Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.

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Title: Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.
Authors: 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.
Source: Journal of medicinal chemistry [J Med Chem] 2020 Oct 08; Vol. 63 (19), pp. 10773-10781. Date of Electronic Publication: 2020 Jul 29.
Publication Type: Journal Article; Research Support, Non-U.S. Gov't
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.0c00499