| Id: | acc1680 |
| Group: | 2sens |
| Protein: | ERalpha |
| Gene Symbol: | Esr1 |
| Protein Id: | P19785 |
| Protein Name: | ESR1_MOUSE |
| PTM: | phosphorylation |
| Site: | Ser118 |
| Site Sequence: | PSPLMLLHPPPQLSPFLHPHG |
| Disease Category: | Endocrine and metabolic diseases |
| Disease: | Prolactinoma |
| Disease Subtype: | |
| Disease Cellline: | MMQ/BRO |
| 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 via pERalpha. The ERalpha inhibitor (fulvestrant) can restore the sensitivity of adenoma cells to bromocriptine." |
| Note: | |
| Score: | 5.0 |
| Pubmed(PMID): | 33173437 |
| Sentence Index: | 33173437_7-8 |
| Sentence: | "ERalpha inhibition abolished E2-induced PRLR upregulation and PRL-induced ERalpha phosphorylation, and fulvestrant, an ERalpha inhibitor, restored pituitary adenoma cell sensitivity to bromocriptine by activating JNK-MEK/ERK-p38 MAPK signaling and cyclin D1 downregulation. Collectively, these data suggest that the interaction between the estrogen/ERalpha and PRL/PRLR pathways may contribute to bromocriptine resistance, and therefore, that combination treatment with fulvestrant and bromocriptine (as opposed to either drug alone) may exert potent antitumor effects on bromocriptine-resistant prolactinomas." |
Sequence & Structure:
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKMPMERALGEVYVDNSKPTVFNYPEGAAYEFNAAAAAAAAASAPVYGQSGIAYGPGSEAAAFSANSLGAFPQLNSVSPSPLMLLHPPPQLSPFLHPHGQQVPYYLENEPSAYAVRDTGPPAFYRSNSDNRRQNGRERLSSSNEKGNMIMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDLEGRNEMGASGDMRAANLWPSPLVIKHTKKNSPALSLTADQMVSALLDAEPPMIYSEYDPSRPFSEASMMGLLTNLADRELVHMINWAKRVPGFGDLNLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAPNLLLDRNQGKCVEGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNSGVYTFLSSTLKSLEEKDHIHRVLDKITDTLIHLMAKAGLTLQQQHRRLAQLLLILSHIRHMSNKGMEHLYNMKCKNVVPLYDLLLEMLDAHRLHAPASRMGVPPEEPSQTQLATTSSTSAHSLQTYYIPPEAEGFPNTI
No data.
No data.
Protein Tractability:
source: Open TargetsNo data.
PTM Intensity:
source: CPTACNo data.
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.
