Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0I1PM)
Name
Poly[ADP-ribose] synthase 1 (PARP1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
ADP-ribosyltransferase diphtheria toxin-like 1; Poly [ADP-ribose] polymerase 1; ADPRT; ADPRT 1; ARTD1; DNA ADP-ribosyltransferase PARP1; NAD(+) ADP-ribosyltransferase 1; NAD(+) ADP-ribosyltransferase-1; NAD(+)Poly [ADP-ribose] polymerase-1; ADP-ribosyltransferase-1; PARP-1; PPOL; Poly(ADP-ribose)polymerase-1; Poly[ADP-ribose] synthase 1; Poly[ADP-ribose] synthetase-1; Protein poly-ADP-ribosyltransferase PARP1
Family Transferase (TFase)  >>  Glycosyltransferases (EC 2.4)
Organism
Homo sapiens (Human)
Gene Name PARP1 Gene ID
142
UniProt ID PARP1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T06273 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MAESSDKLYRVEYAKSGRASCKKCSESIPKDSLRMAIMVQSPMFDGKVPHWYHFSCFWKV
GHSIRHPDVEVDGFSELRWDDQQKVKKTAEAGGVTGKGQDGIGSKAEKTLGDFAAEYAKS
NRSTCKGCMEKIEKGQVRLSKKMVDPEKPQLGMIDRWYHPGCFVKNREELGFRPEYSASQ
LKGFSLLATEDKEALKKQLPGVKSEGKRKGDEVDGVDEVAKKKSKKEKDKDSKLEKALKA
QNDLIWNIKDELKKVCSTNDLKELLIFNKQQVPSGESAILDRVADGMVFGALLPCEECSG
QLVFKSDAYYCTGDVTAWTKCMVKTQTPNRKEWVTPKEFREISYLKKLKVKKQDRIFPPE
TSASVAATPPPSTASAPAAVNSSASADKPLSNMKILTLGKLSRNKDEVKAMIEKLGGKLT
GTANKASLCISTKKEVEKMNKKMEEVKEANIRVVSEDFLQDVSASTKSLQELFLAHILSP
WGAEVKAEPVEVVAPRGKSGAALSKKSKGQVKEEGINKSEKRMKLTLKGGAAVDPDSGLE
HSAHVLEKGGKVFSATLGLVDIVKGTNSYYKLQLLEDDKENRYWIFRSWGRVGTVIGSNK
LEQMPSKEDAIEHFMKLYEEKTGNAWHSKNFTKYPKKFYPLEIDYGQDEEAVKKLTVNPG
TKSKLPKPVQDLIKMIFDVESMKKAMVEYEIDLQKMPLGKLSKRQIQAAYSILSEVQQAV
SQGSSDSQILDLSNRFYTLIPHDFGMKKPPLLNNADSVQAKVEMLDNLLDIEVAYSLLRG
GSDDSSKDPIDVNYEKLKTDIKVVDRDSEEAEIIRKYVKNTHATTHNAYDLEVIDIFKIE
REGECQRYKPFKQLHNRRLLWHGSRTTNFAGILSQGLRIAPPEAPVTGYMFGKGIYFADM
VSKSANYCHTSQGDPIGLILLGEVALGNMYELKHASHISKLPKGKHSVKGLGKTTPDPSA
NISLDGVDVPLGTGISSGVNDTSLLYNEYIVYDIAQVNLKYLLKLKFNFKTSLW
Function
Mainly mediates glutamate and aspartate ADP-ribosylation of target proteins: the ADP-D-ribosyl group of NAD(+) is transferred to the acceptor carboxyl group of glutamate and aspartate residues and further ADP-ribosyl groups are transferred to the 2'-position of the terminal adenosine moiety, building up a polymer with an average chain length of 20-30 units. Mediates the poly(ADP-ribosyl)ation of a number of proteins, including itself, APLF and CHFR.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Cyanocobalamin 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
Complexing agent; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 100 nM (estimated based on the structural similarity with CHEMBL473036 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.790322581
                   Tested Species Homo sapiens (Human)
                   UniProt ID PARP1_HUMAN
          DIG Name: Niacinamide 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
Antioxidant; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 210000 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID PARP1_HUMAN
References
1 Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors. J. Med. Chem. 2009; 52:718-725.
2 Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors. Bioorg Med Chem Lett. 2013 Apr 1; 23(7):1993-6.

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