| Id: | acc3448 |
| Group: | 2sens |
| Protein: | PFKFB3 |
| Gene Symbol: | PFKFB3 |
| Protein Id: | Q16875 |
| Protein Name: | F263_HUMAN |
| PTM: | phosphorylation |
| Site: | Ser461 |
| Site Sequence: | GPNPLMRRNSVTPLASPEPTK |
| Disease Category: | Cancer |
| Disease: | Lung Cancer |
| Disease Subtype: | NSCLC |
| Disease Cellline: | PC9 |
| Disease Info: | |
| Drug: | erlotinib |
| Drug Info: | Erlotinib is a drug used in the treatment of non - small cell lung cancer and pancreatic cancer. It works by blocking the action of an abnormal protein that signals cancer cells to grow. |
| Effect: | suppress |
| Effect Info: | Long - term exposure of NSCLC cells to the tyrosine kinase inhibitor (TKI) erlotinib drives the expression of PFKFB3 (Ser461). Chemical inhibition of PFKFB3 in combination with erlotinib can enhance the anti - proliferative activity of erlotinib in NSCLC cells. |
| Note: | |
| Score: | 5.0 |
| Pubmed(PMID): | 31126985 |
| Sentence Index: | 31126985_7-8 |
| Sentence: | "We demonstrate that exposing NSCLC cells harboring either WT or mutated EGFR to EGF rapidly increases PFKFB3 phosphorylation, expression, and activity and that PFKFB3 inhibition markedly reduces the EGF-mediated increase in glycolysis. Furthermore, we found that prolonged NSCLC cell exposure to the TKI erlotinib drives PFKFB3 expression and that chemical PFKFB3 inhibition synergizes with erlotinib in increasing erlotinib's anti-proliferative activity in NSCLC cells." |
Sequence & Structure:
MPLELTQSRVQKIWVPVDHRPSLPRSCGPKLTNSPTVIVMVGLPARGKTYISKKLTRYLNWIGVPTKVFNVGEYRREAVKQYSSYNFFRPDNEEAMKVRKQCALAALRDVKSYLAKEGGQIAVFDATNTTRERRHMILHFAKENDFKAFFIESVCDDPTVVASNIMEVKISSPDYKDCNSAEAMDDFMKRISCYEASYQPLDPDKCDRDLSLIKVIDVGRRFLVNRVQDHIQSRIVYYLMNIHVQPRTIYLCRHGENEHNLQGRIGGDSGLSSRGKKFASALSKFVEEQNLKDLRVWTSQLKSTIQTAEALRLPYEQWKALNEIDAGVCEELTYEEIRDTYPEEYALREQDKYYYRYPTGESYQDLVQRLEPVIMELERQENVLVICHQAVLRCLLAYFLDKSAEEMPYLKCPLHTVLKLTPVAYGCRVESIYLNVESVCTHRERSEDAKKGPNPLMRRNSVTPLASPEPTKKPRINSFEEHVASTSAALPSCLPPEVPTQLPGQNMKGSRSSADSSRKH
Select PDB:
No data.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTAC| PFKFB3-Ser461 | |
|---|---|
| Cancer | Intensity |
| BRCA | 2.294 |
| COAD | |
| HGSC | |
| ccRCC | 0.179 |
| GBM | -0.038 |
| HNSC | -0.714 |
| LUAD | |
| LUSC | -0.522 |
| non_ccRCC | -0.915 |
| PDAC | 0.005 |
| UCEC | -0.29 |
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.
