695172-03-3Relevant articles and documents
Development of Irreversible Diphenyl Phosphonate Inhibitors for Urokinase Plasminogen Activator
Joossens,Van Der Veken,Lambeir,Augustyns,Haemers
, p. 2411 - 2413 (2007/10/03)
In this letter we report the synthesis and biochemical evaluation of selective, irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator (uPA). A diphenyl phosphonate group was introduced on the substratelike peptide Z-D-Ser-Ala-Arg, and modification of the guanidine side chain was investigated. A guanylated benzyl group appeared the most promising side chain modification. A kapp value in the 103 M -1 s-1 range for uPA was obtained, together with a selectivity index higher than 240 toward other trypsin-like proteases such as tPA, thrombin, plasmin, and FXa.