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Inhibitor Report for: Tamoxifen

Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue (a non-steroidal estrogen receptor antagonist used to treat breast cancer), but as an estrogen (stimulating agent) in cholesterol metabolism, bone density. It is hydrolyzed by carboxylesterase



General
Type: Drug, Not A/B H target
Chemical_Nomenclature: 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine
Canonical SMILES: CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3
InChI: InChI=1S/C26H29NO/c1-4-25(21-11-7-5-8-12-21)26(22-13-9-6-10-14-22)23-15-17-24(18-16-23)28-20-19-27(2)3/h5-18H,4,19-20H2,1-3H3/b26-25-
InChIKey: NKANXQFJJICGDU-QPLCGJKRSA-N
Other name(s): Crisafeno ; Diemon ; Citofen ; Istubol ; Oncomox ; Retaxim ; Tamizam ; Tamoxen ; Valodex
MW: 371.51
Formula: C26H29NO
CAS_number:
PubChem: 2733526
IUPHAR:
Wikipedia: Tamoxifen

Target families
Tamoxifen ligand of proteins in family: Carboxylesterase, Carb_B_Chordata

Stucture of targets
1 structure:
1YA4: Crystal Structure of Human Liver Carboxylesterase 1 in complex with tamoxifen

Protein target
Enzyme: human-CES1

References
Search PubMed for references concerning: Tamoxifen

1 more
    Title: Identification and pharmacological characterization of cholesterol-5,6-epoxide hydrolase as a target for tamoxifen and AEBS ligands
    de Medina P, Paillasse MR, Segala G, Poirot M, Silvente-Poirot S
    Ref: Proc Natl Acad Sci U S A, 107:13520, 2010 : PubMed

            

    Title: Mammalian carboxylesterases: from drug targets to protein therapeutics
    Redinbo MR, Potter PM
    Ref: Drug Discov Today, 10:313, 2005 : PubMed

            

    Title: Identification of two tamoxifen target proteins by photolabeling with 4-(2-morpholinoethoxy)benzophenone
    Mesange F, Sebbar M, Capdevielle J, Guillemot JC, Ferrara P, Bayard F, Poirot M, Faye JC
    Ref: Bioconjug Chem, 13:766, 2002 : PubMed