Search was performed by enabling "High precision" option in Docking precision menu, "Dock" was chosen as the calculation type, "Flexible" for the ligand and "AScore" was used as the scoring function.
For instance, PEGylated gold NPs with a core size of ∼2.3 nm exhibited high tumor targeting efficiencies of 8.3 ± 0.9%ID/g at 12 h post injection (p.i .. Gold nanocages coated with PEG surface ligand also enabled high blood retention and an efficient tumor uptake of 7.9 ± 1.1%ID/g at 24 h p.i.
Availability of these high quality PET ligands will undoubtedly broaden the use of PET imaging in the CNS drug discovery process, enable high quality preclinical and clinical studies, and ultimately result in the identification of novel treatment of neurological disorders of high unmet medical need.
Incorporation of two versatile adaptor components, PrA(G,L) and SA, within a single heterobifunctional structure should enable high-throughput assembly of a variety of bispecific ligands and bifunctional probes in a simple mix-and-use procedure.
This fluorescent PPARγ probe enables high-throughput and homogenous FP assays for the identification of novel endogenous and exogenous PPARγ ligands, and this rational ligand design approach may be applied to other therapeutically important members of the nuclear hormone receptor superfamily.
Ensuring that high-tech enables high-touch.
The coding sequence of piggyBac has been codon-optimised to enable higher levels of transposition in the mouse, and inducible versions have been generated by fusing the transposon to the ERt oestrogen receptor ligand-binding domain [259].
β2-Integrins with high ligand binding affinity have an extended, open conformation where the cytoplasmic tails unclasp enabling the association of signalling molecules with the cytoplasmic domains that build the integrin adhesome.
In both cases, the mechanism switches from being dominated by the conformational selection pathway at low ligand concentration to induced fit at high ligand concentration.
Conditional ligands have enabled the high-throughput production of human leukocyte antigen (HLA) libraries that present defined peptides.
