Highly selective inhibition of histone demethylases by de novo macrocyclic peptides
Aberrant histone modifications are associated to several chronic and highly prevalent worldwide inflammatory and cardiovascular diseases, as well as cancer. One of the primary reasons leading to this scenario is the mutation or dys-regulation of proteins responsible to read and write post-translational histone modifications, particularly methyltransferases and demethylases, commonly known as KDMs.