RESEARCH AND SYNTHESIS OF LIGANDS FOR SCIENTIFIC AND MEDICAL RESEARCH

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.

OBJECTIVES :

  • 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.
PRODUCTS
  • 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.
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