Submission Type
Poster
Abstract
G-quadruplex (G4) DNA has become of increasing interest to the scientific community as anticancer therapies. This intrigue is due mainly to the fact that G4 DNA represents viable targets to inhibit the telomerase enzyme and to block the expression of cancer promoting oncogenes such as c-MYC, RAS and BCL-2. This makes G4 DNA a viable target for anticancer therapeutics to treat previously “undruggable” genes targets. Inspired by natural products, researchers have synthesized benzothiazoles and benzoxazoles, heterocyclic compounds that have been shown to exhibit a broad range of anti-cancer, anti-pathogenic, anti-convulsant, anti-inflammatory, and anti-tubercular bioactivity. The benzothiazole core represents a versatile scaffold that has been found to be a useful framework for creating many stable derivatives. Recent advances in therapeutic screening have identified the benzothiazoles as viable candidates for a novel direction in chemotherapeutic treatment with potentially high selectivity and thus reduced deleterious side effects. In the current study, we have investigated the binding of several benzoquinone-benzothiazole derivatives to a c-MYC G4 DNA sequence. This study was accomplished using a combination of circular dichroism spectroscopy and fluorescence displacement assays. Our data suggests that the identity/nature of the substituent attached directly to the benzoquinone ring component determines the degree to which our compounds bind to the G4 DNA. We have observed that both the addition of an amino group, as well as the location of the amino group influence this interaction. Our findings have implications in the SAR (structure-activity-relationship) when exploring viable drug candidates that targets and inhibits the c-MYC oncogene.
Recommended Citation
Mirabito, Hope and Bulan, Christopher, "175 - Investigating G Quadruplex Interactions in Oncogenes using Benzothiazoles, Benzoquinone, and Benzoxazoles" (2025). GREAT Day Posters. 45.
https://knightscholar.geneseo.edu/great-day-symposium/great-day-2025/posters-2025/45
175 - Investigating G Quadruplex Interactions in Oncogenes using Benzothiazoles, Benzoquinone, and Benzoxazoles
G-quadruplex (G4) DNA has become of increasing interest to the scientific community as anticancer therapies. This intrigue is due mainly to the fact that G4 DNA represents viable targets to inhibit the telomerase enzyme and to block the expression of cancer promoting oncogenes such as c-MYC, RAS and BCL-2. This makes G4 DNA a viable target for anticancer therapeutics to treat previously “undruggable” genes targets. Inspired by natural products, researchers have synthesized benzothiazoles and benzoxazoles, heterocyclic compounds that have been shown to exhibit a broad range of anti-cancer, anti-pathogenic, anti-convulsant, anti-inflammatory, and anti-tubercular bioactivity. The benzothiazole core represents a versatile scaffold that has been found to be a useful framework for creating many stable derivatives. Recent advances in therapeutic screening have identified the benzothiazoles as viable candidates for a novel direction in chemotherapeutic treatment with potentially high selectivity and thus reduced deleterious side effects. In the current study, we have investigated the binding of several benzoquinone-benzothiazole derivatives to a c-MYC G4 DNA sequence. This study was accomplished using a combination of circular dichroism spectroscopy and fluorescence displacement assays. Our data suggests that the identity/nature of the substituent attached directly to the benzoquinone ring component determines the degree to which our compounds bind to the G4 DNA. We have observed that both the addition of an amino group, as well as the location of the amino group influence this interaction. Our findings have implications in the SAR (structure-activity-relationship) when exploring viable drug candidates that targets and inhibits the c-MYC oncogene.
Comments
Sponsored by Ruel McKnight