Small-molecule inhibitor: spinorphin
Name
- Common name
- spinorphin
- Other names
- Leu-Val-Val-Tyr-Pro-Trp-Thr
Inhibition
- History
- Spinorphin is a heptapeptide that was isolated from bovine spinal cord by Nishimura et al. (1993).
- Peptidases inhibited
- Several enkephalin-degrading peptidases from monkey brain were inhibited (Nishimura & Hazato, 1993); these seem to have included an aminopeptidase, dipeptidyl-peptidase III, angiotensin-converting enzyme compound peptidase and neprilysin. The predominant inhibitory activity may be that against dipeptidyl-peptidase III (Ki = 0.5 micromolar: Yamamoto et al., 2002).
- Mechanism
- Inhibition is reversible.
- Pharmaceutical relevance
- Spinorphin has analgesic activity different from that of morphine (Ueda et al., 2000). In addition to its peptidase-inhibiting activity, spinorphin acts as a specific antagonist of the N-formylpeptide receptor subtype FPR (Liang et al., 2001).
Chemistry
- CID at PubChem
- 3081832
- ChEBI
- 488151
- Structure
- Chemical/biochemical name
- Leu-Val-Val-Tyr-Pro-Trp-Thr
- Formula weight
- 877
- Related inhibitors
- The peptide tynorphin is a truncated derivative of spinorphin. The bovine hemoglobin beta-chain contains similar peptide sequences (Zhao & Piot, 1997).
![[spinorphin structure ]](http://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&cid=3081832)
General
- Reviews
- Yamamoto et al. (2002)
