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| Inhibiting angiogenic process | Antiangiogenic compounds | Mechanism of action |
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| Inhibitors of ECM remodeling | Batimastat, Marimastat, AG3340, Neovastat, PEX, TIMP-1,2,3,4 | MMP inhibitors, block endothelial and tumor cell invasion |
| PAI-1,2, uPA Ab, uPAR Ab, Amiloride | uPA inhibitors, block ECM breakdown |
| Minocycline, tetracyclines, cartilage-derived TIMP | Collagenase inhibitors, disrupt collagen synthesis and deposition |
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| Inhibitors of adhesion molecules | Ab: LM609 and Vitaxin, RGD containing peptides, Ab | Block EC adhesion, induce EC apoptosis |
| Benzodiazepine derivatives | Antagonist of |
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| Inhibitors of activated ECs | Endogenous inhibitors: endostatin, angiostatin, aaAT | Block EC proliferation, induce EC apoptosis, inhibit angiogenic switch |
| IFN-α, IFN-γ, IL-12, nitric oxide synthase inhibitors, TSP-1 | Block EC migration and/or proliferation |
| TNP-470, Combretastatin A-4 | Block EC proliferation |
| Thalidomide | Inhibits angiogenesis in vivo |
| Linomide | Inhibits EC migration |
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| Inhibitors of angiogenic inducers or their receptors | IFN-α, PF-4, prolactin fragment | Inhibit bFGF, Inhibit bFGF-induced EC proliferation |
| Suramin and analogues | Bind to various growth factors including bFGF, VEGF, PDGF, inhibit EC migration and proliferation |
| PPS, distamycin A analogues, bFGF Ab, antisense-bFGF | Inhibit bFGF activity |
| Protamine | Binds heparin, inhibits EC migration and proliferation |
| SU5416, soluble Flt-1, dominant-negative Flk-1, VEGF receptor, ribozymes, VEGF Ab | Block VEGF activity |
| Aspirin, NS-398 | COX inhibitors |
| 6AT, 6A5BU, 7-DX | TP antagonists |
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| Inhibitors of EC intracellular signaling | Genistein | Tyrosine kinase inhibitor, blocks uPA, EC migration and proliferation |
| Lavendustin A | Selective inhibitor of protein tyrosine kinase |
| Ang-2 | Inhibits Tie-2 |
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