Mediators of Inflammation / 2017 / Article / Tab 1

Review Article

Autotaxin-Lysophosphatidic Acid: From Inflammation to Cancer Development

Table 1

Targeting the ATX-LPA axis in cancer and inflammation.

NameTargetMechanism of actionPhaseIndication/modelReference

HA130ATXIt binds to the active site of ATX (T210).
IC50 = 28 nM in vitro
PreclinicalMelanoma[25]
PF-8380ATXDirect binding to ATX. Inhibits lysoPLD activity.
IC50 = 2.8 nM isolated ATX
IC50 = 101 nM in vivo
Preclinical(i) Inflammation
(ii) Glioblastoma
[133135]
ONO-8430506ATXDirect 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]
GLPG1690ATXBinding to the hydrophobic pocket and hydrophobic channel of the protein.
IC50 = 131 nM in vitro
Phase IIIdiopathic pulmonary fibrosis[137, 138]
BMS-986020LPA1Inhibits signaling by LPA1Phase IIIdiopathic pulmonary fibrosis[139, 140]
SAR100842LPA1LPA1 antagonistPhase IISystemic sclerosis[141]
BrP-LPAATX
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
[142145]

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