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By analyzing a much larger collection of missense alleles than was previously available, we present evidence that supports the first model of different modes of receptor activation.
Based on available crystal structures and biochemical information, significant new insights have emerged into modes of receptor control, its deregulation in cancer, and the nuances that differentiate the four human receptors.
A set of functionalized analogues of 6 was designed and prepared (Schemes 1 and 2) from the key ester intermediate 19, based on predictions from molecular modeling of modes of receptor binding.
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This review outlines the mechanisms governing the major modes of receptor-mediated endocytosis used in drug delivery and highlights recent approaches using these as targets for in vivo drug delivery of nanoparticles.
As alluded to above, ligand bias and probe-dependence of allosteric modulator effects at mGlu1 suggest different modes of receptor-agonist interactions; therefore, to accurately assess the pharmacology of the nine schizophrenia mutants, we employed both the endogenous agonist glutamate, as well as the synthetic orthosteric agonist (S -3,5-dihydroxyphenylglycine (DHPG).
Studies in which the specific association of a type I BMP receptor with existing clusters of BMPRII is necessary for the initiation of efficient Smad signaling [39], [40], emphasize the importance of understanding the mode of receptor complex oligomerization in directing signaling outcomes for distinct ligands and receptors.
Although further mechanistic models have to await investigations on the mode of receptor G-protein coupling in the olfactory system, it is tempting to speculate that Drosophila ORs couple to heterotrimeric G-proteins although having an inverse membrane topology compared to other GPCRs.
While further mechanistic models have to await investigations on the mode of receptor G-protein coupling in the olfactory system, it is tempting to speculate that Drosophila ORs couple to heterotrimeric G-proteins although having an inverse membrane topology compared to other GPCRs.
Taken together, the positions of phosphorylatable amino acids in the AL are strictly conserved in PSKRs, suggesting a conserved mode of receptor regulation.
However, c-MET also recruits Gab1 via a second mechanism involving the small adaptor protein Grb2, and this represents the only mode of receptor interaction for Gab2 [ 33].
The alternative mode of receptor antagonism favored by Enz has been observed before in the estrogen receptor, where it was termed 'indirect antagonism' (Shiau et al., 2002; Zheng et al., 2012).
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com