Preferred Label : Anti-CD39 Antibody/TGF-beta RII Ectodomain Fusion Protein ES014;
NCIt synonyms : Bifunctional Antibody-Ligand Trap ES014; Anti-CD39 Antibody/TGFb-Trap ES014; Anti-CD39/TGF-b RII Bifunctional Fusion Protein ES014; Bifunctional Fusion Protein ES014;
NCIt definition : A fusion protein composed of a monoclonal antibody directed against the cell surface
receptor CD39 (cluster of differentiation 39; ectonucleoside triphosphate diphosphohydrolase-1;
NTPDase1; ENTPD1) and fused to the transforming growth factor-beta receptor type II
(TGF-beta RII) ectodomain, with potential immunomodulating and antineoplastic activities.
Upon administration, anti-CD39/TGF-beta RII ectodomain fusion protein ES014 specifically
and simultaneously targets and binds to the CD39 antigen and TGF-beta in the tumor
microenvironment (TME), thereby preventing CD39- and TGF-beta-mediated signaling.
By preventing CD39 activation, the conversion and degradation of adenosine triphosphate
(ATP) to adenosine monophosphate (AMP) is abrogated as CD39 is the rate-limiting enzyme
in the ATP-adenosine pathway. This leads to an increase in the extracellular levels
of immunogenic ATP and a decrease in the levels of immunosuppressive adenosine within
the TME. A high level of ATP increases pro-inflammatory cytokine levels and promotes
both T-cell proliferation and the stimulation of dendritic and other myeloid-derived
cells that are necessary for innate and adaptive immunity. The binding to TGF-beta
prevents the activation of TGF-beta RII-mediated signaling pathways and also prevents
the activation of CD39. This further reverses the immunosuppressive nature of the
TME. This may further stimulate a T-cell-mediated anti-tumor immune response and may
inhibit tumor cell proliferation. CD39, a cell surface ectonucleosidase, is upregulated
on tumor cells as an immune evasion strategy; blocking its action may improve anti-tumor
immune responses. TGF-beta is expressed by a number of cancer cell types and is involved
in cancer cell proliferation, tumor progression, and immunosuppression. It suppresses
T-cell activation and induces CD39 expression.;
Molecule name : ES-014; ES 014;
NCI Metathesaurus CUI : CL1792777;
Origin ID : C188121;
UMLS CUI : C5706457;
Semantic type(s)
- concept_is_in_subset
- has_target
