Regulation of Kallikrein Activity

Promoter analysis and hormonal stimulation experiments allowed us to obtain insights into the mechanisms that regulate expression of the human kallikrein genes. In addition to KLK3 and KLK2, and more recently KLK10, no other kallikrein gene promoter has been functionally tested. 

Apart from KLK1, KLK2, and KLK3, no obvious TATA boxes were found in the promoter of other kallikreins. Two major obstacles exist in predicting the promoter response elements the inaccurate localization of 

The majority of hK3 (PSA) in the prostate and seminal plasma is in its free form, with less than 5% complexed with protein C inhibitor [111]. In serum, the majority of hK3 binds to protease inhibitors, and only 15%-25% is in the free form. The hK3-ai-antichymotrypsin complex constitutes 70%-85% of total serum hK3, with the hK3 2-macroglobulin and hK3 o,-antitrypsin complexes representing 15% and 3%, respectively [112-114], 

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