Azaindoles as Zinc-Binding Small-Molecule Inhibitors of the JAMM Protease CSN5.

Altmann, Eva; Erbel, Paul; Renatus, Martin; Schaefer, Michael; Schlierf, Anita; Druet, Adelaide; Kieffer, Laurence; Sorge, Mickael; Pfister, Keith; Hassiepen, Ulrich; Jones, Matthew; Ruedisser, Simon; Ostermeier, Daniela; Martoglio, Bruno; Jefferson, Anne B; Quancard, Jean

Altmann, Eva; Erbel, Paul; Renatus, Martin; Schaefer, Michael; Schlierf, Anita; Druet, Adelaide; Kieffer, Laurence; Sorge, Mickael; Pfister, Keith; Hassiepen, Ulrich; Jones, Matthew; Ruedisser, Simon; Ostermeier, Daniela; Martoglio, Bruno; Jefferson, Anne B; Quancard, Jean.

Afiliação

Altmann E; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Erbel P; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Renatus M; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Schaefer M; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Schlierf A; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Druet A; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Kieffer L; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Sorge M; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Pfister K; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Hassiepen U; Novartis Institutes for BioMedical Research, 4560 Horton Street, Emeryville, CA, 94608-2916, USA.
Jones M; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Ruedisser S; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Ostermeier D; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Martoglio B; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Jefferson AB; Novartis Institutes for BioMedical Research, Novartis Campus, 4002, Basel, Switzerland.
Quancard J; Pharma Research and Early Development, Roche Innovation Center Basel, 4070, Basel, Switzerland.

Angew Chem Int Ed Engl ; 56(5): 1294-1297, 2017 01 24.

Article em En | MEDLINE | ID: mdl-27981705

Assuntos

Complexo do Signalossomo COP9/antagonistas & inibidores; Indóis/metabolismo; Zinco/metabolismo; Sítios de Ligação; Complexo do Signalossomo COP9/genética; Complexo do Signalossomo COP9/metabolismo; Domínio Catalítico; Proliferação de Células/efeitos dos fármacos; Cristalografia por Raios X; Transferência Ressonante de Energia de Fluorescência; Células HCT116; Humanos; Indóis/química; Indóis/farmacologia; Simulação de Acoplamento Molecular; Proteína NEDD8/química; Proteína NEDD8/metabolismo; Subunidades Proteicas/antagonistas & inibidores; Subunidades Proteicas/genética; Subunidades Proteicas/metabolismo; Interferência de RNA; RNA Interferente Pequeno/metabolismo; Proteínas Quinases Associadas a Fase S/química; Proteínas Quinases Associadas a Fase S/metabolismo; Zinco/química

Palavras-chave

CSN5; azaindoles; inhibitors; metalloproteases; ubiquitin ligases

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Zinco / Complexo do Signalossomo COP9 / Indóis Limite: Humans Idioma: En Revista: Angew Chem Int Ed Engl Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Suíça

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