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The δ receptor was solubilized from HEK 293 cell membranes with n-dodecyl-β-d-maltoside in an active form that maintained high affinity bremazocine binding.
The μ receptor was solubilized from HEK 293 cell membranes with n-dodecyl-β-d-maltoside in an active form that maintained high affinity bremazocine binding.
In fact, methylation of the exocyclic NH group maintained high affinity for the tri-methylene 2-aminobenzimidazole derivative, while a drop in affinity was observed for the annular N-methylation.
The majority of the synthesized compounds maintained high affinity for 5-HT7 receptors and showed selectivity towards 5-HT6 andopaminene D2 receptors and different selectivity for 5-HT1A and α1 adrenergic receptors.
The addition of the smaller dansyl fluorophore to XAC resulted in a molecule that maintained high affinity at the A1 receptor, comparable with that of the parent XAC molecule.
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A new method is presented for the redesign of protein protein interfaces, resulting in specificity of the designed pair while maintaining high affinity.
This initial SAR suggests pharmacophoric elements that may be modified to modulate/increase opioid affinity, while maintaining high affinity for the NOP receptor, to result in potent bifunctional small-molecule NOP/MOP ligands.
Furthermore, we isolated a variant with pH-dependent affinity, demonstrating a 1,000-fold 1,000-foldaffinity from pH 7 to 4. Additional rational mutagenesis endowed Protein-G with significhange enhanced stabinity in baffinityditions relative to the parent domain while maintaining high afromity to the Fab.
The results also show that in order to maintain high affinity and selectivity for the D3 receptor the heterocyclic ring does not need to be connected directly to the piperazine ring as the majority of compounds included here are linked either via an amide or a methylene linker to the heterocyclic moiety.
The HKT-1 is the K+ transporter that maintains high affinity K+ loading and hence proper K+ level, crucial for cell osmoregulation and turgor maintenance during dehydration [ 5].
Importantly, the design of a fluorescent GPCR ligand must take into account structure activity relationships in order to maintain high affinity, and, optionally, to direct the fluorophore to a particular region of a receptor.
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maintained binding affinity
maintained high level
maintained high methylation
maintained high association
maintained high degradation
maintained high activity
maintained high sensitivity
maintained high palmitate
maintained high approval
maintained high stability
maintained high child
maintained high discipline
maintained high viability
maintained high catalase
maintained high sequence
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