Enzyme Inhibitory Activities

More recently, screening efforts at Novartis have identified a hydroxamic acid containing a benzothiazinone ring system (32) [108]. This inhibitor is very potent versus S. aureus Ni -PDF (<5nM) and displays good selectivity versus matrix metalloprotease-2 (MMP-2) and MMP-13. Unfortunately (32), and all other analogues prepared, such as carbon isosteres (33), sulfones (34), N-substituted analogues (35) and N-formyl-N-hydroxylamines (36), lacked appreciable antibacterial activity in spite of their potent enzyme inhibitory activity. Further studies performed by Novartis suggest that these molecules are unable to penetrate the outer cell membrane of E. coli, and may bind to the cell membrane of S. aureus [108]. 

Microtiter plates HRP/H202/luminol AP/dioxetanes Firefly luciferin/luciferase Bacterial luciferin/luciferase Detection of enzymes and metabolites by direct or coupled enzyme reactions Determination of antioxidant and enzyme inhibitory activities Immunoassay... 

Nakamura E, Tokuyama H, Yamago S, Shiraki T, Sugiura Y (1996) Biological activity of water-Soluble fullerenes. Structural dependence of DNA cleavage, cytotoxicity, and enzyme inhibitory activities including HIV-Protease inhibition. Bull. Chem. Soc. Jpn. 69 2143-2151. 

M., Cavrini, V. SAR of 9-amino-l,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMEA of tacrine analogues./. Med. Chem. 2000, 43, 2007-2018. 

Hou, W. C., Chen, H. J., and Lin, Y. H. (2003). Antioxidant peptides with angiotensin converting enzyme inhibitory activities and applications for angiotensin converting enzyme purification. ]. Agric. Food Chem. 51,1706-1709. 

Cheung, I. W. Y. and Li-Chan, E. C. Y. (2010). Angiotensin-I-converting enzyme inhibitory activity and bitterness of enzymatically-produced hydrolysates of shrimp (Pandalopsis dispar) processing byproducts investigated by Taguchi design. Food Chem. 122,1003-1012. 

Okamoto, A., Hanagata, H, Matsumoto, E., Kawamura, Y., Koizumi, Y., and Yanagida, F. (1995a). Angiotensin I converting enzyme inhibitory activities of various fermented foods. Biosci. Biotech. Biochem. 59,1147-1149. 

He, H. L., Chen, X. L., Sun, C. Y., Zhang, Y. Z., and Zhou, . C. (2007). High throughput and rapid screening of marine protein hydrolysates enriched in peptides with angiotensin-I-converting enzyme inhibitory activity by capillary electrophoresis. Bioresour. Technol. 98, 3499-3505. 

Kamath, V., Niketh, S., Chandrashekar, A., and Rajini, P. S. (2007). Chymotryptic hydrolysates of a-kafirin, the storage protein of sorghum (Sorghum bicolor) exhibited angiotensin converting enzyme inhibitory activity. Food Chem. 100, 306-311. 

Otani, L., Ninomiya, T., Murakami, M., Osajima, K., Kato, H., and Murakami, T. (2009). Sardine peptide with angiotensin I-converting enzyme inhibitory activity improves glucose tolerance in stroke-prone spontaneously hypertensive rats. Biosci. Biotechnol. Biochem. 73, 2203-2209. 

Cushing s syndrome, gynecomastia, amenorrhea, and precocious puberty have been regarded as reflecting the enzyme-inhibitory activity of isoniazid, with resulting derangement of hormone metabolism in the liver. 

Mucoadhesive Polymers Exhibiting Enzyme Inhibitory Activity. 93... 

This geminal type of functionality occurs when the sugar moiety is in specific stereo orientation, and with acetamido functionality. Additionally, the basic functional group (-NHAc) may act as a binding site with receptors. Such disaccharides should be valuable tools to probe any enzyme inhibitory activity of synthesized (1 -2)-S-thiodisaccharides. 

The seeds of squash plants are rich in a family of trypsin and chymotrypsin inhibitors that are approximately 35 amino acids in size and have been extensively investigated not only for their enzyme inhibitory activity, but also because they are very stable mini-protein scaffolds with applications in protein engineering. The best studied examples are Ecballium elaterium trypsin inhibitor (EETI-II) and Cucurbita maxima trypsin inhibitor (CMTI). Both X-ray and NMR have been used to characterise their structures, which incorporate a cystine-knot motif formed by three conserved disulphide bonds.93 We will describe this motif in more detail in a later section describing the plant cyclotides. 

Mullally, M.M., Meisel, H., and FitzGerald, R.J. 1996. Synthetic peptides corresponding to (3-lactalbumin and (3-lactoglobulin sequences with angiotensin-I-converting enzyme inhibitory activity. Biol. Chem. Hoppe-Seyler 377, 259-260. 

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