast ductal carcinoma in situ | ClinicalTrials |
ESRRG | AFIMOXIFENE | Estrogen-related receptor gamma antagonist | 2 | Recruiting | breast ductal carcinoma in situ | ClinicalTrials ClinicalTrials |
ESRRG | AFIMOXIFENE | Estrogen-related receptor gamma antagonist | 2 | Completed | mastodynia | ClinicalTrials |
ESRRG | AFIMOXIFENE | Estrogen-related receptor gamma antagonist | 2 | Completed | breast cancer | ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACNo data.
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.