Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET03SIX)
Name
PPAR-alpha (PPARA)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Peroxisome proliferator-activated receptor alpha; NR1C1; Nuclear receptor subfamily 1 group C member 1; PPAR; PPAR-alpha; PPARalpha; Peroxisome proliferater-activated receptor alpha
Family Nuclear receptor (NR)  >>  Nuclear hormone receptor (NHR)
Organism
Homo sapiens (Human)
Gene Name PPARA Gene ID
5465
UniProt ID PPARA_HUMAN (click to find more protein-related data of this DBT)
TTD ID T86591 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MVDTESPLCPLSPLEAGDLESPLSEEFLQEMGNIQEISQSIGEDSSGSFGFTEYQYLGSC
PGSDGSVITDTLSPASSPSSVTYPVVPGSVDESPSGALNIECRICGDKASGYHYGVHACE
GCKGFFRRTIRLKLVYDKCDRSCKIQKKNRNKCQYCRFHKCLSVGMSHNAIRFGRMPRSE
KAKLKAEILTCEHDIEDSETADLKSLAKRIYEAYLKNFNMNKVKARVILSGKASNNPPFV
IHDMETLCMAEKTLVAKLVANGIQNKEAEVRIFHCCQCTSVETVTELTEFAKAIPGFANL
DLNDQVTLLKYGVYEAIFAMLSSVMNKDGMLVAYGNGFITREFLKSLRKPFCDIMEPKFD
FAMKFNALELDDSDISLFVAAIICCGDRPGLLNVGHIEKMQEGIVHVLRLHLQSNHPDDI
FLFPKLLQKMADLRQLVTEHAQLVQIIKKTESDAALHPLLQEIYRDMY
Function
Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Dimethyl benzyl carbinyl acetate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Adsorbent; Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 13000 nM (estimated based on the structural similarity with CHEMBL1257776 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.850574713
                   Tested Species Mus musculus (Mouse)
                   UniProt ID PPARA_MOUSE
          DIG Name: Myristic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Penetration agent; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 5400 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PPARA_HUMAN
          DIG Name: Oleic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Penetration agent; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 600 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PPARA_HUMAN
          DIG Name: Palmitic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Penetration agent; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1500 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PPARA_HUMAN
          DIG Name: Sodium stearate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Gelling agent; Glidant; Modified-release agent; Stiffening agent; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 30000 nM (estimated based on the structural similarity with CHEMBL1173381 ) [2]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID PPARA_HUMAN
          DIG Name: Stearic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1100 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PPARA_HUMAN
          DIG Name: Lauric acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antifoaming agent; Emulsifying agent; Lubricant; Penetration agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 30000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PPARA_HUMAN
          DIG Name: Linoleic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Penetration agent; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1100 nM (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PPARA_HUMAN
References
1 A stereo-controlled synthesis of 2,4-dimethyl-4-hydroxy-16-phenylhexadecanoic acid 1,4-lactone and its PPAR activities. Bioorg Med Chem Lett. 2010 Oct 15; 20(20):6017-9.
2 Molecular properties of fatty acids related to PPAR binding and metabolic diseases. Med Chem Res (2013) 22:3126-3133.
3 Molecular recognition of long chain fatty acids by peroxisome proliferator-activated receptor. Med Chem Res (2009) 18:8-19.

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