Id: acc0486
Group: 2sens
Protein: STAT1
Gene Symbol: STAT1
Protein Id: P42224
Protein Name: STAT1_HUMAN
PTM: phosphorylation
Site: Ser727
Site Sequence: QTTDNLLPMSPEEFDEVSRIV
Disease Category: Cancer
Disease: Leukemia
Disease Subtype: AML
Disease Cellline: SET-2
Disease Info:
Drug: cortistatin A
Drug Info: "Cortistatin A is a natural steroidal alkaloid isolated from marine sponges, primarily studied for its potent anti-angiogenic and antiproliferative activities in preclinical research, particularly in the context of cancer therapeutics."
Effect: modulate
Effect Info: "Cortistatin A effectively inhibits the phosphorylation of STAT1(S727) in a dose-dependent manner, thereby suppressing the growth of JAK2-mutated AML."
Note:
Score: 4.0
Pubmed(PMID): 29239838
Sentence Index:
Sentence:

Sequence & Structure:

MSQWYELQQLDSKFLEQVHQLYDDSFPMEIRQYLAQWLEKQDWEHAANDVSFATIRFHDLLSQLDDQYSRFSLENNFLLQHNIRKSKRNLQDNFQEDPIQMSMIIYSCLKEERKILENAQRFNQAQSGNIQSTVMLDKQKELDSKVRNVKDKVMCIEHEIKSLEDLQDEYDFKCKTLQNREHETNGVAKSDQKQEQLLLKKMYLMLDNKRKEVVHKIIELLNVTELTQNALINDELVEWKRRQQSACIGGPPNACLDQLQNWFTIVAESLQQVRQQLKKLEELEQKYTYEHDPITKNKQVLWDRTFSLFQQLIQSSFVVERQPCMPTHPQRPLVLKTGVQFTVKLRLLVKLQELNYNLKVKVLFDKDVNERNTVKGFRKFNILGTHTKVMNMEESTNGSLAAEFRHLQLKEQKNAGTRTNEGPLIVTEELHSLSFETQLCQPGLVIDLETTSLPVVVISNVSQLPSGWASILWYNMLVAEPRNLSFFLTPPCARWAQLSEVLSWQFSSVTKRGLNVDQLNMLGEKLLGPNASPDGLIPWTRFCKENINDKNFPFWLWIESILELIKKHLLPLWNDGCIMGFISKERERALLKDQQPGTFLLRFSESSREGAITFTWVERSQNGGEPDFHAVEPYTKKELSAVTFPDIIRNYKVMAAENIPENPLKYLYPNIDKDHAFGKYYSRPKEAPEPMELDGPKGTGYIKTELISVSEVHPSRLQTTDNLLPMSPEEFDEVSRIVGSVEFDSMMNTV

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
STAT1-Ser727
Cancer Intensity
BRCA 0.237
COAD 0.528
HGSC -2.013
ccRCC -0.034
GBM 1.48
HNSC 0.35
LUAD 0.26
LUSC 0.618
non_ccRCC -1.678
PDAC 0.093
UCEC 0.159

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 727 U Colorectal cancer Phosphorylation 33747209
S 727 U Nephroblastoma Phosphorylation 16799645

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
P42224 STAT1 P Ser727 LQTTDNLLPMS(ph)PEEFDEVSR ARH-77 Rituximab -3.8138 -
P42224 STAT1 P Ser727 LQTTDNLLPMS(ph)PEEFDEVSR ARH-77 Rituximab -1.2378 -
P42224 STAT1 P Ser727 LQTTDNLLPMS(ph)PEEFDEVSR ARH-77 Rituximab -4.0059 -
P42224 STAT1 P Ser727 LQTTDNLLPMS(ph)PEEFDEVSR ARH-77 Rituximab -3.4501 -
P42224 STAT1 P Ser727 LQTTDNLLPMS(ph)PEEFDEVSR ARH-77 Rituximab -3.7206 -
P42224 STAT1 P Ser727 LQTTDNLLPMS(ph)PEEFDEVSR ARH-77 Rituximab -3.8972 -
P42224 STAT1 P Ser727 LQTTDNLLPMS(ph)PEEFDEVSR ARH-77 Rituximab -1.2209 -
P42224 STAT1 P Ser727 LQTTDNLLPMS(ph)PEEFDEVSR ARH-77 Rituximab -1.2194 -

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: