Id: acc4883
Group: 1sens
Protein: PKM2
Gene Symbol: PKM
Protein Id: P14618
Protein Name: KPYM_HUMAN
PTM: phosphorylation
Site: Tyr105
Site Sequence: ESFASDPILYRPVAVALDTKG
Disease Category: Endocrine and metabolic diseases
Disease: High Glucose
Disease Subtype:
Disease Cellline: HUVECs
Disease Info:
Drug: TEPP-46
Drug Info: TEPP-46 is a chemical compound that may be used in pharmacological research or as a drug candidate.
Effect: modulate
Effect Info: TEPP - 46 → Inhibit PKM2 phosphorylation → Inhibit eNOS phosphorylation. The conclusion is that p - PKM2 may be involved in the process of endothelial - dependent vasodilation dysfunction in type 2 diabetes by inhibiting the p - eNOS(Ser1177)/NO pathway.
Note:
Score: 4.0
Pubmed(PMID): 37539568
Sentence Index:
Sentence:

Sequence & Structure:

MSKPHSEAGTAFIQTQQLHAAMADTFLEHMCRLDIDSPPITARNTGIICTIGPASRSVETLKEMIKSGMNVARLNFSHGTHEYHAETIKNVRTATESFASDPILYRPVAVALDTKGPEIRTGLIKGSGTAEVELKKGATLKITLDNAYMEKCDENILWLDYKNICKVVEVGSKIYVDDGLISLQVKQKGADFLVTEVENGGSLGSKKGVNLPGAAVDLPAVSEKDIQDLKFGVEQDVDMVFASFIRKASDVHEVRKVLGEKGKNIKIISKIENHEGVRRFDEILEASDGIMVARGDLGIEIPAEKVFLAQKMMIGRCNRAGKPVICATQMLESMIKKPRPTRAEGSDVANAVLDGADCIMLSGETAKGDYPLEAVRMQHLIAREAEAAIYHLQLFEELRRLAPITSDPTEATAVGAVEASFKCCSGAIIVLTKSGRSAHQVARYRPRAPIIAVTRNPQTARQAHLYRGIFPVLCKDPVQEAWAEDVDLRVNFAMNVGKARGFFKKGDVVIVLTGWRPGSGFTNTMRVVPVP

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

No data.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC
PKM-Tyr105
Cancer Intensity
BRCA
COAD 0.101
HGSC 1.503
ccRCC
GBM -0.058
HNSC 0.541
LUAD -0.685
LUSC
non_ccRCC -1.402
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 105 P Pancreatic cancer Phosphorylation 36244646
Y 105 P Lung adenocarcinoma Phosphorylation 36428781
Y 105 U Breast cancer Phosphorylation 29440169
Y 105 U Prostate cancer Phosphorylation 36400183
Y 105 U Cervical cancer Phosphorylation 33800513
Y 105 U Head and neck squamous cell carcinoma Phosphorylation 35054968

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: DecryptM
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK A549 Dasatinib 11.1239 -
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK A549 PD325901 10.9252 -
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK Ramos Rituximab -7.4771 -
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK Ramos Rituximab -2.9008 -
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK Ramos Rituximab -2.088 -
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK Ramos Rituximab -1.4437 -
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK Ramos Rituximab -0.8108 -
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK RPMI8226 BTZ 8.5367 -
P14618 PKM P Tyr105 TATESFASDPILY(ph)RPVAVALDTK RPMI8226 BTZ 7.3588 -

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: funscoR

No data.

Cross Links: