6MDQ

Crystal structure of equine serum albumin in complex with testosterone

6MDQ の概要

• エントリーDOI: 10.2210/pdb6mdq/pdb
• 分子名称: Serum albumin, CITRATE ANION, TESTOSTERONE, ... (4 entities in total)
• 機能のキーワード: albumin, equine serum albumin, testosterone, csgid, structural genomics, center for structural genomics of infectious diseases, transport protein
• 由来する生物種: Equus caballus (Horse)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 66912.23

構造登録者

Czub, M.P.,Majorek, K.A.,Shabalin, I.G.,Handing, K.B.,Venkataramany, B.S.,Cymborowski, M.T.,Satchell, K.J.,Joachimiak, A.,Minor, W.,Center for Structural Genomics of Infectious Diseases (CSGID) (登録日: 2018-09-05, 公開日: 2018-09-26, 最終更新日: 2024-11-20)

主引用文献

Czub, M.P.,Venkataramany, B.S.,Majorek, K.A.,Handing, K.B.,Porebski, P.J.,Beeram, S.R.,Suh, K.,Woolfork, A.G.,Hage, D.S.,Shabalin, I.G.,Minor, W.
Testosterone meets albumin - the molecular mechanism of sex hormone transport by serum albumins.
Chem Sci, 10:1607-1618, 2019

PubMed Abstract: Serum albumin is the most abundant protein in mammalian blood plasma and is responsible for the transport of metals, drugs, and various metabolites, including hormones. We report the first albumin structure in complex with testosterone, the primary male sex hormone. Testosterone is bound in two sites, neither of which overlaps with the previously suggested Sudlow site I. We determined the binding constant of testosterone to equine and human albumins by two different methods: tryptophan fluorescence quenching and ultrafast affinity extraction. The binding studies and similarities between residues comprising the binding sites on serum albumins suggest that testosterone binds to the same sites on both proteins. Our comparative analysis of albumin complexes with hormones, drugs, and other biologically relevant compounds strongly suggests interference between a number of compounds present in blood and testosterone transport by serum albumin. We discuss a possible link between our findings and some phenomena observed in human patients, such as low testosterone levels in diabetic patients.

PubMed: 30842823
DOI: 10.1039/c8sc04397c

実験手法

X-RAY DIFFRACTION (2.15 Å)