ck2-dependent phosphorylation of progesterone receptors (PR) on Ser81 regulates PR-B isoform-specific target gene expression in breast cancer cells

Mol Cell Biol. 2011 Jun;31(12):2439-52. doi: 10.1128/MCB.01246-10. Epub 2011 Apr 25.

Abstract

Progesterone receptors (PR) are critical mediators of mammary gland development and contribute to breast cancer progression. Progestin-induced rapid activation of cytoplasmic protein kinases leads to selective regulation of growth-promoting genes by phospho-PR species. Herein, we show that phosphorylation of PR Ser81 is ck2 dependent and progestin regulated in intact cells but also occurs in the absence of PR ligands when cells enter the G(1)/S phase of the cell cycle. T47D breast cancer cells stably expressing a PR-B mutant receptor that cannot be phosphorylated at Ser79/81 (S79/81A) formed fewer soft agar colonies. Regulation of selected genes by PR-B, but not PR-A, also required Ser79/81 phosphorylation for basal and/or progestin-regulated (BIRC3, HSD11β2, and HbEGF) expression. Additionally, wild-type (wt) PR-B, but not S79/81A mutant PR, was robustly recruited to a progesterone response element (PRE)-containing transcriptional enhancer region of BIRC3; abundant ck2 also associated with this region in cells expressing wt but not S79/81A PR. We conclude that phospho-Ser81 PR provides a platform for ck2 recruitment and regulation of selected PR-B target genes. Understanding how ligand-independent PRs function in the context of high levels of kinase activities characteristic of breast cancer is critical to understanding the basis of tumor-specific changes in gene expression and will speed the development of highly selective treatments.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 2 / genetics
  • 11-beta-Hydroxysteroid Dehydrogenase Type 2 / metabolism
  • Animals
  • Baculoviral IAP Repeat-Containing 3 Protein
  • Breast Neoplasms / genetics*
  • Breast Neoplasms / metabolism
  • Casein Kinase II / genetics
  • Casein Kinase II / metabolism*
  • Cell Line, Tumor
  • Female
  • Gene Expression Regulation, Neoplastic*
  • Heparin-binding EGF-like Growth Factor
  • Humans
  • Inhibitor of Apoptosis Proteins / genetics
  • Inhibitor of Apoptosis Proteins / metabolism
  • Intercellular Signaling Peptides and Proteins / genetics
  • Intercellular Signaling Peptides and Proteins / metabolism
  • Mice
  • Phosphorylation
  • Promoter Regions, Genetic
  • Protein Isoforms / genetics
  • Protein Isoforms / metabolism*
  • Receptors, Progesterone / genetics
  • Receptors, Progesterone / metabolism*
  • Serine / metabolism*
  • Transcription, Genetic
  • Ubiquitin-Protein Ligases

Substances

  • HBEGF protein, human
  • Hbegf protein, mouse
  • Heparin-binding EGF-like Growth Factor
  • Inhibitor of Apoptosis Proteins
  • Intercellular Signaling Peptides and Proteins
  • Protein Isoforms
  • Receptors, Progesterone
  • progesterone receptor B
  • Serine
  • 11-beta-Hydroxysteroid Dehydrogenase Type 2
  • HSD11B2 protein, human
  • BIRC3 protein, human
  • Baculoviral IAP Repeat-Containing 3 Protein
  • Ubiquitin-Protein Ligases
  • Casein Kinase II