Recombinant truncated and microsomal heme oxygenase-1 and -2: differential sensitivity to inhibitors

Vukomanovic, Dragic, McLaughlin, Brian, Rahman, Mona N., Vlahakis, Jason Z., Roman, Gheorghe, Dercho, Ryan A., Kinobe, Robert, Hum, Maaike, Brien, James F., Jia, Zongchao, Szarek, Walter A., and Nakatsu, Kanji (2010) Recombinant truncated and microsomal heme oxygenase-1 and -2: differential sensitivity to inhibitors. Canadian Journal of Physiology and Pharmacology, 88 (4). pp. 480-486.

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Abstract

Recombinant truncated forms of heme oxygenase-1 and -2 (HO-1 and HO-2) were compared with their crude microsomal counterparts from brain and spleen tissue of adult male rats with respect to their inhibition by azole-based, nonporphyrin HO inhibitors. The drugs tested were an imidazole-alcohol, an imidazole-dioxolane, and a triazole-ketone. Both the recombinant and crude forms of HO-2 were similarly inhibited by the 3 drugs. The crude microsomal spleen form of HO-1 was more susceptible to inhibition than was the truncated recombinant form. This difference is attributed to the extra amino acids in the full-length enzyme. These observations may be relevant in the design of drugs as inhibitors of HO and other membrane proteins.

Item ID: 15636
Item Type: Article (Research - C1)
ISSN: 1205-7541
Keywords: heme oxygenase, recombinant truncated human heme oxygenase, inhibitor, selectivity, microsomal
Date Deposited: 05 Apr 2011 04:54
FoR Codes: 07 AGRICULTURAL AND VETERINARY SCIENCES > 0707 Veterinary Sciences > 070710 Veterinary Pharmacology @ 50%
06 BIOLOGICAL SCIENCES > 0699 Other Biological Sciences > 069999 Biological Sciences not elsewhere classified @ 50%
SEO Codes: 92 HEALTH > 9201 Clinical Health (Organs, Diseases and Abnormal Conditions) > 920199 Clinical Health (Organs, Diseases and Abnormal Conditions) not elsewhere classified @ 100%
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