Targeting RSK2 in human malignancies

Expert Opin Ther Targets. 2011 Jan;15(1):11-20. doi: 10.1517/14728222.2010.531013. Epub 2010 Oct 25.

Abstract

Importance of the field: p90 ribosomal S6 kinase 2 (RSK2) belongs to a Ser/Thr kinase family containing four members, RSK1 - 4, which play an essential role in a number of cellular functions including cell cycle, survival and proliferation. Recent advances reveal a crucial role of RSK2 in oncogenesis and tumor progression, making RSK2 an attractive therapeutic target for cancer treatment.

Area covered in this review: Recent findings identifying the role of RSK2 in human cancers, including hematopoietic malignancies and solid tumors. Therapeutic implications of targeting RSK2 are also discussed with regard to clinical circumstance.

What the reader will gain: A better understanding of molecular mechanisms underlying RSK2 activation and its contribution to human cancers and also insight into the development of novel targeted cancer therapy.

Take home message: The significance of RSK2 in cancer cell survival, proliferation, invasion and tumor metastasis varies amongst human malignancies and depends on the signaling properties of the oncogenes and cellular microenvironment of the transformed cells. Thus, further exploitation of RSK2 signaling and its dynamic interaction with other crucial oncogenic and pro-metastatic pathways in different human malignancies is needed for more effective therapeutic interventions.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation
  • Cell Survival
  • Drug Delivery Systems
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / physiopathology
  • Protein Kinase Inhibitors / pharmacology
  • Ribosomal Protein S6 Kinases, 90-kDa / antagonists & inhibitors*
  • Ribosomal Protein S6 Kinases, 90-kDa / metabolism

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Ribosomal Protein S6 Kinases, 90-kDa
  • ribosomal protein S6 kinase, 90kDa, polypeptide 3