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The ubiquitous ATP binding site offers a global target for protein kinase inhibitors.
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To better understand such network abnormalities, in silico screening of TF/uDBP binding sites offers a valuable approach, and we have shown that this can facilitate discovery of cis-regulatory modules, design of targeted dODN therapies, and interpretation of GWAS hits at non-coding loci.
The Akt substrate-binding site offers a large number of potential interactions to an appropriately designed small molecule and can form the basis for the development of selective inhibitors.
The tetrameric folding of β-tryptase and the pair-wise distribution of its substrate binding sites offer a unique opportunity for development of inhibitors that span two adjacent binding sites.
While assessment of the MPEP binding site offers insight into the binding kinetics of mGluR5 drugs that target this site, it must be noted that there is a family of mGluR5 allosteric modulators that do not bind to this site [ 27- 29], and currently there are no radioligands available to directly assess the density and affinity of these non-MPEP sites.
Investigation of these dehydrogenases shows that sequence similarities near the cofactor binding site offer the best prediction as to whether or not a related dehydrogenase is from a mycofactocin-encoding genome.
The HIV-1 envelope gp120, which features both the virus receptor (CD4) and coreceptor (CCR5/CXCR4) binding sites, offers multiple sites for therapeutic intervention.
This work suggests that the substrate-binding site offers new opportunities for targeted drug design.
Discovery of this second site offers a new way to explain the observation that β-catenin and Groucho proteins exhibit mutually exclusive binding patterns in in vitro and in vivo binding assays.
Perhaps his Web site offers a clue?
Allosteric binding sites, as opposed to traditional orthosteric binding sites, offer unparalleled opportunities for drug discovery by providing high levels of selectivity, mimicking physiological conditions, affording fewer side effects because of desensitization/downregulation, and engendering ligands with chemotypes divergent from orthosteric ligands.
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CEO of Professional Science Editing for Scientists @ prosciediting.com