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Inhibition of mammalian collagenases by thiol-containing peptides

✍ Scribed by Robert D. Gray; Robert B. Miller; Arno F. Spatola

Publisher: John Wiley and Sons
Year: 1986
Tongue: English
Weight: 422 KB
Volume: 32
Category: Article
ISSN: 0730-2312
DOI: 10.1002/jcb.240320108

No coin nor oath required. For personal study only.

✦ Synopsis

The following thiol-containing peptide analogues of the carboxyl side of the collagenase-sensitive bond of collagen were synthesized and tested as inhibitors of collagenases partially purified from homogenates of rabbit V-2 tumor and culture medium of pig synovium: HSCH2CH

The compounds are listed in order of their inhibitory potency when assayed with nonfibrillar-acid-soluble calf skin collagen at pH 7.6, 35°C. The best inhibitor (111) gave 50% inhibition between 1 and 4 pM. I1 was a competitive inhibitor with a Ki value of 75 pM. The enzymes preferred an isobutyl side chain at the 2-carbon position, and, where tested (111, IV), did not discriminate strongly between stereoisomers at the chiral2-carbon. Increasing the length of the inhibitor did not markedly increase potency.

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