Advances in Medicinal Chemistry, Vol. 5 - download pdf or read online

By Allen B. Reitz

ISBN-10: 0762305932

ISBN-13: 9780762305933

Quantity five of Advances in Medicinal Chemistry comprises 4 fascinating and distinctive debts 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 relevant fearful process. In bankruptcy 2, there's an summary of the improvement 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 constructed.

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158Remarkably, the ECs0 for FK506 to promote neurite outgrowth in the presence of a submaximal (1 ng/mL) concentration of NGF was found to be 500 picomolar. In the absence of exogenous NGF, FK506 was ineffective in PC-12 cells. This result suggested that the compound worked by enhancing the sensitivity of the PC- 12 cells to the trophic factor. Rapamycin and cyclosporin A produced similar results in PC-12 cells. The result with rapamycin was extremely significant. In the NOS-related studies described above, rapamycin consistently antagonized the effects of FK506, consistent with a calcineurin-mediated mechanism.

B o n e ~ N H of Ile-56, and between the side chain---OH of Tyr-82 and the amide carbonyl of the ketoamide moiety. The cyclohexylpropyl ester chain of FK506 lies in a shallow hydrophobic groove on the protein surface. Figure 6 depicts the solvent-accessible protein surface of these two subsites of the FKBP domain. In addition to FK506, the structures of a number of other macrocyclic and nonmacrocyclic ligands bound to FKBP12 have been solved by X-ray or NMR. These include the C-21 ethyl analogue of FK506, ascomycin, ~85rapamycin, 182'186the nonimmunosuppressive analogue L685,818 (18-hydroxyascomycin), 187 and several small molecule inhibitors.

These studies provide a fascinating example of the subtle interplay between local protein conformation and ligand conformation as the two partners adjust to find the most favorable complex. Molecular dynamics simulations of FK506 binding to native FKBP12 suggest the dynamical interplay between protein and ligand during the binding process. 232Ivery and Weiler's computational modeling studies suggested that initial binding of the pipecolate region of FK506 and the hydrophobic pocket of FKBP12 is followed by a hingelike movement of the 80s loop to close over the pyranose region of the ligand.

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

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