A novel molecular design of thrombin receptor antagonist

Tsugumi Fujita; Masahide Nakajima; Yoshihisa Inoue; Takeru Nose; Yasuyuki Shimohigashi

doi:10.1016/S0960-894X(99)00202-4

A novel molecular design of thrombin receptor antagonist

Tsugumi Fujita, Masahide Nakajima, Yoshihisa Inoue, Takeru Nose, Yasuyuki Shimohigashi

Division for Experimental Natural Science

Research output: Contribution to journal › Article › peer-review

12 Citations (Scopus)

Abstract

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)Phe-Aad(= α-aminoadipic acid)-Leu-Arg-Asn-Pro-NH₂ was found to be a potent antagonist.

Original language	English
Pages (from-to)	1351-1356
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	9
Issue number	10
DOIs	https://doi.org/10.1016/S0960-894X(99)00202-4
Publication status	Published - May 17 1999

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(99)00202-4

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AU - Inoue, Yoshihisa

AU - Nose, Takeru

AU - Shimohigashi, Yasuyuki

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A novel molecular design of thrombin receptor antagonist

Abstract

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