Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.
Bioorganic & Medicinal Chemistry Letters(2019)
摘要
The connection between Netherton syndrome and overactivation of epidermal/dermal proteases particularly KLK5 has been well established. To treat sufferers of this severe condition we wished to develop a topical KLK5 inhibitor in order to normalise epidermal shedding and reduce the associated inflammation and itching. In this paper we describe structure-based optimisation of a series of brightly coloured weak KLK5 inhibitors into colourless, non-irritant molecules with good KLK5 activity and selectivity over a range of serine proteases.
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关键词
KLK1,KLKB1,KLK5,KLK7,KLK8,LEKTI,NS,SPINK5
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