The findings could enable the current supply of the drug - now extracted from animal tissue - to be replaced or supplemented by the synthetic version. The new process also can be applied as a tool for drug discovery, according to the researchers.
Heparin is a complex carbohydrate used to stop or prevent blood from clotting during medical procedures and treatments such as kidney dialysis, heart bypass surgery, stent implantation, indwelling catheters, knee and hip replacements, and deep vein thrombosis. The annual worldwide sales of heparin are estimated at $3 billion.
"We have synthetically prepared heparin in quantities large enough for use in human medical treatments by engineering recently discovered heparin biosynthetic enzymes," says Robert Linhardt, the Ann and John H. Broadbent Jr. '59 Senior Constellation Professor of Biocatalysis and Metabolic Engineering at Rensselaer Polytechnic Institute. "These discoveries will enable us to effectively replace a variable raw material - heparin derived from processed animal organs - with a synthetic material - synthetic heparin - and have the same therapeutic result."
Research in Linhardt's group at the Center for Biotechnology and Interdisciplinary Studies at Rensselaer focuses on complex carbohydrates such as heparin. After determining the structure of these molecules, researchers study their biological activities to establish a structure-activity relationship that may reveal lead compounds for new drug development.
Researchers at MIT first prepared a synthetic heparin, but, in amounts of less than 1 microgram, it was insufficient to treat humans, says Linhardt. One human dose of heparin is approximately 100 milligrams.