Selective PARP11 inhibitor for the treatment of cancer

​​​­Summary
The current technology is a highly selective and potent inhibitor of PARP11 that could serve as an immuno-oncology therapeutic and enhance CAR-T cell therapies.

Technology Overview
Recent work identified PARP11 as a key component in driving tumor microenvironments (Nature Cancer, 2022), and suppression of PARP11 augmented the therapeutic benefits of chimeric antigen receptor (CAR) T cells.

The current technology is ITK7, a highly-selective and potent PARP11 inhibitor for utility as a cancer therapeutic.  Features of ITK7 include:

• Greater than 200-fold selectivity for PARP11 over other PARP family members.
• Potent inhibition of PARP11 with an IC₅₀ in the low nanomolar range.
• Demonstrated ability to inhibit PARP11-dependent auto-MARylation in HeLa cells, with an absence of effects on PARP1 auto-PARylation.
• An ability to drive PARP11 disassociation from the nuclear envelope, consistent with data that cellular localization of PARP11 is regulated by its catalytic activity.
   

Publication
Kirby I, et al., “A Potent and Selective PARP11 Inhibitor Suggests Coupling between Cellular Localization and Catalytic Activity.” Cell Chemical Biology 25(2018): 1547-1553. Link

Licensing Opportunity
This technology is available for licensing.