Homodimer symmetric nature

As had been predicted prior to the determination of the X-ray structure, the proteinase assembles its catalytic machinery using a C2 symmetric homodimer (as opposed to a monomer in renin). The symmetrical nature of the enzyme suggested that C2 symmetric inhibitors might be effective. The X-ray structure also revealed the presence of an ordered water molecule bound to two of the carbonyl groups of the inhibitor. Displacement of such a water molecule with an inhibitor should, theoretically, lead to greatly enhanced activity. This theory was exploited with a class of cyclic inhibitors that mimicked the interactions of the water molecule with functionality within the inhibitor leading to highly potent and compact inhibitors, e.g., XM-323 (see Scheme 9) (15). 

HIV reverse transcriptase (HIV RT) and protease (HIV PR) are essential for the matnration and prodnction of infectious viral particles. A combined inhibition of HIV RT and HIV PR is capable of redncing the viral load in blood patients. These enzymes, which exist respectively as an heterodimer and an homodimer for HIV RT and HIV PR, are well characterized more than 170 strnctnres of HIV PR and its complexes with varions inhibitors have been solved by protein crystallography techniqnes." " Thns, a dipalmi-toylated derivative of 2,7-naphthalene disulfonic acid demonstrated a micromolar activity for both HFV-l and HIV-2 RT (Figure Symmetrical nature of HIV PR was... 

Strong, R. K. (2002). Asymmetric ligand recognition by the activating natural killer cell receptor NKG2D, a symmetric homodimer. Mol. Immunol. 38, 1029-1037. 

Strong, R. K. (2002). Asymmetric ligand recognition by the activating natural killer cell receptor NKG2D, a symmetric homodimer. Mol. Immunol. 38, 1029-1037. Sugamura, K., Asao, H., Kondo, M., Tanaka, N., Ishii, N., Nakamura, M., and Takeshita,... 

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