Preferred Label : Bispecific CD80-lgG4Fc-IL-2v Fusion Protein GI-102;
NCIt definition : A bi-specific Fc fusion protein composed of the N-terminal ectodomain of human CD80
(B7.1) fused to a human immunoglobulin G4 (IgG4) Fc fragment and linked to an interleukin
(IL)-2 variant (IL-2v) as a C-terminal moiety, with potential immunostimulatory, immune
checkpoint inhibitory and antineoplastic activities. Upon administration of bispecific
CD80-IgG4Fc-IL-2v fusion protein GI-102, the CD80 moiety targets and binds to cytotoxic
T-lymphocyte-associated antigen 4 (CTLA4; CTLA-4) expressed on T-cells. This prevents
the binding of CTLA-4 to endogenous CD80, enables the binding of CD80 to CD28, which
leads to CD28-mediated signaling, and results in the activation of T-cells in the
tumor microenvironment (TME). This promotes T-cell activity. The IL-2v moiety may
stimulate a local immune response and activate natural killer (NK) cells and cytotoxic
T-cells. This may enhance the activity of neoantigen specific T-cells and potentiates
the T-cell-mediated immune response against tumor cells. CD80 is a co-stimulatory
molecule expressed on activated antigen presenting cells (APCs) that plays a key role
in T-cell activation upon binding to CD28 on T-cells. On the other hand, binding of
CD80 to CTLA-4 prevents CD80-CD28 engagement, thereby inhibiting T-cell activity and
immune activation. CTLA-4 is a member of the immunoglobulin superfamily (IgSF) and
an inhibitory molecule upregulated by T-cells following T-cell activation. It plays
a key role in the downregulation of the immune system. The IL-2v moiety cannot bind
to IL-2 receptor-alpha (CD25, IL2Ra) and does not activate regulatory T-cells (Tregs).;
Molecule name : GI 102; GI-102;
NCI Metathesaurus CUI : CL1915075;
Origin ID : C200811;
UMLS CUI : C5854598;
Semantic type(s)
- concept_is_in_subset
