Small-molecule degraders for Nudix Hydrolase 5, NUDT5
Applications: Treatment of cancer, inflammatory and metabolic diseases
Novel degrader molecules that degrade rather than inhibit human NUDT5 for therapeutic benefit.
Features
Benefits
Exploits a novel scaffolding role of NUDT5 in purine metabolism, which is dependent on its scaffolding function rather than its catalytic activity.
Broad targeting potential through its scaffolding interactions: targeting of PPAT exemplified, but potentially can be extended to other pathway members, such as GART, PAICS, ATIC, PFAS, HPRT1, SAICAR, AICAR.
Heterocycle-containing linker connecting NUDT5 with CRBN E3 ligase complex.
Provides balance of properties for efficient degradation and excellent solubility.
PROTAC linker could connect NUDT5 to any degradation pathway, i.e., not only via E3 ligase.
Customisable degradation based on specific needs.
Can be administered in combination with another compound.
Reducing side effects or toxicity of a second drug administered in treatment of cancer, inflammatory, autoimmune or metabolic disorder.