Trigone is active in the field of research and synthesis of ligands for scientific and medical research. Our strategy is based on a triple interactive approach that boost creativity in the development of tools for scientific biological research: organic synthesis of new products or ligands of biological targets, biochemical and biological testing of these new compounds, structure-activity relationships and planning of better ligands.
- To design, prepare and deliver new ligands for biological receptors as nuclear steroid receptors.
- To develop tools to study biological mechanism of steroid hormones and antagonists like tamoxifen (anti- breast cancer drug).
- To aid the study of different isoforms of estrogen nuclear receptor (ERa) and other steroid receptors (PgR, AR, ...).
- To develop model of medical imaging, diagnosis and treatment of steroid hormones dependent cancers.
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- Non-steroid ligands of ER (tamoxifen-like class), including ITAZ (4-Iodotamoxifen aziridine), agent for affinity covalent labelling of ERα and potentially of P-gP (P glycoprotein).
- Kit "ER PROFILER" for the analysis of ER isoforms by SDS-PAGE and autoradiography techniques.
- High affinity ligands for estrogen receptor (ER) (agonist class), including Z-CMIV (Z-17α-iodovinyl-11β-chloromethyl-estradiol), "superaffinity" ligand of ERα (10 times higher affinity than estradiol) with strong interaction between receptor and chloromethyl group. Z-CMIV is also highly selective with negligible affinity for estradiol transport protein TEBG/SBP.
- High affinity ligands of other steroid receptors.
- Ligands and inhibitors of non-receptor steroid binding proteins like SHBG transport proteins and steroid-metabolizing enzymes.