Abstract:
:Novel peptides containing the sequence -Pro-Leu-Ama(NHOH)- were synthesized and characterized by spectroscopic techniques. Their inhibitory properties towards the activated form of native human gelatinase B (MMP-9) and the catalytic domain of neutrophil collagenase (cdMMP-8) were determined. The most effective inhibitor synthesized exhibits Ki values of 2 x 10(-6) M (cdMMP-8) and 5 x 10(-9) M (MMP-9) thus attaining interesting discrimination between the tested metalloproteinases. A most important feature of this type of inhibitor is its peptide nature making the compounds similar to natural substrates. In spite of the peptide character of the inhibitors synthesized, the P1-P1'-peptide bond shows a high resistance to cleavage by the proteinases.
journal_name
FEBS Lettjournal_title
FEBS lettersauthors
Krumme D,Wenzel H,Tschesche Hdoi
10.1016/s0014-5793(98)01128-4subject
Has Abstractpub_date
1998-10-02 00:00:00pages
209-12issue
2eissn
0014-5793issn
1873-3468pii
S0014-5793(98)01128-4journal_volume
436pub_type
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