Definition
Heparin is a naturally occurring sulfated polysaccharide, and as such it is composed of many sugar units or saccharides. It has a long history being first marketed as a pharmaceutical product in the USA in 1939. It is still used in the prevention and treatment of coagulation disorders. It is an anticoagulant, inhibiting the clotting of blood collected into a tube, and an antithrombotic, inhibiting the formation of clots in blood vessels in the body (Mulloy et al. 2016).
Structure and Origin
The structure of heparin is complex. It is a completely linear molecule resembling a long chain (unlike many other polysaccharides which may be branched). It is made up of alternating glucosamine and uronic acid monosaccharide units, heavily substituted with sulfates attached to the nitrogen in the glucosamine, and oxygen in the glucosamines and the uronic acids (N- and O-sulfates,...
References
Alban S (2012) Adverse effects of heparin. Handb Exp Pharmacol 207:211–263. https://doi.org/10.1007/978-3-642-23056-1_10
Biran R, Pond D (2017) Heparin coatings for improving blood compatibility of medical devices. Adv Drug Deliv Rev 112:12–23. https://doi.org/10.1016/j.addr.2016.12.002
Gong F, Jemth P, Escobar Galvis ML et al (2003) Processing of macromolecular heparin by heparanase. J Biol Chem 278(37):35152–35158. https://doi.org/10.1074/jbc.M300925200
Gresele P, Busti C, Paganelli G (2012) Heparin in the prophylaxis and treatment of venous thromboembolism and other thrombotic diseases. Handb Exp Pharmacol 207:179–209. https://doi.org/10.1007/978-3-642-23056-1_9
Gupta S, Tiruvoipati R, Green C, Botha J, Tran H (2015) Heparin induced thrombocytopenia in critically ill: diagnostic dilemmas and management conundrums. World J Crit Care Med 4(3):202–212. https://doi.org/10.5492/wjccm.v4.i3.202
Harris EN, Baggenstoss B, Weigel PH (2009) Rat and human HARE/stabilin-2 are clearance receptors for high- and low-molecular-weight heparins. Am J Physiol Gastrointest Liver Physiol 296:G1191–G1199
Johansen KB, Balchen T (2013) Tinzaparin and other low-molecular-weight heparins: what is the evidence for differential dependence on renal clearance? Exp Hematol Oncol 2:21. https://doi.org/10.1186/2162-3619-2-21
Mohamed S, Coombe DR (2017) Heparin mimetics: their therapeutic potential. Pharmaceuticals (Basel) 10(4):78. https://doi.org/10.3390/ph10040078
Mulloy B, Hogwood J, Gray E (2010) Assays and reference materials for current and future applications of heparins. Biologicals 38:459–466
Mulloy B, Hogwood J, Gray E, Lever R, Page CP (2016) Pharmacology of heparin and related drugs. Pharmacol Rev 68:76–141
Ori A, Wilkinson MC, Fernig DG (2011) A systems biology approach for the investigation of the heparin/heparan sulfate interactome. J Biol Chem 286:19892–19904
Ourri B, Vial L (2019) Lost in (clinical) translation: recent advances in heparin neutralization and monitoring. ACS Chem Biol 14(12):2512–2526. https://doi.org/10.1021/acschembio.9b00772
Pomin VH, Mulloy B (2018) Glycosaminoglycans and proteoglycans. Pharmaceuticals 11:27. https://doi.org/10.3390/ph11010027
Signorelli SS, Scuto S, Marino E, Giusti M, Xourafa A, Gaudio A (2019) Anticoagulants and osteoporosis. Int J Mol Sci 20(21):5275. https://doi.org/10.3390/ijms20215275
Szajek AY, Chess E, Johansen K et al (2016) The US regulatory and pharmacopeia response to the global heparin contamination crisis. Nat Biotechnol 34:625–630
Van der Meer J-Y, Kellenbach E, van den Bos L-J (2017) From farm to pharma: an overview of industrial heparin manufacturing methods. Molecules 22:1025. https://doi.org/10.3390/molecules22061025
Veverka V, Henry AJ, Slocombe PM et al (2009) Characterization of the structural features and interactions of sclerostin: molecular insight into a key regulator of Wnt-mediated bone formation. J Biol Chem 284:10890–10900
Zhang Y, Zhang M, Tan L, Pan N, Zhang L (2019) The clinical use of Fondaparinux: a synthetic heparin pentasaccharide. Prog Mol Biol Transl Sci 163:41–53
Author information
Authors and Affiliations
Corresponding author
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2021 Springer Nature Switzerland AG
About this entry
Cite this entry
Mulloy, B., Coombe, D.R. (2021). Heparin and Related Drugs. In: Offermanns, S., Rosenthal, W. (eds) Encyclopedia of Molecular Pharmacology. Springer, Cham. https://doi.org/10.1007/978-3-030-21573-6_10070-1
Download citation
DOI: https://doi.org/10.1007/978-3-030-21573-6_10070-1
Received:
Accepted:
Published:
Publisher Name: Springer, Cham
Print ISBN: 978-3-030-21573-6
Online ISBN: 978-3-030-21573-6
eBook Packages: Springer Reference Biomedicine and Life SciencesReference Module Biomedical and Life Sciences