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Platelet-activating factor (PAF) and its receptor (PAFr) have been implicated in a wide range of diseases and disorders that originate from the activation of inflammatory pathways. Although the exact structure of the binding site on the PAFr remains unknown, the PAFr is a well-established therapeutic target, and an array of structurally diverse PAFr antagonists have been identified. These include compounds that are structurally similar to the natural PAF ligand, synthetic heterocycles, complex polycyclic natural products, and various metal complexes. This review provides an update on more than 20 years of progress in this area. The development and synthesis of new PAFr antagonists, structure-activity relationship studies, the biological activity of these molecules, and their therapeutic potential are discussed.

Item Type:	Refereed Article
Keywords:	ginkgolides, inflammatory diseases, platelet-activating factor, thienodiazepines, xanthones
Research Division:	Biomedical and Clinical Sciences
Research Group:	Medical microbiology
Research Field:	Medical bacteriology
Objective Division:	Manufacturing
Objective Group:	Human pharmaceutical products
Objective Field:	Human pharmaceutical treatments
UTAS Author:	Hyland, IK (Ms Isabel Hyland)
UTAS Author:	O'Toole, RF (Dr Ronan O'Toole)
UTAS Author:	Smith, JA (Associate Professor Jason Smith)
UTAS Author:	Bissember, AC (Associate Professor Alex Bissember)
ID Code:	127815
Year Published:	2018
Web of Science® Times Cited:	14
Deposited By:	Medicine
Deposited On:	2018-08-17
Last Modified:	2019-12-03
Downloads:	9 View Download Statistics