The bump-and-hole method is a tool in chemical genetics for studying a specific isoform in a protein family without perturbing the other members of the family. The unattainability of isoform-selective inhibition due to structural homology in protein families is a major challenge of chemical genetics. With … See more Inspiration for the bump-and-hole method was drawn from mutant E. coli strains which carried an A294S mutant version of phenylalanine tRNA synthetase and survived exposure to p-FluoroPhe, a slightly bumped … See more As structural information about protein-ligand interfaces have become available, bump-and-hole pairs have been used to elucidate the substrates of specific proteins from … See more Webbump-and-hole-systems; the nucleotide-based substrate analog must be delivered across the plasma membrane and into the Golgi compartment, and the cell must stably express …
Organic synthesis toward small-molecule probes and drugs PNAS
WebOne such effort, dubbed the bump-and-hole approach, has convincingly demonstrated that engineering at the protein-small molecule interface constitutes a powerful method for elucidating the function of a specific … WebOct 18, 2024 · Achieving orthogonality through steric or shape complementarity, commonly known as the bump-and-hole approach, has emerged as one of the most powerful ASCG techniques in recent years (Bishop et al., 2001) ( Figure 1 ). black label society tuning
Chemical biology. A bump-and-hole approach to engineer …
WebAuxin regulates transcriptional response via its receptors, TIR1 and AFB F-box proteins. Here we report an engineered, orthogonal auxin-TIR1 receptor pair, developed through a … WebNational Center for Biotechnology Information black label society tour dates 2021