Nicotinamide phosphoribosyl-transferases (NAMPT) are enzymes that play a role in targeting cancer metabolism, while beta lactamases are involved in bacterial resistance to beta-lactam antibiotics. Many protein inhibitors exhibit such property which is often correlated with their cellular potency. In order to understand such a phenomenon, the present article conducts an analysis of the dynamic b...

We report the discovery of antibacterial leads, keto- and diketo-acids, targeting two prenyl transferases: undecaprenyl diphosphate synthase (UPPS) and dehydrosqualene synthase (CrtM). The leads were suggested by the observation that keto- and diketo-acids bind to the active site Mg(2+)/Asp domain in HIV-1 integrase, and similar domains are present in prenyl transferases. We report the x-ray cr...

The article reviews the state of knowledge on the biosynthesis of cardenolides in the genus Digitalis. It summarizes studies with labelled and unlabelled precursors leading to the formulation of the putative cardenolide pathway. Alternative pathways of cardenolide biosynthesis are discussed as well. Special emphasis is laid on enzymes involved in either pregnane metabolism or the modification o...

The purpose of this report is to review the relationship between genetic polymorphisms involved in carcinogen metabolism, alcohol metabolism and cell-cycle control with the risk of head and neck cancer. The review was performed on available studies on genetic polymorphisms and head and neck cancer (HNC) published in PubMed up to September 2011. 246 primary articles and 7 meta-analyses were publ...

Mantle, T. J., Mannervik, B. and Hayes, J. D., eds.), pp. 2 1 1-22 1, CRC Press, Boca Raton, FL Andersson, C., Mosialou, E., Weinander, R., Hebert, H. and Morgenstern, R. (1993) in Structure and Function of Glutathione Transferases (Tew, K. D., Pickett, C. B.. Mantle, T. J., Mannervik, B. and Hayes, J. D., eds.), pp. 109-1 16, CRC Press, Boca Raton, FL Nicholson, D. W (1993) in Structure and Fu...

In the title compound, C14H12BrN, the tricyclic ring system is essentially planar (r.m.s. deviation 0.026 Å). The carbon atoms of the ethyl group deviate from the mean plane by 0.148 (9) (CH2) and 1.59 (1) Å (CH3). In the crystal, H⋯π contacts [2.698-2.898 Å] shorter than the van der Waals contact distance of 3.70 Å are observed. A scalable to gram quantities selective synthesis of mono-bromine...

The present invention provides a process for the synthesis of an α,β-unsaturated ester from a mono-olefinester using Fe(CO).sub.5.

A Pseudomonas sp. rapidly metabolized several nonchlorinated analogues of DDT, with the exception of 2,2-diphenylethanol, as the sole carbon source. Several of the mono-p-chloro-substituted diphenyl analogues were also metabolized as the sole carbon source by the bacterium. The resulting chlorinated aromatic acid metabolites were not further metabolized. The isolate was unable to metabolize p,p...

The structures of the compounds 1,2-bis(diphenylphosphino)benzene, C(30)H(24)P(2), [2-(diphenylphosphino)phenyl]methyldiphenylphosphonium iodide, C(31)H(27)P(2)(+).I(-), and [2-(dimethylphosphino)phenyl]trimethylphosphonium iodide, C(11)H(19)P(2)(+).I(-), show that quaternization only occurs at one P centre and results in significantly shorter P-C bonds and larger C-P-C angles, consistent with ...

The S → N acylation rates of thioester functionalized coumarins on heptakis-[6-deoxy-6-(2-aminoethylsulfanyl)]-β-cyclodextrin were measured. A high yield of mono-acylation was achieved with products that form self-inclusion compounds. The differential fluorescence response of the functionalized cyclodextrins upon binding biomacromolecules shows the potential of the constructs as probes.