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Translocation of the mammalian CPC seems to depend on a reduction in the centromere binding affinity and an increase in the microtubule binding affinity of the CPC.
Also, heating of β-lg at 75 °C for 10 to 20 min modified the binding parameters of 2-nonanone, with a decrease in binding affinity and an increase in stoichiometry (O'Neill and Kinsella 1988).
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Pharmacokinetic studies both in situ and in vivo demonstrated a higher tissue binding affinity and a greater expanse of intrahepatic distribution by galactosylated SCR lipoplexes.
In vitro screening of fluoromethyl bridge-fused ring (BFR) analogues of WAY-100635 (5b, 5b and 5c) has shown a high binding affinity and a good selectivity for the 5-HT1A receptor.
MD simulations and subsequent MM GBSA calculations revealed that the hydrophobic interactions between all compounds and HSP90α contributed the most to the binding affinity and a good linear correlation was obtained between the calculated and the experimental binding free energies (R = 0.88).
To our surprise their results demonstrated both agonists to have a more favorable receptor binding affinity and a better tumor uptake in vivo, whereas the saturation assay resulted in more binding sites for 67/natGa-DOTA-Tyr3-octreotide on the used breast cancer cell line (ZR75 1) than natGa-NODAGA-JR11 and 67/natGa-DOTA-Tyr3-octreotate.
Palonosetron is a potent and highly selective 5-HT3 RA with a strong binding affinity and a longer plasma-elimination half-life relative to the older 5-HT3 RAs [ 3].
65 The in vitro mitogenicity has been investigated and IDeg was found to have a low IGF-1 receptor binding affinity and a low mitogenic/metabolic potency ratio.
Palonosetron is a second-generation 5-HT3 receptor antagonist with an even higher receptor binding affinity, and a prolonged mean half-life of about 40 h [ 8].
The K d values in the HiTS-FLIP datasets range from 8 nM to 1000 nM, where a small K d represents high binding affinity and a large K d represents low binding affinity.
As noted in Tables 1 and 2, the methylation of cytidine nucleobases in the major groove of hairpin DNAs 7, 10, and 11 led in each case to decreased Fe·BLM binding affinity and a decrease in DNA cleavage products.
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