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

By Allen B. Reitz

Quantity five of Advances in Medicinal Chemistry includes 4 fascinating and particular debts of the shut interface among man made chemistry, structure-activity relationships, biochemistry, and pharmacology. In bankruptcy 1, there's a entire survey of the immunophilin zone particularly focussing on neuroregenerative functions within the valuable apprehensive method. In bankruptcy 2, there's an outline of the advance of a effective 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 capability remedy for the therapy of schizophrenia. In bankruptcy four, there's a precis of the profitable software within which powerful non-peptide inhibitors of HIV protease from the AIDS virus have been constructed.

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B) GPI 1046 titration. (C) Rapamycin titration. (D) Overlay of saturation endpoints for FK506, GPI 1046, and rapamycin. (E) GPI 1456 and 1495 overlay. (F) Overlay of all three nonimmunosuppressive ligands at saturation point. Immunophilins Ligand:Protein 45 ratios b l a c k - 0:1" b l u e - 1:2; red - 2:1- g r e e n - 3:1; p u r p l e - >5:1 Figure 13. Continued. 46 GREGORY S. HAMILTON and CHRISTINE THOMAS Figure 13. Continued. Immunophilins 47 Figure13. Continued. Figure 13d is an overlay of the saturation point of GPI ligands, 1495 and 1456, urea, and sulfonamide ligands, respectively.

238'239The regional distribution of FKBP12 mapped closely to that of calcineurin, a finding immediately suggestive of a physiological association. Cyclophilin's distribution also paralleled that of calcineurin extensively, although it was found in some regions lacking calcineurin. Particularly high levels of immunophilins are found in the hippocampus, dopaminergic neurons of the nigrostriatal pathway, and cerebellar granule cells. The distributions of FKBP12 and CyPA do not entirely overlap: CyPA is enriched in the brain stem and largely absent from the caudate nucleus, while the opposite is true of both FKBP12 and calcineurin.

78 Immunophilins 25 Figure 4. X-ray structures of cyclosporin A bound to cyclophilin A (left) and FK506 bound to FKBP12 (right). The proteins are depicted in ribbon format, color-coded by secondary structure, and the ligands are shown in space-filling representation. A. FKBPs The structures of FKBP12 (in complex with FK506), FKBP25 (in complex with rapamycin), and FKBP52 (the N-terminal domain) are on file at the Brookhaven Protein Data Bank. The protein structures and rotamase domains of these three FKBPs, s a n s ligands, are depicted in Figure 5 for comparison and reference in the following discussion of the FKBPs.

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