The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons

JF Moruno-Manchon, EC Koellhoffer… - Aging (Albany …, 2017 - pmc.ncbi.nlm.nih.gov
Aging (Albany NY), 2017pmc.ncbi.nlm.nih.gov
The G-quadruplex is a non-canonical DNA secondary structure formed by four DNA strands
containing multiple runs of guanines. G-quadruplexes play important roles in DNA
recombination, replication, telomere maintenance, and regulation of transcription. Small
molecules that stabilize the G-quadruplexes alter gene expression in cancer cells. Here, we
hypothesized that the G-quadruplexes regulate transcription in neurons. We discovered that
pyridostatin, a small molecule that specifically stabilizes G-quadruplex DNA complexes …
The G-quadruplex is a non-canonical DNA secondary structure formed by four DNA strands containing multiple runs of guanines. G-quadruplexes play important roles in DNA recombination, replication, telomere maintenance, and regulation of transcription. Small molecules that stabilize the G-quadruplexes alter gene expression in cancer cells. Here, we hypothesized that the G-quadruplexes regulate transcription in neurons. We discovered that pyridostatin, a small molecule that specifically stabilizes G-quadruplex DNA complexes, induced neurotoxicity and promoted the formation of DNA double–strand breaks (DSBs) in cultured neurons. We also found that pyridostatin downregulated transcription of the Brca1 gene, a gene that is critical for DSB repair. Importantly, in an in vitro gel shift assay, we discovered that an antibody specific to the G-quadruplex structure binds to a synthetic oligonucleotide, which corresponds to the first putative G-quadruplex in the Brca1 gene promoter. Our results suggest that the G-quadruplex complexes regulate transcription in neurons. Studying the G-quadruplexes could represent a new avenue for neurodegeneration and brain aging research.
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