2020
DOI: 10.24820/ark.5550190.p011.348
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Identifying bioactivity of pseudo-natural products using the Cell Painting assay

Abstract: Natural Products (NP) are a major source of inspiration to develop novel bioactive substances. Various strategies were developed to make use of the relevance of NPs in drug design strategies. It has been shown that NP-derived fragments may still be of biological relevance. Thus, combining various different NP-derived fragments may result in new biologically relevant molecules. These compounds retain some physicochemical properties of NPs but are not accessible through biosynthesis and were therefore termed pse… Show more

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Cited by 3 publications
(2 citation statements)
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“…Comparison of the CP profile of a hit molecule with the profiles of reference compounds whose modes of actions and targets are known can then provide target hypotheses, potentially enabling target identification. [32][33][34][35][36][37] In our implementation of post-imaging analysis following the feature calculation by the open-source software CellProfiler, 579 Z-scores of morphological features are deduced per compound. The Z-score of a morphological feature represents the difference between a morphological feature and its relative DMSO control.…”
Section: Determination Of Lysosomotropismmentioning
confidence: 99%
“…Comparison of the CP profile of a hit molecule with the profiles of reference compounds whose modes of actions and targets are known can then provide target hypotheses, potentially enabling target identification. [32][33][34][35][36][37] In our implementation of post-imaging analysis following the feature calculation by the open-source software CellProfiler, 579 Z-scores of morphological features are deduced per compound. The Z-score of a morphological feature represents the difference between a morphological feature and its relative DMSO control.…”
Section: Determination Of Lysosomotropismmentioning
confidence: 99%
“…[48][49]63,108,[112][113] Biological activities of pseudo-NPs are usually assessed using "unbiased assays", that involve screening against biological systems instead of monitoring a single target in a phenotypic screen. [49,64,108,110,114] For example, phenotypic screening of pseudo-NP identified first-in-class chemical probes such as the chromopyrones 105 that possesses a dual inhibition of glucose transporters GLUT-1/3 as well as exhibiting anticancer activity by inhibiting cancer cells growth. [115] Additionally, the pseudo-NP myokinasib (106) inhibits myosin light chain kinase ChemMedChem 1 (MLCK1), whereas the pseudo-NP indocinchonia 107 inhibits autophagy (Figure 8b).…”
Section: Design Of Pseudo-natural Productsmentioning
confidence: 99%