PMADS

Id:	acc0496
Group:	1sens
Protein:	PPARgamma
Gene Symbol:	PPARG
Protein Id:	P37231
Protein Name:	PPARG_HUMAN
PTM:	phosphorylation
Site:	Ser84
Site Sequence:	TPHYEDIPFTRTDPVVADYKY
Disease Category:	Cancer
Disease:	Hepatocellular Carcinoma
Disease Subtype:
Disease Cellline:	HepG2
Disease Info:
Drug:	PD0325901
Drug Info:	"PD0325901 is a selective MEK1/MEK2 inhibitor that suppresses tumor cell proliferation by targeting the ERK signaling pathway, primarily used in preclinical research for its potential anticancer properties. "
Effect:	modulate
Effect Info:	The MEK inhibitor PD0325901 can inhibit tumor growth by suppressing the phosphorylation of PPARgamma.
Note:
Score:	4.0
Pubmed(PMID):	27769068
Sentence Index:	27769068_0
Sentence:	Phosphorylation of PPARgamma at Ser84 promotes glycolysis and cell proliferation in hepatocellular carcinoma by targeting PFKFB4.

Sequence & Structure:

MGETLGDSPIDPESDSFTDTLSANISQEMTMVDTEMPFWPTNFGISSVDLSVMEDHSHSFDIKPFTTVDFSSISTPHYEDIPFTRTDPVVADYKYDLKLQEYQSAIKVEPASPPYYSEKTQLYNKPHEEPSNSLMAIECRVCGDKASGFHYGVHACEGCKGFFRRTIRLKLIYDRCDLNCRIHKKSRNKCQYCRFQKCLAVGMSHNAIRFGRMPQAEKEKLLAEISSDIDQLNPESADLRALAKHLYDSYIKSFPLTKAKARAILTGKTTDKSPFVIYDMNSLMMGEDKIKFKHITPLQEQSKEVAIRIFQGCQFRSVEAVQEITEYAKSIPGFVNLDLNDQVTLLKYGVHEIIYTMLASLMNKDGVLISEGQGFMTREFLKSLRKPFGDFMEPKFEFAVKFNALELDDSDLAIFIAVIILSGDRPGLLNVKPIEDIQDNLLQALELQLKLNHPESSQLFAKLLQKMTDLRQIVTEHVQLLQVIKKTETDMSLHPLLQEIYKDLY

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target	Drug name	MOA	Phase	Status	Disease	Source
PPARG	BEZAFIBRATE	Peroxisome proliferator-activated receptor agonist	4	-	cardiovascular disease	ATC
PPARG	PIOGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	4	-	diabetes mellitus	ATC
PPARG	PIOGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	4	Completed	diabetes mellitus	ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials
PPARG	PIOGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	4	Recruiting	diabetes mellitus	ClinicalTrials
PPARG	ROSIGLITAZONE MALEATE	Peroxisome proliferator-activated receptor gamma agonist	4	-	diabetes mellitus	DailyMed
PPARG	ROSIGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	4	Completed	diabetes mellitus	ClinicalTrials
PPARG	PIOGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	4	Not yet recruiting	diabetes mellitus	ClinicalTrials
PPARG	PIOGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	4	Unknown status	diabetes mellitus	ClinicalTrials
PPARG	ROSIGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	4	-	diabetes mellitus	DailyMed ATC
PPARG	TROGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	4	-	diabetes mellitus	ATC
PPARG	OLSALAZINE SODIUM	Peroxisome proliferator-activated receptor gamma agonist	4	-	ulcerative colitis	DailyMed DailyMed DailyMed DailyMed DailyMed
PPARG	BALSALAZIDE DISODIUM	Peroxisome proliferator-activated receptor gamma agonist	4	-	ulcerative colitis	DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed
PPARG	MESALAMINE	Peroxisome proliferator-activated receptor gamma agonist	4	Recruiting	ulcerative colitis	ClinicalTrials ClinicalTrials
PPARG	MESALAMINE	Peroxisome proliferator-activated receptor gamma agonist	4	Unknown status	ulcerative colitis	ClinicalTrials
PPARG	MESALAMINE	Peroxisome proliferator-activated receptor gamma agonist	4	-	ulcerative colitis	DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed
PPARG	MESALAMINE	Peroxisome proliferator-activated receptor gamma agonist	4	Completed	ulcerative colitis	ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials
PPARG	PIOGLITAZONE HYDROCHLORIDE	Peroxisome proliferator-activated receptor gamma agonist	4	-	liver disease	DailyMed DailyMed DailyMed
PPARG	MESALAMINE	Peroxisome proliferator-activated receptor gamma agonist	4	-	proctitis	DailyMed DailyMed DailyMed
PPARG	PIOGLITAZONE HYDROCHLORIDE	Peroxisome proliferator-activated receptor gamma agonist	4	-	type 2 diabetes mellitus	DailyMed DailyMed DailyMed EMA DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed FDA DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed DailyMed
PPARG	PIOGLITAZONE HYDROCHLORIDE	Peroxisome proliferator-activated receptor gamma agonist	4	Completed	type 2 diabetes mellitus	ClinicalTrials ClinicalTrials
PPARG	ROSIGLITAZONE MALEATE	Peroxisome proliferator-activated receptor gamma agonist	4	-	type 2 diabetes mellitus	DailyMed DailyMed DailyMed DailyMed FDA DailyMed
PPARG	ROSIGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	3	Terminated	metabolic syndrome	ClinicalTrials
PPARG	PIOGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	3	Unknown status	metabolic syndrome	ClinicalTrials
PPARG	ROSIGLITAZONE	Peroxisome proliferator-activated receptor gamma agonist	3	Completed	cardiovascular disease	ClinicalTrials
PPARG	IMIGLITAZAR	Peroxisome proliferator-activated receptor gamma agonist	3	Completed	diabetes mellitus	ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

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

PPARG-Ser84
Cancer	Intensity
BRCA	0.707
COAD	-0.707
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD

Residue	Position	State	Disease	Class	PMID
T	166	D	Fatty liver	Phosphorylation	36329235
K	268	U	Type 2 diabetes	Acetylation	32409492
K	293	U	Type 2 diabetes	Acetylation	32409492
-	-	U	Obesity	Neddylation	26990658
S	112	U	Breast cancer	Phosphorylation	36139700
Y	74	U	Colon cancer/carcinoma	Phosphorylation	26718225
Y	108	U	Cancer	Phosphorylation	33164261
S	273	U	Triple-negative breast cancer	Phosphorylation	33240752

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

No data.

Function score:

source: funscoR

No data.

Cross Links:

CTD
DMRdb