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The methylation of H3R2 and H3K4 abolishes or weakens the binding affinity, suggesting that these two amino acids may be involved in the binding.
In a previous preclinical study, the main advantage of -[18F]flubatine compared to -[18F]flubatine was its higher binding affinity suggesting that -[18F]flubatine might be able to detect also slight reductions of α4β2 nAChRs and could be more sensitive than -[18F]flubatine in early stages of Alzheimer's disease.
A single mutation (Ile87Ala) in the same CD loop region of the Epstein-Barr virus IL-10 (ebvIL-10) also reduces IL-10R1 binding affinity, suggesting that ebvIL-10 and 9D7Fab use similar allosteric mechanisms to modulate IL-10R1 affinity and biological activity.
Using alanine point mutants of GB1, we show that the amplitude of mechanical stability enhancement of GB1 by Fc does not correlate with the binding affinity, suggesting that binding affinity only affects the population of GB1/human Fc (hFc) complex at a given concentration of hFc, but does not affect the intrinsic mechanical stability of the GB1/hFc complex.
These molecules have good binding affinity suggesting that the receptor does not require a flat molecule.
The reduced susceptibility of F1174L mutated ALK to crizotinib inhibition results from an increase in ATP binding affinity, suggesting that higher doses of crizotinib may mitigate the resistance.
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Lastly, correlations drawn between T6PP active site structure, inhibitor structure and inhibitor binding affinity suggest that the aryl d-glucopyranoside 6-sulfate prototypes will find future applications as a platform for development of tailored second-generation T6PP inhibitors.
These modifications to the binding affinity suggest that in order to obtain accurate binding affinity data in structural investigations truly reflective of the in vivo setting, the type and duration of stimulation and the effect this stimulation has on the proteins of interest needs to be fully understood.
These compounds were initially evaluated for histamine H3 receptor binding affinities, suggesting that a propoxy chain linker between the amine and the core ring could be essential for optimal binding affinity.
In heavy chain variable or light chain variable domains, the introduction of additional disulfide bonds into the framework region did not reduce antigen-binding affinity, suggesting that generating disulfide bonds may be a method for stabilizing IgG and antibody fragments, such as the antigen-binding fragment, and single-chain and single-domain antibodies.
The data reported by McKeon and colleagues show that phosphorylation increases the DNA-binding affinity, suggesting that transcriptional repression might be caused by inhibiting several functions of the molecule.
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