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Structure-based discovery of LpxC inhibitors.
Zhang, Jing; Chan, Audrey; Lippa, Blaise; Cross, Jason B; Liu, Christopher; Yin, Ning; Romero, Jan Antoinette C; Lawrence, Jonathan; Heney, Ryan; Herradura, Prudencio; Goss, Jennifer; Clark, Cynthia; Abel, Cassandra; Zhang, Yanzhi; Poutsiaka, Katherine M; Epie, Felix; Conrad, Mary; Mahamoon, Azard; Nguyen, Kien; Chavan, Ajit; Clark, Edward; Li, Tong-Chuan; Cheng, Robert K; Wood, Michael; Andersen, Ole A; Brooks, Mark; Kwong, Jason; Barker, John; Parr, Ian Barrie; Gu, Yugui; Ryan, M Dominic; Coleman, Scott; Metcalf, Chester A.
Afiliación
  • Zhang J; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA. Electronic address: jackzhang49@yahoo.com.
  • Chan A; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Lippa B; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Cross JB; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Liu C; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Yin N; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Romero JA; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Lawrence J; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Heney R; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Herradura P; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Goss J; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Clark C; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Abel C; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Zhang Y; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Poutsiaka KM; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Epie F; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Conrad M; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Mahamoon A; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Nguyen K; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Chavan A; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Clark E; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Li TC; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Cheng RK; Evotec UK, Ltd., 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, UK.
  • Wood M; Evotec UK, Ltd., 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, UK.
  • Andersen OA; Evotec UK, Ltd., 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, UK.
  • Brooks M; Evotec UK, Ltd., 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, UK.
  • Kwong J; Evotec UK, Ltd., 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, UK.
  • Barker J; Evotec UK, Ltd., 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, UK.
  • Parr IB; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Gu Y; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Ryan MD; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Coleman S; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
  • Metcalf CA; Cubist Pharmaceuticals Inc., 65 Hayden Avenue, Lexington, MA 02421, USA.
Bioorg Med Chem Lett ; 27(8): 1670-1680, 2017 04 15.
Article en En | MEDLINE | ID: mdl-28302397
ABSTRACT
The emergence and spread of multidrug-resistant (MDR) Gram negative bacteria presents a serious threat for public health. Novel antimicrobials that could overcome the resistance problems are urgently needed. UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) is a cytosolic zinc-based deacetylase that catalyzes the first committed step in the biosynthesis of lipid A, which is essential for the survival of Gram-negative bacteria. Our efforts toward the discovery of novel LpxC inhibitors are presented herein.
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Inhibidores Enzimáticos / Amidohidrolasas / Bacterias Gramnegativas / Antibacterianos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article
Texto completo
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Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Inhibidores Enzimáticos / Amidohidrolasas / Bacterias Gramnegativas / Antibacterianos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article