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Location-agnostic site-specific protein bioconjugation via Baylis Hillman adducts

Covalent Modifiers

link] Proteins labelled site-specifically with small molecules are valuable assets for chemical biology and drug development. Nat Commun 15 , 859 (2024). The unique reactivity profile of the 1,2-aminothiol moiety of N -terminal cysteines ( N -Cys) of proteins renders it highly attractive for regioselective protein labelling.

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Target-directed cancer: protein-ligand interactions  

Drug Target Review

In 2007 Dr van Montfort joined the Institute of Cancer Research (London, UK), where he holds a joint position between the Centre for Cancer Drug Discovery (CCDD) and the Division of Structural Biology. In 2019 he became Reader in Structural Biology and Cancer Drug Discovery.

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Obstacles and innovations of macrocyclic drug development

Drug Target Review

What are macrocycles and why are they interesting for drug discovery? Traditionally, drug discovery has focused on small-molecule therapeutics, typically with a molecular weight of less than 500 Daltons. 1 However, there has recently been an increased interest in so-called beyond rule-of-five compounds, such as macrocycles.