Journal article

The Novel Small-molecule Annexin-A1 Mimetic, Compound 17b, Elicits Vasoprotective Actions in Streptozotocin-induced Diabetic Mice.

Sarah A Marshall, Cheng Xue Qin, Maria Jelinic, Kelly O'Sullivan, Minh Deo, Jesse Walsh, Mandy Li, Laura J Parry, Rebecca H Ritchie, Chen Huei Leo

International Journal of Molecular Sciences | MDPI AG | Published : 2020

Open access

Abstract

The formyl peptide receptor (FPR) family are a group of G-protein coupled receptors that play an important role in the regulation of inflammatory processes. It is well-established that activation of FPRs can have cardioprotective properties. Recently, more stable small-molecule FPR1/2 agonists have been described, including both Compound 17b (Cmpd17b) and Compound 43 (Cmpd43). Both agonists activate a range of signals downstream of FPR1/2 activation in human-engineered FPR-expressing cells, including ERK1/2 and Akt. Importantly, Cmpd17b (but not Cmpd43) favours bias away from intracellular Ca2+ mobilisation in this context, which has been associated with greater cardioprotection in response ..

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University of Melbourne Researchers

Grants

Awarded by DARP


Funding Acknowledgements

This study was funded in part by a grant-in-aid from the Diabetes Australia Research Trust to CXQ, CHL, LJP, and RHR (Y18G-QINC) and by the National Health and Medical Research Council of Australia, including NHMRC Early Career Research Fellowships to SM (ID1160684) and MJ (ID1146314), and an NHMRC Senior Research Fellowship and grant to RHR (ID1059960 and ID1081770). CXQ is a National Hear Foundation Future Fellow. CHL received the Faculty Early Career Award (Ministry of Education, Singapore). This research was also supported by the Victorian Government of Australia's Operational Infrastructure Support Program.