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ChemInform Abstract: QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS OF 6-ANILINOURACILS AS INHIBITORS OF BACILLUS SUBTILIS DNA POLYMERASE III
- Source :
- Chemischer Informationsdienst. 15
- Publication Year :
- 1984
- Publisher :
- Wiley, 1984.
-
Abstract
- Quantitative structure-activity relationships (QSAR) of a series of 6-anilinouracil derivatives were developed for their inhibitory activity against the wild-type DNA polymerase III (pol III) and a mutant enzyme, pol III/azp-12, derived from Bacillus subtilis. Interaction between inhibitors and both enzymes appears to result solely from hydrophobic binding. Comparison of the substituent contributions indicates increased hydrophobic character and a minor change of shape of the inhibitor binding site of the mutant enzyme. Because the two enzymes have identical Km values for substrates, the inhibitor binding site is thought to be distinct from the enzyme active site.
- Subjects :
- chemistry.chemical_classification
Quantitative structure–activity relationship
biology
Chemistry
DNA polymerase
Substituent
Active site
General Medicine
Bacillus subtilis
biology.organism_classification
RNA polymerase III
chemistry.chemical_compound
Enzyme
Biochemistry
biology.protein
Binding site
Subjects
Details
- ISSN :
- 00092975
- Volume :
- 15
- Database :
- OpenAIRE
- Journal :
- Chemischer Informationsdienst
- Accession number :
- edsair.doi...........fd39d0b93e662967b179a47e07178bd5