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The directed inhibition of a particular Rho-GTPase regulatory pathway can lead to the complete inhibition of specific cytoskeletal dynamics, thus potentially allowing for both potency and specificity.
Still, there is a need to greatly improve both potency and specificity based on the current rather poor performance of cystatins in biotechnological applications.
Contemporary medicinal chemistry faces diverse challenges from several directions, including the need for both potency and specificity of any therapeutic agent.
The inhibitory data against RTKs in this study demonstrated that variation of the 4-anilino substituents of these analogs dictates both potency and specificity of inhibitory activity against various RTKs.
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The inhibitory data against the RTKs in this study demonstrate that variation of the 6-ethylaryl substituents as well as the N4-phenyl substituents of these analogs does indeed control both the potency and specificity of inhibitory activity against RTKs.
The inhibitory data against the RTKs in this study demonstrates that variation of the substituent(s) in the benzyl ring of these 2-amino-4-anilino 6-benzyl pyrrolo[2,3-d]pyrimidines does indeed control both the potency and specificity of inhibitory activity against RTKs.
This makes the effective concentrations of inhibitor delivered to tissues difficult to assess and raises questions about both the potency and specificity of pathway inhibition in these studies [ 16].
Protein-protein interactions are likely to represent one of the next major classes of therapeutic targets, with PPIDs showing great potential for further optimization, both in terms of potency and specificity.
However, most of the reported radiotracers failed to visualize COX-2 in vivo due to multiple challenges including low metabolic stability, insufficient inhibitory potency and specificity for COX-2, and high non-specific binding to other targets.
We demonstrated the potency and specificity of these peptides as Mcl-1-specific reagents in BH3 profiling assays.
With direct analysis of zebrafish embryos treated with a specific small molecule, it should be possible to determine its potency and specificity through phenotypic determination coupled with profiling a panel of representative kinases.
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