Researchers at UCI have engineered a class of Hv1 polypeptide modulators that selectively modulate Hv1 voltage gated channels while leaving other voltage gated channels unaffected. With no Hv1 modulators currently on the market, this class of Hv1 polypeptide modulators could provide solutions in birth control, autoimmune therapies, and tumor reduction.
·Birth Control – Inhibition of sperm maturation
·Autoimmune Therapies -Reducing reactive oxygen species (ROS) in white blood cells
·Cancer Therapeutics - Tumor reduction
·Polypeptides selectively target only Hv1 voltage gated channels
·Includes both reversible and irreversible modulators
·Cell type specific response
·Effective at inhibiting ROS production in white blood cells and sperm capacitation in μM range
Cells use voltage gated channels to create gradients which are used for important cellular functions. The ability to modulate these voltage gated channels allows for control of important cellular functions. The Hv1 voltage gated channel is an attractive therapeutic target due to its high expression in some metastatic cancers, its role in sperm maturation, and its use by white blood cells to produce reactive oxygen species for inflammatory responses. Currently no selective Hv1 channel inhibitors are on the market.
Researchers at UCI have developed a class of polypeptides that act as selective Hv1 channel modulators. These polypeptides can reversibly or irreversibly inhibit the Hv1 channel. The unique structure of the modulators allows them to selectively target the Hv1 channel while leaving other voltage gated channels unaffected.The polypeptide modulators can also have their amino acid sequence tailored to fine-tune the channel inhibition.Preliminary results have shown efficacy for limiting ROS production and sperm maturation at μM concentrations. The UCI Hv1 polypeptide modulator shows promise for applications in birth control, autoimmune therapy, and cancer.
In vivo and in vitro studies are currently in progress to identify which embodiment is most effective for delivery in humans.
|United States Of America||Published Application||20190330285||10/31/2019||2019-915|