Direct evidence of edge-to-face CH/π interaction for PAR-1 thrombin receptor activation.

Dose-Response Relationship, Drug Healthy Volunteers Humans Ligands Molecular Structure Peptide Fragments / chemistry Phenylalanine / chemistry Platelet Aggregation / drug effects Receptor, PAR-1 / antagonists & inhibitors Structure-Activity Relationship
CH/π interaction Fluorophenylalanine Phenylalanine Thrombin receptor

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
01 12 2021
Historique:
received: 20 07 2021
revised: 12 10 2021
accepted: 17 10 2021
pubmed: 19 11 2021
medline: 19 1 2022
entrez: 18 11 2021
Statut: ppublish

Résumé

Heptapeptide SFLLRNP is a receptor-tethered ligand of protease-activated receptor 1 (PAR-1), and its Phe at position 2 is essential for the aggregation of human platelets. To validate the structural elements of the Phe-phenyl group in receptor activation, we have synthesized a complete set of S/Phe/LLRNP peptides comprising different series of fluorophenylalanine isomers (F

Identifiants

DOI: 10.1016/j.bmc.2021.116498 PMID: 34794000
pubmed: 34794000
pii: S0968-0896(21)00506-X
doi: 10.1016/j.bmc.2021.116498
pii:
doi:

Substances chimiques

Ligands 0
Peptide Fragments 0
Receptor, PAR-1 0
thrombin receptor peptide SFLLRNP 145229-76-1
Phenylalanine 47E5O17Y3R

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

116498

Informations de copyright

Copyright © 2021 Elsevier Ltd. All rights reserved.

Auteurs

Daisuke Asai (D)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan.

Naoko Inoue (N)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan.

Makiko Sugiyama (M)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan.

Tsugumi Fujita (T)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan.

Yutaka Matsuyama (Y)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan.

Xiaohui Liu (X)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan.

Ayami Matsushima (A)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan.

Takeru Nose (T)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan.

Tommaso Costa (T)

Department of Pharmacology, Istituto Superiore di Sanità, 00161 Rome, Italy.

Yasuyuki Shimohigashi (Y)

Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty of Sciences, Kyushu University, Fukuoka 819-0395, Japan; Risk Science Research Institute, Ikimatsudai 3-7-5, Nishi-ku, Fukuoka 819-0044, Japan. Electronic address: shimo@kyudai.jp.

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Classifications MeSH

questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Personnes › Bénévoles › Volontaires sains › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Acides aminés, peptides et protéines › Peptides › Fragments peptidiques › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Acides aminés, peptides et protéines › Acides aminés › Acides aminés essentiels › Phénylalanine › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Phénomènes physiologiques respiratoires et circulatoires › Phénomènes physiogiques du sang › Hémostase › Activation plaquettaire › Agrégation plaquettaire › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs activés par la protéinase › Récepteurs à la thrombine › Récepteur de type PAR-1 › Direct evidence of edge-to-face CH/π...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Direct evidence of edge-to-face CH/π...