Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET07LSR)
Name
Tyrosyl-DNA phosphodiesterase 2 (TDP2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
TRAF and TNF receptor-associated protein; Tyr-DNA phosphodiesterase 2; Tyrosyl-RNA phosphodiesterase; VPg unlinkase; 5'-Tyr-DNA phosphodiesterase; 5'-tyrosyl-DNA phosphodiesterase; EAPII; ETS1-associated protein 2; ETS1-associated protein II; TDP2; hTDP2
Family Hydrolase (HDase)  >>  Ester bond hydrolase (EC 3.1)
Organism
Homo sapiens (Human)
Gene Name TDP2 Gene ID
51567
UniProt ID TYDP2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T04696 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MELGSCLEGGREAAEEEGEPEVKKRRLLCVEFASVASCDAAVAQCFLAENDWEMERALNS
YFEPPVEESALERRPETISEPKTYVDLTNEETTDSTTSKISPSEDTQQENGSMFSLITWN
IDGLDLNNLSERARGVCSYLALYSPDVIFLQEVIPPYYSYLKKRSSNYEIITGHEEGYFT
AIMLKKSRVKLKSQEIIPFPSTKMMRNLLCVHVNVSGNELCLMTSHLESTRGHAAERMNQ
LKMVLKKMQEAPESATVIFAGDTNLRDREVTRCGGLPNNIVDVWEFLGKPKHCQYTWDTQ
MNSNLGITAACKLRFDRIFFRAAAEEGHIIPRSLDLLGLEKLDCGRFPSDHWGLLCNLDI
IL
Function
DNA repair enzyme that can remove a variety of covalent adducts from DNA through hydrolysis of a 5'-phosphodiester bond, giving rise to DNA with a free 5' phosphate. Catalyzes the hydrolysis of dead-end complexes between DNA and the topoisomerase 2 (TOP2) active site tyrosine residue. Hydrolyzes 5'- phosphoglycolates on protruding 5' ends on DNA double-strand breaks (DSBs) due to DNA damage by radiation and free radicals.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Hydrazine yellow 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
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 3500 nM (estimated based on the structural similarity with CHEMBL3813826 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.777777778
                   Tested Species Homo sapiens (Human)
                   UniProt ID TYDP2_HUMAN
References
1 Discovery of selective inhibitors of tyrosyl-DNA phosphodiesterase 2 by targeting the enzyme DNA-binding cleft. Bioorg Med Chem Lett. 2016 Jul 15; 26(14):3232-3236.

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