Substrate und Inhibitoren

Z-AEVD-FMK is an irreversible inhibitor of caspase-10 and related caspases. At 10 µM, it can prevent the initiation of Fas signaling by caspase-10 in Jurkat T lymphoma cells, preventing Bid cleavage into its active form, caspase cascade activation, and apoptosis.

Ac-LETD-AFC is a fluorogenic substrate that can be cleaved specifically by caspase-8. Caspase activity can be quantified by fluorescent detection of free AFC (also known as 7-amino-4-trifluoromethylcoumarin), which is excited at 400 nm and emits at 505 nm.

Gly-Pro-pNA is a chromogenic substrate that can be cleaved by the circulating enzyme, dipeptidyl peptidase IV (DPP IV). Enzyme activity can be quantified by colorimetric detection of free p-nitroanilide at 405 nm. DPP IV inactivates the two peptides responsible for a majority of nutrient-stimulated insulin secretion: glucose-dependent insulinotropic polypeptide (GIP) and...

alpha-Bungarotoxin is a snake venom-derived toxin that irreversibly binds nicotinic acetylcholine receptors (Ki = ~2.5 µM in rat) present in skeletal muscle, blocking action of acetylcholine at the postsynaptic membrane and leading to paralysis. It has been widely used to characterize activity at the neuromuscular junction, which has numerous applications in neuroscience...

Abz-Ala-Pro-Glu-Glu-Ile-Met-Arg-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human neutrophil elastase (kcat/Km = 531 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm, em = 420 nm).

Abz-Val-Ala-Asp-Nva-Arg-Asp-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human proteinase 3 (kcat/Km = 1,570 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm, em = 420 nm).

Aeruginosins are tetrapeptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosins inhibit serine/threonine protein phosphatases (PPs). In endothelial cells, aeruginosins decrease levels of IL-8 and ICAM-1 and inhibit NF-kappaB activity. Aeruginosins may also bind thrombin and exhibit antithrombotic activity.

Aeruginosamides are linear ribosomal peptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosamides may inhibit serine/threonine protein phosphatases (PPs) or exhibit antithrombotic activity.

Aeruginosamides are linear ribosomal peptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosamides may inhibit serine/threonine protein phosphatases (PPs) or exhibit antithrombotic activity.

Aeruginosamides are linear ribosomal peptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosamides may inhibit serine/threonine protein phosphatases (PPs) or exhibit antithrombotic activity.

Aeruginosamides are linear ribosomal peptides isolated from cyanobacteria such as Microcystis aeruginosa. Like other cyanotoxins, aeruginosamides may inhibit serine/threonine protein phosphatases (PPs) or exhibit antithrombotic activity.

Anabaenopeptins are cyclopentapeptides isolated from cyanobacteria such as Microcystis aeruginosa and Oscillatoria agardhii. Anabaenopeptins and other cyanotoxins are typically inhibitors of serine/threonine protein phosphatases (PPs). Anabaenopeptins may also inhibit carboxypeptidases. Anabaenopeptins B and F are considered "nontoxic" compared to other variants.