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A small-molecule inhibitor of C5 complement protein.
Jendza, Keith; Kato, Mitsunori; Salcius, Michael; Srinivas, Honnappa; De Erkenez, Andrea; Nguyen, Anh; McLaughlin, Doug; Be, Celine; Wiesmann, Christian; Murphy, Jason; Bolduc, Philippe; Mogi, Muneto; Duca, Jose; Namil, Abdel; Capparelli, Michael; Darsigny, Veronique; Meredith, Erik; Tichkule, Ritesh; Ferrara, Luciana; Heyder, Jessica; Liu, Fang; Horton, Patricia A; Romanowski, Michael J; Schirle, Markus; Mainolfi, Nello; Anderson, Karen; Michaud, Gregory A.
Afiliação
  • Jendza K; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Kato M; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Salcius M; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Srinivas H; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Basel, Switzerland.
  • De Erkenez A; Ophthalmology, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Nguyen A; Ophthalmology, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • McLaughlin D; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Be C; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Basel, Switzerland.
  • Wiesmann C; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Basel, Switzerland.
  • Murphy J; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Bolduc P; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Mogi M; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Duca J; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Namil A; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Capparelli M; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Darsigny V; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Meredith E; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Tichkule R; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Ferrara L; Ophthalmology, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Heyder J; Ophthalmology, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Liu F; Ophthalmology, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Horton PA; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Romanowski MJ; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Schirle M; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Mainolfi N; Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Anderson K; Ophthalmology, Novartis Institutes of Biomedical Research, Cambridge, MA, USA.
  • Michaud GA; Chemical Biology and Therapeutics, Novartis Institutes of Biomedical Research, Cambridge, MA, USA. gregory.michaud@novartis.com.
Nat Chem Biol ; 15(7): 666-668, 2019 07.
Article em En | MEDLINE | ID: mdl-31209353
ABSTRACT
The complement pathway is an important part of the immune system, and uncontrolled activation is implicated in many diseases. The human complement component 5 protein (C5) is a validated drug target within the complement pathway, as an anti-C5 antibody (Soliris) is an approved therapy for paroxysmal nocturnal hemoglobinuria. Here, we report the identification, optimization and mechanism of action for the first small-molecule inhibitor of C5 complement protein.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Complemento C5 / Bibliotecas de Moléculas Pequenas Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Complemento C5 / Bibliotecas de Moléculas Pequenas Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article