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It is part of a local hydrophobic core that includes L498 on α3 S, M616 on α4 S, and L629 on α5 S. When mutated to isoleucine, a derivative comparable to leucine itself in both size and charge, the residue can still stably reside in and maintain this environment.
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The activity of the pyridine derivatives was comparable to benzene derivatives.
In our opinion, this option seems less likely because results in the group treated with a combination of metformin and sulfonylurea derivatives were comparable to those on monotherapy with metformin.
The mre11-H59A strain was of intermediate sensitivity to IR, less resistant than the Jel1 parental strain or the Jel1 mre11Δ derivative expressing MRE11, but comparable to the derivatives expressing mre11-D56N, mre11-D56A or mre11-H125N, and more resistant than Jel1 mre11Δ or its derivative expressing mre11-H213Y (Fig. 2).
The light harvesting efficiency of mono-methoxy derivative (11) would be comparable to TC4.
Betulin and betulinic acid have been involved in chemical modulation, leading to highly active derivatives, some of them comparable to clinically used drugs [3, 7].
Novel BODIPY derivatives exhibited photophysical properties comparable to commercially available BODIPY FL EDA (4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene-3-propionyl ethylenediamine).
While substitution of Phe4 by a phenethyl group (4) decreased μ affinity (Kiμ=13.3 nM), the same derivative containing Dmt (12) was comparable to EM-2 but also acquired weak δ antagonism (pA2=7.05).
Significantly, our data also suggest that the RS domain is not required for enhancer-dependent SR protein functions, at least in the context of IgM M1-M2, as the levels of splicing of IgM M1-M2 and IgM-derivative substrates with ΔNΔRS were comparable to, or greater than, those observed with SF2/ASF.
In particular, compound 10 was the most potent derivative with EC50 = 0.3 μM, comparable to that of nevirapine used as reference drug.
Nedaplatin (cis-diammine-glycolate O,O′-platinum II, 254-S) is a second-generation platinum derivative that has an antitumour activity comparable to that of cisplatin (Kobayashi et al, 1991) but is less toxic to the kidney (Kameyama et al, 1990), as seen in preclinical experiments.
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com