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Heparin prepared synthetically could replace animal-derived drug

Researchers at Rensselaer Polytechnic Institute and University of North Carolina at Chapel Hill have discovered an alternative way to produce heparin, a drug commonly used to stop or prevent blood from clotting.

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 can also 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.

Research 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. One human dose of heparin is approximately 100 milligrams.

Rensselaer and UNC-Chapel Hill researchers successfully synthesized hundreds of milligrams of heparin by developing a large-scale process involving engineered enzymes and co-factor recycling. The new, scaleable process can be applied to synthesize other heparin-based structures that regulate cell growth and may have applications in wound healing or cancer treatment, according to the researchers.