Drug Designing by Blocking Enzyme Activity, Biotechnology Research, Trimethoprim, Dihydrofolate Reducase, Bacteria

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Home >> Industrial and Microbial Biotechnology >>Drug Discovery and Drug Designing >> Drug Designing by Blocking Enzyme Activity

Drug designing by blocking enzyme activity

Since most drugs act by modifying or blocking the activity of an enzyme, a deeper understanding of suitable chosen target enzymes should lead to major advance:; in rational drug designing. Following two examples will illustrate the utility of drug designing as an important area of biotechnology research.

Trimethoprim (TMP).

This clinically important antimicrobial drug provides an important example to demonstrate drug designing. This drug inhibits the enzyme dihydrofolate reducase (dHFR) in bacteria and is frequently used to treat urinary tract infections, but in high concentrations it attacks even human dHFR, thus becoming harmful (toxic), if used by the patient. In view of this, the structures of different dHFRs have been compared, so that TMP with greater specificity for bacterial enzyme could be designed. Since TMP shows flexibility in its three dimensional structure in association with enzyme dHFR, efforts have been made to sythesize TMP, which will have a rigid three dimensional structure in association with bacterial enzyme dHFR, so that it may not be able to attack human dHFR.

Inhibitor of renin

Inhibitors of the enzyme renin are also being actively modelled. The enzyme catalyses the first in a series of reactions that lead to elevated blood pressure. Models of renin have been prepared on the basis of known structures of similar other proteins like aspartic proteinases and pepsin. This led to the designing of nonpeptide inhibitors that mimic intermediate product in the reaction of renin with its substrate, so that native renin will not function. These inhibitors may be useful for treating hypertensions.

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