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Synthesis of 5-deazaflavin derivatives and their activation of p53 in cells.
It is demonstrated that the nitro group present in all three of the original lead compounds [1-3 (HL198C-E)] is not essential for observation of this biological activity of 5-deazaflavin derivatives. Expand
Bacterial diaminopimelate metabolism as a target for antibiotic design.
The search for antibiotic compounds has recently taken on a new urgency. The world-wide increase in bacterial resistance to current antibiotics impacts both hospital and community based programs forExpand
Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo.
Ex vivo biodistribution studies of [(123)I]5 in mice bearing subcutaneous glioblastoma xenografts revealed that the tracer had the ability to be retained in tumor tissue and bind to PARP-1 with specificity, and these findings support further investigations of [( 123)I?]5 as a noninvasive PARp-1 SPECT imaging agent. Expand
For the record: The three‐dimensional structure of the ternary complex of Corynebacterium glutamicum diaminopimelate dehydrogenase‐NADPH‐L‐2‐amino‐6‐methylene‐pimelate
The structure of the ternary complex reported here provides a structural rationale for the nature and potency of the inhibition exhibited by the unsaturated l‐2‐amino‐6‐methylene‐pimelate against the dehydrogenase. Expand
123I‐NKJ64: A novel single photon emission computed tomography radiotracer for imaging the noradrenaline transporter in brain
The data indicate that further evaluation of 123I‐NKJ64 in nonhuman primates is warranted in order to determine its utility as a SPECT radiotracer for imaging the NAT in brain. Expand
Structural insights into stereochemical inversion by diaminopimelate epimerase: an antibacterial drug target.
Crystal structures of diaminopimelate (DAP) epimerase from Haemophilus influenzae with two different isomers of the irreversible inhibitor and substrate mimic aziridino-DAP permit a detailed description of this pyridoxal 5'-phosphate-independent amino acid racemase active site and delineate the electrostatic interactions that control the exquisite substrate selectivity of DAP epimerases. Expand
The stereoselective synthesis of aziridine analogues of diaminopimelic acid (DAP) and their interaction with dap epimerase.
Aziridine analogues of diaminopimelic acid (DAP) have been prepared stereoselectively for the first time and evaluated as inhibitors of DAP epimerase and are consistent with the two base mechanism proposed for the epimerization of ll-D AP and meso-DAP by DAPEpimerase. Expand