Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T80896 Target Info
Target Name Estrogen receptor beta (ESR2)
Synonyms
Oestrogen receptor beta; Nuclear receptor subfamily 3 group A member 2; NR3A2; Erbeta; ESTRB; ER-beta; Beta-1
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Target Type Successful Target
Gene Name ESR2
Biochemical Class Nuclear hormone receptor
UniProt ID
ESR2_HUMAN
Co-Targets of This Target  Top
Co-Target Name Epidermal growth factor receptor (EGFR) Successful Target
UniProt ID EGFR_HUMAN
Gene Name EGFR
Synonyms
Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB
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Representative Drug(s) Genistein Drug Info IC50 = 0.1 ug.mL-1 [1]
Co-Target Name Estrogen receptor (ESR) Successful Target
UniProt ID ESR1_HUMAN
Gene Name ESR1
Synonyms
Nuclear receptor subfamily 3 group A member 1; NR3A1; Estradiol receptor; ESR; ER-alpha; ER
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Representative Drug(s) ARZOXIFENE Drug Info EC50 = 0.2 nM Click to Show More [2]
2 Erteberel Drug Info Ki = 2.29 nM [3]
3 Genistein Drug Info IC50 = 9.7 nM [4]
Co-Target Name Estrogen-related receptor-alpha (ESRRA) Successful Target
UniProt ID ERR1_HUMAN
Gene Name ESRRA
Synonyms
Nuclear receptor subfamily 3 group B member 1; NR3B1; Estrogen-relatedreceptor, alpha; Estrogen-relatedreceptor alpha; Estrogen-related receptor alpha; Estrogen receptor-like 1; ESRL1; ERRalpha; ERR1; ERR-alpha
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Representative Drug(s) Genistein Drug Info IC50 = 10 nM [5]
Co-Target Name Aldehyde oxidase (AOX1) Successful Target
UniProt ID AOXA_HUMAN
Gene Name AOX1
Synonyms
AOX1
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Representative Drug(s) Genistein Drug Info IC50 = 340 nM [6]
Co-Target Name Dipeptidyl peptidase 4 (DPP-4) Successful Target
UniProt ID DPP4_HUMAN
Gene Name DPP4
Synonyms
Tcell activation antigen CD26; TP103; T-cell activation antigen CD26; Dipeptidyl peptidase IV; Dipeptidyl peptidase 4 soluble form; DPP-IV; DPP IV; DPP 4; CD26; Adenosine deaminase complexing protein-2; Adenosine deaminase complexing protein 2; ADCP2; ADCP-2; ADABP
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Representative Drug(s) Genistein Drug Info IC50 = 480 nM [7]
Co-Target Name Monoamine oxidase (MAO) Successful Target
UniProt ID AOFA_HUMAN; AOFB_HUMAN
Gene Name NO-GeName
Synonyms
Human monoamine oxidase
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Representative Drug(s) Genistein Drug Info IC50 = 900 nM [8]
Co-Target Name DNA topoisomerase II alpha (TOP2A) Clinical trial Target
UniProt ID TOP2A_HUMAN
Gene Name TOP2A
Synonyms
DNA topoisomerase II, alpha isozyme; DNA topoisomerase 2alpha; DNA topoisomerase 2-alpha
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Representative Drug(s) Genistein Drug Info IC50 = 30 ug.mL-1 [9]
Co-Target Name Estrogen-related receptor-beta (ESRRB) Literature-reported Target
UniProt ID ERR2_HUMAN
Gene Name ESRRB
Synonyms
Steroid hormone receptor ERR2; Nuclear receptor subfamily 3 group B member 2; NR3B2; Estrogen-related receptor beta; Estrogen receptor-like 2; ESRL2; ERRB2; ERR-beta; ERR beta-2
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Representative Drug(s) Genistein Drug Info IC50 = 395 nM [5]
References  Top
REF 1 Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents. J Nat Prod. 1992 Nov;55(11):1529-60.
REF 2 Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. J Med Chem.2015 Jun 25;58(12):4888-904.
REF 3 Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: functionalization of the benzopyran A-ring. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5082-5.
REF 4 Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones. Bioorg Med Chem Lett. 2007 Jan 1;17(1):118-22.
REF 5 ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4053-6.
REF 6 Aldehyde oxidase: an enzyme of emerging importance in drug discovery. J Med Chem. 2010 Dec 23;53(24):8441-60.
REF 7 Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. Eur J Med Chem. 2018 May 10;151:145-157.
REF 8 The mitochondrial monoamine oxidase-aldehyde dehydrogenase pathway: a potential site of action of daidzin. J Med Chem. 2000 Nov 2;43(22):4169-79.
REF 9 Flavonoids as DNA topoisomerase antagonists and poisons: structure-activity relationships. J Nat Prod. 1995 Feb;58(2):217-25.

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