Related Experiment Video

Updated: Mar 7, 2026

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
08:45

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors

Published on: July 17, 2020

6.7K

Targeting PAK1

Galina Semenova1, Jonathan Chernoff2

  • 1Cancer Biology Program, Fox Chase Cancer Center, Philadelphia, PA.

Biochemical Society Transactions
|February 17, 2017
PubMed

Insights

p21-Activated kinase 1 (PAK1) is a key target for cancer and neurological disorder therapies. Various PAK1 inhibitors show promise as research tools and potential therapeutic agents, requiring further safety and efficacy studies.

Area of Science:

  • Oncology
  • Neuroscience
  • Pharmacology

Background:

  • p21-Activated kinase 1 (PAK1) is frequently dysregulated in cancers and neurological disorders.
  • PAK1 plays a central role in multiple oncogenic signaling pathways.
  • PAK1 is a tractable target for small-molecule inhibition.

Purpose of the Study:

  • To review the therapeutic potential of PAK1 inhibitors.
  • To highlight the utility of PAK1 inhibitors as laboratory tools.
  • To discuss the future clinical development of PAK1 inhibitors.

Main Methods:

  • Development of ATP-competitive, allosteric, and peptide inhibitors.
  • Preclinical evaluation of PAK1-targeting compounds.
  • One PAK1 inhibitor has undergone clinical trial evaluation.

Main Results:

  • Several PAK1 inhibitors with distinct properties have been developed.
  • These inhibitors serve as valuable tools for biological and disease research.
  • Promising therapeutic potential exists for PAK1-targeting agents.

Conclusions:

  • PAK1 inhibitors represent promising therapeutic candidates for cancer and neurological diseases.
  • Further investigation into the safety and efficacy of PAK1 inhibitors is crucial for clinical development.
Keywords:
cancerprotein–serine–threonine kinasessignalingsmall moleculestherapeutics

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