A novel molecular design of thrombin receptor antagonist

In a computer modeling of transmembrane domains of human thrombin receptor, Lys-158 was found near the ligand binding site. To capture this basic residue, analogs of peptide ligand containing a series of acidic amino acids were synthesized and assayed for human platelet aggregation, and Ser-( p-F)Ph...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-05, Vol.9 (10), p.1351-1356
Hauptverfasser:	Fujita, Tsugumi, Nakajima, Masahide, Inoue, Yoshihisa, Nose, Takeru, Shimohigashi, Yasuyuki
Format:	Artikel
Sprache:	eng
Schlagworte:	Antithrombins - chemical synthesis Antithrombins - chemistry Antithrombins - metabolism Binding Sites Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Computer Simulation Drug Design Humans Lysine - metabolism Medical sciences Models, Molecular Pharmacology. Drug treatments Platelet Aggregation Inhibitors - chemical synthesis Platelet Aggregation Inhibitors - chemistry Platelet Aggregation Inhibitors - metabolism Receptors, Thrombin - antagonists & inhibitors Receptors, Thrombin - chemistry Receptors, Thrombin - metabolism Static Electricity Structure-Activity Relationship
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