Phospho-Hirudin (pY63 variant)
Synthetic phosphotyrosine-63 hirudin analog with higher thrombin affinity than native sulfo-hirudin — Volkova 2023 steered-MD + in vitro plasma assay.
Mechanistic Evidence Box
Preclinical / mechanistic- Page type
- Compound profile
- Evidence type
- Synthetic phosphotyrosine-63 hirudin analog with higher thrombin affinity than native sulfo-hirudin — Volkova 2023 steered-MD + in vitro plasma assay.
- Evidence level
- In vitro
- Drug vs leech
- Synthetic analog
- Safety domains
- Bleeding
Clinical translation limit
Phospho-hirudin's superior in silico binding and in vitro plasma activity do NOT establish clinical efficacy. No FDA-approved phospho-hirudin derivative exists; clinical hirudin analogs (lepirudin, desirudin, bivalirudin) use different post-translational modifications.
Molecular Profile
- Category
- Anticoagulant
- Evidence tier
- Preclinical
- Molecular weight
- 7,000 Da
- Source species
- Hirudo medicinalis (sequence template)
- Discovered
- 2023 · Volkova A, Semenyuk P
Biological Targets
- → thrombin (Factor IIa); Tyr63 phosphate enhances binding to exosite I
Key Citations
- Volkova A, Semenyuk P (2023), Proteins · PMID 37860993
External Resources
Related Anticoagulant Compounds
Hirudin
The most potent natural thrombin inhibitor — and the molecular template for three FDA-approved direct thrombin inhibitor drugs.
Antistasin
Factor Xa inhibitor — prototype molecule that inspired the entire DOAC drug class (rivaroxaban, apixaban).
Ghilanten
Factor Xa inhibitor with anti-metastatic activity in animal cancer models — translational dual-use compound.
Lefaxin
Factor Xa inhibitor with anti-inflammatory properties.