Exact(1)
Increasing hydrophobicity, however, reduces the CAMP selectivity for bacterial over eukaryotic host membranes, thereby causing the risk of detrimental side-effects.
Similar(59)
To further investigate the cGMP selectivity mechanism of CNB-B, we solved a low-temperature X-ray structure bound with cAMP at 1.3 Å.
They are activated endogenously by cAMP and with some pharmacological selectivity by 8-pCPT-2'-O-Me-cAMP 90.
Although the fluorescence signal change was small, this sensor had high cGMP affinity (1 µM) and selectivity for cGMP over cAMP (400-fold) comparable to cGES-DE5 (Figure 1C).
Although the FRET change in magnitude is modest relative to of the previous reported sensors [14] [16], this sensor had both of high cGMP affinity (40 nM) and high selectivity for cGMP over cAMP (>1000-fold >1000-foldC).
Another sensor, termed "cygnet-1" [ 106], was constructed to have high selectivity for cGMP over cAMP.
To enable specific activation of PKA-I, cAMP analog combinations with improved isozyme selectivity were synthesized.
As predicted, butaprost and 11-deoxy-PGE1 induced a raise in cAMP levels, consistent with the receptor selectivity pattern.
We used [125I]-CGRP and [125I]-AMG 334 binding assays to measure AMG 334/CGRP-receptor interactions, cell-based cAMP assays to study functional activity and selectivity of AMG 334, and a laser Doppler model in cynomolgus (cyno) macaque to assess the pharmacodynamic effects of blocking capsaicin-induced increases in dermal blood flow with AMG 334.
As observed in HT-29 cells all three agonists triggered changes in cAMP that were consistent with their reported receptor selectivity profiles (Fig. 6B).
Specifically, we will show how NMR was utilized to reveal the dynamical basis of cyclic nucleotide affinity, selectivity, agonism and antagonism in multiple eukaryotic cAMP and cGMP receptors.
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