Abstract
Identifying bioactivity of pseudo-natural products using the Cell Painting assay
Highlights
Compounds resemble NPs but are not obtainable through biosynthesis and were termed pseudoNatural Products.[10,11] This term was previously employed by Suga et al to describe circular peptides[12,13] and Oshima et al to describe products from intercepted biosynthetic pathways
Biochemical assays evaluate the binding of a small molecule to the hypothesized isolated target of interest, which can be for instance a protein or a complex of proteins in the case of Protein-Protein interactions (PPi)
Pseudo-NPs combine fragments from NPs in ways not found in Nature
Summary
A few principles have been taken into account in the development of the pseudo-NP approach.[10]. Pseudo-NPs may reach such structural complexity through appropriate synthetic pathways. An appropriate balance of heteroatoms in the resulting scaffold could be aimed for by combining fragments either rich in nitrogen or oxygen atoms, respectively more predominant in synthetic and natural compounds. Combining NP fragments from NPs with distinct bioactivities may help to maximize the discovery rate of novel bioactivity. Combining NP fragments that are biosynthetically unrelated may facilitate the binding to different targets of distinctive pathways, which may result in unprecedented bioactivities. To further increase the number of possibilities, NP fragments could be associated with different linkage types (Figure 1). It is possible to vary the connection positions of the NP fragments to maximize the number of possibilities
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