Conformational Plasticity of Human Protease-Activated Receptor 1 upon Antagonist- and Agonist-Binding.

Spoerri, Patrizia M; Sapra, K Tanuj; Zhang, Cheng; Mari, Stefania A; Kato, Hideaki E; Kobilka, Brian K; Müller, Daniel J

Spoerri, Patrizia M; Sapra, K Tanuj; Zhang, Cheng; Mari, Stefania A; Kato, Hideaki E; Kobilka, Brian K; Müller, Daniel J.

Afiliación

Spoerri PM; Department of Biosystems Science and Engineering, Eidgenössische Technische Hochschule (ETH) Zurich, 4058 Basel, Switzerland.
Sapra KT; Department of Biosystems Science and Engineering, Eidgenössische Technische Hochschule (ETH) Zurich, 4058 Basel, Switzerland.
Zhang C; Department of Cellular Physiology and Medicine, Stanford University School of Medicine, Palo Alto, CA 94305, USA.
Mari SA; Department of Biosystems Science and Engineering, Eidgenössische Technische Hochschule (ETH) Zurich, 4058 Basel, Switzerland.
Kato HE; Department of Cellular Physiology and Medicine, Stanford University School of Medicine, Palo Alto, CA 94305, USA.
Kobilka BK; Department of Cellular Physiology and Medicine, Stanford University School of Medicine, Palo Alto, CA 94305, USA.
Müller DJ; Department of Biosystems Science and Engineering, Eidgenössische Technische Hochschule (ETH) Zurich, 4058 Basel, Switzerland. Electronic address: daniel.mueller@bsse.ethz.ch.

Structure ; 27(10): 1517-1526.e3, 2019 10 01.

Article en En | MEDLINE | ID: mdl-31422910

Asunto(s)

Guanidinas/farmacología; Oligopéptidos/farmacología; Fragmentos de Péptidos/farmacología; Receptor PAR-1/química; Receptor PAR-1/metabolismo; Sitios de Unión; Guanidinas/química; Humanos; Ligandos; Modelos Moleculares; Oligopéptidos/química; Fragmentos de Péptidos/química; Unión Proteica; Estructura Secundaria de Proteína; Receptor PAR-1/agonistas; Receptor PAR-1/antagonistas & inhibidores; Imagen Individual de Molécula

Palabras clave

G protein-coupled receptor (GPCR); atomic force microscopy (AFM); energetic properties; free energy landscape; functional states; human protease-activated receptor 1 (PAR1); kinetic properties; ligand binding; mechanical properties; single-molecule force spectroscopy (SMFS); structural stiffness

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oligopéptidos / Fragmentos de Péptidos / Receptor PAR-1 / Guanidinas Límite: Humans Idioma: En Revista: Structure Asunto de la revista: BIOLOGIA MOLECULAR / BIOQUIMICA / BIOTECNOLOGIA Año: 2019 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Estados Unidos

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