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

UniChem : NKANXQFJJICGDU-QPLCGJKRSA-N

Wikipedia : Tamoxifen

Target

Families : Tamoxifen ligand of proteins in family
Carboxylesterase Carb_B_Chordata

Structure :
1YA4

Protein :
human-CES1

References (4)

Title : Identification and pharmacological characterization of cholesterol-5,6-epoxide hydrolase as a target for tamoxifen and AEBS ligands - de Medina_2010_Proc.Natl.Acad.Sci.U.S.A_107_13520
Author(s) : de Medina P , Paillasse MR , Segala G , Poirot M , Silvente-Poirot S
Ref : Proc Natl Acad Sci U S A , 107 :13520 , 2010
Abstract :
PubMedSearch : de Medina_2010_Proc.Natl.Acad.Sci.U.S.A_107_13520
PubMedID: 20615952

Title : Mammalian carboxylesterases: from drug targets to protein therapeutics - Redinbo_2005_Drug.Discov.Today_10_313
Author(s) : Redinbo MR , Potter PM
Ref : Drug Discov Today , 10 :313 , 2005
Abstract :
PubMedSearch : Redinbo_2005_Drug.Discov.Today_10_313
PubMedID: 15749280

Title : Structural insights into drug processing by human carboxylesterase 1: tamoxifen, mevastatin, and inhibition by benzil - Fleming_2005_J.Mol.Biol_352_165
Author(s) : Fleming CD , Bencharit S , Edwards CC , Hyatt JL , Tsurkan L , Bai F , Fraga C , Morton CL , Howard-Williams EL , Potter PM , Redinbo MR
Ref : Journal of Molecular Biology , 352 :165 , 2005
Abstract :
PubMedSearch : Fleming_2005_J.Mol.Biol_352_165
PubMedID: 16081098
Gene_locus related to this paper: human-CES1

Title : Identification of two tamoxifen target proteins by photolabeling with 4-(2-morpholinoethoxy)benzophenone - Mesange_2002_Bioconjug.Chem_13_766
Author(s) : Mesange F , Sebbar M , Capdevielle J , Guillemot JC , Ferrara P , Bayard F , Poirot M , Faye JC
Ref : Bioconjug Chem , 13 :766 , 2002
Abstract :
PubMedSearch : Mesange_2002_Bioconjug.Chem_13_766
PubMedID: 12121132