Id: | acc1444 |
Group: | 2sens |
Protein: | ULK1 |
Gene Symbol: | ULK1 |
Protein Id: | O75385 |
Protein Name: | ULK1_HUMAN |
PTM: | phosphorylation |
Site: | Ser467 |
Site Sequence: | RSSAIRRSGSTSPLGFARASP |
Disease Category: | Cancer |
Disease: | Glioma |
Disease Subtype: | |
Disease Cellline: | U251? |
Disease Info: | |
Drug: | xanthatin |
Drug Info: | - |
Effect: | modulate |
Effect Info: | "Drugs kill tumors by increasing the phosphorylation of Akt (ser473), a downstream target of PI3K, and then directly activating mTORC1 through the phosphorylation of mTOR at the Ser2448 site, thereby reducing the level of phosphorylated ULK1." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 36572650 |
Sentence Index: | 36572650_4-5 |
Sentence: | "In this study, we report that xanthatin suppressed glioma cells proliferation and induced apoptosis in a time- and concentration-dependent manner, and was accompanied by autophagy inhibition displaying a significantly reduced LC3 punctate fluorescence and LC3II/I ratio, decreased level of Beclin 1, while increased accumulation of p62. Notably, treating glioma cells with xanthatin resulted in obvious activation of the PI3K-Akt-mTOR signaling pathway, as indicated by increased mTOR and Akt phosphorylation, decreased ULK1 phosphorylation, which is important in modulating autophagy." |
Sequence & Structure:
MEPGRGGTETVGKFEFSRKDLIGHGAFAVVFKGRHREKHDLEVAVKCINKKNLAKSQTLLGKEIKILKELKHENIVALYDFQEMANSVYLVMEYCNGGDLADYLHAMRTLSEDTIRLFLQQIAGAMRLLHSKGIIHRDLKPQNILLSNPAGRRANPNSIRVKIADFGFARYLQSNMMAATLCGSPMYMAPEVIMSQHYDGKADLWSIGTIVYQCLTGKAPFQASSPQDLRLFYEKNKTLVPTIPRETSAPLRQLLLALLQRNHKDRMDFDEFFHHPFLDASPSVRKSPPVPVPSYPSSGSGSSSSSSSTSHLASPPSLGEMQQLQKTLASPADTAGFLHSSRDSGGSKDSSCDTDDFVMVPAQFPGDLVAEAPSAKPPPDSLMCSGSSLVASAGLESHGRTPSPSPPCSSSPSPSGRAGPFSSSRCGASVPIPVPTQVQNYQRIERNLQSPTQFQTPRSSAIRRSGSTSPLGFARASPSPPAHAEHGGVLARKMSLGGGRPYTPSPQVGTIPERPGWSGTPSPQGAEMRGGRSPRPGSSAPEHSPRTSGLGCRLHSAPNLSDLHVVRPKLPKPPTDPLGAVFSPPQASPPQPSHGLQSCRNLRGSPKLPDFLQRNPLPPILGSPTKAVPSFDFPKTPSSQNLLALLARQGVVMTPPRNRTLPDLSEVGPFHGQPLGPGLRPGEDPKGPFGRSFSTSRLTDLLLKAAFGTQAPDPGSTESLQEKPMEIAPSAGFGGSLHPGARAGGTSSPSPVVFTVGSPPSGSTPPQGPRTRMFSAGPTGSASSSARHLVPGPCSEAPAPELPAPGHGCSFADPITANLEGAVTFEAPDLPEETLMEQEHTEILRGLRFTLLFVQHVLEIAALKGSASEAAGGPEYQLQESVVADQISLLSREWGFAEQLVLYLKVAELLSSGLQSAIDQIRAGKLCLSSTVKQVVRRLNELYKASVVSCQGLSLRLQRFFLDKQRLLDRIHSITAERLIFSHAVQMVQSAALDEMFQHREGCVPRYHKALLLLEGLQHMLSDQADIENVTKCKLCIERRLSALLTGICA
Select PDB:
No data.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACULK1-Ser467 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | |
GBM | |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC |
PTM-Disease Association:
source: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
S | 556 | D | Psoriasis | Phosphorylation | 34421918 |
S | 317 | D | Melanoma | Phosphorylation | 34759263 |
S | 757 | D | Melanoma | Phosphorylation | 34759263 |
S | 556 | D | Gastric cancer | Phosphorylation | 33037394 |
S | 555 | D | Melanoma | Phosphorylation | 34759263 |
K | 571 | P | Breast cancer | Ubiquitination | 35670107 |
S | 757 | P | Non-small cell lung cancer/carcinoma | Phosphorylation | 23921130 |
K | 568 | P | Breast cancer | Ubiquitination | 35670107 |
S | 495 | P | Breast cancer | Phosphorylation | 35670107 |
S | 495 | U | Glioma | Phosphorylation | 31378785 |
S | 757 | U | Melanoma | Phosphorylation | 34759263 |
S | 555 | U | Melanoma | Phosphorylation | 34759263 |
S | 533 | U | Glioma | Phosphorylation | 31378785 |
K | 68 | U | Acute liver failure | Acetylation | 33431796 |
S | 469 | U | Glioma | Phosphorylation | 31378785 |
S | 317 | U | Melanoma | Phosphorylation | 34759263 |
S | 317 | U | Late onset Parkinson's disease | Phosphorylation | 35605642 |
S | 555 | U | Granulomatosis with polyangiitis | Phosphorylation | 37720230 |
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: DecryptMProtein | Gene | PTM | Position | Modified sequence | Cell | Drug | pEC50 | Regulation | Experiment |
---|---|---|---|---|---|---|---|---|---|
O75385 | ULK1 | P | Ser467;Ser469 | SGS(ph)TS(ph)PLGFAR | A431 | Afatinib | 8.681 | - | |
O75385 | ULK1 | P | Ser467;Ser469 | SGS(ph)TS(ph)PLGFAR | A431 | Gefitinib | 9.1965 | - | |
O75385 | ULK1 | P | Ser467;Ser469 | SGS(ph)TS(ph)PLGFAR | BT-474 | Lapatinib | 6.0856 | - |
pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.
Function score:
source: funscoRNo data.