Higher Affinity CD44 Antagonists
CD44 receptors, abundant on cancer cell surfaces, promote cell adhesion, metastasis and tumor growth. Selective antagonists of the CD44-HA (hyaluronic acid) interaction could help distinguish CD44-specific effects from interactions between HA and other receptors and prove valuable in cancer treatment and atherosclerotic research. While 5- or 8-amino-1,2,3,4-tetrahydroisoquinolines (5a- or 8a-THIQ) show only modest affinity for CD44 (400-800uM), this new technology provides 8-amino isomers (THIQ-HA disaccharide and tetrasaccharide conjugates) expected to have at least a 10-fold higher affinity for CD44, showing promise as more potent antagonists of HA binding.
Selectively Antagonize CD44-HA Interaction
Currently, no alternatives to these CD44 antagonists exist. Small molecule agents such as those in this technology provide distinct advantages over either biotherapeutics (cost), or oligosaccharide (selectivity) alternatives, and represent the first known molecules to selectively antagonize the HA interaction at CD44 only.
BENEFITS AND FEATURES:
- CD44-HA (hyaluronic acid) specific binding
- Higher affinity for CD44
- Potent antagonists of HA binding
- Cancer treatment
- Atherosclerotic research
- Studying CD44-HA specific effects
Phase of Development - Lead optimization