4.0 Review

Small molecule ectonucleotide pyrophosphatase/phosphodiesterase 1 inhibitors in cancer immunotherapy for harnessing innate immunity

Journal

BULLETIN OF THE KOREAN CHEMICAL SOCIETY
Volume 44, Issue 2, Pages 88-99

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/bkcs.12646

Keywords

cancer immunotherapy; cGAMP; ENPP1; ENPP1 inhibitor; innate immunity; STING

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This review discusses the role of ENPP1 in innate immunity and its application as an immunomodulator in cancer immunotherapy, particularly as an ENPP1 inhibitor.
Ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) was recently identified as a major hydrolase of an endogenous stimulator of interferon genes (STING) agonist, 2 ',3 '-cyclic guanosine monophosphate-adenosine monophosphate (cGAMP). ENPP1 is a promising therapeutic target in cancer immunotherapy, in which the inhibition of ENPP1 enhances anticancer immunity via STING-mediated innate immune activation. This review highlights the role of ENPP1 in innate immunity and the recent discovery of small molecule ENPP1 inhibitors as immunomodulators in cancer immunotherapy.

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