Discovery and evaluation of PRL trimer disruptors for novel anticancer agents

Yunpeng Bai, Zhi Hong Yu, Zhong Yin Zhang

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

Overexpression of PRL phosphatases (PRL1, PRL2, and PRL3) has been found in a variety of late-stage tumors and their distant metastatic sites. Therefore, the oncogenic PRL phosphatases represent intriguing targets for cancer therapy. There is considerable interest in identifying small molecule inhibitors targeting PRLs as novel anticancer agents. However, it has been difficult to acquire phosphatase activity-based PRL inhibitors due to the unusual wide and shallow catalytic pockets of PRLs revealed by crystal structure studies. Here, we present a novel method to identify PRL1 inhibitors by targeting the PRL1 trimer interface and the procedure to characterize their biochemical and cellular activity.

Original languageEnglish (US)
Title of host publicationMethods in Molecular Biology
PublisherHumana Press Inc.
Pages121-138
Number of pages18
Volume1447
DOIs
StatePublished - 2016

Publication series

NameMethods in Molecular Biology
Volume1447
ISSN (Print)10643745

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Keywords

  • MTT assay
  • PRL phosphatases
  • Transwell migration assay
  • Trimerization
  • Virtual screening
  • Wound healing assay

ASJC Scopus subject areas

  • Medicine(all)
  • Molecular Biology
  • Genetics

Cite this

Bai, Y., Yu, Z. H., & Zhang, Z. Y. (2016). Discovery and evaluation of PRL trimer disruptors for novel anticancer agents. In Methods in Molecular Biology (Vol. 1447, pp. 121-138). (Methods in Molecular Biology; Vol. 1447). Humana Press Inc.. https://doi.org/10.1007/978-1-4939-3746-2_8