Id: acc0542
Group: 1sens
Protein: Smad3
Gene Symbol: SMAD3
Protein Id: P84022
Protein Name: SMAD3_HUMAN
PTM: phosphorylation
Site: Thr8
Site Sequence: --MSSILPFTPPIVKRLLGWK
Disease Category: Cancer
Disease: Pancreas Cancer
Disease Subtype:
Disease Cellline: PANC-1
Disease Info:
Drug: metformin
Drug Info: "Metformin is an oral antihyperglycemic agent used primarily in the treatment of type 2 diabetes, which works by reducing hepatic glucose production and enhancing peripheral insulin sensitivity."
Effect: modulate
Effect Info: "Metformin reduces the phosphorylation of Smad2/3 in pancreatic cancer cells, thereby inhibiting tumors."
Note:
Score: 4.0
Pubmed(PMID): 29956804
Sentence Index:
Sentence:

Sequence & Structure:

MSSILPFTPPIVKRLLGWKKGEQNGQEEKWCEKAVKSLVKKLKKTGQLDELEKAITTQNVNTKCITIPRSLDGRLQVSHRKGLPHVIYCRLWRWPDLHSHHELRAMELCEFAFNMKKDEVCVNPYHYQRVETPVLPPVLVPRHTEIPAEFPPLDDYSHSIPENTNFPAGIEPQSNIPETPPPGYLSEDGETSDHQMNHSMDAGSPNLSPNPMSPAHNNLDLQPVTYCEPAFWCSISYYELNQRVGETFHASQPSMTVDGFTDPSNSERFCLGLLSNVNRNAAVELTRRHIGRGVRLYYIGGEVFAECLSDSAIFVQSPNCNQRYGWHPATVCKIPPGCNLKIFNNQEFAALLAQSVNQGFEAVYQLTRMCTIRMSFVKGWGAEYRRQTVTSTPCWIELHLNGPLQWLDKVLTQMGSPSIRCSSVS

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
K 333 D Nonalcoholic steatohepatitis Acetylation 32305562
K 341 D Renal fibrosis Acetylation 37777567
K 378 D Nonalcoholic steatohepatitis Acetylation 32305562
K 378 D Renal fibrosis Acetylation 37777567
K 20 U Triple-negative breast cancer Acetylation 34392614
K 117 U Triple-negative breast cancer Acetylation 34392614
K 333 U Melanoma Acetylation 29520103
K 53 U Cancer Methylation 35085106
K 333 U Cancer Methylation 35085106
T 179 U Breast cancer Phosphorylation 33051597
S 213 U Prostate cancer Phosphorylation 36536346

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
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A549 PD325901 8.2796 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK PC-9 LapatinibAZD4547 7.7503 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK K562 Dasatinib 9.5274 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK K562 Dasatinib 10.7804 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK K562 Dasatinib 10.9352 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK K562 Dasatinib 9.7204 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK ARH-77 Rituximab -3.7406 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A549 Tideglusib 10.995 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVKR A549 Staursporin 6.8192 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A549 Staursporin 7.5238 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A549 Pictilisib 6.1701 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A431 Afatinib 8.2785 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A549 Nintedanib 3.7483 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A549 Dasatinib 6.762 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVKR A549 Dasatinib 11.016 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A549 Dactolisib 8.9804 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A549 AZD8055 8.3524 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVKR A459 MK2206 8.395 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A431 Gefitinib 7.2523 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A431 Gefitinib 16.5229 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A431 Dasatinib 6.6113 -
P84022 SMAD3 P Thr8 SSILPFT(ph)PPIVK A431 Dasatinib 9 -

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: