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Progress in the Development of Platelet‐Activating Factor Receptor (PAFr) Antagonists and Applications in the Treatment of Inflammatory Diseases
Author(s) -
Hyland Isabel K.,
O'Toole Ronan F.,
Smith Jason A.,
Bissember Alex C.
Publication year - 2018
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201800401
Subject(s) - platelet activating factor receptor , platelet activating factor , receptor , ligand (biochemistry) , chemistry , pharmacology , inflammation , computational biology , biology , antagonist , immunology , biochemistry
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.