| Id: | acc0850 |
| Group: | 2sens |
| Protein: | AKT |
| Gene Symbol: | Akt1 |
| Protein Id: | P47196 |
| Protein Name: | AKT1_RAT |
| PTM: | phosphorylation |
| Site: | Ser473 |
| Site Sequence: | ERRPHFPQFSYSASGTA---- |
| Disease Category: | Endocrine and metabolic diseases |
| Disease: | Pituitary Tumor |
| Disease Subtype: | |
| Disease Cellline: | GH3 |
| Disease Info: | |
| Drug: | BEZ235 |
| Drug Info: | "BEZ235 is a dual pan-class I PI3K and mTOR inhibitor targeting p110alpha/gamma/delta/beta isoforms (IC50: 4nM/5nM/7nM/75nM) and mTOR (IC50: 20.7nM), primarily used in preclinical research." |
| Effect: | modulate |
| Effect Info: | "In vitro, BEZ235 reduced the phosphorylation levels of Akt and pS6, as well as the phosphorylation of mTOR at the Ser2448 site, in a dose - dependent manner. However, in in - vivo models, BEZ235 significantly increased the phosphorylation of Akt, which may lead to cell resistance." |
| Note: | |
| Score: | 4.0 |
| Pubmed(PMID): | 26983879 |
| Sentence Index: | 26983879_5-6 |
| Sentence: | "In vivo, the effect was transient, with a decrease in mitotic index and increase in apoptosis; long-term treatment had no significant inhibitory effect on tumor growth. In contrast, while NVP-BKM120 had little effect in vitro, it dramatically limited tumor growth in vivo Increased Akt phosphorylation observed only in the NVP-BEZ235-treated tumors may explain the differential response to the two inhibitors." |
Sequence & Structure:
MNDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVEQRESPLNNFSVAQCQLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKRQEEETMDFRSGSPSDNSGAEEMEVALAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKILKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLSRERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGIKDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFELILMEEIRFPRTLGPEAKSLLSGLLKKDPTQRLGGGSEDAKEIMQHRFFANIVWQDVYEKKLSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
No data.
No data.
Protein Tractability:
source: Open TargetsNo data.
PTM Intensity:
source: CPTACNo data.
PTM-Disease Association:
source: PTMD| Residue | Position | State | Disease | Class | PMID |
|---|---|---|---|---|---|
| S | 473 | D | Major depressive disorder | Phosphorylation | 16959794 |
| S | 473 | D | Type 2 diabetes | Phosphorylation | 34057658 ; 36374861 |
| S | 473 | U | Status epilepticus | Phosphorylation | 35562960 |
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: DecryptMNo data.
Function score:
source: funscoRNo data.
