The key objectives of medicinal chemistry are to efficiently design and synthesize bioactive
compounds that have the potential to become safe and efficacious drugs. Most medicinal …

The case for a renewed focus on Nature in drug discovery is reviewed; not in terms of
natural product screening, but how and why biomimetic molecules, especially those …

The past decade has seen a substantial increase in successful examples of the combination
of chemo-and biocatalysis for multistep syntheses. This is driven by obvious advantages …

The pharmaceutical industry, driven by an increasing need to deliver new and more effective
medicines to patients, is increasingly turning to the use of engineered biocatalysts for both …

The past two decades have witnessed the emergence of macrocycles, including macrocyclic
peptides, as a promising yet underexploited class of de novo drug candidates. Both …

Click chemistry, proposed nearly 20 years ago, promised access to novel chemical space by
empowering combinatorial library synthesis with a “few good reactions”. These click …

Enzyme catalysis, enabled by advances in protein engineering and directed evolution, is
beginning to transform chemical synthesis in the pharmaceutical industry. This review …

DNA-encoded library technology (DELT) was introduced to our medicinal chemistry society
more than 20 years ago. The application of DELT in the development of clinical candidates …

Enzyme catalysis is gaining increasing importance in synthetic chemistry. Nowadays, the
growing number of biocatalysts accessible by means of bioinformatics and enzyme …

The discovery of organic ligands that bind specifically to proteins is a central problem in
chemistry, biology, and the biomedical sciences. The encoding of individual organic …