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- W2022113016 abstract "New 3-amidinophenylalanine-derived matriptase inhibitors were developed and tested against the related trypsin-like serine proteases matriptase-2, thrombin and factor Xa. The strongest matriptase inhibition was found for compounds containing an N-terminal 2′,4′-dichloro- or 2′,4′-dimethoxy-biphenyl-3-sulfonyl group. The combination with a C-terminal piperidyl-cyclohexylurea residue provided the first monobasic matriptase inhibitor with a Ki value < 3 nM and excellent selectivity over thrombin. The X-ray structure of a representative analogue in complex with thrombin superimposed with matriptase provides information regarding the selectivity profile observed in this study." @default.
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- W2022113016 date "2012-01-01" @default.
- W2022113016 modified "2023-10-03" @default.
- W2022113016 title "New 3-amidinophenylalanine-derived inhibitors of matriptase" @default.
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- W2022113016 doi "https://doi.org/10.1039/c2md20074k" @default.
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