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Fragment-Based Screening of a Natural Product Library against 62 Potential Malaria Drug Targets Employing Native Mass Spectrometry.

Vu, Hoan and Pedro, Liliana and Mak, Tin and McCormick, Brendan and Rowley, Jessica and Liu, Miaomiao and Di Capua, Angela and Williams-Noonan, Billy and Pham, Ngoc B and Pouwer, Rebecca and Nguyen, Bao and Andrews, Katherine T and Skinner-Adams, Tina and Kim, Jessica and Hol, Wim G J and Hui, Raymond and Crowther, Gregory J and Van Voorhis, Wesley C and Quinn, Ronald J (2018) Fragment-Based Screening of a Natural Product Library against 62 Potential Malaria Drug Targets Employing Native Mass Spectrometry. ACS infectious diseases, 4 (4). pp. 431-444. ISSN 2373-8227

Abstract

Natural products are well known for their biological relevance, high degree of three-dimensionality, and access to areas of largely unexplored chemical space. To shape our understanding of the interaction between natural products and protein targets in the postgenomic era, we have used native mass spectrometry to investigate 62 potential protein targets for malaria using a natural-product-based fragment library. We reveal here 96 low-molecular-weight natural products identified as binding partners of 32 of the putative malarial targets. Seventy-nine (79) fragments have direct growth inhibition on Plasmodium falciparum at concentrations that are promising for the development of fragment hits against these protein targets. This adds a fragment library to the published HTS active libraries in the public domain.

Item Type: Article
Date Deposited: 09 Feb 2019 00:45
Last Modified: 09 Feb 2019 00:45
URI: https://oak.novartis.com/id/eprint/38884

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