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Fig. 3 Integrin αVβ3 receptor binding of the hybrid probe.
In the blocking study, the cellular uptake decreased to 72.2 % in the presence of RGD2 (10 μM), indicating specific binding of the hybrid probe to the integrin αVβ3 expressed on tumor cells (Fig. 4b).
Immunofluorescence staining showed the formation of new blood vessels in tumor tissues, suggesting that the tumor uptake was due to specific binding of the hybrid probe to integrin αVβ3 expressed on tumor cells.
A control experiment with Na3[Fe(OH)6Mo6O18] up to two molar equivalents showed no quenching of the tryptophan signal at either pH value (5.5 and 7.4), which revealed no binding in the vicinity of tryptophan 214 and thus indicated the importance of the aromatic moieties in the binding of the hybrid POMs reported herein.
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We hypothesize that the cytotoxic mechanism of TfR-lytic peptide is initiated by binding of the TfR-binding moiety of the hybrid peptide to TfR molecules on the cell surface, after which the lytic moiety of the hybrid peptide preferentially disintegrates the cancer cell membrane, induces mitochondrial damage, and triggers apoptotic cell death.
Whereas the extracellular loop 2 is engaged in the binding of the scopolamine-based hybrid structures, it plays a minor role for the binding of atropine-based dualsteric ligands.
The AAG component in the model was a representation of both plasma binding proteins, with the "hybrid" binding affinity estimated to fit the data.
We found that the binding of porphyrin hybrids occured through intercalation and groove binding mode in addition interaction with the amino acid residues constituting the active cavity of Topo IIβ.
The receptors are present either as homodimers or hybrid receptors composed of IGF1R and IR heterodimers, and are activated by binding of the ligands IGF1 and IGF2, as well as insulin when the hybrid receptor is present [ 10].
For example, it could be possible to construct a chimeric avidin-BBP-dimer [ 37] to adjust the ligand-binding properties of the resultant hybrid protein.
This result suggests that tumor uptake of the hybrid probe was attributable to its binding to integrin αVβ3.
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binding of the regulatory
binding of the specific
binding of the primary
binding of the endogenous
binding of the native
binding of the active
binding of the nuclear
binding of the full
binding of the other
binding of the extracellular
binding of the monoclonal
binding of the bivalent
binding of the monomeric
binding of the secondary
binding of the human
binding of the activated
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