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The P2 homo-phenylalanine residue does not fill the S2 binding pocket, which is quite shallow, but likely confers potency by contributing a hydrophobic interaction at a 'ledge' formed from Gly-Gly.
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These findings in molecular recognition conferring potency and selectivity facilitated illustrative studies on nAChR structure-guided insecticide design, yielding outstandingly potent and selective candidate compounds with novel pharmacophores.
To validate our co-crystal structure and identify residues that confer potency for Ac-AChBP, we conducted surface plasmon resonance (SPR) analysis to study the binding affinities of LvIA and its mutants.
The different lipid-A structures of P. aeruginosa versus E. coli confer potency differences which are apparent in vitro [ 64, 65], and in vivo [ 66].
Although the cyclic TSP-1 peptides did not confer potency equivalent to ABT-510, they are active and exhibit excellent stability, thus demonstrating an opportunity for SFTI-1 and MCoTI-II frameworks in developing the next generation of thrombospondin mimetics.
All the compounds examined conferred unusual potency in a tumor cell cytotoxicity assay.
Lastly, a crystal structure of idelalisib bound to the p110δ subunit of PI3Kδ furthers our understanding of the binding interactions that confer the potency and selectivity of idelalisib.
In this Digest, we illustrate protein and RNA modulators that exploit this design principle, with all of the examples based on the displacement or replacement of a magnesium ion, and which can confer a potency advantage.
Chemical modifications that increase the hybridization affinity of oligonucleotides are reasoned to confer higher potency, i.e., modified oligonucleotides can be dosed at lower concentrations to achieve the same effect.
The DFG/TAE226 contact in FAK is likely to confer high potency (Table 2) and selectivity [20].
Their functional assays confirmed that the mutation H1047R strongly conferred oncogenic potency while moderate and weak potency was induced by the variants H1047L and H1047Y, respectively.
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