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 bills of the shut interface among man made chemistry, structure-activity relationships, biochemistry, and pharmacology. In bankruptcy 1, there's a accomplished survey of the immunophilin zone in particular focussing on neuroregenerative functions within the significant worried method. 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 strength treatment for the therapy of schizophrenia. In bankruptcy four, there's a precis of the profitable application within which effective non-peptide inhibitors of HIV protease from the AIDS virus have been built.

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The proline-binding pocket is formed by Trp-59 of the c~-helix and the side chains of Tyr-26, Phe-46, Phe-99, Val-55, and Ile-56, and is occupied by the pipecolinyl ring of FK506. The adjacent site, occupied by the pyranose ring, is a cavity formed by the sidechains of Ile-91, His-87, Phe-36, Tyr-82, and Asp-37. Hydrogen bonds are formed between the ester carbonyl of FK506 and the back- 28 GREGORY S. HAMILTON and CHRISTINE THOMAS Figure 6. FK506-FKBP12 interactions, from the X-ray structure. (A) FK506 (red) in binding pocket surrounded by 40s, 50s and 80s loops of FKBP12.

FKBP12 expression correlated with mitosis in proliferating cells but not with DNA synthesis. The results suggest that FKBP12 may be important in cardiac development, and may function by affecting cellular Ca +2 levels. A recent report on FKBP12 knockout mice is consistent with this. 166 Shou et al. reported that mutant mice deficient in FKBP12 had normal skeletal muscle but exhibited severe cardiac defects, including severe dilated cardiomyopathy and ventricular septal defects. In situ hybridization experiments revealed that FKBP52 mRNA is overexpressed in rabbit and rat testes, relative to other organs.

Similar residues which shift due to ligand binding enable identification of those residues which are involved in the binding pocket or neighboring regions affected upon complex formation. In Figure 13, titration spectra of FKBP12 with FK506, GPI 1046, and rapamycin show significant shifts in similar peak resonances. The numbered residues are those which are involved in the ligand-binding pocket or surrounding loop regions, or those which exhibit sizeable shift changes. Both FK506 44 GREGORY S. HAMILTON and CHRISTINE THOMAS and rapamycin bind in similar fashion as previously discussed.

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