Hirudin

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(Redirected from
Desirudin
)
Hirudin
SCOP2
4htc / SCOPe / SUPFAM
Available protein structures:
Pfam  structures / ECOD  
PDBRCSB PDB; PDBe; PDBj
PDBsumstructure summary

Hirudin is a naturally occurring peptide in the salivary glands of blood-sucking leeches (such as Hirudo medicinalis) that has a blood anticoagulant property.[2] This is essential for the leeches' habit of feeding on blood, since it keeps a host's blood flowing after the worm's initial puncture of the skin.

Hirudin (MEROPS I14.001) belongs to a superfamily (MEROPS IM) of

protease inhibitors that also includes haemadin (MEROPS I14.002) and antistasin (MEROPS I15).[3][4]

Structure

During his years in

homogeneous preparations of hirudin.[8]

Biological activity

A key event in the final stages of

blood clot. The principal inhibitor of thrombin in normal blood circulation is antithrombin.[8] Similar to antithrombin, the anticoagulant activity of hirudin is based on its ability to inhibit the procoagulant activity of thrombin
.

Hirudin is the most potent natural inhibitor of thrombin. Unlike antithrombin, hirudin binds to and inhibits only the activated thrombin, with a specific activity on fibrinogen.

serum proteins, and can also act on complexed
thrombin.

Medical use

Hirudin variant-1
Identifiers
OrganismHirudo medicinalis
Symbol?
UniProt
P01050
Search for
StructuresSwiss-model
DomainsInterPro

It is difficult to extract large amounts of hirudin from natural sources, so a method for producing and purifying this protein (specifically P01050 in the infobox) using recombinant biotechnology has been developed. This has led to the development and marketing of a number of hirudin-based anticoagulant pharmaceutical products, including:

  • recombinant hirudin derived from
    Hansenula
     (Thrombexx, Extrauma)
  • lepirudin (Refludan) – differs by one amino acid substitution and removal of sulfate group on Tyr63
  • desirudin
    (Revasc/Iprivask) – differs by removal of sulfate group on Tyr63
  • bivalirudin – peptide fragment

Several other direct thrombin inhibitors are derived chemically from hirudin.

See also

References

  1. ^ PDB: 4HTC​
  2. doi:10.1098/rspl.1883.0135
    .
  3. ^ "InterPro". www.ebi.ac.uk.
  4. ^ "Clan IM". MEROPS - the Peptidase Database.
  5. S2CID 29110118
    .
  6. PMID 2765488
    .
  7. PMID 2374926
    .
  8. ^
    PMID 1920434
    .
  9. PMID 9579630
    .

External links
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