Table 3 Small molecules/agents as therapeutics against NLRP3 inflammasome activation
From: An update on the regulatory mechanisms of NLRP3 inflammasome activation
Small molecule/ agent | Chemical class | Interaction with target | Ref. |
|---|---|---|---|
Targeting NLRP3 NACHT domain | |||
MCC950/CRID3 | Diarylsulfonylurea compound | Binds to Walker B motif of NACHT ATPase | |
CY-09 | CFTR(inh)-172 analog | Binds to Walker A motif of NACHT ATPase | |
OLT1177 | β-sulfonyl nitrile compound | Directly targets ATPase and inhibits NLRP3 inflammasome oligomerization | |
BOT-4-one | Benzoxathiole derivative | Alkylates NLRP3 to impair ATPase activity | |
Tranilast | Tryptophan metabolite | Binds to NACHT domain and inhibits NLRP3 oligomerization | |
Targeting NEK7-NLRP3 interaction | |||
Oridonin | Diterpenoid purified from Rabdosia rubescens | Irreversibly binds to NLRP3 Cys279 and inhibits NLRP3–NEK7 interaction | |
Rg3 | Ginsenoside extracted from Panax ginseng | Abrogates NEK7-NLRP3 interaction, and subsequently inhibits NLRP3-ASC interaction, ASC oligomerization, and speckle formation | |
C1-27 (& 25) | Benzenesulfonamide derivative | Inhibits GSTO1-1, which is NEK7 deglutathionylating enzyme | |
Artemisinin | Sesquiterpene lactone isolated from Artemisia annua | Targets and inhibits interaction between NEK7 and NLRP3 | |
Targeting PYD | |||
KN3014 | Piperidine-containing compound | Directly targets PYD and inhibits the interaction between NLRP3 and ASC | |
β-carotene | Provitamin A carotenoid | Binds to NLRP3 PYD | |
ASCPYD/H2-H3 peptide | Peptide corresponding to H2-H3 segment of ASC PYD | Binds to NLRP3 PYD and selectively inhibits NLRP3 inflammasome | |
