Therapeutic Target Details
| Target ID: | T11 |
| Target Name: | Caspase-3 |
| Synonyms: | Apopain; CASP-3; CPP-32; CPP32; Cysteine protease CPP32; Protein Yama; SCA-1; SREBP cleavage activity 1; CASP3 |
| GENE: | CASP3 |
| Action: | inhibitor |
| Class: | Enzyme |
| UniProtKB ID: | P42574 |
| Entry Name: | CASP3_HUMAN |
| Related Drugs: | Emricasan |
| Mechanism: | Hepatocyte caspase 3 activation in NASH-related apoptosis, fibrogenesis and fibrosis which in part is mediated via CCR2-dependent infiltration of Ly6c positive monocytes. |
| Reference (PMIDs): | 24795036 |
| Candidate ID | Source ID | Source Type | Compound Type | Candidate Name | Inclusion Criteria | |
|---|---|---|---|---|---|---|
| R0104 | DB00282 | approved | small molecule | Pamidronic acid | Therapeutic strategy associated | Details |
| R0249 | DB00710 | approved; investigational | small molecule | Ibandronate | Therapeutic strategy associated | Details |
| R0372 | DB01017 | approved; investigational | small molecule | Minocycline | Target associated | Details |
| R0575 | DB03124 | experimental | small molecule | 5-[4-(1-Carboxymethyl-2-Oxo-Propylcarbamoyl)-Benzylsulfamoyl]-2-Hydroxy-Benzoic Acid | Target associated | Details |
| R0960 | DB06255 | experimental | small molecule | Incadronic acid | Therapeutic strategy associated | Details |
| R0963 | DB06263 | investigational | small molecule | Amrubicin | Therapeutic strategy associated | Details |
| R1033 | DB06506 | investigational | small molecule | Repinotan | Indication associated | Details |
| R1109 | DB06862 | experimental | small molecule | 2-HYDROXY-5-(2-MERCAPTO-ETHYLSULFAMOYL)-BENZOIC ACID | Target associated | Details |
| R1125 | DB07696 | experimental | small molecule | methyl (3S)-3-[(tert-butoxycarbonyl)amino]-4-oxopentanoate | Target associated | Details |
| R1137 | DB08213 | experimental | small molecule | 1-METHYL-5-(2-PHENOXYMETHYL-PYRROLIDINE-1-SULFONYL)-1H-INDOLE-2,3-DIONE | Target associated | Details |
| Compound ID | Source ID | Source Type | Compound Name | Molecular Weight | Molecular Formula | Molecular Species | |
|---|---|---|---|---|---|---|---|
| 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 |
| B000015 | CHEMBL100643 | Small molecule | -- | 486.52 | C25H30N2O8 | ACID | Details |
| B000016 | CHEMBL100741 | Small molecule | -- | 364.4 | C18H24N2O6 | NEUTRAL | Details |
| B000017 | CHEMBL100769 | Small molecule | -- | 426.51 | C24H30N2O5 | NEUTRAL | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A00095 | 35221291 | J Pharmacol Exp Ther | Resveratrol attenuates HFD-induced hepatic lipotoxicity by up-regulating Bmi-1 expression. | Details |
| A00754 | 34979142 | Toxicol Appl Pharmacol | Scopoletin and umbelliferone protect hepatocytes against palmitate- and bile acid-induced cell death by reducing endoplasmic reticulum stress and oxidative stress. | Details |
| A00879 | 34943221 | Biology (Basel) | Beta vulgaris L. (Beetroot) Methanolic Extract Prevents Hepatic Steatosis and Liver Damage in T2DM Rats by Hypoglycemic, Insulin-Sensitizing, Antioxidant Effects, and Upregulation of PPARα. | Details |
| A01161 | 34848360 | J Ethnopharmacol | Crocetin ameliorates non-alcoholic fatty liver disease by modulating mitochondrial dysfunction in L02 cells and zebrafish model. | Details |
| A01185 | 34836315 | Nutrients | Network Pharmacology Exploration Reveals Anti-Apoptosis as a Common Therapeutic Mechanism for Non-Alcoholic Fatty Liver Disease Treated with Blueberry Leaf Polyphenols. | Details |
| A01443 | 34743980 | Eur J Pharmacol | Preventive and therapeutic role of betaine in liver disease: A review on molecular mechanisms. | Details |
| A01477 | 34733981 | Ann Transl Med | TLR2 inhibition ameliorates the amplification effect of LPS on lipid accumulation and lipotoxicity in hepatic cells. | Details |
| A01679 | 34657040 | Cytogenet Genome Res | PinX1 Depletion Improves Liver Injury in a Mouse Model of Nonalcoholic Fatty Liver Disease via Increasing Telomerase Activity and Inhibiting Apoptosis. | Details |
| A01787 | 34618611 | Immunopharmacol Immunotoxicol | Capillin protects against non-alcoholic steatohepatitis through suppressing NLRP3 inflammasome activation and oxidative stress. | Details |
| A02243 | 34448436 | J Histochem Cytochem | Independent of Calorie Intake, Short-term Alternate-day Fasting Alleviates NASH, With Modulation of Markers of Lipogenesis, Autophagy, Apoptosis, and Inflammation in Rats. | Details |
| A02388 | 34393793 | Front Pharmacol | Extracts of Vine Tea Improve Diet-Induced Non-Alcoholic Steatohepatitis Through AMPK-LXRα Signaling. | Details |
| A02606 | 34311531 | Biomed Pharmacother | FTZ attenuates liver steatosis and fibrosis in the minipigs with type 2 diabetes by regulating the AMPK signaling pathway. | Details |
| A02693 | 34280397 | Eur J Pharmacol | Thymosin beta 4 alleviates non-alcoholic fatty liver by inhibiting ferroptosis via up-regulation of GPX4. | Details |
| A02777 | 34245170 | J Food Biochem | Ziziphus spina-christi (L.) fortified with Camellia sinensis mediates apoptosis, Notch-1 signaling, and mitigates obesity-induced non-alcoholic fatty liver. | Details |
| A03926 | 33815655 | Oxid Med Cell Longev | Effect of Different Exercise Intensities on Hepatocyte Apoptosis in HFD-Induced NAFLD in Rats: The Possible Role of Endoplasmic Reticulum Stress through the Regulation of the IRE1/JNK and eIF2α/CHOP Signal Pathways. | Details |
| A04289 | 33675775 | Biochem Pharmacol | Activation of FXR modulates SOCS3/Jak2/STAT3 signaling axis in a NASH-dependent hepatocellular carcinoma animal model. | Details |
| A04764 | 33513383 | J Steroid Biochem Mol Biol | Long-term androgen excess induces insulin resistance and non-alcoholic fatty liver disease in PCOS-like rats. | Details |
| A04822 | 33493657 | Pharmacol Res | Baicalin and the liver-gut system: Pharmacological bases explaining its therapeutic effects. | Details |
| A05012 | 33410857 | Food Funct | Aloin protects mice from diet-induced non-alcoholic steatohepatitis via activation of Nrf2/HO-1 signaling. | Details |
| A05039 | 33397952 | Nat Commun | Hepatocyte-specific IL11 cis-signaling drives lipotoxicity and underlies the transition from NAFLD to NASH. | Details |