tonsil inhibitor, small molecule, use of a small molecule or inhibitor, three-dimensional crystal, methods for selecting or designing a small molecule, to identify a tonsil ard binding inhibitor to histone h4, to predict the inhibiting effect of tonsil and to identify a tonsil inhibitor and / or determine the inhibitory effect of a putative tonsil inhibitor, polynucleotide sequence or isolated amino acid sequence, and tonsil mutant polypeptide.

摘要

The present invention relates to small molecules that interfere with the conformational space of the tonsil ard occupied by the histone tail h4. These small molecules target the tonsil binding pocket that encompasses the h4 k12-r23 residues and act by preventing or disrupting the binding of the h4 tail k12-r23 residues to the tonsl ard via direct competition or via the allosteric disruption of the h4 tail. binding bag. The present inventors have identified and solved the structure of a histone reader tonson domain called ard (ankyrin repeat domain).