Advances in Medicinal Chemistry, Vol. 5 by Allen B. Reitz

By Allen B. Reitz

Quantity five of Advances in Medicinal Chemistry comprises 4 interesting and distinctive money owed of the shut interface among artificial chemistry, structure-activity relationships, biochemistry, and pharmacology. In bankruptcy 1, there's a entire survey of the immunophilin quarter in particular focussing on neuroregenerative purposes within the valuable frightened approach. In bankruptcy 2, there's an outline of the advance of a powerful analgesic compound that works through modulation of neuronal nicotinic acetylcholine receptors. In bankruptcy three, there's a description of dopamine D-2 autoreceptor partial agonists as power remedy for the therapy of schizophrenia. In bankruptcy four, there's a precis of the profitable application during which effective non-peptide inhibitors of HIV protease from the AIDS virus have been constructed.

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Other changes (D37V, TM F99W 142) abolished both rotamase and ligand binding activities. 192'193 Arg-42 and Gly-89/Ile-90 are part of the 40s and 80s flexible loops, respectively, surrounding the binding pocket. The recently solved X-ray crystal structures of the FKBP12-FK506calcineurin ternary complex provide a detailed picture of these interactions. 195'196 Figure 7 depicts the F K B P 1 2 - F K 5 0 6 complex in space-filling representation, with the key calcineurin-binding residues of FKBP highlighted in color.

195'196 Figure 7 depicts the F K B P 1 2 - F K 5 0 6 complex in space-filling representation, with the key calcineurin-binding residues of FKBP highlighted in color. The C15-C21 effector region of FK506 is a complementary surface to a cleft in calcineurin; the allyl group of the immunosuppressant penetrates deeply into a pocket on the surface of the phosphatase. The regions ofFKBP12 noted in Figure 7 (Asp-37-Asp-41, Arg-42-Phe-46, and His-87-Ile-90) also contact calcineurin. The FKBP12-FK506 complex does not bind at the enzymatic active site of calcineurin, but lies about 10 A distant.

Almost exactly superimposable spectra suggest that the binding and conformation of the two complexes are closely similar. Due to the different structural classes of the ligands, one might expect to see significant differences in the conformation of the complexes. Therefore, this overlay suggests very similar effects on the conformation of the complex upon binding and complete three-dimensional structure determination would give insight into the exact structural models of the complex. The last panel of Figure 13 shows all three GPI ligands at the saturation point overlaid.

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