title: In vitro study of Organization for Economic Co-operation and Development (OECD) endocrine disruptor screening and testing methods- establishment of a recombinant rat androgen receptor (rrAR) binding assay.
abstract: The androgen receptor (AR) binding assay can be used to determine the ability of probable endocrine disruptors (EDs) to compete with synthetic androgen methyltrienolone (R1881) for binding to recombinant rat AR (rrAR). In this study, we assessed AR binding of various chemicals using Lexius Freyberger's method. The rank of relative binding affinity (RBA, IC(50)) on the tested chemicals was trenbolone 1.3 x 10(-8) M (RBA 138) > dihydrotesterone (DHT) 1.8 x 10(-8) M (RBA 100) > methyl testosterone 5.7 x 10(-8) M (RBA 31.6) > nonylphenol (NP) 1.3 x 10(-5) M (RBA 0.14) > bisphenol A (BPA) 1.1 x 10(-4) M (RBA 0.016) > isobutyl paraben 3.1 x 10(-4) M (RBA 0.0058) > butyl paraben 6.2 x 10(-4) M (RBA 0.0029) > propyl paraben 9.7 x 10(-4) M (RBA 0.0019). However, di(n-butyl) phthalate (DBP) and di(2-ethylhexyl) phthalate (DEHP), known anti-androgenic chemicals, did not show any significant AR binding activity. Our data suggests that in vitro AR binding assay may be useful as a screening tool for potential EDs.
authors.forename: Tae Sung
authors.initials: TS
authors.lastname: Kim
authors.forename: Chang Yong
authors.initials: CY
authors.lastname: Yoon
authors.forename: Ki Kyung
authors.initials: KK
authors.lastname: Jung
authors.forename: Soon Sun
authors.initials: SS
authors.lastname: Kim
authors.forename: Il Hyun
authors.initials: IH
authors.lastname: Kang
authors.forename: Jung Hee
authors.initials: JH
authors.lastname: Baek
authors.forename: Min Soo
authors.initials: MS
authors.lastname: Jo
authors.forename: Hyung Sik
authors.initials: HS
authors.lastname: Kim
authors.forename: Tae Seok
authors.initials: TS
authors.lastname: Kang
mesh_terms: D000818:Animals; D003993:Dibutyl Phthalate / Q000378:metabolism; D013196:Dihydrotestosterone / Q000378:metabolism; D052244:Endocrine Disruptors / Q000378:metabolism*; D015741:Metribolone / Q000378:metabolism; D051381:Rats; D011944:Receptors, Androgen / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism
chemical_list: D052244:Endocrine Disruptors; D011944:Receptors, Androgen; D011994:Recombinant Proteins; D013196:Dihydrotestosterone; D003993:Dibutyl Phthalate; D015741:Metribolone