Drug Discovery and Development

Carole Duboc, Sabine Lahja Flitsch · JACS Au · 2024

Chemistry has played an integral part in drug discovery and development and will continue to be essential in addressing the global health challenges we face as a society.The inspiration for molecular design has often come from Nature, with Natural Products providing bioactive scaffolds that can be structurally modified to enhance activity and improve selectivity.Initially, small molecule drugs such as salicylic acids, penicillins, or taxols set the foundation, complemented later by non-natural scaffolds identified through screening extensive synthetic compound libraries against targets.In recent years, more complex biopharmaceuticals, including nucleic acids, carbohydrates, and proteins, have become more prominent, with about 50 out of 100 of the top brand name drugs by retail sales in 2022 falling under the category of "biologics" or "new modalities". 1 In this virtual issue, we have selected 26 recently published works in Drug Discovery and Development from issues of JACS Au, including Articles, Letters, and Perspectives.Readers will find in this collection of papers an exciting and active field of research that is broad and highly interdisciplinary, ranging from metal-based methodologies to natural product (bio)synthesis, the development of chemical toolboxes for screening and target identification, to advancements in biologics and drug delivery systems.

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