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33 Sulfur-based zinc-binding groups also showed some selectivity in compounds like Largazole, a potent and selective HDACi for HDAC1 and 2. It is a densely functionalized macrocyclic peptide isolated from the Cyanobacterium symploca sp. by Luesch and coworkers.
Rottlerin has been shown to inhibit PKCδ with some selectivity over other PKC isoforms, while Ro 32-0432 iselectiveve for conventional isoforms (reviewed in [ 12]).
We recognize that we have selected the two most extreme receptor proteins for this study and that some selectivity may lie with AFB1 4.
"Some selectivity has crept into the market".
Compounds in this group exhibited single digit nano-molar potency and some selectivity between the two enzymes.
This observation suggests that cecropin B shows some selectivity with respect to lipid composition of the membrane.
Some selectivity for the inhibition of the tumor-associated versus the cyctosolic isoform II with some of these compounds has also been evidenced.
In vitro binding studies on cinnamoyl morphinamines showed moderate affinity for all opiate receptors with some selectivity for mu opioid receptors, while cinnamoyl codeinamines only showed affinity for mu opioid receptors.
The kinase inhibition results indicated that two compounds inhibited casein kinase 1δ/ε (CK1δ/ε) with some selectivity over related kinases, namely CDK5/p25, GSK-3α/β, and DYRK1A.
Although the outward current appeared to show some selectivity for protons, it was not sensitive to Zn2+ or temperature and the H+-selective component could not be separated from a larger conductance of unknown selectivity.
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Apicidin, which like depsipeptide has some selectivity for class 1 HDACs (Bieliauskas and Pflum, 2008), did not generally mimic the drug sensitivity profiles of either depsipeptide or TSA, showing a narrower range of activity with a smaller distribution of IC50 values across the non-uveal melanoma cell line panel (compare Figure 2A with Figure 1C).
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