Current status of PTP-based therapeutics

Rongjun He, Zhong-Yin Zhang

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

Protein tyrosine phosphorylation regulates virtually all aspects of cellular function. Proper levels of protein tyrosine phosphorylation are controlled by protein-tyrosine kinases (PTKs) and protein-tyrosine phosphatases (PTPs). Deregulation of tyrosine phosphorylation-mediated signaling is a major cause of cancer. Indeed, PTKs represent an important class of anti-cancer drug targets with more than 20 drugs already approved by the FDA. Several PTPs are also implicated in tumor onset, progression and metastasis, and have attracted attention as potential therapeutic targets for cancer treatment. The most recognized members of the PTP family include PTP1B, SHP2, CDC25, and PRLs. PTP1B plays a positive role in breast cancer progression; SHP2 germ line and somatic gain-of-function mutations cause Noonan Syndrome, juvenile myelomonocytic leukemia, acute myeloid leukemia, and solid tumors; CDC25 regulates cell cycle progression and is overexpressed in a number of human cancers; and the PRLs are overexpressed in cancer and have been linked to tumor metastasis. Hence, inhibitors directed against these PTPs can serve as potential novel anti-cancer agents. This chapter provides an overview of the mechanisms of these oncogenic PTPs in promoting cancer, the approaches for inhibitor discovery, as well as the current status of drug development targeting these phosphatases.

Original languageEnglish (US)
Title of host publicationProtein Tyrosine Phosphatases in Cancer
PublisherSpringer New York
Pages335-353
Number of pages19
ISBN (Electronic)9781493936496
ISBN (Print)9781493936472
DOIs
StatePublished - Jan 1 2016

Keywords

  • Cancer
  • CDC25
  • Drug development
  • Inhibitor design
  • Potency and specificity
  • PRL
  • Protein-tyrosine phosphatase
  • PTP1B
  • SHP2
  • Therapeutics

ASJC Scopus subject areas

  • Medicine(all)
  • Biochemistry, Genetics and Molecular Biology(all)

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  • Cite this

    He, R., & Zhang, Z-Y. (2016). Current status of PTP-based therapeutics. In Protein Tyrosine Phosphatases in Cancer (pp. 335-353). Springer New York. https://doi.org/10.1007/978-1-4939-3649-6_13