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SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease.
Wityak, John; Prime, Michael E; Brookfield, Frederick A; Courtney, Stephen M; Erfan, Sayeh; Johnsen, Siw; Johnson, Peter D; Li, Marie; Marston, Richard W; Reed, Laura; Vaidya, Darshan; Schaertl, Sabine; Pedret-Dunn, Anna; Beconi, Maria; Macdonald, Douglas; Muñoz-Sanjuan, Ignacio; Dominguez, Celia.
Afiliação
  • Wityak J; CHDI Management/CHDI Foundation , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.
  • Prime ME; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Brookfield FA; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Courtney SM; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Erfan S; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Johnsen S; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Johnson PD; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Li M; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Marston RW; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Reed L; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Vaidya D; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Schaertl S; Evotec AG , Manfred Eigen Campus, Essener Bogen 7, 22419 Hamburg, Germany.
  • Pedret-Dunn A; Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon, OX14 4SA, United Kingdom.
  • Beconi M; CHDI Management/CHDI Foundation , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.
  • Macdonald D; CHDI Management/CHDI Foundation , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.
  • Muñoz-Sanjuan I; CHDI Management/CHDI Foundation , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.
  • Dominguez C; CHDI Management/CHDI Foundation , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.
ACS Med Chem Lett ; 3(12): 1024-8, 2012 Dec 13.
Article em En | MEDLINE | ID: mdl-24900424
We report a series of irreversible transglutaminase 2 inhibitors starting from a known lysine dipeptide bearing an acrylamide warhead. We established new SARs resulting in compounds demonstrating improved potency and better physical and calculated properties. Transglutaminase selectivity profiling and in vitro ADME properties of selected compounds are also reported.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2012 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Estados Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2012 Tipo de documento: Article País de afiliação: Estados Unidos País de publicação: Estados Unidos