Preferred Label : Cintirorgon;
NCIt synonyms : RORg Agonist LYC-55716;
NCIt definition : An orally bioavailable agonist of retinoic acid-related orphan receptor gamma (RORg),
with potential immunomodulatory and antineoplastic activities. Upon oral administration
of cintirorgon, this agent selectively binds to the nuclear receptor transcription
factor RORg, forming a receptor complex that translocates to the nucleus, and binds
to ROR response elements (ROREs), enhancing the function, proliferation and survival
of type 17 T-cells, including Th17 (helper T-cells) and Tc17 (cytotoxic T-cells).
This may increase the expression of co-stimulatory molecules and decrease the expression
of co-inhibitory molecules on T-cells leading to increased production of cytokines
and chemokines by T-cells, decreased proliferation of regulatory T-cells (Tregs),
and abrogation of tumor-induced immunosuppression. This ultimately induces a T-cell-mediated
immune response against cancer cells and leads to a reduction in tumor cell growth.
RORg, the nuclear receptor transcription factor that is involved in Th17/Tc17 differentiation,
plays a key role in immune activation.;
UNII : LPN433P0EA;
InChIKey : GULSIMHVQYBADX-FQEVSTJZSA-N;
CAS number : 2055536-64-4; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2055536-64-4
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G-SRS /a ;
Molecule name : LYC-55716;
NCI Metathesaurus CUI : CL514576;
Origin ID : C131294;
UMLS CUI : C5235392;
- Automatic exact mappings (from CISMeF team)
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target