Ilomastat Explained

Ilomastat (INN),[1] (codenamed GM6001, proprietary name Galardin®) is a broad-spectrum matrix metalloproteinase inhibitor.[2] [3] [4]

This chemotherapy agent is considered to have application in skincare products for its antiaging properties.

Ilomastat is a member of the hydroxamic acid class of reversible metallopeptidase inhibitors. The anionic state of the hydroxamic acid group forms a bidentate complex with the active site zinc.[5]

Examples of enzymes that ilomastat inhibit include rabbit MMP9,[6] thermolysin,[2] peptide deformylase,[7] and anthrax lethal factor endopeptidase (LF) produced by the bacterium Bacillus anthracis.[8] [9]

Notes and References

  1. Web site: International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 36. World Health Organization. 23 February 2017. 148.
  2. Grobelny D, Poncz L, Galardy RE . Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids . Biochemistry . 31 . 31 . 7152–4 . August 1992 . 1322694 . 10.1021/bi00146a017.
  3. Schultz GS, Strelow S, Stern GA, Chegini N, Grant MB, Galardy RE, Grobelny D, Rowsey JJ, Stonecipher K, Parmley V . Treatment of alkali-injured rabbit corneas with a synthetic inhibitor of matrix metalloproteinases . Invest. Ophthalmol. Vis. Sci. . 33 . 12 . 3325–31 . November 1992 . 1385350 .
  4. Santiskulvong C, Rozengurt E . Galardin (GM 6001), a broad-spectrum matrix metalloproteinase inhibitor, blocks bombesin- and LPA-induced EGF receptor transactivation and DNA synthesis in rat-1 cells . Exp. Cell Res. . 290 . 2 . 437–46 . November 2003 . 14568001 . 10.1016/S0014-4827(03)00355-0.
  5. Web site: Small-molecule inhibitor J16.402: galardin . Wellcome Trust Sanger Institute . MEROPS - the Peptidase Database . 2010-09-07 . 2010-10-04 .
  6. 1655675 . 32 . An inhibitor of the matrix metalloproteinase synthesized by rabbit corneal epithelium . 1991 . Invest Ophthalmol Vis Sci . 2997–3001 . Fini ME, Cui TY, Mouldovan A, Grobelny D, Galardy RE, Fisher SJ. 11 .
  7. Balakrishnan A, Patel B, Sieber SA, Chen D, Pachikara N, Zhong G, Cravatt BF, Fan H . Metalloprotease inhibitors GM6001 and TAPI-0 inhibit the obligate intracellular human pathogen Chlamydia trachomatis by targeting peptide deformylase of the bacterium . J. Biol. Chem. . 281 . 24 . 16691–9 . June 2006 . 16565079 . 10.1074/jbc.M513648200 . free .
  8. Kocer SS, Walker SG, Zerler B, Golub LM, Simon SR . Metalloproteinase inhibitors, nonantimicrobial chemically modified tetracyclines, and ilomastat block Bacillus anthracis lethal factor activity in viable cells . Infect. Immun. . 73 . 11 . 7548–57 . November 2005 . 16239558 . 1273843 . 10.1128/IAI.73.11.7548-7557.2005 .
  9. Turk BE, Wong TY, Schwarzenbacher R, Jarrell ET, Leppla SH, Collier RJ, Liddington RC, Cantley LC . The structural basis for substrate and inhibitor selectivity of the anthrax lethal factor . Nat. Struct. Mol. Biol. . 11 . 1 . 60–6 . January 2004 . 14718924 . 10.1038/nsmb708 . 39119275 .

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