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Homodimer and Symmetrical Ligands

Dimerization of a biologically active molecule represents an alternative approach in the optimization process of a lead compound. Generally, the duplication of the pharmacophore leads to an equivalent or more active derivative which exhibits different selectivity profile and pharmacokinetic properties. Enzyme inhibition will be improved when using homodimer inhibitors. Antagonists and agonists of specific receptors could be transformed respectively into agonists and antagonists of another receptor subtype. Several examples will be reported and discussed below. [Pg.383]


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,... [Pg.145]


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Homodimer

Homodimers

Ligands symmetric

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