Therapeutic Target Details
| Target ID: | T10 |
| Target Name: | Caspase-1 |
| Synonyms: | CASP-1; ICE; IL-1 beta-converting enzyme; IL-1BC; IL1BC; IL1BCE; Interleukin-1 beta convertase; Interleukin-1 beta-converting enzyme; p45; CASP1 |
| GENE: | CASP1 |
| Action: | inhibitor |
| Class: | Enzyme |
| UniProtKB ID: | P29466 |
| Entry Name: | CASP1_HUMAN |
| Related Drugs: | Emricasan |
| Mechanism: | Intervention with a caspase-1 inhibitor attenuated the development of NASH, liver fibrosis and insulin resistance. Data support the importance of inflammasome/caspase-1 in the development of NASH and demonstrate that therapeutic intervention in the already ongoing disease process is feasible. |
| Reference (PMIDs): | 27121255 |
| Candidate ID | Source ID | Source Type | Compound Type | Candidate Name | Inclusion Criteria | |
|---|---|---|---|---|---|---|
| R0372 | DB01017 | approved; investigational | small molecule | Minocycline | Target associated | Details |
| R0636 | DB04875 | investigational | small molecule | Pralnacasan | Therapeutic strategy associated | Details |
| R0763 | DB05301 | investigational | small molecule | LAX-101 | Target associated | Details |
| R0822 | DB05507 | investigational | small molecule | VX-765 | Therapeutic strategy associated | Details |
| R0996 | DB06372 | approved; investigational | biotech | Rilonacept | Therapeutic strategy associated | Details |
| R1128 | DB07733 | experimental | small molecule | 1-METHYL-3-TRIFLUOROMETHYL-1H-THIENO[2,3-C]PYRAZOLE-5-CARBOXYLIC ACID (2-MERCAPTO-ETHYL)-AMIDE | Target associated | Details |
| R1129 | DB07744 | experimental | small molecule | Z-Val-Ala-Asp fluoromethyl ketone | Target associated | Details |
| R1133 | DB07916 | experimental | small molecule | 3-{6-[(8-HYDROXY-QUINOLINE-2-CARBONYL)-AMINO]-2-THIOPHEN-2-YL-HEXANOYLAMINO}-4-OXO-BUTYRI ACID | Target associated | Details |
| Compound ID | Source ID | Source Type | Compound Name | Molecular Weight | Molecular Formula | Molecular Species | |
|---|---|---|---|---|---|---|---|
| B000001 | CHEMBL10 | Small molecule | SB-203580 | 377.44 | C21H16FN3OS | NEUTRAL | Details |
| B000002 | CHEMBL100114 | Small molecule | -- | 444.48 | C23H28N2O7 | NEUTRAL | Details |
| B000005 | CHEMBL100405 | Small molecule | -- | 414.46 | C22H26N2O6 | NEUTRAL | Details |
| B000006 | CHEMBL100409 | Small molecule | -- | 483.35 | C22H24Cl2N2O6 | NEUTRAL | Details |
| B000009 | CHEMBL100559 | Small molecule | -- | 547.51 | C22H24F3N3O8S | ACID | Details |
| B000010 | CHEMBL100578 | Small molecule | -- | 415.45 | C21H25N3O6 | NEUTRAL | Details |
| B000011 | CHEMBL100588 | Small molecule | -- | 493.51 | C23H31N3O9 | ACID | Details |
| B000012 | CHEMBL100591 | Small molecule | -- | 547.51 | C22H24F3N3O8S | ACID | Details |
| B000014 | CHEMBL1006 | Small molecule | AMIFOSTINE | 214.23 | C5H15N2O3PS | ZWITTERION | Details |
| B000015 | CHEMBL100643 | Small molecule | -- | 486.52 | C25H30N2O8 | ACID | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00123 | 35213000 | Methods Mol Biol | Ex Vivo Dual-Hit Method for Inflammasome Activation in Liver. | Details |
| A00319 | 35138995 | Pharm Biol | Jinlida granules ameliorate the high-fat-diet induced liver injury in mice by antagonising hepatocytes pyroptosis. | Details |
| A00949 | 34922061 | Clin Res Hepatol Gastroenterol | Upregulated NLRP3 inflammasome activation is attenuated by anthocyanins in patients with nonalcoholic fatty liver disease: A case-control and an intervention study. | Details |
| A01136 | 34859106 | J Immunol Res | Hyperlipidemia May Synergize with Hypomethylation in Establishing Trained Immunity and Promoting Inflammation in NASH and NAFLD. | Details |
| A01428 | 34752711 | Annu Rev Pathol | Role of the Inflammasome in Liver Disease. | Details |
| A01787 | 34618611 | Immunopharmacol Immunotoxicol | Capillin protects against non-alcoholic steatohepatitis through suppressing NLRP3 inflammasome activation and oxidative stress. | Details |
| A01901 | 34566670 | Front Physiol | Gardenoside Hinders Caspase-1-Mediated Hepatocyte Pyroptosis Through the CTCF/DPP4 Signaling Pathway. | Details |
| A02064 | 34513923 | Front Mol Biosci | The Specific NLRP3 Antagonist IFM-514 Decreases Fibrosis and Inflammation in Experimental Murine Non-Alcoholic Steatohepatitis. | Details |
| A02136 | 34492534 | Int Immunopharmacol | Antcin A alleviates pyroptosis and inflammatory response in Kupffercells of non-alcoholic fatty liver disease by targeting NLRP3. | Details |
| A02373 | 34399601 | Int J Immunopathol Pharmacol | Melatonin ameliorates hepatic steatosis by inhibiting NLRP3 inflammasome in db/db mice. | Details |
| A02428 | 34374253 | Zhongguo Ying Yong Sheng Li Xue Za Zhi | [Effects of GPR81 agonist on insulin resistance in rats with nonalcoholic fatty liver disease]. | Details |
| A02790 | 34239622 | Dis Markers | Jiangzhi Ligan Decoction Inhibits GSDMD-Mediated Canonical/Noncanonical Pyroptosis Pathways and Alleviates High-Fat Diet-Induced Nonalcoholic Fatty Liver Disease. | Details |
| A02860 | 34213784 | Phytother Res | Corosolic acid ameliorates non-alcoholic steatohepatitis induced by high-fat diet and carbon tetrachloride by regulating TGF-β1/Smad2, NF-κB, and AMPK signaling pathways. | Details |
| A03252 | 34070893 | Mar Drugs | Attenuating Effects of Dieckol on High-Fat Diet-Induced Nonalcoholic Fatty Liver Disease by Decreasing the NLRP3 Inflammasome and Pyroptosis. | Details |
| A03374 | 34026086 | Food Sci Nutr | Alpha-lipoic acid alleviates NAFLD and triglyceride accumulation in liver via modulating hepatic NLRP3 inflammasome activation pathway in type 2 diabetic rats. | Details |
| A03493 | 33984334 | Metabolism | A new mechanism of obeticholic acid on NASH treatment by inhibiting NLRP3 inflammasome activation in macrophage. | Details |
| A03585 | 33941551 | BMJ Open Diabetes Res Care | Insulin resistance and liver histopathology in metabolically unhealthy subjects do not correlate with the hepatic abundance of NLRP3 inflammasome nor circulating IL-1β levels. | Details |
| A03615 | 33930586 | Clin Res Hepatol Gastroenterol | Pathogenetic mechanisms of nonalcoholic fatty liver disease and inhibition of the inflammasome as a new therapeutic target. | Details |
| A03656 | 33918059 | J Pers Med | Animal Evidence for Synergistic Induction of Hepatic Injury by Dietary Fat and Alcohol Consumption and Its Potential Mechanisms. | Details |
| A03714 | 33894425 | Cell Mol Gastroenterol Hepatol | Caspase-11-Mediated Hepatocytic Pyroptosis Promotes the Progression of Nonalcoholic Steatohepatitis. | Details |