By Allen B. Reitz
Quantity five of Advances in Medicinal Chemistry comprises 4 interesting and distinctive bills of the shut interface among artificial chemistry, structure-activity relationships, biochemistry, and pharmacology. In bankruptcy 1, there's a accomplished survey of the immunophilin zone particularly focussing on neuroregenerative purposes within the significant fearful method. In bankruptcy 2, there's an outline of the improvement 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 power remedy for the remedy of schizophrenia. In bankruptcy four, there's a precis of the profitable software during which effective non-peptide inhibitors of HIV protease from the AIDS virus have been constructed.
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Additional info for Advances in Medicinal Chemistry, Vol. 5
Neuroimmunophilins and Nervous System Effects of Immunosuppressant Drugs Soon after the discovery of FKBP12, Northern blot analysis of mRNA demonstrated the presence of the immunophilin throughout the body, including the brain. 237 When rat brain homogenates were monitored for [3H]FK506 binding, Snyder's group found that FKBP12 levels in the brain were much higher than in immune tissues, nearly 50-fold greater. 238 This discovery was made just at the time of the literature reports on calcineurin as the target of the FKBP12-FK506 and cyclophilin-CsA 50 GREGORY S.
An overlay of the binding site residues and immunosuppressant, FK506, show nearly superimposable images. As discussed above, mutagenesis studies identified Gly-89 and Ile-90 in FKBP12 (Pro-97 and Lys-98 in FKBP13) as key residues for CN binding. Lys-98 in FKBP13 projects further into the hydrophobic binding cavity, thus disrupting the pocket. In addition, Arg-42 in FKBP12 is substituted by a Gln-50 in FKBP13. 47 This difference breaks the salt triad interaction found between Tyr-26, Asp- 37, and Arg-42 in FKB P 12 (Tyr- 34, Asp-45, and Asn- 50 in FKB P 13, respectively).
FKBP52 The solution structure of the N-terminal domain of FKBP52, which contains the first FKBP domain, has recently been solved using homoand heteronuclear multidimensional NMR. 2~176 The N-terminal domain has 49% sequence identity with hFKBP12 and contains completely conserved binding pocket residues. The overall structure is very similar 34 GREGORY S. HAMILTON and CHRISTINE THOMAS to hFKBP12 and consists of six antiparallel I]-sheets and one hydrophobic tx-helix (see Figure 5). The uncommon loop crossing found in FKBP12 is present also in FKBP52.
Advances in Medicinal Chemistry, Vol. 5 by Allen B. Reitz