Drug Designing by Blocking Enzyme Activity,Trimethoprim,Dimensional Structure,Inhibitor of Renin,Peptide Inhibitors

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	Drug Designing by Blocking Enzyme Activity -Since most drugs act by modifying or blocking the activity of an enzyme, a deeper understanding of suitably chosen target enzymes should lead to major advances 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 reductase (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 may be designed. Since TMP shows flexibility in its three dimensional structure in association with enzyme dHFR, efforts have been made to synthesize 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 proteinase and pepsin. This led to the designing of non peptide inhibitors that mimic intermediate product in the reaction of renin with its substate, so that native renin will not function. These inhibitors may be useful for treating hypertensions.