Id: acc3252
Group: 2sens
Protein: TPH-1
Gene Symbol: TPH1
Protein Id: P17752
Protein Name: TPH1_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: NECA
Drug Info: "NECA is a drug, but without more context, specific details about its nature and uses cannot be provided."
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:
Sentence:

Sequence & Structure:

MIEDNKENKDHSLERGRASLIFSLKNEVGGLIKALKIFQEKHVNLLHIESRKSKRRNSEFEIFVDCDINREQLNDIFHLLKSHTNVLSVNLPDNFTLKEDGMETVPWFPKKISDLDHCANRVLMYGSELDADHPGFKDNVYRKRRKYFADLAMNYKHGDPIPKVEFTEEEIKTWGTVFQELNKLYPTHACREYLKNLPLLSKYCGYREDNIPQLEDVSNFLKERTGFSIRPVAGYLSPRDFLSGLAFRVFHCTQYVRHSSDPFYTPEPDTCHELLGHVPLLAEPSFAQFSQEIGLASLGASEEAVQKLATCYFFTVEFGLCKQDGQLRVFGAGLLSSISELKHALSGHAKVKPFDPKITCKQECLITTFQDVYFVSESFEDAKEKMREFTKTIKRPFGVKYNPYTRSIQILKDTKSITSAMNELQHDLDVVSDALAKVSRKPSI

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
TPH1 TELOTRISTAT ETIPRATE Tryptophan 5-hydroxylase inhibitor 4 - carcinoid tumor EMA
TPH1 TELOTRISTAT ETIPRATE Tryptophan 5-hydroxylase inhibitor 4 - neuroendocrine neoplasm EMA
TPH1 TELOTRISTAT ETIPRATE Tryptophan 5-hydroxylase inhibitor 4 - Diarrhea FDA
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 3 Recruiting large cell neuroendocrine carcinoma ClinicalTrials
TPH1 TELOTRISTAT Tryptophan 5-hydroxylase inhibitor 3 Completed carcinoid syndrome ClinicalTrials
ClinicalTrials
ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 3 Withdrawn carcinoid heart disease ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 3 Withdrawn small intestine neuroendocrine tumor, well differentiated, low or intermediate grade ClinicalTrials
TPH1 TELOTRISTAT Tryptophan 5-hydroxylase inhibitor 2 Completed ulcerative colitis ClinicalTrials
TPH1 RODATRISTAT ETHYL Tryptophan 5-hydroxylase 1 inhibitor 2 Completed pulmonary arterial hypertension ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 2 Active, not recruiting pancreatic carcinoma ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 2 Active, not recruiting pancreatic adenocarcinoma ClinicalTrials
TPH1 TELOTRISTAT Tryptophan 5-hydroxylase inhibitor 2 Completed carcinoid syndrome ClinicalTrials
ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 2 Withdrawn carcinoid syndrome ClinicalTrials
TPH1 TELOTRISTAT Tryptophan 5-hydroxylase inhibitor 2 Recruiting carcinoid syndrome ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 2 Withdrawn neuroendocrine neoplasm ClinicalTrials
ClinicalTrials
TPH1 TELOTRISTAT Tryptophan 5-hydroxylase inhibitor 2 Recruiting neuroendocrine neoplasm ClinicalTrials
TPH1 TELOTRISTAT Tryptophan 5-hydroxylase inhibitor 2 Terminated neuroendocrine neoplasm ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 2 Terminated biliary tract cancer ClinicalTrials
TPH1 RODATRISTAT ETHYL Tryptophan 5-hydroxylase 1 inhibitor 1 Completed pulmonary arterial hypertension ClinicalTrials
TPH1 TELOTRISTAT Tryptophan 5-hydroxylase inhibitor 1 Completed liver disease ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 1 Completed liver disease ClinicalTrials
TPH1 TELOTRISTAT Tryptophan 5-hydroxylase inhibitor 1 Completed kidney disease ClinicalTrials
TPH1 TELOTRISTAT ETHYL Tryptophan 5-hydroxylase inhibitor 1 Completed carcinoid syndrome 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

No data.

PTM-Disease Association:

source: PTMD

No data.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: