The FDA approvals of afatinib and ibrutinib in 2013 led to a heightened interest in cysteine-reactive covalent inhibitors. However, there are few methods to discover new cysteine-reactive inhibitors for enzymes for which reversible binding scaffolds are not known. To this end, we rationally designed a chemical system to attach a...
Total synthesis of natural products provides an avenue for investigation of complex chemical scaffolds, not only delivering access to biologically impactful molecules but also lending a deeper understanding of their inherent chemical reactivity. Expansion of reaction methodology, optimization of biological activity, and absolute structural confirmation can all be accomplished via...
Part 1. The complex folded structures associated with RNA allow for specific protein-RNA interactions and also create binding sites for small molecules. Developing organic molecules that can bind RNA with high affinity and specificity is a challenge that must be overcome for RNA to be considered a viable drug target....