Inhibition of K-RAS4B by a Unique Mechanism of Action: Stabilizing Membrane-Dependent Occlusion of the Effector-Binding Site.

Fang, Zhenhao; Marshall, Christopher B; Nishikawa, Tadateru; Gossert, Alvar D; Jansen, Johanna M; Jahnke, Wolfgang; Ikura, Mitsuhiko

Fang, Zhenhao; Marshall, Christopher B; Nishikawa, Tadateru; Gossert, Alvar D; Jansen, Johanna M; Jahnke, Wolfgang; Ikura, Mitsuhiko.

Afiliação

Fang Z; Department of Medical Biophysics, University of Toronto, Princess Margaret Cancer Centre, University Health Network, Toronto, ON M5G 2M9, Canada.
Marshall CB; Department of Medical Biophysics, University of Toronto, Princess Margaret Cancer Centre, University Health Network, Toronto, ON M5G 2M9, Canada. Electronic address: cmarshal@uhnresearch.ca.
Nishikawa T; Department of Medical Biophysics, University of Toronto, Princess Margaret Cancer Centre, University Health Network, Toronto, ON M5G 2M9, Canada.
Gossert AD; Chemical Biology and Therapeutics, Novartis Institutes for BioMedical Research, Basel 4002, Switzerland; Institute for Molecular Biology and Biophysics, Department of Biology, ETH Zürich, Zürich 8093, Switzerland.
Jansen JM; Department of Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Emeryville, CA 94608, USA.
Jahnke W; Chemical Biology and Therapeutics, Novartis Institutes for BioMedical Research, Basel 4002, Switzerland.
Ikura M; Department of Medical Biophysics, University of Toronto, Princess Margaret Cancer Centre, University Health Network, Toronto, ON M5G 2M9, Canada. Electronic address: mikura@uhnresearch.ca.

Cell Chem Biol ; 25(11): 1327-1336.e4, 2018 11 15.

Article em En | MEDLINE | ID: mdl-30122370

Assuntos

Antineoplásicos/química; Antineoplásicos/farmacologia; Inibidores Enzimáticos/química; Inibidores Enzimáticos/farmacologia; Piperidinas/química; Piperidinas/farmacologia; Proteínas Proto-Oncogênicas p21(ras)/antagonistas & inibidores; Animais; Descoberta de Drogas; Humanos; Indóis/química; Indóis/farmacologia; Bicamadas Lipídicas/metabolismo; Modelos Moleculares; Proteínas Proto-Oncogênicas p21(ras)/química; Proteínas Proto-Oncogênicas p21(ras)/metabolismo

Palavras-chave

HADDOCK; KRAS; NMR; cancer; drug discovery; membrane-associated protein; nanodisc; paramagnetic relaxation enhancement; phospholipid bilayer; prenylation

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidinas / Proteínas Proto-Oncogênicas p21(ras) / Inibidores Enzimáticos / Antineoplásicos Limite: Animals / Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article

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