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SX-PCK9
is a novel family of antagonists for the PCSK9 interaction with
LDLR for the potential treatment of hypercholesterolemia. Initial
in vitro assays have demonstrated specific antagonist activity against
published interaction sites. The project has also identified several
unpublished interactions. The program is now iteratively testing
synthetic mimetics to enhance activity and understanding at these
induced fit interfaces.
SX-ARPC
is a novel family of compounds that have demonstrated an in vitro
ability to down regulate the AR pathway by antagonizing the androgen
receptor outside of the ligand binding domain.
Optimized versions of these compounds have potential as a novel
therapeutics for Prostate Cancer.
SX-RDS1
is a novel set of DNA Repair Inhibitors discovered to enhance the
effectiveness of radiation therapy in a non-toxic manner. These
compounds have been designed to dramatically reduce the frequency
and dose of radiation therapy through a unique mechanism of action
which gently disables cellular DNA repair mechanisms without interfering
with p53 pathways.
SX-HIV1 is
a family of retroviral integrase inhibitors designed to prohibit
the multimerization of the highly conserved integrase enzyme used
by many human retroviruses including HIV. This multimerization process
is critical to the integration of viral genetic material with the
DNA of the infected host cell.
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