title: Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors.
abstract: We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological activity. We show the results of recent SAR studies on a novel series of phenylacetic derivatives supported by a combined approach of mutagenesis experiments and conformational analysis. The results suggest novel insights on the fine role of the propionic/acetic chain in the modulation of CXCL8 receptors.
authors: Research Center, Dompé pha.r.ma s.p.a., via Campo di Pile, 67100, L'Aquila, Italy.
authors: Manolo Rocco
authors: MR
authors: Sablone
authors: Maria Candida
authors: MC
authors: Cesta
authors: Alessio
authors: A
authors: Moriconi
authors: Andrea
authors: A
authors: Aramini
authors: Cinzia
authors: C
authors: Bizzarri
authors: Claudia
authors: C
authors: Di Giacinto
authors: Rosa
authors: R
authors: Di Bitondo
authors: Isabelle
authors: I
authors: Gloaguen
authors: Massimiliano
authors: M
authors: Aschi
authors: Marcello
authors: M
authors: Crucianelli
authors: Riccardo
authors: R
authors: Bertini
authors: Marcello
authors: M
authors: Allegretti
mesh_terms: D000494:Allosteric Regulation; D000495:Allosteric Site; D002625:Chemistry, Organic / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002633:Chemotaxis; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D008958:Models, Molecular; D008968:Molecular Conformation; D016296:Mutagenesis; D009154:Mutation; D023062:Receptors, Interleukin-8A / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D023062:Receptors, Interleukin-8A