The QUIMOLMAT group's article "Reversible Control of DNA Binding with Cucurbituril-Induced Supramolecular 4,4′-Bipyridinium-Peptide Dimers" gets the cover of the March volume of the journal Bioconjugate Chemistry (JCR2019 = 4,031).
Many cellular processes in living organisms are mediated by complex regulatory networks based on non-covalent interactions between a relatively small number of proteins. These proteins perform their function by exchanging their state between homo- and hetero-oligomeric assemblies or mono- and bivalent states.
In this work, the researchers show that 4,4`-bipyridinium units connected to the basic region of the GCN4 bZip transcription factor can be used to control conjugate dimerization by forming a supramolecular complex with cucurbituryl. This supramolecular complex is able to selectively recognize its target in double-stranded DNA and its binding can be reversible by the application of an external stimulus, e.g. a pH change.
Transcription factors are proteins responsible for the main control mechanism of gene transcription in eukaryotic cells, activating or inhibiting gene expression. Therefore, a malfunction of these mechanisms has serious consequences such as the appearance of diseases including cancer. A deeper understanding of these mechanisms and their modulation can contribute to the treatment of these diseases.
The cover image illustrates the molecular complex formed by a 4,4'-bipyridinium dimer connected to the GCN4 bZip transcription factor and a cucurbituryl supramolecule. This complex appears reversibly bound to a DNA double strand.
The article in Bioconjugate Chemistry, 2021, 32, 3, 507-511.The cover can be found HERE