Article ID Journal Published Year Pages File Type
2006439 Peptides 2011 6 Pages PDF
Abstract

Kallikrein-related peptidases (KLKs) are a group of serine proteases, expressed in several tissues. Their activity is regulated by inhibitors including members of the serine protease of Kazal-type (SPINK) family. Recently, we discovered that SPINK6 is expressed in human skin and inhibits KLK5, KLK7, KLK14 but not KLK8. In this study we tested whether SPINK6 inhibits other members of the KLK family and caspase-14. Using chromogenic substrates, SPINK6 exhibited inhibitory activity against KLK12 and KLK13 with Ki around 1 nM, KLK4 with Ki = 27.3 nM, KLK6 with Ki = 140 nM, caspase-14 with a Ki approximating 1 μM and no activity against KLK1, KLK3 and KLK11. Taken together, SPINK6 is a potent inhibitor of distinct KLKs members.

► SPINK6 inhibits KLK4. ► SPINK6 inhibits KLK6. ► SPINK6 inhibits KLK12. ► SPINK6 inhibits KLK13. ► SPINK6 does not inhibit KLK3 and KLK11.

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Life Sciences Biochemistry, Genetics and Molecular Biology Biochemistry
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