Mannose 2, 3, 4, 5, 6-<i>O</i>-pentasulfate (MPS): a partial activator of human heparin cofactor II with anticoagulation potential

Bano, Shadabi; Khan, Abdul Burhan; Fatima, Sana; Rashid, Qudsia; Prakash, Amresh; Gupta, Neha; Ahmad, Irshad; Ansari, Shoyab; Lynn, Andrew M.; Abid, Mohammad; Jairajpuri, Mohamad Aman

doi:10.1080/07391102.2022.2053749

Cited by 2 publications

(2 citation statements)

References 39 publications

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“…In vivo HCII is potentiated by dermatan sulfate (Tovar et al, 2005) with some specificity in this interaction; a hexasaccharide containing 2-O-sulfated iduronic acid and 4-O-sulfated N-acetyl-galactosamine (Maimone and Tollefsen, 1990). Interaction with heparin requires no specific sequence (Huntington, 2006) with other polyanions also able to bind and potentiate HCII (Colwell et al, 1999;Bano et al, 2022). Interaction with heparin induces conformational changes in HCII, similar to that of AT leading to exposure of the RCL (O'Keeffe et al, 2004).…”

Section: Potentiation Of Heparin Cofactor IImentioning

confidence: 99%

Pharmacology of Heparin and Related Drugs: An Update

et al. 2023

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Section: Potentiation Of Heparin Cofactor IImentioning

confidence: 99%

Pharmacology of Heparin and Related Drugs: An Update

et al. 2023

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“…Recently, one effort by the Jairajpuri group has been reported to identify NSGM-based HCII activators. The group identified that mannose 2,3,4,5,6- O -pentasulfate (MPS, Figure ) is a partial activator of human HCII with significant anti-coagulation potential . Thus, it appears that a major opportunity for developing synthetic and homogeneous non-saccharide activators of HCII is available.…”

Section: Synthetic Sulfated Inhibitors Of Coagulation Factorsmentioning

confidence: 99%

Designing Smaller, Synthetic, Functional Mimetics of Sulfated Glycosaminoglycans as Allosteric Modulators of Coagulation Factors

et al. 2023

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Natural glycosaminoglycans (GAGs) are arguably the most diverse collection of natural products. Unfortunately, this bounty of structures remains untapped. Decades of research has realized only one GAG-like synthetic, small-molecule drug, fondaparinux. This represents an abysmal output because GAGs present a frontier that few medicinal chemists, and even fewer pharmaceutical companies, dare to undertake. GAGs are heterogeneous, polymeric, polydisperse, highly water soluble, synthetically challenging, too rapidly cleared, and difficult to analyze. Additionally, GAG binding to proteins is not very selective and GAG-binding sites are shallow. This Perspective attempts to transform this negative view into a much more promising one by highlighting recent advances in GAG mimetics. The Perspective focuses on the principles used in the design/discovery of drug-like, synthetic, sulfated small molecules as allosteric modulators of coagulation factors, such as antithrombin, thrombin, and factor XIa. These principles will also aid the design/discovery of sulfated agents against cancer, inflammation, and microbial infection.

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Mannose 2, 3, 4, 5, 6-O-pentasulfate (MPS): a partial activator of human heparin cofactor II with anticoagulation potential

Cited by 2 publications

References 39 publications

Pharmacology of Heparin and Related Drugs: An Update

Pharmacology of Heparin and Related Drugs: An Update

Designing Smaller, Synthetic, Functional Mimetics of Sulfated Glycosaminoglycans as Allosteric Modulators of Coagulation Factors

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