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Table 5 Inhibitors that target enzymes involved in PTM regulation of the NLRP3 inflammasome

From: Inflammasome activation controlled by the interplay between post-translational modifications: emerging drug target opportunities

Inhibitor

Target

Inhibition mechanism

Selectivity

Clinical status

Diseases

Ref.

SP600125

JNK1

JNK-1-induced NLRP3 S198 (S194) phosphorylation

JNK1, 2, 3

–

 

[29]

CRT0066101

PKD

PKD-induced NLRP3 S295 (S291) phosphorylation

PKD1, 2, 3

–

 

[31]

Gö 6976

PKD

PKD-induced NLRP3 S295 (S291) phosphorylation

PKD1, 2, 3

–

 

[31]

CID755673

PKD

PKD-induced NLRP3 S295 (S291) phosphorylation

PKD1, 2, 3

–

 

[31]

kb NB 142–70

PKD

PKD-induced NLRP3 S295 (S291) phosphorylation

PKD1, 2, 3

–

 

[31]

R406

Syk

Syk-induced ASC Y146 (Y144) phosphorylation

Syk

Phase I

 

[40, 57]

Piceatannol

Syk

Syk-induced ASC Y146 (Y144) phosphorylation

Syk

–

 

[67]

PF-562271

PYK2/FAK

PYK2-induced ASC Y146 (Y144) phosphorylation

PYK2/FAK

–

 

[45]

PF-431396

PYK2/FAK

PYK2-induced ASC Y146 (Y144) phosphorylation

PYK2/FAK

–

 

[45]

PF-573228

FAK

unknown

FAK

–

 

[45]

LFM-A13

BTK

ASC oligomerization

BTK

  

[61]

CGI1746

BTK

ASC oligomerization

BTK

  

[62]

Ibrutinib

BTK

ASC oligomerization

BTK

Approved

Mantle cell lymphoma, chronic lymphocytic leukemia

[61, 62]

G5

BRCC3

BRCC-induced NLRP3 deubiquitination

DUB pan inhibitor

–

 

[9]

HBX19818

USP7

USP7-induced NLRP3 deubiquitination

USP7

–

 

[8]

P005091

USP7

USP7-induced NLRP3 deubiquitination

USP7

–

 

[8]

P22077

USP7/USP47

USP7/USP47-induced NLRP3 deubiquitination

USP7/USP47

–

 

[8]

  1. Amino acid residues shown above refer to human NLRP3, those in brackets refer to mouse NLRP3 residues