Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0393754 (HSA)
2,996 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Boron neutron capture therapy (BNCT) is an experimental, binary treatment for brain cancer which requires as the first step that tumor tissue is targeted with a boron-10 containing compound. Subsequent exposure to a thermal neutron flux results in destructive, short range nuclear reaction within 10 microm of the boron compound. The success of the therapy requires than the BNCT agents be well localized in tumor, rather than healthy tissue. The MEPHISTO spectromicroscope, which performs microchemical analysis by x-ray absorption near edge structure (XANES) spectroscopy from microscopic areas, has been used to study the distribution of trace quantities of boron in human brain cancer tissues surgically removed from patients first administered with the compound Na2B12H11SH (BSH). The interpretation of XANES spectra is complicated by interference from physiologically present sulfur and phosphorus, which contribute structure in the same energy range as boron. We addressed this problem with the present extensive set of spectra from S, B, and P in relevant compounds. We demonstrate that a linear combination of sulfate, phosphate and BSH XANES can be used to reproduce the spectra acquired on boron-treated human brain tumor tissues. We analyzed human glioblastoma tissue from two patients administered and one not administered with BSH. As well as weak signals attributed to BSH, x-ray absorption spectra acquired from tissue samples detected boron in a reduced chemical state with respect to boron in BSH. This chemical state was characterized by a sharp absorption peak at 188.3 eV. Complementary studies on BSH reference samples were not able to reproduce this chemical state of boron, indicating that it is not an artifact produced during sample preparation or x-ray exposure. These data demonstrate that the chemical state of BSH may be altered by in vivo metabolism.
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PMID:Spectromicroscopy of boron in human glioblastomas following administration of Na2B12H11SH. 1108 67

Synthesis and evaluation of a new class of photochemically activated heterobifunctional chelating agents for protein modification is described. Selective functionalization of perfluoroaryl azides by versatile phosphorus hydrazide ligating systems 2 and 3 for the complexation of transition metals and analogous radiometals form the basis for these new agents. The utility of the photogenerated precursors from these bifunctional agents to form covalent attachments is demonstrated through examination of C-H bond insertion on cyclohexane. Representative amide-coupled phosphorus hydrazides 5 and 6 provide >78% insertion of the probe into unactivated C-H bonds of cyclohexane with short photolysis times. Photoconjugation of the photoactivable heterobifunctional chelating agent 6 and its Pd metalated analog 7 with HSA is also evaluated. The uncomplexed chelate appears to add to HSA with high efficiency, consistent with the observed 82% bond insertion into model solvents. Covalent attachment of 7, evaluated through the use of (109)Pd, was estimated to be between 49% and 74% with the uncertainty arising because of prephotolysis association of the (109)Pd complex with HSA. The application of in situ (19)F NMR to distinguish between bond insertion and noninsertion processes is demonstrated. These results suggest that functionalized perfluoroaryl azido phosphorus hydrazides may find utility as heterobifunctional photolabeling agents for attaching radionuclides to proteins and antibodies.
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PMID:Chemistry of Bifunctional Photoprobes. 1. Perfluoroaryl Azido Functionalized Phosphorus Hydrazides as Novel Photoreactive Heterobifunctional Chelating Agents: High Efficiency Nitrene Insertion on Model Solvents and Proteins. 1167 42

Three novel phosphorus-containing analogues of H(5)DTPA (DTPA = diethylenetriaminepentaacetate) were synthesised (H6L1, H5L2, H5L3). These compounds have a -CH2-P(O)(OH)-R function (R = OH, Ph, CH2NBn2) attached to the central nitrogen atom of the diethylenetriamine backbone. An NMR study reveals that these ligands bind to lanthanide(III) ions in an octadentate fashion through the three nitrogen atoms, a P-O oxygen atom and four carboxylate oxygen atoms. The complexed ligand occurs in several enantiomeric forms due to the chirality of the central nitrogen atom and the phosphorus atom upon coordination. All lanthanide complexes studied have one coordinated water molecule. The residence times (tau(M)298) of the coordinated water molecules in the gadolinium(III) complexes of H6L1 and H5L2 are 88 and 92 ns, respectively, which are close to the optimum. This is particularly important upon covalent and noncovalent attachment of these Gd(3+) chelates to polymers. The relaxivity of the complexes studied is further enhanced by the presence of at least two water molecules in the second coordination sphere of the Gd(3+) ion, which are probably bound to the phosphonate/phosphinate moiety by hydrogen bonds. The complex [Gd(L3)(H2O)](2-) shows strong binding ability to HSA, and the adduct has a relaxivity comparable to MS-325 (40 s(-1) mM(-1) at 40 MHz, 37 degrees C) even though it has a less favourable tau(M) value (685 ns). Transmetallation experiments with Zn(2+) indicate that the complexes have a kinetic stability that is comparable to-or better than-those of [Gd(dtpa)(H2O)](2-) and [Gd(dtpa-bma)(H2O)].
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PMID:Lanthanide(III) complexes of novel mixed carboxylic-phosphorus acid derivatives of diethylenetriamine: a step towards more efficient MRI contrast agents. 1467 62

The (low loaded) biological nutrient removing activated sludge process is the generally accepted and applied municipal wastewater treatment method in the Netherlands. The hydraulical and biological flexibility, robustness and cost efficiency of the process for advanced removal of nutrients like nitrogen and phosphorus without (too much) chemicals results in a wide application of the activated sludge process within Dutch waterboards. Presumably, wastewater treatment plants will have to contribute to the improvement of the quality of the receiving surface waters by producing cleaner effluent. In this perspective, the Dutch research organisation STOWA initiated a research project entitled "The Boundaries of the Activated Sludge Process" to investigate the possibilities and limitations of activated sludge processes to improve the effluent quality. It is concluded that the activated sludge process as applied and operated at WWTP's in the Netherlands has the potential to perform even better than the current effluent discharge standards (10 mg Ntotal/l and 1 mg Ptotal/l). Reaching the B-quality effluent (<5mg Ntotal/l and <0.3 mg Ptotal/l) will be possible at almost all WWTPs without major adjustments under the conditions that: the sludge load is below 0.06 kg BOD/kg TSS.d the internal recirculation is above 20 the BOD/N ratio of the influent is above 3. Complying with the A-quality effluent (<2.2 Ntotal/l and <0.15 mg Ptotal/l) seems to be difficult (but not impossible) and requires more attention and insight into the activated sludge process. Optimisation measures to reach the A-quality effluent are more thorough and are mostly only achievable by additional construction works (addition of activated sludge volume, increasing recirculation capacity, etc.). It is furthermore concluded that the static HSA-results are comparable to the dynamic ASM-results. So, for fast determinations of the limits of technology of different activated sludge processes static modelling seems to by sufficient.
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PMID:The limits and ultimate possibilities of technology of the activated sludge process. 1900 24