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Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
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Small molecule targeting of PTPs in cancer

John S Lazo1, Kelley E McQueeney1, James C Burnett2

  • 1Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, United States.

The International Journal of Biochemistry & Cell Biology
|September 26, 2017
PubMed

Insights

Protein tyrosine phosphatases (PTPs) are key in cancer. New small molecule inhibitors offer hope for novel cancer treatments by targeting these critical enzymes.

Area of Science:

  • Biochemistry
  • Oncology
  • Medicinal Chemistry

Background:

  • Protein tyrosine phosphatases (PTPs) play a crucial role in human cancer development and progression.
  • Historically, PTPs have been underrepresented as drug targets, hindering the development of effective inhibitors.

Purpose of the Study:

  • To review recent advancements in the discovery of small molecule inhibitors targeting cancer-relevant PTPs.
  • To highlight the biological annotation and therapeutic potential of these novel compounds.

Main Methods:

  • Biochemical studies of PTPs.
  • Small molecule screening campaigns.
  • Lead structure identification and characterization.

Main Results:

  • Identification of potent and mechanistically diverse small molecule PTP inhibitors.
  • These inhibitors facilitate the exploration of PTPs' cellular roles in cancer.
  • Compounds show promise for new cancer therapeutic strategies.

Conclusions:

  • Recent advances are transforming PTPs into viable drug targets for cancer therapy.
  • Novel small molecule inhibitors represent a potential inflection point for treating various cancers.
Keywords:
Allosteric inhibitionCancerChemical probesDrug-like inhibitorsTyrosine phosphatases

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