Structural Basis

Knowledge of the chemistry of local anaesthetics also helps in finding possible substitutes, e.g., the replacement of an ester by an amide agent which neither cross-reacts, nor is likely to cause allergy by itself. Many other compounds have local anaesthetic properties, and may be thought of as potential alternatives, e.g., certain phenothiazine antihistamines and propranolol (the jS-adrenoceptor blocker). [Pg.269]

However, these compounds are either irritant, or their side effects preclude their use. [Pg.270]

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We saw in Chapter 12 that aromaticity reveals itself in various ways Qualitatively aro matic compounds are more stable and less reactive than alkenes Quantitatively their heats of hydrogenation are smaller than expected Theory especially Huckels rule furnishes a structural basis for aromaticity Now lets examine some novel fea tures of their NMR spectra... [Pg.530]

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By comparing the crystal structures of these complexes with a further complex of the 434 repressor DNA-binding domain and a synthetic DNA containing the operator region OR3, Harrison has been able to resolve at least in part the structural basis for the differential binding affinity of 434 Cro and repressor to the different 434 operator regions. [Pg.137]

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The serine proteinases all have the same substrate, namely, polypeptide chains of proteins. However, different members of the family preferentially cleave polypeptide chains at sites adjacent to different amino acid residues. The structural basis for this preference lies in the side chains that line the substrate specificity pocket in the different enzymes. [Pg.212]

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The pA of 1,3-dithiane is 36.5 (Cs" ion pair in THF). The value for 2-phenyl-1,3-dithiane is 30.5. There are several factors which can contribute to the anion-stabilizing effect of sulfur substituents. Bond dipole effects contribute but carmot be the dominant factor because oxygen substituents do not have a comparable stabilizing effect. Polarizability of sulfur can also stabilize the carbanion. Delocalization can be described as involving 3d orbitals on sulfur or hyperconjugation with the a orbital of the C—S bond. MO calculations favor the latter interpretation. An experimental study of the rates of deprotonation of phenylthionitromethane indicates that sulfur polarizability is a major factor. Whatever the structural basis is, there is no question that thio substituents enhance... [Pg.423]

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Structural basis of protein kinase C activation by heterocyclic tumor promoters 98ACR163. [Pg.238]

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Die cytosolic loop between TMs 13 and 14 (KCO I) and TMs 16-17 (KCO II) were identified as critical for KatpCO binding to SURs (Fig. 4d). T1286 and Ml 290 appeared to be particularly important. Close local association of sulfonylurea and KCO binding regions might represent the structural basis for negative allosteric coupling of the sites. [Pg.236]

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It is not clear why some organisms have two 14-3-3 isoforms while others have up to 12. Binding 14-3-3 inhibits the plant enzyme nitrate reductase and there appears to be no selectivity between plant 14-3-3 isoforms in fact yeast and human isoforms appear to work equally as well in vitro. The best example where selectivity has been demonstrated is human 14-3-3o. 14-3-3o Preferential homodimerizes with itself and crystallization revealed a structural basis for this isoform s dimerization properties as well as for its specific selectivity for target binding proteins. Here partner specificity is the result of amino acid differences outside of the phosphopeptide-binding cleft. [Pg.1027]

Nissen P, Hansen J, Ban N et al (2000) The structural basis of ribosome activity in peptide bond synthesis. Science 289 920-930... [Pg.1090]

Brodersen DE, Clemons WM, Carter AP et al (2000) The structural basis for the action of the antibiotics tetracycline, pactamycin and hygromycin B on the 30S ribosomal subunit. Cell 103 1143-1154... [Pg.1090]

Schlunzen F, Zarivach R, Harms J et al (2001) Structural basis for the interaction of antibiotics with the peptidyl transferase centre in eubacteria. Nature 413 814-821... [Pg.1090]

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