Table 1.
ECM as a therapeutic target in cancer
| Drug illustration | Function | Characteristic |
|---|---|---|
| Halofuginone | Inhibiting TGF-β signaling pathway and collagen synthesis | Anticoccidial drug |
| Fresolimumab | Inhibiting collagen synthesis | Monoclonal antibody targeting TGF-β |
| Collagenases | Collagen degradation | Enzyme |
| Relaxin | Promoting the synthesis of collagenase | Hormone |
| MMPs | Collagen degradation | Enzyme |
| GS-6624 | Inhibition of collagen cross-linking | Monoclonal antibody targeting LOXL2 |
| SB-431542 and SB-505124 | Inhibiting ALK4/5/7 kinase to block TGF-β pathway | Imidazole analog |
| Ki26894 | Inhibitor of TGFβR1 | Small-molecule inhibitor |
| Candesartan | Angiotensin receptor blockers | Long-acting angiotensin receptor antagonist |
| 4-methylumbelliferone (4-MU) | Inhibitor of HA synthesis | Umbelliferone derivatives |
| Hyaluronidase | HA degradation | Enzyme |
| BC-1 | Targeting fibronectin for drug delivery | Monoclonal antibody |
| L19 | Targeting fibronectin for delivering drugs and radionuclide | Monoclonal antibody |
| APTEDB | Targeting fibronectin for drug delivery | High-affinity peptides |
| Vitaxin | Targeting integrin and preventing angiogenesis | Monoclonal antibody targeting integrin αvβ3 |
| Volociximab | Targeting integrin and inhibiting neoangiogenesis | Monoclonal antibody targeting α5β1 integrin |
| 1a-RGD | Targeting the RGD-integrins interaction | Small-molecule integrin antagonist |
| Cilengitide | Inhibitor of αvβ3 and αvβ5 integrins | Specific peptide antagonist |
| Imatinib, nilotinib, and dasatinib | Inhibiting tyrosine kinase and DDR signaling pathway | Benzene ammonia pyrimidine derivatives |
| Bivatuzumab | Blocking CD44-HA interaction | Monoclonal antibody against CD44v6 |
| Verbascoside | Inhibitor for CD44 dimerization | phenylpropanoids |
| Tranilast | Suppressing TGF-β signaling and expression of extracellular matrix components | Derivative of the amino acid tryptophan |
| Pirfenidone | Inhibiting TGF-β/Smad and anti-inflammation | Pyridones |
| Fasudil | Rho-kinase inhibitor | Isoquinoline sulfonamide derivatives |
| Metformin | Reducing TGF-β signaling, IL-1β, and M2 tumor-associated macrophages infiltration | Biguanides |
| Dexamethasone | Suppressing angiogenesis and normalizes vessel morphology | Glucocorticoid steroid |
| Hydroxychloroquine | Macropinocytosis inhibitors | Derivatives of 4-aminoquinoline |
| All-trans retinoic acid | Retinoic acid receptor agonists | Vitamin |
| Defactinib | FAK inhibitors and antiangiogenic effect | Benzamides |
| Ibrutinib | Inhibitor of Bruton tyrosine kinase to interrupt BCR signaling in CLL | Benzene ammonia pyrimidine derivatives |
| RG7356 | Blocking the signaling of CD44 in CLL | Humanized monoclonal antibody for CD44 |