Application of small molecule FPR1 antagonists in the treatment of cancers

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Publication date
2020-10
Author
Ahmet, Djevdet S.
Basheer, H.A.
Salem, Anwar
Lu, Di
Aghamohammadi, Amin
Weyerhäuser, P.
Bordiga, A.
Almeniawi, J.
Rashid, S.
Cooper, Patricia A.
Keyword
Formylpeptide receptor-1 (FPR1)
Small molecule antagonist
Treatment of cancers
Rights
© The Author(s) 2020. This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.
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Abstract
The formylpeptide receptor-1 (FPR1) is a member of the chemotactic GPCR-7TM formyl peptide receptor family, whose principle function is in trafficking of various leukocytes into sites of bacterial infection and inflammation. More recently, FPR1 has been shown to be expressed in different types of cancer and in this context, plays a significant role in their expansion, resistance and recurrence. ICT12035 is a selective and potent (30 nM in calcium mobilisation assay) small molecule FPR1 antagonist. Here, we demonstrate the efficacy of ICT12035, in a number of 2D and 3D proliferation and invasion in vitro assays and an in vivo model. Our results demonstrate that targeting FPR1 by a selective small molecule antagonist, such as ICT12035, can provide a new avenue for the treatment of cancers.
URI
http://hdl.handle.net/10454/18145
Version
Published version
Citation
Ahmet DS, Basheer HA, Salem A et al (2020) Application of small molecule FPR1 antagonists in the treatment of cancers. Scientific Reports. 10: 17249.
Link to publisher’s version
https://doi.org/10.1038/s41598-020-74350-z
Type
Article
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