Antagonism of the TXA2 receptor by seratrodast: a structural approach.
The crystal structure of seratrodast (AA-2414), a potent thromboxane A2 (TXA2) receptor antagonist, served as starting point to docking studies with the modeled human TXA2 receptor. This structural approach provides rational basis for the design of new antagonists within the aryl sulfonamide family.
Wouters
J
J
Dept. of Chemistry, Facultés Universitaires Notre-Dame de la Paix, Namur, Belgium. jwouters@scf.fundp.ac.be
Durant
F
F
Masereel
B
B
D000818:Animals; D016227:Benzoquinones / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D015195:Drug Design; D006168:Guinea Pigs; D006538:Heptanoic Acids / Q000737:chemistry* / Q000494:pharmacology; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011448:Prostaglandin Antagonists / Q000737:chemistry* / Q000494:pharmacology; D017482:Receptors, Thromboxane / Q000037:antagonists & inhibitors / Q000737:chemistry*; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology
C120544:BM 144; D016227:Benzoquinones; D006538:Heptanoic Acids; D011448:Prostaglandin Antagonists; D017482:Receptors, Thromboxane; D013449:Sulfonamides; C060230:seratrodast