Id: acc4282
Group: 1sens
Protein: FOXO3a
Gene Symbol: Foxo3
Protein Id: O43524
Protein Name: FOXO3_HUMAN
PTM: phosphorylation
Site: Ser253
Site Sequence: GKAPRRRAVSMDNSNKYTKSR
Disease Category: Endocrine and metabolic diseases
Disease: Diabetes Mellitus
Disease Subtype: type 1 diabetic
Disease Cellline:
Disease Info:
Drug: Lapatinib
Drug Info: Lapatinib is a medication used in the treatment of certain types of breast cancer. It works by inhibiting specific proteins involved in cancer cell growth.
Effect: modulate
Effect Info: "Lapatinib treatment also significantly attenuated the increased phosphorylation levels of EGFR, ErbB2, ERK1/2, AKT, ROCK2, and IkB - alpha induced by diabetes, and normalized the reduced levels of phosphorylated FOXO3A and eNOS (Ser1177) in diabetic MVBs. "
Note:
Score: 4.0
Pubmed(PMID): 26114862
Sentence Index:
Sentence:

Sequence & Structure:

MAEAPASPAPLSPLEVELDPEFEPQSRPRSCTWPLQRPELQASPAKPSGETAADSMIPEEEDDEDDEDGGGRAGSAMAIGGGGGSGTLGSGLLLEDSARVLAPGGQDPGSGPATAAGGLSGGTQALLQPQQPLPPPQPGAAGGSGQPRKCSSRRNAWGNLSYADLITRAIESSPDKRLTLSQIYEWMVRCVPYFKDKGDSNSSAGWKNSIRHNLSLHSRFMRVQNEGTGKSSWWIINPDGGKSGKAPRRRAVSMDNSNKYTKSRGRAAKKKAALQTAPESADDSPSQLSKWPGSPTSRSSDELDAWTDFRSRTNSNASTVSGRLSPIMASTELDEVQDDDAPLSPMLYSSSASLSPSVSKPCTVELPRLTDMAGTMNLNDGLTENLMDDLLDNITLPPSQPSPTGGLMQRSSSFPYTTKGSGLGSPTSSFNSTVFGPSSLNSLRQSPMQTIQENKPATFSSMSHYGNQTLQDLLTSDSLSHSDVMMTQSDPLMSQASTAVSAQNSRRNVMLRNDPMMSFAAQPNQGSLVNQNLLHHQHQTQGALGGSRALSNSVSNMGLSESSSLGSAKHQQQSPVSQSMQTLSDSLSGSSLYSTSANLPVMGHEKFPSDLDLDMFNGSLECDMESIIRSELMDADGLDFNFDSLISTQNVVGLNVGNFTGAKQASSQSWVPG

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

No data.

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 253 U Breast cancer Phosphorylation 36797347
S 253 U Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 24067903

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
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK BT-474 Pertuzumab -4.1912 up
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Afatinib 8.0116 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK PC-9 Lapatinib 6.2743 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK PC-9 GeftinibAZD4547-1to80 8.5342 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK BT-474 Lapatinib 5.9797 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Gefitinib 6.455 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Gefitinib 6.3906 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Gefitinib 6.5284 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Gefitinib 6.0854 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Gefitinib 6.1089 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Dasatinib 5.6546 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Dasatinib 5.8236 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Afatinib 8.1476 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Afatinib 7.9038 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Afatinib 7.7225 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Dasatinib 5.7235 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Afatinib 7.9491 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Afatinib 8.0487 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Afatinib 7.9485 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Dasatinib 6.0991 down
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Dasatinib 5.9459 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Dasatinib 5.8337 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Dasatinib 5.7274 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Dasatinib 5.7384 down
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK PC-9 Gefitinib 3.646 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK PC-9 Gefitinib 6.0289 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK PC-9 AZD4547 5.5207 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK PC-9 AZD4547 10.2858 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK MDA-MB-175 Trastuzumab -3.2585 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK HeLa A486 6.5779 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK HeLa A485 6.2502 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK PC-9 Lapatinib 6.712 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK BT-474 Trastuzumab -4.7623 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK A549 PD325901 7.2718 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK BT-474 Trastuzumab -1.3222 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK BT-474 Pertuzumab -3.8033 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A549 PD325901 4.8628 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK A459 Selumetinib 5.0307 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A459 Selumetinib 8.5854 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Imatinib 9.0922 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNKYTK A431 Imatinib 13.0022 -
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Gefitinib 6.6699 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Gefitinib 6.1431 -
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Gefitinib 6.167 -
O43524 FOXO3 P Ser253 AVS(ph)MDNSNK A431 Dasatinib 7.2507 -
O43524 FOXO3 P Ser253 RAVS(ph)MDNSNK A431 Dasatinib 7.2514 -

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: