PMADS

Id:	acc3249
Group:	2sens
Protein:	CREB
Gene Symbol:	CREB1
Protein Id:	P16220
Protein Name:	CREB1_HUMAN
PTM:	phosphorylation
Site:	unclear
Site Sequence:
Disease Category:	Immune system diseases
Disease:	Inflammatory
Disease Subtype:	Inflammatory Bowel Disease
Disease Cellline:	KRJ-I
Disease Info:
Drug:	MRS1754
Drug Info:	"MRS1754 is a drug that may have specific pharmacological effects and applications, which require further research to fully understand."
Effect:	modulate
Effect Info:	"Under hypoxic conditions, the ADORA2B receptor activates the MAPK/CREB signaling pathway. TPH - 1 is activated through phosphorylation and synthesizes more 5 - hydroxytryptamine (5 - HT). The ADORA2B agonist NECA can enhance 5 - HT release, while the antagonist MRS1754 can significantly inhibit this process. 5 - HT plays a central role in the regulatory function of EC cells."
Note:
Score:	4.0
Pubmed(PMID):	23638125
Sentence Index:	23638125_9-10
Sentence:	"Hypoxia stimulated 5-HT release maximally at 30 mins, an effect amplified by NECA and selectively inhibited by MRS1754, through phosphorylationation of TPH-1 and activation of VMAT-1. Transient transfection with Renilla luciferase under hypoxia transcriptional response element (HRE) control identified that ADORA2B activated HIF-1alpha signaling under hypoxic conditions."

Sequence & Structure:

MTMESGAENQQSGDAAVTEAENQQMTVQAQPQIATLAQVSMPAAHATSSAPTVTLVQLPNGQTVQVHGVIQAAQPSVIQSPQVQTVQISTIAESEDSQESVDSVTDSQKRREILSRRPSYRKILNDLSSDAPGVPRIEEEKSEEETSAPAITTVTVPTPIYQTSSGQYIAITQGGAIQLANNGTDGVQGLQTLTMTNAAATQPGTTILQYAQTTDGQQILVPSNQVVVQAASGDVQTYQIRTAPTSTIAPGVVMASSPALPTQPAEEAARKREVRLMKNREAARECRRKKKEYVKCLENRVAVLENQNKTLIEELKALKDLYCHKSD

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 intensity data of this site,
show all other sites!

CREB1-Ser108
Cancer	Intensity
BRCA
COAD	-0.707
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC	0.707

CREB1-Ser111
Cancer	Intensity
BRCA	-0.935
COAD	0.719
HGSC
ccRCC	-0.651
GBM
HNSC	1.355
LUAD	-0.796
LUSC	-0.759
non_ccRCC
PDAC
UCEC	1.067

CREB1-Ser142
Cancer	Intensity
BRCA	1.677
COAD	-0.547
HGSC	-0.852
ccRCC	-0.202
GBM
HNSC	-1.472
LUAD	0.449
LUSC	0.862
non_ccRCC
PDAC
UCEC	0.086

CREB1-Ser143
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

CREB1-Ser270
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

CREB1-Ser271
Cancer	Intensity
BRCA	0.671
COAD	0.307
HGSC	-2.002
ccRCC
GBM
HNSC
LUAD	0.269
LUSC
non_ccRCC	0.591
PDAC
UCEC	0.164

CREB1-Ser340
Cancer	Intensity
BRCA
COAD	0.347
HGSC	0.586
ccRCC
GBM	1.14
HNSC
LUAD
LUSC	-1.245
non_ccRCC
PDAC	-0.829
UCEC

PTM-Disease Association:

source: PTMD

Residue	Position	State	Disease	Class	PMID
-	-	P	Neuroblastoma	Phosphorylation	10366032
-	-	P	Alzheimer's disease	Phosphorylation	24523906

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