Endocrine Abstracts

Experimental results have shown that the presence of endocrine disrupting chemicals (EDCs) such as the diphenyl compound DDT and its analogue DDE, allosterically cause the release of the stably bound dihydrotestosterone (DHT) from the steroid binding site of the Androgen Receptor (AR) ligand binding domain. It was hypothesized that EDCs mediate this effect via binding to the Binding Function 3 (BF3) surface binding site. Mutations of three BF 3 amino acids (F673K, F673W, G724R...

The androgen receptor (AR) is required for the development of the male phenotype and traits. Some compounds, including diphenylethers and diphenylamines, inhibit AR activity by binding to a surface cleft named binding function 3 (BF-3). Such inhibitors bind by hydrophobic interactions between the two phenyl groups and the BF-3 site. A similar diphenyl group structure is found in 4,4′ DDT, 4,4′ DDE, 4,4′ DDD, and 2,4′ DDD, whic...

The androgen receptor (AR) is required for the development of the male phenotype and traits. Some compounds, including diphenylethers and diphenylamines, inhibit AR activity by binding to a surface cleft named binding function 3 (BF-3). Such inhibitors bind by hydrophobic interactions between the two phenyl groups and the BF-3 site. A similar diphenyl group structure is found in 4,4′ DDT, 4,4′ DDE, 4,4′ DDD, and 2,4′ DDD, whic...

Androgen receptor (AR) is an important target for inhibition by some endocrine disrupting chemicals. Some diphenyl compounds inhibit AR activity by binding to a hydrophobic surface binding site, BF3. A similar diphenyl structure is found in 4.4’ DDT and its breakdown product 4.4’ DDE. Previous results showed that DDT, DDE, and related compounds induced the release of bound dihydrotestosterone from the AR ligand binding domain with IC50 values ranging fro...

The androgen receptor (AR) function is inhibited by endocrine disrupting chemicals (EDCs) such as DDT and DDE leading to problems in embryonic development and negative health outcomes for adults. EDCs may bind in the steroid binding pocket and disrupt AR function by leading to altered receptor conformations. However, this may not be the only way EDCs interfere with the receptor. Estébanez-Perpiñá et al identified binding function 3 (BF3) as a surface bi...