Table 2.
Natural (yellow) and synthetic (light blue) inhibitors of thrombin whose complexes have been structurally characterized.
| Ligand | Description | Reference |
|---|---|---|
| AGAP008004-PA | Recombinant P5 fragment of cE5, a salivary protein from the major African malaria vector Anopheles gambiae | [55] |
| Anophelin | Anticoagulant from the malaria vector Anopheles albimanus | [56] |
| Avathrin | Thrombin inhibitor derived from a multicopy precursor in the salivary glands of the ixodid tick Amblyomma variegatum | [57] |
| Bivalirudin | Artificial anticoagulant peptide, mimic of hirudin, composed of 20 residues | [58] |
| Boophilin | Multifunctional kunitz-type proteinase inhibitor from the cattle tick Rhipicephalus microplus | [59] |
| CVS995 synthetic peptide | Divalent thrombin inhibitor that contains an alpha-keto-amide transition-state mimetic linking an active site binding group and a group that binds to the fibrinogen-binding exosite | [60] |
| Hemadin | Thrombin inhibitor from the land-living leech Haemadipsa sylvestris | [61] |
| Hirudin | Protein isolated from the salivary glands of the medicinal leech Hirudo medicinalis | [62] |
| Hirugen | N-acetyl-Hir53′-64′ with sulfato-Tyr63′, where Hir53′-64′ corresponds to the C-terminal residues of hirudin | [63] |
| Hirullin | A natural COOH-terminal peptide isolated from the leech Hirudinaria manillensis | [64] |
| Hirulog | Synthetic hirudin peptide analog | [63] |
| Hirunorm | Synthetic hirudin peptide analog | [65] |
| Hirutonin | Synthetic hirudin peptide analog | [66] |
| IgA fab | Randomly acquired antithrombin antibody found in a patient who presented a traumatic subdural hematoma | [67] |
| Madanin-1 | Small cysteine-free thrombin inhibitor that facilitate blood feeding in the tick Haemaphysalis longicornis | [68] |
| Nonapeptide inhibitor | Synthetic hirudin peptide analog | [69] |
| Ornithodorin | Protein isolated from the blood sucking soft tick Ornithodoros moubata | [70] |
| Peptide inhibitor | C-terminal hirugen-like segment of a bivalent thrombin inhibitor | [71] |
| Rhodniin | Protein isolated from the assassin bug Rhodnius prolixus | [72] |
| Staphylocoagulase | Cofactor secreted by Staphylococcus aureus that activates prothrombin | [73] |
| Suramin | Hexasulfonated naphthylurea first made by O. Dressel, R. Kothe and B. Heymann at Bayer AG laboratories in Elberfeld | [74] |
| Synthetic inhibitor | Hirudin-based fibrinogen recognition exosite peptide inhibitor | [64] |
| Synthetic peptide | Synthetic peptide; sequence: Sin YEPI Hyp EE Smf Alc Q (Sin, succinic acid; Hyp, 4-hydroxyproline; Smf, 4-sulfomethyl-l-phenylalanine; and Alc, 2-amino-3-cyclohexyl-propionic acid) | [75] |
| Synthetic thrombin inhibitor P798 | Synthetic bivalent thrombin inhibitor that comprises an active site blocking segment, a fibrinogen recognition exosite blocking segment, and a linker | [76] |
| Synthetic thrombin inhibitor P596 | Bivalent peptidyl pyridinium methyl ketone inhibitor | [77] |
| Triabin | Protein from the saliva of the blood-sucking triatomine bug Triatoma pallidipennis | [30] |
| Tsetse thrombin inhibitor | Anticoagulant peptide produced in the salivary glands of the tsetse fly Glossina morsitans | [78] |
| Variegin | Thrombin inhibitor isolated from the tropical bont tick Amblyomma variegatum | [79] |