Extending the σ-Hole Motif for Sequence-Specific Recognition of the DNA Minor Groove.

ABSTRACT: The majority of current drugs against diseases, such as cancer, can bind to one or more sites in a protein and inhibit its activity. There are, however, well-known limits on the number of druggable proteins, and complementary current drugs with compounds that could selectively target DNA or RNA would greatly enhance the availability of cellular probes and therapeutic progress. We are focusing on the design of sequence-specific DNA minor groove binders that, for example, target the promoter sites of transcription factors involved in a disease. We have started with AT-specific minor groove binders that are known to enter human cells and have entered clinical trials. To broaden the sequence-specific recognition of these compounds, several modules that have H-bond acceptors that strongly and s

SUBMITTER: Guo P 

PROVIDER: S-EPMC7849046 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature