Review Article
Autotaxin-Lysophosphatidic Acid: From Inflammation to Cancer Development
Table 1
Targeting the ATX-LPA axis in cancer and inflammation.
| Name | Target | Mechanism of action | Phase | Indication/model | Reference |
| HA130 | ATX | It binds to the active site of ATX (T210). IC50 = 28 nM in vitro | Preclinical | Melanoma | [25] | PF-8380 | ATX | Direct binding to ATX. Inhibits lysoPLD activity. IC50 = 2.8 nM isolated ATX IC50 = 101 nM in vivo | Preclinical | (i) Inflammation (ii) Glioblastoma | [133–135] | ONO-8430506 | ATX | Direct binding to ATX. Inhibits lysoPLD activity. IC50 = 4.5 nM isolated ATX IC50 = 4.1–11.6 nM in vivo | Preclinical | (i) Breast cancer (ii) BCa metastasis (iii) Thyroid cancer | [19, 28, 121, 136] | GLPG1690 | ATX | Binding to the hydrophobic pocket and hydrophobic channel of the protein. IC50 = 131 nM in vitro | Phase II | Idiopathic pulmonary fibrosis | [137, 138] | BMS-986020 | LPA1 | Inhibits signaling by LPA1 | Phase II | Idiopathic pulmonary fibrosis | [139, 140] | SAR100842 | LPA1 | LPA1 antagonist | Phase II | Systemic sclerosis | [141] | BrP-LPA | ATX LPA1 LPA2 LPA3 LPA4 LPA5 | Direct binding to ATX. Inhibits lysoPLD activity. IC50: 600 nM ex vivo Direct binding and inhibition of LPA1–5 | Preclinical | (i) Rheumatoid arthritis (ii) Breast cancer (iii) Pancreatic cancer (iv) Glioma | [142–145] |
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