منابع مشابه
Polyarginines are potent furin inhibitors.
The ubiquitous serine endoprotease furin has been implicated in the activation of bacterial toxins and viral glycoproteins as well as in the metastatic progression of certain tumors. Although high molecular mass bioengineered serpin inhibitors have been well characterized, no small nontoxic nanomolar inhibitors have been reported to date. Here we describe the identification of such inhibitors u...
متن کاملCationic Cell-Penetrating Peptides Are Potent Furin Inhibitors
Cationic cell-penetrating peptides have been widely used to enhance the intracellular delivery of various types of cargoes, such as drugs and proteins. These reagents are chemically similar to the multi-basic peptides that are known to be potent proprotein convertase inhibitors. Here, we report that both HIV-1 TAT47-57 peptide and the Chariot reagent are micromolar inhibitors of furin activity ...
متن کاملPotent furin inhibitors for the treatment of infectious diseases
Background: Furin and furin-like proprotein convertases are involved in disease related processes and emerged as potential drug targets. Results: The incorporation of basic acyl residues in P5 position provides highly potent inhibitors of furin, PC1/3, PC4, PACE4, and PC5/6. Conclusion: These inhibitors could be potential drugs for the treatment of infectious diseases. Significance: Development...
متن کاملSynthetic peptides derived from the prosegments of proprotein convertase 1/3 and furin are potent inhibitors of both enzymes.
Proprotein convertases (PCs) are Ca(2+)-dependent serine proteases of the subtilisin/kexin family which are known specifically to cleave propeptide and proprotein substrates at the C-terminal of R-X-(K/R)-R/ to generate the relevant biologically active peptides. PCs are initially synthesized as enzymically inactive proenzyme forms where the prosegments play an important inhibitory role to the r...
متن کاملResveratrol oligomers are potent MRP1 transport inhibitors.
BACKGROUND Knowledge of the structure-activity relationships of multidrug resistance protein 1 (MRP1, ABCC1) inhibitors may aid in developing potent inhibitors that can be used to circumvent MRP1-mediated multidrug resistance. MATERIALS AND METHODS Six stilbenes were examined for their ability to inhibit MRP1-mediated transport of 2',7'-bis-(carboxypropyl)-5(6)-carboxyfluorescein (BCPCF) from...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 2000
ISSN: 0021-9258
DOI: 10.1074/jbc.m003848200