Inhibiting keratinocyte activation and proliferation, for treatment of dermatological disorders such as psoriasis or actinic precancerous states

摘要

The use of inhibitors (I) of dipeptidyl peptidase IV (DP IV) or analogous enzymes is claimed for inhibiting the activation and proliferation of keratinocytes (including malignantly transformed keratinocytes) and tumor cells derived from keratinocytes.- DETAILED DESCRIPTION - An INDEPENDENT CLAIM is included for (I)-containing pharmaceutical preparations for use as above.- ACTIVITY - Antiinflammatory; dermatological; antipsoriatic; cytostatic.- MECHANISM OF ACTION - Dipeptidyl peptidase IV inhibitor; DNA synthesis inhibitor.- Inhibition of DP IV in keratinocytes suppresses activation and DNA synthesis in these cells and thus suppresses proliferation. Addition of N( epsilon )-4-nitrobenzyloxycarbonyl-L-lysine-thiazolidide (Ia) at 2 mu M reduced DNA synthesis (measured after 72 hours) in cultured NHEK Ad human keratinocytes by ca. 50 %