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Activation could mean ligand modification or ligand transcytosis to a membrane environment conducive to signaling.
Cellular uptake and particularly endosomal escape is regarded as being pivotal for successful siRNA therapy, but no chemical modification or ligand conjugation has so far convincingly improved these properties.
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This explains the fundamental question of how the minor differences elicited by substitutions of single bps among REs or mutational, post-translational modification or ligand-binding events can lead to vastly different functional effects.
Prenylation is frequently associated to reversible post-translational modifications or ligand binding events such as palmitoylation, phosphorylation or GTP-binding [5].
The standard microarray experiments cannot measure the transcription factor activities (TFAs) directly, since TFAs are subject to post-translational modifications or ligand binding in order to exert their function.
This label-free screening method requires no modification to protein or ligand.
This number includes SLiM interfaces from three different categories of ELM (LIG or ligand, MOD or modification, and TRG or targeting) and 14 different classes (Fig. 3c).
Optimally, and especially for protein kinases, a broad range of crystal structures should be obtained to characterize target flexibility, structure modulation via co-factor binding or posttranslational modification, ligand induced conformational changes, and off-target complex structures for selectivity optimization.
In a ligand-dependent receptor-mediated cellular system (or ligand cellular system), key structural modifications surrounding ligand binding are expected to cause outliers.
Proteins that communicate a biological event (either ligand binding, enzymatic modification, or protease cleavage) into a measurable output are highly desirable for diagnostic applications.
TF activity is frequently modulated at the post-translational level through ligand binding, covalent modification, or changes in sub-cellular localization.
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