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Verfasst von:Park, Chang Gyun [VerfasserIn]   i
 Adnan, Karim Md [VerfasserIn]   i
 Cho, Hyunki [VerfasserIn]   i
 Ryu, Chang Seon [VerfasserIn]   i
 Yoon, Juyong [VerfasserIn]   i
 Kim, Young Jun [VerfasserIn]   i
Titel:A combined in vitro-in silico method for assessing the androgenic activities of bisphenol A and its analogues
Verf.angabe:Chang Gyun Park, Karim Md Adnan, Hyunki Cho, Chang Seon Ryu, Juyong Yoon, Young Jun Kim
E-Jahr:2024
Jahr:4 May 2024
Umfang:10 S.
Fussnoten:Online verfügbar: 4. Mai 2024, Artikelversion: 11. Mai 2024 ; Gesehen am 21.10.2024
Titel Quelle:Enthalten in: Toxicology in vitro
Ort Quelle:Amsterdam [u.a.] : Elsevier Science, 1987
Jahr Quelle:2024
Band/Heft Quelle:98(2024) vom: Juni, Artikel-ID 105838, Seite 1-10
ISSN Quelle:1879-3177
Abstract:Interactions between endocrine-disruptor chemicals (EDCs) and androgen receptor (AR) have adverse effects on the endocrine system, leading to human reproductive dysfunction. Bisphenol A (BPA) is an EDC that can damage both the environment and human health. Although numerous BPA analogues have been produced as substitutes for BPA, few studies have evaluated their endocrine-disrupting abilities. We assessed the (anti)-androgenic activities of BPA and its analogues using a yeast-based reporter assay. The BPA analogues tested were bisphenol S (BPS), 4-phenylphenol (4PP), 4,4′-(9-fluorenyliden)-diphenol (BPFL), tetramethyl bisphenol F (TMBPF), and tetramethyl bisphenol A (TMBPA). We also conducted molecular docking and dynamics simulations to assess the interactions of BPA and its analogues with the ligand-binding domain of human AR (AR-LBD). Neither BPA nor its analogues had androgenic activity; however, all except BPFL exerted robust anti-androgenic effects. Consistent with the in vitro results, anti-androgenic analogues of BPA formed hydrogen bonding patterns with key residues that differed from the patterns of endogenous hormones, indicating that the analogues display in inappropriate orientations when interacting with the binding pocket of AR-LBD. Our findings indicate that BPA and its analogues disrupt androgen signaling by interacting with the AR-LBD. Overall, BPA and its analogues display endocrine-disrupting activity, which is mediated by AR.
DOI:doi:10.1016/j.tiv.2024.105838
URL:Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.

kostenfrei: Volltext: https://doi.org/10.1016/j.tiv.2024.105838
 kostenfrei: Volltext: https://www.sciencedirect.com/science/article/pii/S0887233324000687
 DOI: https://doi.org/10.1016/j.tiv.2024.105838
Datenträger:Online-Ressource
Sprache:eng
Sach-SW:Androgen receptor
 BPA
 BPA analogues
 Endocrine-distrupting chemicals
 methods
 reporter assay
K10plus-PPN:1906305978
Verknüpfungen:→ Zeitschrift

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