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Review
. 2005 Sep;105(9):3352-70.
doi: 10.1021/cr020456u.

Chemistry and structural biology of androgen receptor

Wenqing Gao  1 , Casey E Bohl, James T Dalton
Affiliations
Review

Chemistry and structural biology of androgen receptor

Wenqing Gao et al. Chem Rev. 2005 Sep.
No abstract available

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Figures

Figure 1
Figure 1
Structural organization of the AR gene and protein.
Figure 2
Figure 2
Amino acid sequence identity among members of the steroid receptor family (adapted from ref 19). Sequence alignment was performed using William Pearson's LALIGN program.
Figure 3
Figure 3
Crystal structures of wild-type AR ligand-binding domain bound with DHT (1I37.pdb): (A) front view; (B) ligand view. Space filled atoms are (black) carbon and (red) oxygen. The activation function 2 region (helices 3, 4, and 12) is highlighted in green.
Figure 4
Figure 4
AF2 antagonist model, as illustrated by crystal structures of wild-type estrogen receptor α ligand-binding domain bound with (A) estradiol (1ERE.pdb) and (B) raloxifene (1ERR.pdb). Estradiol is shown in yellow; raloxifene is shown in green. Helix 12 is highlighted in red. Helix 12 folds over the activation function 2 (AF2) region when antagonist (raloxifene) binds to the estrogen receptor α ligand-binding domain.
Figure 5
Figure 5
Interactions of FxxLF or LxxLL motifs with the AR or estrogen receptor ligand-binding domain: upper panels, hydrogen-bonding interactions (shown as yellow dotted line) between peptide and activation function 2 region residues; lower panels, surface view of the activation function 2 interface, in which side chains of the hydrophobic residues of FxxLF and LxxLL motifs are shown as spheres; (A) FxxLF bound to AR activation function 2 interface (1T7R.pdb); (B) LxxLL bound to AR activation function 2 interface (1T7F.pdb); (C) LxxLL bound to estrogen receptor α activation function 2 interface (1GWQ.pdb).
Figure 6
Figure 6
Testosterone synthesis (adapted from ref 62). Abbreviations are as follows: P450scc, cholesterol side-chain cleavage enzyme; HSD, hydroxy steroid dehydrogenase.
Figure 7
Figure 7
Testosterone metabolism (adapted from ref 72). Abbreviationsare as follows: G, glucuronide; HSD, hydroxy steroid dehydrogenase; UGT, UDP-glucuronosyltransferase.
Figure 8
Figure 8
Testosterone esters.
Figure 9
Figure 9
Steroidal (DHT) and nonsteroidal (R-bicalutamide) ligand interactions with AR ligand-binding domain binding pocket. R-Bicalutamide (green) W741L complex (1Z95.pdb) and DHT (gold) WT complex (1T7R.pdb) are shown as side views (A,B) and top views (C,D) of the steroidal plane. H bonds are labeled as yellow dotted lines.
See this image and copyright information in PMC

References

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