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While the parent compound is devoid of activity, both metabolites of fexinidazole are active against intracellular L. donovani amastigotes.
We employed the NK3-selective agonist, senktide, which selectively and potently activates NK3 receptors in rat brain, but is virtually devoid of activity at NK1 receptors (Laufer et al. 1986a,b; Wormser et al. 1986).
As expected, mutants Q43X and S19fsX51, which produce truncated forms of receptor, were devoid of activity.
Conversely, analogous monocarboxy caffeoyl analogs exhibited only modest inhibition, while the corresponding 3,4-dihydroxybenzoyl-substituted compounds were devoid of activity.
[d-Trp4]URP and [d-Tyr6]URP both induced a robust increase in [Ca2+]c in astrocytes while [Orn5]URP was totally devoid of activity.
The compounds are selective upstream inhibitors of FcεR1-dependent human mast cell degranulation and proved to be devoid of activity in downstream ionomycin mediated degranulation.
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High rates of enzymatic hydrolysis were achieved for untreated C. homosphaera biomass with enzymes containing endoglucanase and β-glucosidase activities and devoid of cellobiohydrolase activity.
Another American trypanosome, Trypanosoma rangeli, expresses a homologous protein that has sialidase activity but is devoid of transglycosidase activity.
Although derived from the glucocorticoid cortisol acetate, it was designed to be devoid of glucocorticoid activity while retaining efficacious anti-angiogenic activity.
All compounds were devoid of bactericidal activity against four bacterial strains (50.00 μg/mL) and antiprotozoal activity against Trichomonas vaginalis (200.00 μg/mL).
Indeed, it was recently reported that proteins devoid of measurable activity (e.g. GH61) can significantly improve the activity of PCW-degrading enzymes [ 30, 31].
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