Small molecule drug discovery natural products

Small molecule carbohydrates, lipids, natural products, drugs, drug-like molecules synthesis platform, ligand discovery, antibody binding screens, enzymatic assays, phenotypic cell-based screens, diagnostics, target deconvolution 12, 14-16, 21, 22, 25-32, 39, 40, 43, 44, 46, 48, 53, 55-65, 78... 

There are two distinct routes to the discovery of small molecule drugs (1) from natural products and (2) from rational design. 

The selection and quality of a screening library with drug-like and lead-like structures is a critical endeavour. The features of drug-like and lead-like structures continue to be better defined, at the same time as the diversity of drug-like and lead-like molecular space continues to be explored and categorised. Other areas of development focus on the discovery of small molecules suitable for modulating protein-protein interactions, with a greater focus on natural product-like compounds. 

Technological advances have provided a path to integrate the chemical diversity found in natural products in high-throughput drug discovery programmes. Many of the previous bottlenecks that made natural product discovery a slow laborious process have been effectively removed. Automation in NMR and MS has provided a path toward automated isolation of active molecules. Sensitivity improvements in NMR probe technology have allowed structures to be determined with very small quantities of material. On the other hand,... 

Natural products have played a disproportionate role in the discovery of leads and the development of successful drugs. Close to 50% of the marketed drugs based on small molecules for the last 25 years have come from natural products, and the... 

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