Angiotension converting enzyme

Fig. 10. Pharmacophores for angiotension-converting enzyme. Distances in nm. (a) The stmcture of a semirigid inhibitor and distances between essential atoms from which one pharmacophore was derived (79). (b) In another pharmacophore, atom 1 is a potential zinc ligand (sulfhydryl or carboxylate oxygen), atom 2 is a neutral hydrogen bond acceptor, atom 3 is an anion (deprotonated sulfur or charged oxygen), atom 4 indicates the direction of a hydrogen bond to atom two, and atom 5 is the central atom of a carboxylate, sulfate, or phosphate of which atom 3 is an oxygen, or atom 5 is an unsaturated carbon when atom 3 is a deprotonated sulfur. The angle 1- -2- -3- -4 is —135 to —180° or 135 to 180°, and 1- -2- -3- -5 is —90 to 90°.

SH Kubo, RJ Cody. Clinical pharmacokinetics of the angiotension converting enzyme inhibitors. Clin Pharmacokinet 10 377-391, 1985. 

Another type of antihypertensive agent is a calcium channel blocker. This was discussed under amlodipine (no. 6) in Section 3.6. Finally, angiotension-converting enzyme (ACE) inhibitors are used in severe... 

To synthesize short peptides, at high volume and low cost, chemist prefer to use the N carboxyanhydrides (NCA) of aminoacids, protected if necessary on the side chain reactive functional groups. This is the case for intermediates of angiotensing converting enzyme peptides such as L-alanyl-L-proline and Ns-(TFA)-L-lysyl-L-proline. 

The synthesis of microginin, an angiotension converting enzyme inhibitory pentapeptide, involves the multiple steps wherein DEPC is used as coupling agent.73 A key component 193 required for the synthesis of microginin is obtained from N-protected amino acid (191) and amine 192. 

Angiotension Converting Enzyme (ACE) (EC 3.4.15.1). (Kinase II dipeptidylpeptidase A). This cleaves the Gly -Phe amide bond of the pentapeptides releasing the fragment Tyr-Gly-Gly. 

Shihabi, Z.K. Analysis of angiotension-converting enzyme by capillary electrophoresis. J. Chromatogr. A, 853,185,1999. 

In CE, catalytic activity can be measured in several ways (1) incubation in the capillary, (2) online, postcapillary reaction, and (3) incubation outside the capillary. If a long incubation step is needed then it is more convenient to perform the incubation outside the instrument. Proteolytic enzymes with low activity are well suited for analysis by CE in this manner. Several enzymes have been analyzed by CE such as chloramphenicol acetyl transferase, glutathione peroxidase, ornithine transcarbamylase, angiotension converting enzyme, and Cathepsin D (Figure 4). 

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