Chaim Gilon

Chaim Gilon

Chaim Gilon

Institute of Chemistry, The Hebrew University, Jerusalem, Israel
p: 02-6585276

 

Development and application of technologies for the conversion of bioactive peptides and active regions in proteins into drugs. Over the years we have developed technologies such as: Backbone Cyclization, Cycloscan, Combinatorial Cycloscan and Helix Walk. These technologies are based on the design and synthesis of libraries with conformational diversity based on a parent active peptide or active region in protein and screening them for their biological activity, metabolic stability and intestinal bioavailability. From these libraries the most active, selective, metabolically stable and orally bioavailble peptidomimetic with drug properties is selected for in vivo preclinical studies. Few recent examples for the application of these technologies: (1) discovery of a novel mocrocyclic, orally available, potent inhibitor of HIV-1 replication in cells, a drug lead for AIDS (2) potent orally available, mimetic of a-MSH that inhibits weight gain in mice. (3) extremely highly potent (pictogram/animal) drug lead that cure rheumatoid arthritis.