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Proline-Directed Androgen Receptor Phosphorylation.

Gao Y, Chen S - J Mol Genet Med (2013)

Bottom Line: The androgen receptor (AR) has been identified for decades and mediates essential steroid functions.This review is focused on the reported activities and significance of AR phosphorylation, with particular emphasis on proline-directed serine/threonine phosphorylation that occurs predominantly on the receptor.The marked enrichment of AR phosphorylation in the most diverse N-terminal domain suggests that targeting AR phosphorylation can be synergistic to antagonizing the C-terminal domain by clinical antiandrogens.

View Article: PubMed Central - PubMed

Affiliation: Division of Hematology/Oncology, Beth Israel Deaconess Medical Center, Harvard Medical School 330 Brookline, MA 02115, USA.

ABSTRACT

The androgen receptor (AR) has been identified for decades and mediates essential steroid functions. Like most of biological molecules, AR functional activities are modulated by post-translational modifications. This review is focused on the reported activities and significance of AR phosphorylation, with particular emphasis on proline-directed serine/threonine phosphorylation that occurs predominantly on the receptor. The marked enrichment of AR phosphorylation in the most diverse N-terminal domain suggests that targeting AR phosphorylation can be synergistic to antagonizing the C-terminal domain by clinical antiandrogens.

No MeSH data available.


AR linear amino acid sequences in the vicinity of Ser81 and Ser94 residues.(A) Alignment of human, chimpanzee, mouse and rat AR with highlighted conserved residues (in red) and polyglutamine region (underlined); (B) Schematic drawing indicates that Ser81 phosphorylation is correlated to AR functional activities.
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Figure 3: AR linear amino acid sequences in the vicinity of Ser81 and Ser94 residues.(A) Alignment of human, chimpanzee, mouse and rat AR with highlighted conserved residues (in red) and polyglutamine region (underlined); (B) Schematic drawing indicates that Ser81 phosphorylation is correlated to AR functional activities.

Mentions: Next, we will concentrate on three Pro-directed Ser residues (Ser81, Ser94, and Ser650) that are most robustly phosphorylated based on multiple phosphoamino acid and mass-specanalyses (Figure 2) [12,14]. Although Ser81 is apparently the highest androgen-stimulated AR phosphorylation residues, this event cannot be readily captured by mass-spec due to its particular embedment in the Poly-Q stretch that would compromise the fragmentation efficiency during digestion and processing (Figure 2 and 3) [17].


Proline-Directed Androgen Receptor Phosphorylation.

Gao Y, Chen S - J Mol Genet Med (2013)

AR linear amino acid sequences in the vicinity of Ser81 and Ser94 residues.(A) Alignment of human, chimpanzee, mouse and rat AR with highlighted conserved residues (in red) and polyglutamine region (underlined); (B) Schematic drawing indicates that Ser81 phosphorylation is correlated to AR functional activities.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4389684&req=5

Figure 3: AR linear amino acid sequences in the vicinity of Ser81 and Ser94 residues.(A) Alignment of human, chimpanzee, mouse and rat AR with highlighted conserved residues (in red) and polyglutamine region (underlined); (B) Schematic drawing indicates that Ser81 phosphorylation is correlated to AR functional activities.
Mentions: Next, we will concentrate on three Pro-directed Ser residues (Ser81, Ser94, and Ser650) that are most robustly phosphorylated based on multiple phosphoamino acid and mass-specanalyses (Figure 2) [12,14]. Although Ser81 is apparently the highest androgen-stimulated AR phosphorylation residues, this event cannot be readily captured by mass-spec due to its particular embedment in the Poly-Q stretch that would compromise the fragmentation efficiency during digestion and processing (Figure 2 and 3) [17].

Bottom Line: The androgen receptor (AR) has been identified for decades and mediates essential steroid functions.This review is focused on the reported activities and significance of AR phosphorylation, with particular emphasis on proline-directed serine/threonine phosphorylation that occurs predominantly on the receptor.The marked enrichment of AR phosphorylation in the most diverse N-terminal domain suggests that targeting AR phosphorylation can be synergistic to antagonizing the C-terminal domain by clinical antiandrogens.

View Article: PubMed Central - PubMed

Affiliation: Division of Hematology/Oncology, Beth Israel Deaconess Medical Center, Harvard Medical School 330 Brookline, MA 02115, USA.

ABSTRACT

The androgen receptor (AR) has been identified for decades and mediates essential steroid functions. Like most of biological molecules, AR functional activities are modulated by post-translational modifications. This review is focused on the reported activities and significance of AR phosphorylation, with particular emphasis on proline-directed serine/threonine phosphorylation that occurs predominantly on the receptor. The marked enrichment of AR phosphorylation in the most diverse N-terminal domain suggests that targeting AR phosphorylation can be synergistic to antagonizing the C-terminal domain by clinical antiandrogens.

No MeSH data available.