2004
DOI: 10.1074/jbc.m400484200
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Abstract: Polyarginine-containing peptides represent potent inhibitors of furin, a mammalian endoprotease that plays an important role in metabolism, activation of pathogenic toxins, and viral proliferation. The therapeutic use of D-polyarginines is especially interesting because they are not cleaved by furin and possess inhibitory potency almost equal to L-polyarginines. In this study we attempted to determine the important elements within polyarginines that contribute to effective inhibition. Structure-function analys… Show more

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Cited by 109 publications
(114 citation statements)
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“…Exogenous inhibitors as regulators of processing enzymes have been under much investigation (86)(87)(88)(89)(90)(91)(92)(93)(94)(95)(96), but few selective inhibitors exist. Specific active-site directed inhibitors of processing enzymes are desirable for mechanistic studies, but such inhibitors are unlikely to provide selective regulation for processing specific proneuropeptide or prohormones, since each protease appears to process multiple proneuropeptide substrates.…”
Section: Inhibitors and Modulators Of Processing Enzymesmentioning
confidence: 99%
“…Exogenous inhibitors as regulators of processing enzymes have been under much investigation (86)(87)(88)(89)(90)(91)(92)(93)(94)(95)(96), but few selective inhibitors exist. Specific active-site directed inhibitors of processing enzymes are desirable for mechanistic studies, but such inhibitors are unlikely to provide selective regulation for processing specific proneuropeptide or prohormones, since each protease appears to process multiple proneuropeptide substrates.…”
Section: Inhibitors and Modulators Of Processing Enzymesmentioning
confidence: 99%
“…The PCs are also involved in a large number of pathologies, including bacterial and viral infections, as well as cancer and metastasis. Therefore, these enzymes are intensely investigated as drug targets (3), using for example, peptide-derived compounds (4)(5)(6)(7)(8)(9), nonpeptidic small molecule compounds (10,11), and protein-based inhibitors (12)(13)(14)(15).…”
mentioning
confidence: 99%
“…Data for Furin and PACE4 are also provided for comparison (Cameron et al, 2000;Kacprzak et al, 2004). Differences in assay ionic strength are noted: Furin and PACE4 assays for poly-L-arginine peptides and hexa-D-arginine were done at 5 mM CaCl 2 (Cameron et al, 2000); Furin and PACE4 assays for nona-D-arginine were done at 0.1 mM CaCl 2 (Cameron et al, 2000;Kacprzak et al, 2004). sible to ensure that the peptide targets a PC.…”
mentioning
confidence: 99%