HIV enzymes

HIV diagnosis is made either by a positive HIV enzyme-linked immunosorbent assay (ELISA) or rapid test (these tests may be positive as soon as 3 to 6 weeks after infection) and then confirmed by a positive confirmatory test, usually the HIV Western blot (Table 84-1). 

Source. Casidy R, Frey R. Drug Strategies to Target HIV Enzyme Kinetics and Enzyme Inhibitors, Washington University. http //wunmr.wustl.edu/EduDev/Lab I itorials/F[IV/ DrugStrategies.html [accessed May 21,2003]. 

Fusions may also be designed against which antibodies may be raised that can be used for detection. An example is the tripeptide Glu-Glu-Phe motif for the immunoaffinity of HIV enzymes which is recognized by the YLl/2 monoclonal antibody to a-tubulin (Stammers et ah, 1991). 

The synthesis of a water-soluble diphenylmethano-bridged fullerene 122 was achieved by hydrolyzing the bis (acetamide) 121 with acetic acid-aqueous hydrochloric acid and then converting it into the bis(succinamide) 122 by treatment with succinic anhydride (Scheme 4.25) [158]. Compound 122 is soluble in water at pH > 7. This is an important requirement for the investigation of the biological activity of fullerenes. Remarkably, 122 is an inhibitor for the HIV enzymes protease (HIV-P) and reverse transcriptase (HIV-RT) [159]. As suggested by molecular modeling. 

The majority of preparations in clinical phases have been found through conventional screening methods and interfere in the inhibition of either reverse transcriptase or HIV protease. The cycle of replication is shown in Figure 13.13. New programs target control and inhibition of all three HIV enzymes, such as reverse transcriptase, protease, and integrase, as well as regulator proteins such as Tat,... 

E. The HIV proteins synthesized by the host cell are produced as a long polyprotein that must be cleaved to the active HIV enzymes and structural proteins. HIV protease inhibitors bind to and inhibit the aspartic protease that hydrolyzes the polyprotein, thus preventing the assembly of infective viral particles. 

Camarasa M-J, Velazquez S, San-Felix A et al (2006) Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase a single mode of inhibition for the three HIV enzymes Antiviral Res 71 260-267... 

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