Therapeutic Target Details
| Target ID: | T41 |
| Target Name: | X-box-binding protein 1 |
| Synonyms: | XBP-1; XBP1; Tax-responsive element-binding protein 5, TREB-5 |
| GENE: | XBP1 |
| Action: | inhibitor |
| Class: | Protein |
| UniProtKB ID: | P17861 |
| Entry Name: | XBP1_HUMAN |
| Related Drugs: | None |
| Mechanism: | The severity of liver disease in patients with NASH was positively correlated with XBP1 expression. Macrophage XBP1 exacerbates the development of steatohepatitis by increasing M1 macrophage transition and pro-inflammatory cytokines secretion, which promote lipid accumulation and inflammatory response in hepatocyte. Macrophage Xbp1 depletion inhibits fibrogenesis and hepatic stellate cells activation. Hepatocyte XBP1 aggravates the development of steatohepatitis by promoting lipid accumulation via enhancing lipogenesis and inhibiting lipolysis. Pharmacological XBP1 inhibitors might bring light to the treatment of steatohepatitis. |
| Reference (PMIDs): | 35292349 |
| Drug ID | Drug Name | Type | DrugBank ID | Targets | Category | Latest Progress |
|---|
| Candidate ID | Source ID | Source Type | Compound Type | Candidate Name | Inclusion Criteria |
|---|
| Compound ID | Source ID | Source Type | Compound Name | Molecular Weight | Molecular Formula | Molecular Species | |
|---|---|---|---|---|---|---|---|
| B001511 | CHEMBL117966 | Small molecule | -- | 280.24 | C14H8N4O3 | NEUTRAL | Details |
| B002082 | CHEMBL1224755 | Small molecule | -- | 276.34 | C18H16N2O | NEUTRAL | Details |
| B002394 | CHEMBL1256686 | Small molecule | CALCIMYCIN | 523.63 | C29H37N3O6 | ACID | Details |
| B002823 | CHEMBL1299463 | Small molecule | -- | 445.42 | C23H19F4N3O2 | NEUTRAL | Details |
| B003031 | CHEMBL1300317 | Small molecule | -- | 285.39 | C17H23N3O | NEUTRAL | Details |
| B003085 | CHEMBL1300494 | Small molecule | -- | 506.66 | C25H26N6O2S2 | NEUTRAL | Details |
| B003257 | CHEMBL1301125 | Small molecule | -- | 487.94 | C27H22ClN3O4 | NEUTRAL | Details |
| B003348 | CHEMBL1301480 | Small molecule | -- | 366.85 | C20H19ClN4O | NEUTRAL | Details |
| B003588 | CHEMBL1302406 | Small molecule | -- | 480.85 | C22H20Cl3N3OS | NEUTRAL | Details |
| B003795 | CHEMBL1303281 | Small molecule | -- | 385.45 | C22H15N3O2S | NEUTRAL | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A01134 | 34859513 | Phytother Res | Scutellarin ameliorates hepatic lipid accumulation by enhancing autophagy and suppressing IRE1α/XBP1 pathway. | Details |
| A05000 | 33419084 | Antioxidants (Basel) | Antioxidant and Anti-Inflammatory Effects of Korean Black Ginseng Extract through ER Stress Pathway. | Details |
| A07158 | 32597296 | Autophagy | The unfolded protein response regulates hepatic autophagy by sXBP1-mediated activation of TFEB. | Details |
| A09968 | 31541078 | Exp Mol Med | Deacetylation of XBP1s by sirtuin 6 confers resistance to ER stress-induced hepatic steatosis. | Details |
| A22175 | 24766485 | Clin Sci (Lond) | Endoplasmic reticulum stress does not contribute to steatohepatitis in obese and insulin-resistant high-fat-diet-fed foz/foz mice. | Details |
| A28774 | 35024320 | Acta Pharm Sin B | A small molecule UPR modulator for diabetes identified by high throughput screening. | Details |