Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0NH5X)
Name
Estrogen receptor beta (ESR2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Oestrogen receptor beta; Nuclear receptor subfamily 3 group A member 2; Beta-1; ER-beta; ESTRB; Erbeta; NR3A2;
Family Nuclear receptor (NR)  >>  Nuclear hormone receptor (NHR)
Organism
Homo sapiens (Human)
Gene Name ESR2 Gene ID
2100
UniProt ID ESR2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T80896 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MDIKNSPSSLNSPSSYNCSQSILPLEHGSIYIPSSYVDSHHEYPAMTFYSPAVMNYSIPS
NVTNLEGGPGRQTTSPNVLWPTPGHLSPLVVHRQLSHLYAEPQKSPWCEARSLEHTLPVN
RETLKRKVSGNRCASPVTGPGSKRDAHFCAVCSDYASGYHYGVWSCEGCKAFFKRSIQGH
NDYICPATNQCTIDKNRRKSCQACRLRKCYEVGMVKCGSRRERCGYRLVRRQRSADEQLH
CAGKAKRSGGHAPRVRELLLDALSPEQLVLTLLEAEPPHVLISRPSAPFTEASMMMSLTK
LADKELVHMISWAKKIPGFVELSLFDQVRLLESCWMEVLMMGLMWRSIDHPGKLIFAPDL
VLDRDEGKCVEGILEIFDMLLATTSRFRELKLQHKEYLCVKAMILLNSSMYPLVTATQDA
DSSRKLAHLLNAVTDALVWVIAKSGISSQQQSMRLANLLMLLSHVRHASNKGMEHLLNMK
CKNVVPVYDLLLEMLNAHVLRGCKSSITGSECSPAEDSKSKEGSQNPQSQ
Function
Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Sodium methylparaben 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
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 1860 nM (estimated based on the structural similarity with CHEMBL15841 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.919642857
                   Tested Species Homo sapiens (Human)
                   UniProt ID ESR2_HUMAN
          DIG Name: Ethylparaben 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
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 1860 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ESR2_HUMAN
References
1 Discovery of natural estrogen receptor modulators with structure-based virtual screening. Bioorg Med Chem Lett. 2013 Jun 1; 23(11):3329-33.

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