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Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.
Nagle, Advait; Biggart, Agnes; Be, Celine; Srinivas, Honnappa; Hein, Andreas; Caridha, Diana; Sciotti, Richard J; Pybus, Brandon; Kreishman-Deitrick, Mara; Bursulaya, Badry; Lai, Yin H; Gao, Mu-Yun; Liang, Fang; Mathison, Casey J N; Liu, Xiaodong; Yeh, Vince; Smith, Jeffrey; Lerario, Isabelle; Xie, Yongping; Chianelli, Donatella; Gibney, Michael; Berman, Ashley; Chen, Yen-Liang; Jiricek, Jan; Davis, Lauren C; Liu, Xianzhong; Ballard, Jaime; Khare, Shilpi; Eggimann, Fabian Kurt; Luneau, Alexandre; Groessl, Todd; Shapiro, Michael; Richmond, Wendy; Johnson, Kevin; Rudewicz, Patrick J; Rao, Srinivasa P S; Thompson, Christopher; Tuntland, Tove; Spraggon, Glen; Glynne, Richard J; Supek, Frantisek; Wiesmann, Christian; Molteni, Valentina.
  • Nagle A; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Biggart A; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Be C; Novartis Institutes for Biomedical Research, CH-4056 Basel, Switzerland.
  • Srinivas H; Novartis Institutes for Biomedical Research, CH-4056 Basel, Switzerland.
  • Hein A; Novartis Institutes for Biomedical Research, CH-4056 Basel, Switzerland.
  • Caridha D; Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
  • Sciotti RJ; Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
  • Pybus B; Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
  • Kreishman-Deitrick M; Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
  • Bursulaya B; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Lai YH; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Gao MY; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Liang F; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Mathison CJN; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Liu X; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Yeh V; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Smith J; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Lerario I; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Xie Y; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Chianelli D; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Gibney M; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Berman A; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Chen YL; Novartis Institute of Tropical Diseases, Emeryville, California 94608, United States.
  • Jiricek J; Novartis Institute of Tropical Diseases, Emeryville, California 94608, United States.
  • Davis LC; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Liu X; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Ballard J; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Khare S; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Eggimann FK; Novartis Institutes for Biomedical Research, CH-4056 Basel, Switzerland.
  • Luneau A; Novartis Institutes for Biomedical Research, CH-4056 Basel, Switzerland.
  • Groessl T; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Shapiro M; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Richmond W; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Johnson K; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Rudewicz PJ; Novartis Institute of Tropical Diseases, Emeryville, California 94608, United States.
  • Rao SPS; Novartis Institute of Tropical Diseases, Emeryville, California 94608, United States.
  • Thompson C; Novartis Institutes for Biomedical Research, Cambridge, Massachusetts 02139, United States.
  • Tuntland T; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Spraggon G; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Glynne RJ; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Supek F; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
  • Wiesmann C; Novartis Institutes for Biomedical Research, CH-4056 Basel, Switzerland.
  • Molteni V; Genomics Institute of the Novartis Research Foundation (GNF), San Diego, California 92121, United States.
J Med Chem ; 63(19): 10773-10781, 2020 10 08.
Article en En | MEDLINE | ID: mdl-32667203

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Oxazoles / Pirimidinas / Inhibidores de Proteasoma / Leishmaniasis Visceral / Antiprotozoarios Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Año: 2020 Tipo del documento: Article

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Oxazoles / Pirimidinas / Inhibidores de Proteasoma / Leishmaniasis Visceral / Antiprotozoarios Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Año: 2020 Tipo del documento: Article