Heparan Sulfate (HS) Inhibitor Development Service at CD BioGlyco

HS is a complex polysaccharide that occurs naturally within the human body and is renowned for its anticoagulant properties. This molecule plays a crucial role in various biological processes, including cell signaling, inflammation regulation, and tissue development. Due to its unique structure and diverse functions, HS is a subject of great interest in biomedical research and therapeutic development. CD BioGlyco provides professional and comprehensive HS inhibitor development services based on years of in-depth research and understanding of HS.

• First, we synthesize potential HS inhibitors by molecular modeling, structure-activity relationships, and other methods of targeted synthetic chemical design for identified targets. This involves the design and synthesis of multiple structurally similar compounds for subsequent activity and selectivity assessment.
• Then, we identify compounds with potential inhibitory effects by validating and screening for biological activity against HS. Subsequently, the synthesized compounds are evaluated for biological activity, including in vitro and in vivo assays, to determine their ability to inhibit HS as well as their effects on cells or animal models. Then, based on the results of the bioactivity evaluation, the structures of the compounds are optimized to improve their activity and selectivity.
• Finally, after pharmacokinetic and toxicological evaluation of the optimized and active inhibitors, the compounds are subjected to further in vivo and in vitro studies to ensure the safety and efficacy of the compounds.

Fig.1 Classification of HS inhibitors. (CD BioGlyco)

Applications

• Tumor progression and metastasis can be inhibited through the use of HS inhibitors that interfere with the interaction of tumor cells with the basement membrane and extracellular matrix.
• HS is one of the strongest naturally occurring anticoagulant substances in the body. HS inhibitors can help reduce the risk of thrombosis and provide an idea for research on anticoagulant drugs.
• HS inhibitors may attenuate the inflammatory response by regulating the adhesion and migration of inflammatory cells, so the inhibitors have also been applied to the development of anti-inflammatory drugs.

Frequently Asked Questions

• What is HS?
  HS is a complex polysaccharide composed of glucosamine and sulfate groups. It is found in most cells and tissues and plays an important role, especially in the extracellular matrix. HS has a variety of functions in living organisms. First, it can act as a cell surface receptor and bind to a variety of bioactive molecules (such as cytokines, growth factors, viruses, etc.) to regulate cell signal transduction and communication. Second, it can act as a major component of the extracellular matrix and be involved in cell-cell interactions, tissue development, and cell migration. In addition, HS can also regulate physiological processes such as blood clotting, inflammation, and tumor development.
• What is the biosynthesis process of HS?
  The first step in the biosynthesis of HS is the synthesis of the basic units of the core polysaccharide chain, namely glucosamine, and glucose, by the intracellular metabolic pathway. In the endoplasmic reticulum, a series of enzymes mediate the polymerization of glucosamine and glucose, forming the basic structure of the core polysaccharide chain. In the Golgi apparatus and the transport vesicles of the Golgi apparatus, specific sites on the core polysaccharide chain are sulfated. This process requires the involvement of a variety of enzymes, including sulfate transferases. Finally, some proteins may bind to the core polysaccharide chain to form proteoglycan complexes that may be modified and processed to further form HS.

Fig.2 Schematic illustration of HS biosynthesis. (Li & Kusche-Gullberg, 2016)

At CD BioGlyco, we provide complete solutions for the development of Glycosaminoglycan Inhibitors, including HS inhibitors. By utilizing our vast expertise, we offer professional and high-quality support to clients engaged in scientific projects. If you need the service mentioned above, please contact us for more information.