Drug Development
Reports Summarize Drug Development Study Results from University of Lille
Published in Drug Week, January 21st, 2011
2011 JAN 21 -- "In situ click chemistry has been successfully applied to probe the ligand binding domain of EthR, a mycobacterial transcriptional regulator known to control the sensitivity of Mycobacterium tuberculosis to several antibiotics. Specific protein-templated ligands were generated in situ from one azide and six clusters of 10 acetylenic fragments," scientists in Lille, France report.
"Comparative X-ray structures of EthR complexed with either clicked ligand BDM14950 or Its azide precursor showed ligand-dependent conformational Impacts on the protein architecture. This approach revealed two mobile phenylalanine residues that control the access to...
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Source: Drug Week (2011-01-21)
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