Application of small molecule FPR1 antagonists in the treatment of cancers

被引：12

作者：

Ahmet, Djevdet S. ^{[1
]}

Basheer, Haneen A. ^{[2
]}

Salem, Anwar ^{[1
]}

Lu, Di ^{[1
]}

Aghamohammadi, Amin ^{[1
]}

Weyerhaeuser, Patrick ^{[3
]}

Bordiga, Andrea ^{[4
]}

Almeniawi, Juman ^{[1
]}

Rashid, Sabah ^{[1
]}

Cooper, Patricia A. ^{[1
]}

Shnyder, Steven D. ^{[1
]}

Vinader, Victoria ^{[1
]}

Afarinkia, Kamyar ^{[1
]}

机构：

[1] Univ Bradford, Inst Canc Therapeut, Richmond Rd, Bradford BD7 1DP, W Yorkshire, England

[2] Zarqa Univ, Fac Pharm, POB 132222, Zarqa 13132, Jordan

[3] Univ Med Mainz, Inst Toxikol, Gebaude 905-4 OG,Obere Zahlbacher Str 67, D-55131 Mainz, Germany

[4] Univ Torino, Dipartimento Sci & Tecnol Farmaco, Via P Giuria 9, I-10125 Turin, Italy

来源：

SCIENTIFIC REPORTS | 2020年 / 10卷 / 01期

关键词：

FORMYL-PEPTIDE RECEPTOR; EXPRESSION; GLIOBLASTOMA; INVASION; LIGAND; ROLES; ANXA1;

D O I：

10.1038/s41598-020-74350-z

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

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.

引用

页数：12

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