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Application of small molecule FPR1 antagonists in the treatment of cancers

Djevdet S Ahmet1, Haneen A Basheer2, Anwar Salem1

  • 1Institute of Cancer Therapeutics, University of Bradford, Richmond Road, Bradford, BD7 1DP, UK.

Scientific Reports
|October 15, 2020
PubMed

Insights

A novel small molecule, ICT12035, effectively inhibits formylpeptide receptor-1 (FPR1) in cancer. This FPR1 antagonist shows promise for developing new cancer therapies by targeting tumor expansion and recurrence.

Area of Science:

  • Oncology
  • Immunology
  • Pharmacology

Background:

  • Formylpeptide receptor-1 (FPR1) is a G protein-coupled receptor involved in leukocyte trafficking during infection and inflammation.
  • FPR1 is increasingly recognized for its role in cancer progression, including tumor expansion, resistance to therapy, and recurrence.
  • Targeting FPR1 presents a potential therapeutic strategy for various cancers.

Purpose of the Study:

  • To evaluate the efficacy of ICT12035, a selective small molecule FPR1 antagonist, in preclinical cancer models.
  • To investigate the potential of targeting FPR1 as a novel cancer treatment strategy.

Main Methods:

  • In vitro assays assessing cancer cell proliferation and invasion in 2D and 3D cultures.
  • In vivo studies using a relevant animal model to evaluate ICT12035's anti-cancer effects.
  • Calcium mobilization assays to confirm FPR1 antagonist potency (30 nM).

Main Results:

  • ICT12035 demonstrated significant efficacy in inhibiting cancer cell proliferation and invasion in vitro.
  • The FPR1 antagonist showed promising anti-tumor activity in the in vivo model.
  • ICT12035 is a potent and selective inhibitor of FPR1.

Conclusions:

  • Selective small molecule antagonism of FPR1, exemplified by ICT12035, is a viable therapeutic approach for cancer.
  • Targeting FPR1 may offer a new avenue for treating cancers by inhibiting tumor growth and spread.
  • Further investigation into ICT12035 for cancer treatment is warranted.

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