Rationales Design von Thrombinhemmstoffen: Von Fibrinogen und Hirudin zu synthetischen Antikoagulanzien

Steinmetzer, Torsten; Stürzebecher, Jörg

doi:10.1002/pauz.200400068

Cited by 6 publications

(1 citation statement)

References 15 publications

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“…Lepirudin and desirudin are recombinant hirudins that were developed by recombinant technology in Saccharomyces cerevisiae [ 80 ]. Bivalirudin is an engineered 20-amino acid, synthetic analogue of hirudin [ 81 ]. All hirudin derivatives are also used parenterally.…”

Section: Current Thrombin Inhibitorsmentioning

confidence: 99%

Thrombin Inhibition by Argatroban: Potential Therapeutic Benefits in COVID-19

Aliter

Al‐Horani

2020

Cardiovasc Drugs Ther

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Thrombin is a trypsin-like serine protease with multiple physiological functions. Its role in coagulation and thrombosis is wellestablished. Nevertheless, thrombin also plays a major role in inflammation by activating protease-activated receptors. In addition, thrombin is also involved in angiogenesis, fibrosis, and viral infections. Considering the pathogenesis of COVID-19 pandemic, thrombin inhibitors may exert multiple potential therapeutic benefits including antithrombotic, anti-inflammatory, and antiviral activities. In this review, we describe the clinical features of COVID-19, the thrombin's roles in various pathologies, and the potential of argatroban in COVID-19 patients. Argatroban is a synthetic, small molecule, direct, competitive, and selective inhibitor of thrombin. It is approved to parenterally prevent and/or treat heparin-induced thrombocytopenia in addition to other thrombotic conditions. Argatroban also possesses anti-inflammatory and antiviral activities and has a well-established pharmacokinetics profile. It also appears to lack a significant risk of drug-drug interactions with therapeutics currently being evaluated for COVID-19. Thus, argatroban presents a substantial promise in treating severe cases of COVID-19; however, this promise is yet to be established in randomized, controlled clinical trials.

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Section: Current Thrombin Inhibitorsmentioning

confidence: 99%

Thrombin Inhibition by Argatroban: Potential Therapeutic Benefits in COVID-19

Aliter

Al‐Horani

2020

Cardiovasc Drugs Ther

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Anticoagulants in Use

Zichichi

Ammar

et al. 2022

Transfusion Practice in Clinical Neurosciences

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Peptide and protein based pharmaceuticals

Mező

2013

Amino Acids, Peptides and Proteins

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It is predicted that in the 21st century there will be more and more new drug investments that violates the Lipinski's “rule-of-five”. Among them, peptides have received increased interest in the current drug therapies. Advantages of peptide-based pharmaceuticals are the high potency and selectivity as well as their low accumulation in tissues; thus, they have potentially lower toxicity than the small drug molecules. Furthermore, the high chemical and biological diversity of peptides provide a broad range of targets, which could represent a basis for personalized medication. Currently, there are more than 70 approved peptide drugs on the market, generating an annual sale close to USD 20 billion in 2012. About half of them are presented in this chapter, which ones are used for the treatment of diabetes, cancers, multiple sclerosis, HIV, hereditary angioedema, respiratory distress syndrome, prevention of thrombosis or relief pain. Next to the structures of the peptide-based pharmaceuticals, their biological activity on the mentioned diseases will be shortly discussed. An outlook for the new peptide-based drug development indicates high perspectives of this area.

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Rationales Design von Thrombinhemmstoffen: Von Fibrinogen und Hirudin zu synthetischen Antikoagulanzien

Cited by 6 publications

References 15 publications

Thrombin Inhibition by Argatroban: Potential Therapeutic Benefits in COVID-19

Thrombin Inhibition by Argatroban: Potential Therapeutic Benefits in COVID-19

Anticoagulants in Use

Peptide and protein based pharmaceuticals

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