Preferred Label : Autotaxin Inhibitor IOA-289;
NCIt synonyms : ATX Inhibitor IOA-289; ENPP2 Inhibitor IOA-289;
NCIt definition : An orally bioavailable small molecule inhibitor of autotaxin (ATX; ectonucleotide
pyrophosphatase/phosphodiesterase family member 2; ENPP2), with potential antifibrotic
and antineoplastic activities. Upon oral administration, ATX inhibitor IOA-289 targets
and binds to both the substrate pocket and the lysophosphatidic acid (LPA) carrier
channel of ATX, thereby inhibiting the activity of ATX. This both directly inhibits
the proliferation of tumor cells and reduces fibrosis in the tumor microenvironment
(TME), allowing lymphocytes to infiltrate into the tumor and enhancing immune responses
against tumor cells. ATX, a secreted glycoprotein with lysophospholipase D activity,
hydrolyzes lysophosphatidylcholine (LPC) to LPA. LPA-mediated signaling plays an important
role in cellular migration, proliferation and survival in fibrotic response. ATX and
LPA are overexpressed in many tumors.;
Molecule name : IOA 289; IOA-289;
NCI Metathesaurus CUI : CL1912837;
Origin ID : C192808;
UMLS CUI : C5785431;
Semantic type(s)
- concept_is_in_subset
- has_target
