| Autor: |
Coats EA; Division of Pharmacology and Medicinal Chemistry, College of Pharmacy, University of Cincinnati, Ohio 45267-0004., Skau KA, Caperelli CA, Solomacha D |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of enzyme inhibition [J Enzyme Inhib] 1992; Vol. 6 (4), pp. 271-82. |
| DOI: |
10.3109/14756369309020177 |
| Abstrakt: |
A series of N-substituted glucosamines has been designed, synthesized, and tested as inhibitors of yeast hexokinase. All derivatives exhibited competitive inhibition kinetics with respect to glucose. Quantitative structure-activity relationships were derived from the resulting inhibition data. The most significant equation demonstrated the existence of highly specific steric effects for the seven meta-substituted benzoylglucosamines included in the relationship. Molecular modeling of potential complexes between the inhibitors and the hexokinase substrate binding site strongly suggests that the steric effects arise from potential contacts with two amino acid residues lying in the region occupied by the amide substituents. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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