Fundamentals of Medicinal Chemistry

(Brent) #1

A.12 Enzyme structure and species


The structure of a specific enzyme may vary from species to species. These

differences, which tend to be the replacement of one or a few amino acid residue

by alternative residues, may be important in that they may form selective targets

for drugs. For example, differences in the structures of human and bacterial

DHFR result in the antibacterial trimethoprin binding specifically to bacter-

ial DHFR (see section 7.5.1).

The structure of an enzyme can also vary within a person, since different

genes may encode enzymes that catalyse the same reaction. These enzymes are

known asisozymes. Isozymes are often specific for different types of tissue. For

example, lactate dehydrogenase (LDH) is produced in two forms, the M-type

(muscle) and the H-type (heart). The M-type is predominates in tissue subject to

anaerobic conditions, such as skeletal muscle and liver tissue, whereas the

H-type predominates in tissue under aerobic conditions, such as the heart.

Isozymes may be used as a diagnostic aid. For example, the presence of

H-type LDH in the blood indicates a heart attack, since heart attacks cause

the death of heart muscle with the subsequent release of H-type LDH into the

circulatory system.

Variations in the structures of enzymes within a species can also occur

between and within ethnic groups of the same species. For example, a number

of different alcohol dehydrogenase isoenzymes have been observed in some

Asians.

260 APPENDIX 12 ENZYME STRUCTURE AND SPECIES

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