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1
Novel combretastatin A-4 derivative XN0502 induces cell cycle arrest and apoptosis in A549 cells.
2010-03-30

Combretastatin A-4 (CA-4) is a tubulin-binding compound currently in phase II trial as a tumor vascular-targeting agent. The present study evaluates the anti-tumor activities and establishes the mechanism of the action of 4-(4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-pyrazol-3-amine(XN0502), a novel synthesized CA-4 analogue, in an effort towards ...

PubMed

2
Nature � Macmillan Publishers Ltd 1998 8

. They include a derivative of the antimalarial drug qinghaosu, the Alzheimer's drug huperzine A4 , and the anti

E-print Network

3
Synthesis of novel 26-substituted milbemycin A4 derivatives and their acaricidal activities.
2004-07-01

A series of novel 26-substituted milbemycin A4 derivatives was synthesized from 5-O-t-butyldimethylsilyl-26-hydroxymilbemycin A4 prepared by selenium dioxide oxidation of 5-O-t-butyldimethylsilyl-milbemycin A4. Their acaricidal activities were assessed ...

PubMed

4
Search for Singlet Oxygen in the Decomposition of Hydrogen ...
1985-03-26

... and BA; the derivatives of elements of groups 3A, 4A, 5A, and 6A and D0 configuration (except niobium); the oxides of actinides and lanthanides ...

DTIC Science & Technology

5
S100A4 Regulates Macrophage Chemotaxis
2010-08-01

S100A4, a member of the S100 family of Ca2+-binding proteins, is directly involved in tumor metastasis. In addition to its expression in tumor cells, S100A4 is expressed in normal cells and tissues, including fibroblasts and cells of the immune system. To examine the contribution of S100A4 to ...

PubMed Central

6
MEASUREMENT OF HYDROXYL RADICAL ACTIVITY IN A SOIL SLURRY USING THE SPIN TRAP A-(4-PYRIDYL-1-OXIDE)-N-TERT-BUTYLNITRONE

The spin trap compound a-(4-pyridyl-1-oxide)N-tert-butylnitrone (4-POBN) served as a probe to estimate the activity of Fenton-derived hydroxyl radicals (.OH) in a batch suspension comprised of silica sand and crushes goethite ore. The rate of probe disappearance was used to anal...

EPA Science Inventory

7
Milbemycin alpha17 and related compounds synthesized from milbemycin A4: synthetic procedure and acaricidal activities.
2003-10-01

Milbemycin alpha17, a 14-demethyl congener of milbemycin A4, has been reported as a natural product. In this paper, we report the successful development of a chemical derivation method to synthesize milbemycin alpha17 from milbemycin A4, as well as our use of a similar method to prepare ...

PubMed

8
New Boron-Nitrogen Analogues of Uracil Derivatives
1989-07-01

... BN bond formation. On heating of the salts 4a--4c under vacuum, the betaine 5a was obtained. ,F R\\ N- I 11 R' R II 0 0 5 a: R = RI = CH3 ...

DTIC Science & Technology

9
Compact Quasi-Axisymmetric Stellarator Reactor.
2003-01-01

We report the progress made in assessing the potential of compact, quasi-axisymmetric stellarators as powerproducing reactors. Using an aspect ratio A=4.5 configuration derived from NCSX and optimized with respect to the quasiaxisymmetry and MHD stability...

National Technical Information Service (NTIS)

10
26 CFR 1.1402(a)-4 - Rentals from real estate.
2009-04-01

...business of selling real estate to customers with a view to the gains and profits that may be derived from such sales is...example, constitutes such service; whereas the furnishing of heat and light, the cleaning of public entrances, exits,...

Code of Federal Regulations, 2010

11
Evidence that. beta. -amyloid protein in Alzheimer's disease is not derived by normal processing
1990-04-27

The {beta}-amyloid protein ({beta}/A4), derived from a larger amyloid precursor protein (APP), is the principal component of senile plaques in Alzheimer's disease. APP is an integral membrane glycoprotein and is secreted as a carboxyl-terminal truncated molecule. APP cleavage, which is a membrane-associated event, occurred at ...

Energy Citations Database

12
Synthesis of milbemycins alpha9, alpha10, alpha11, alpha12, alpha14, alpha15, alpha20, alpha21, alpha22, alpha23, alpha26, alpha27, delta(2,3),delta(4,26)-milbemycins A3, A4 from milbemycins A3, A4, and their acaricidal activities.
2002-11-01

Chemical derivation methods to prepare 26-acyloxy and 26-hydroxymilbemycins, which had been reported as natural products, milbemycins alpha9, alpha10, alpha11, alpha12, alpha14, alpha15, alpha20, alpha21, alpha22, alpha23, alpha26, alpha27 from milbemycins A3, A4 were reported. Delta(2,3),delta(4,26)-milbemycins A3, ...

PubMed

13
The Nuclear Factor-kB Pathway Regulates Cytochrome P450 3A4 Protein Stability
2008-06-01

We have previously observed that CYP3A4 protein levels are suppressed by inhibition of the proteasome in primary cultured hepatocytes. Because this result is opposite of what would be expected if CYP3A4 is degraded by the proteasome, it seems likely that there is another protein that is susceptible to proteasomal degradation that regulates CYP3A4 ...

Energy Citations Database

14
Improving T cell therapy for relapsed EBV negative Hodgkins Lymphoma by targeting upregulated MAGE-A4.
2011-09-01

Rationale: Patients with Hodgkin's Lymphoma (HL) relapsing after hematopoietic stem cell transplant (HSCT) have limited options for long-term cure. We have shown that infused cytotoxic T cells (CTL) targeting Epstein Barr virus (EBV)-derived proteins induced complete remissions in EBV+ HL patients. A limitation of this approach is that up to 70% of relapsed HL tumors are ...

PubMed

15
Immunogenicity of HLA-A1-restricted peptides derived from S100A4 (metastasin 1) in melanoma patients.
2009-01-13

S100A4 (metastasin 1) belongs to the S100 family of Ca(2+) binding proteins. While not present in most differentiated adult tissues, S100A4 is upregulated in the micromilieu of tumors. It is primarily expressed by tumor-associated macrophages, fibroblasts, and tumor endothelial cells. Due to its strong induction in ...

PubMed

16
CYP3A4-MEDIATED OXYGENATION VERSUS DEHYDROGENATION OF RALOXIFENE
2010-06-01

Raloxifene was approved in 2007 by the FDA for the chemoprevention of breast cancer in postmenopausal women at high risk for invasive breast cancer. Approval was based in part on the improved safety profile for raloxifene relative to the standard treatment of tamoxifen. However, recent studies have demonstrated the ability of raloxifene to form reactive intermediates and act as a mechanism-based ...

PubMed Central

17
N=2 supersymmetric a=4-Korteweg-de Vries hierarchy derived via Gardner's deformation of Kaup-Boussinesq equation
2010-08-15

We consider the problem of constructing Gardner's deformations for the N=2 supersymmetric a=4-Korteweg-de Vries (SKdV) equation; such deformations yield recurrence relations between the super-Hamiltonians of the hierarchy. We prove the nonexistence of supersymmetry-invariant deformations that retract to Gardner's formulas for the ...

Energy Citations Database

18
Antineoplastic agents. 379. Synthesis of phenstatin phosphate.
1998-05-01

A structure-activity relationship (SAR) study of the South African willow tree (Combretum caffrum) antineoplastic constituent combretastatin A-4 (1b) directed at maintaining the (Z)-stilbene relationship of the olefin diphenyl substituents led to synthesis of a potent cancer cell growth inhibitor designated phenstatin (3b). Initially phenstatin silyl ether ...

PubMed

19
Synthesis and biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors.
2007-12-14

A series of pyrazoline derivatives with beta-amino acyl group were synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV. Several pyrazoline derivatives exhibited submicromolar inhibitory activities against DPP-IV. X-ray co-crystal structure of initial hit compound 1h was determined. Among this series, carboxylic acid substituted ...

PubMed

20
Crystal structure of the Ca(2+)-form and Ca(2+)-binding kinetics of metastasis-associated protein, S100A4.
2008-04-22

S100A4 takes part in control of tumour cell migration and contributes to metastatic spread in in vivo models. In the active dimeric Ca(2+)-bound state it interacts with multiple intracellular targets. Conversely, oligomeric forms of S100A4 are linked with the extracellular function of this protein. We report the 1.5A X-ray crystal structure of Ca(2+)-bound ...

PubMed

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21
Construction and evaluation of drug-metabolizing cell line for bioartificial liver support system.

Focusing on drug metabolism in liver, we constructed and evaluated a drug-metabolizing bioartificial liver (BAL) support system. In a previous study, we constructed ammonia-metabolizing CHO and hepatoma-derived HepG2 cell lines by recombination of the glutamine synthetase (GS) gene. For further mimicking of liver metabolism, the human hepatoma-derived cell ...

PubMed

22
Depletion of regulatory T cells facilitates growth of established tumors: a mechanism involving the regulation of myeloid-derived suppressor cells by lipoxin A4.
2010-11-10

Regulatory T cells (Tregs) are thought to facilitate tumor development by suppressing protective antitumor immune responses. However, recent clinical and laboratory studies show that Tregs are a favorable element against cancer. In this study, we provide evidence that Tregs have both promoting and inhibiting effects on tumors, depending on the stage of tumor development. By using 0.5 mg ...

PubMed

23
Zimmermann normal products and the Wilson expansion
1974-11-01

The principal part and asymptotic form of the Wilson short distance expansion is derived in the framework of Bogoliubov-Parasiuk-Hepp-Zimmermann renormalized perturbation theory. Use is made of the Zimmermann normal product techniques with all work being performed in the scalar A4 model. The expansion of the product of four field ...

NASA Astrophysics Data System (ADS)

24
Research report Serotonin transporter and BDNF genetic variants interact to predict

Research report Serotonin transporter and BDNF genetic variants interact to predict cognitive gene, the Val66Met polymorphism of the brain-derived neurotrophic factor (BDNF) gene, and cognitive, results are consistent with previous research demonstrating biological epistasis between SLC6A4 and BDNF

E-print Network

25
Light weight concurrency in OCaml: continuations, monads, events, and friends

, thread creation and the memory footprint of a thread are compared. The trampolined style of programming in appendix B. Trampolined style (derived from continuation passing style), monadic style, event-based program in Section A.4 page 20 Trampolined style [8] is a simple way to provide application level concurrency through

E-print Network

26
Estimated Number of New Cancer Cases in 1990 By Racial / Ethnic Group

National Cancer Institute A-4 SEER Program APPENDIX 2. Estimated Number of New Cases of Selected Cancers in the United States by Racial/Ethnic Group, 1990 - Men (Estimates derived by multiplying �average annual� age-specific incidence rates for the

Cancer.gov

27
Characterization of Molecular Factors Critical to the S100A4 (A metastasis-Associated Protein) - Dependent Increase in Motility of Breast Cancer Cells.
2004-01-01

Our studies show that S100A4 localizes to lamellipodia structures in a migrating breast cancer-derived cell line and colocalizes with a known S100A4- interacting protein, heavy chain IIA (MHC-IIA) at the leading edge. We also demonstrate that S100A4 mutan...

National Technical Information Service (NTIS)

28
Antibody Specificity to Oncogene-Derived Peptides for Breast Cancer Detection.
1996-01-01

This report describes the work carried out on the specificity of four oncogenic peptide-monoclonal antibody interactions. Monoclonal antibody 172-12A4, which was raised against a peptide from v-erbB was assayed by ELISA with a set of 152 substitution anal...

National Technical Information Service (NTIS)

29
Antibody Specificity to Oncogene-Derived Peptides for Breast Cancer Detection.
1995-01-01

This report describes the initial work carried out on the specifcity of two peptide-antibody interactions. Monoclonal antibody 172-12A4, which was raised against the peptide LGSGAFGTIYKGC from V-erbB, was screened against several peptide libraries and yie...

National Technical Information Service (NTIS)

30
17 CFR 41.27 - Prohibition of dual trading in security futures products by floor brokers.
2009-04-01

...contract market or registered derivatives transaction execution facility for an account described in paragraphs (a)(4)(i)-(v) of this section. (b) Dual Trading Prohibition. (1) No floor broker shall engage in dual trading in a...

Code of Federal Regulations, 2010

31
Establishing Derived Manding for Specific Amounts with Three Children: An Attempt at Synthesizing Skinner's "Verbal Behavior" with Relational Frame Theory
2008-12-01

Participants were 2 typically developing children, aged 9 and 10 years, and 1 child, aged 4 years, with a reported severe speech delay. Five specific mand functions were trained such that participants learned to mand for the delivery or removal of tokens to the value of -2, -1, 0, +1, and +2, by presenting an arbitrary stimulus (A1, A2, A3, A4, and A5, ...

ERIC Educational Resources Information Center

32
On homotopy groups of the suspended classifying spaces.

In this paper, we determine the homotopy groups \\pi_4(\\Sigma K(A,1)) and \\pi_5(\\Sigma K(A,1)) for abelian groups A by using different facts and methods from group theory and homotopy theory: derived functors, the Carlsson simplicial construction, the Baues-Goerss spectral sequence, homotopy decompositions and the methods of algebraic K-theory. As the applications, we also ...

E-print Network

33
An Efficient Synthetic Strategy for Obtaining 4-Methoxy Carbon Isotope Labeled Combretastatin A-4 Phosphate and Other Z-Combretastatins1
2010-03-26

Human cancer and other clinical trials under development employing combretastatin A-4 phosphate (1b, CA4P) should benefit from the availability of a [11C]-labeled derivative for position emission tomography (PET). In order to obtain a suitable precursor for addition of a [11C]methyl group ...

PubMed Central

34
A new method to determine the shear coefficient of Timoshenko beam theory
2011-07-01

The frequencies ? of flexural vibrations in a uniform beam of arbitrary cross-section and length L are analysed by expanding the exact elastodynamics equations in powers of the wavenumber q=m?/L, where m is the mode number: ?2=A4q4+A6q6+?. The coefficients A4 and A6 are obtained without further assumptions; the ...

NASA Astrophysics Data System (ADS)

35
Metastasis-Inducing S100A4 and RANTES Cooperate in Promoting Tumor Progression in Mice
2010-04-28

BackgroundThe tumor microenvironment has been described as a critical milieu determining tumor growth and metastases. A pivotal role of metastasis-inducing S100A4 in the development of tumor stroma has been proven in animal models and verified in human breast cancer biopsies. Expression and release of S100A4 has been shown in various types of stroma ...

PubMed Central

36
Neural differentiation in cleavage-arrested ascidian blastomeres induced by a proteolytic enzyme.
1993-04-01

1. As previously reported, ectodermal a4-2 blastomeres isolated from 8-cell embryos of the ascidian, Halocynthia roretzi or aurantium, and cultured under conditions of cleavage arrest always differentiated into an epidermal phenotype, showing long-lasting Ca(2+)-dependent action potentials and/or tunic on the cell surface. ...

PubMed Central

37
Differential Inhibition of Cytochromes P450 3A4 and 3A5 by the Newly Synthesized Coumarin Derivatives 7-Coumarin Propargyl Ether and 7-(4-Trifluoromethyl)coumarin Propargyl Ether
2008-07-24

The abilities of 7-coumarin propargyl ether (CPE) and 7-(4-trifluoromethyl) coumarin propargyl ether (TFCPE) to act as mechanism-based inactivators of P450 3A4 and 3A5 in the reconstituted system have been investigated using 7-benzyloxy-4-(trifluoromethyl) coumarin (BFC) and testosterone as probes. CPE inhibited the BFC O-debenzylation activity of P450 ...

PubMed Central

38
anti-Diastereo- and Enantioselective Carbonyl (Hydroxymethyl)allylation from the Alcohol or Aldehyde Oxidation Level: Allyl Carbonates as Allylmetal Surrogates
2010-04-07

Enantioselective transfer hydrogenation of carbonate 1a in the presence of aromatic, allylic or aliphatic alcohols 2a�2i employing a cyclometallated iridium C,O-benzoate derived from allyl acetate, 4-cyano-3-nitrobenzoic acid and (S)-SEGPHOS delivers products of (hydroxymethyl)allylation 4a4i in good isolated yields (60�74%), ...

PubMed Central

39
Iridium Catalyzed anti-Diastereo- and Enantioselective Carbonyl (Trimethylsilyl)allylation from the Alcohol or Aldehyde Oxidation Level
2010-07-07

Using the ortho-cyclometallated ?-allyl iridium precatalyst (R)-I derived from [Ir(cod)Cl]2, 4-cyano-3-nitrobenzoic acid, (R)-SEGPHOS and allyl acetate, enantioselective transfer hydrogenation of ?-(trimethylsilyl)allyl acetate in the presence of aldehydes 2a�2i mediated by isopropanol delivers products of (trimethylsilyl)allylation ...

PubMed Central

40
Protein phosphorylation inhibits production of Alzheimer amyloid beta/A4 peptide.
1993-10-01

The major component of amyloid plaque cores and cerebrovascular amyloid deposits found in Alzheimer disease is the beta/A4 peptide, which is derived from the Alzheimer amyloid protein precursor (APP). Recent evidence suggests that abnormalities in beta/A4 peptide production or beta/A4 peptide aggregation may underlie cerebral amyloidosis. In the present study, treatment of ...

PubMed Central

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41
A Derived Transfer of Functions and the Implicit Association Test
2007-09-01

Participants were trained in a series of interrelated conditional discriminations that aimed to establish four 4-member equivalence classes (i.e., A1�B1�C1�D1, A2�B2�C2�D2, A3�B3�C3�D3, A4�B4�C4�D4). During this training, the four A stimuli (i.e., A1, A2, A3, and A4) were compounded with pictures containing positive or negative ...

PubMed Central

42
[Azoles. 27. Nitroimidazole derivatives, their antibacterial and fungicidal activity and electron affinity].
1989-12-01

Nitroimidazole derivatives 3a-3g, 4a-4g and 5-8 were synthesized by treating 4,5-dinitro- and 2-methyl-4,5-dinitroimidazole (1,2) with phenacyl bromide, its p-substituted derivatives or epichlorohydrin. 1-(3-Chloro-2-hydroxypropyl)-4,5-dinitroimidazole (5) and its 2-methyl derivative 6 have ...

PubMed

43
Amberlite-IRA-402 (OH) ion exchange resin mediated synthesis of indolizines, pyrrolo [1,2-a] quinolines and isoquinolines: antibacterial and antifungal evaluation of the products.
2011-03-05

A number of indolizines and pyrrolo[1,2-a]quinolines/isoquinolines were prepared from phenacyl pyridinium, quinolinium and isoquinolinium salts derived from the reaction of the heterocycles with 2-bromo acetophenone with alkynes and alkenes using amberlite-IRA-402 (OH) ion exchange resin as the base. Antibacterial and antifungal studies were carried out against thirteen ...

PubMed

44
42 CFR 85a.4 - Procedures for initiating investigations of places of employment.
2010-10-01

...initiating investigations of places of employment. 85a.4 Section 85a.4...HEALTH INVESTIGATIONS OF PLACES OF EMPLOYMENT § 85a.4 Procedures for initiating investigations of places of employment. (a) Except as...

Code of Federal Regulations, 2010

45
22 CFR 3a.4 - Procedure for requesting approval.
2009-04-01

...2009-04-01 false Procedure for requesting approval. 3a.4 Section 3a.4 Foreign Relations DEPARTMENT OF STATE GENERAL...FOREIGN GOVERNMENTS BY MEMBERS OF THE UNIFORMED SERVICES § 3a.4 Procedure for requesting approval....

Code of Federal Regulations, 2010

46
12 CFR 269a.4 - Investigator.
2011-01-01

... 2011-01-01 2011-01-01 false Investigator. 269a.4 Section 269a.4 Banks and...RESERVE SYSTEM DEFINITIONS § 269a.4 Investigator. The term investigator means the officer designated by the...

Code of Federal Regulations, 2011

47
Discovery of Leukotriene A4 Hydrolase Inhibitors Using Metabolomics Biased Fragment Crystallography�
2009-07-20

We describe a novel fragment library termed fragments of life (FOL) for structure-based drug discovery. The FOL library includes natural small molecules of life, derivatives thereof, and biaryl protein architecture mimetics. The choice of fragments facilitates the interrogation of protein active sites, allosteric binding sites, and protein?protein interaction surfaces for ...

PubMed Central

48
rad18405.tab

$vpn'Cl 002d &a+. 002d &a+. 002d &a+. 002d &a+. \\002d &a+. H002d &a+4 002d &a+4 002d &a+4 002d &a+4 002d &a+4 002d ...

NASA Website

49
Structure of Ca2+-Bound S100A4 and Its Interaction with Peptides Derived from Nonmuscle Myosin-IIA�
2008-04-15

S100A4, also known as mts1, is a member of the S100 family of Ca2+-binding proteins that is directly involved in tumor invasion and metastasis via interactions with specific protein targets, including nonmuscle myosin-IIA (MIIA). Human S100A4 binds two Ca2+ ions with ...

PubMed Central

50
Construction of hybrid biphenyl (bph) and toluene (tod) genes for functional analysis of aromatic ring dioxygenases.
1994-01-28

Multicomponent enzyme complexes of biphenyl (BP) dioxygenase (Dox) encoded by the gene cluster, bphA1A2A3A4 in Pseudomonas pseudoalcaligenes strain KF707 [Taira et al., J. Biol. Chem. 267 (1992) 4844-4858] and toluene Dox encoded by the gene cluster, todC1C2BA in P. putida strain F1 [Zylstra et al., J. Biol. Chem. 264 (1989) 14940-14946], show high ...

PubMed

51
Moore, J.C., Klaus, A., et al., 1998 Proceedings of the Ocean Drilling Program, Initial Reports, Vol. 171A

sediments with high concentrations of sand and carbonate at Site 672. Anomalies in pore-fluid geochemistry suggest fluid flow in this unit. Lithologic properties derived from the logs indicate sand layers density (g/cm3)XRD Minerology Core density (g/cm3) Logunits Age Core Lithology Recovery 1a 1b 1c 2 3 4a 4b

E-print Network

52
Hyperentropic systems and the generalized second law of thermodynamics
2011-08-04

The holographic bound asserts that the entropy $S$ of a system is bounded from above by a quarter of the area ${\\cal A}$ of a circumscribing surface measured in Planck areas: $S\\leq {\\cal A}/4{\\ell^2_P}$. This bound is widely regarded a desideratum of any fundamental theory. Moreover, it was argued that the holographic bound is necessary for the ...

E-print Network

53
Does the Casimir force need corrections?
2011-03-31

The Casimir force $\\cF = -\\frac{\\pi^2\\hbar c}{240a^4}$, which attracts to each other two perfectly conducting parallel plates separated by the distance $a$ in vacuum, is one of the blueprints of the reality of vacuum fluctuations. Following the recent conjecture, that quantum fields should be described in terms of the fields depending on the resolution ...

E-print Network

54
Antimicrobial evaluation of imines and thiazolidinones derived from 3-phenylpropane hydrazide.

Methyl 3-phenylpropanoate (1), after hydrazination into 3-phenylpropanehydrazide (2), was converted into N-arylidene-3-phenylpropane hydrazides (3a-e), which on cyclization with thioglycolic acid yielded N-(4-oxo-2-arylthiazolidin-3-yl)-3-phenylpropanamides (4a-e). All the proposed structures of newly synthesized compounds were in full agreement with the spectral data. Due to para substitution, ...

PubMed

55
The role of human cytochrome P4503A4 in biotransformation of tissue-specific derivatives of 7H-dibenzo[c,g]carbazole.
2011-07-21

The environmental pollutant 7H-dibenzo[c,g]carbazole (DBC) and its derivative, 5,9-dimethylDBC (DiMeDBC), produced significant and dose-dependent levels of micronuclei followed by a substantial increase in the frequency of apoptotic cells in the V79MZh3A4 cell line stably expressing the human cytochrome P450 (hCYP) 3A4. In contrast, ...

PubMed

56
Mineral catalysis of the formation of the phosphodiester bond in aqueous solution: The possible role of montmorillonite clays
1989-01-01

The binding of adenosine to Na+-montmorillonite 22A is greater than 5'-AMP, at neutral pH. Adenine derivatives bind more strongly to the clay than the corresponding uracil derivatives. These data are consistent with the protonation of the adenine by the acidic clay surface and a cationic binding of the protonated ring to the anionic clay surface. Other ...

NASA Astrophysics Data System (ADS)

57
Intrinsic Sexually Dimorphic Expression of the Principal Human CYP3A4 Correlated with Suboptimal Activation of GH/Glucocorticoid-Dependent Transcriptional Pathways in Men.
2011-09-27

Cytochrome P450 (CYP)3A4 is the principal and most abundant human isoform of CYP responsible for the metabolism of more than 50% of all consumed drugs and innumerable endogenous compounds. Expression of CYP3A4 is sexually dimorphic and regulated by the combined actions of GH and glucocorticoids. In the case of the rat, nearly all of the CYPs are ...

PubMed

58
In vivo anti-tumour effect of 3'-sulphonoquinovosyl 1'-monoacylglyceride isolated from sea urchin (Strongylocentrotus intermedius) intestine.
1997-01-01

Extracts from sea urchin intestine were screened for new anti-tumour drugs. Four glycolipids, 3'-sulphonoquinovosyl-1', 2'-diacylglyceride (A-4), 3'-sulphonoquinovosyl-1'-monoacylglyceride (2'-lyso A-4, A-5), NeuGc(alpha)2-6Glc(beta)1-1ceramide (A-6) and HSO3-8NeuGc(alpha)2-6Glc(beta)1-1ceramide (A-7), were ...

PubMed Central

59
Identification of Two Novel HLA-A*0201-Restricted CTL Epitopes Derived from MAGE-A4
2010-02-14

MAGE-A antigens belong to cancer/testis (CT) antigens that are expressed in tumors but not in normal tissues except testis and placenta. MAGE-A antigens and their epitope peptides have been used in tumor immunotherapy trials. MAGE-A4 antigen is extensively expressed in various histological types of tumors, so it represents an attractive target for tumor ...

PubMed Central

60
VEGF-A and Tenascin-C produced by S100A4+ stromal cells are important for metastatic colonization.
2011-09-12

Increased numbers of S100A4(+) cells are associated with poor prognosis in patients who have cancer. Although the metastatic capabilities of S100A4(+) cancer cells have been examined, the functional role of S100A4(+) stromal cells in metastasis is largely unknown. To study the contribution of S100A4(+) stromal cells in metastasis, we used transgenic mice that express viral thymidine kinase under ...

PubMed

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61
Synthesis, antimicrobial and anticancer activity of new thiosemicarbazone derivatives.
2010-11-25

Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, ...

PubMed

62
Synthesis, Antimicrobial and Anticancer Activity of New Thiosemicarbazone Derivatives.
2010-11-25

Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, ...

PubMed

63
Recent progress in the estimation of laminar and turbulent wall-bounded flows
2005-11-01

We present recent progress on a range of techniques to estimate the flow state based on a history of noisy measurements from an array of flush-mounted skin-friction and pressure sensors on a wall:(A) Model predictive estimation (a.k.a. 4D-var) in a ``multiscale retrograde'' framework (Bewley & Protas, Physica D 2004);(B) Kalman filtering based on an ...

NASA Astrophysics Data System (ADS)

64
Discovery of novel methanone derivatives acting as antimycobacterial agents.
2011-03-14

A series of pyrazoline derivatives were synthesized and in vitro activity against Mycobacterium tuberculosis H37Rv was carried out. Among the synthesized compounds, compounds (4d) and (4f) 4-aminophenyl-3-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-ylmethanone and ...

PubMed

65
4,5-Diaryl-3-aminopyrazole derivatives as analogs of Combretastatin A-4: synthesis and biological evaluation.
2011-02-02

A series of cis-restricted 4,5-diaryl-3-aminopyrazole derivatives were synthesized and tested for their cytotoxic activity in vitro against five human cancer cell lines (K562, ECA-109, A549, SMMC-7721, and PC-3). Compounds 5a, 5b, 5d, and 6b showed potent cytotoxicity against all tested cell lines. Primary mechanism research on compound 5a indicated that it was a potent ...

PubMed

66
Molecular analysis and physicochemical properties of electrophoretic variants of wild soybean Glycine soja storage proteins.
2005-05-01

Cultivated soybeans (Glycine max) are derived from wild soybeans (Glycine soja) and can be crossed with them to produce fertile offspring. The latter exhibit greater genetic variation than the former, suggesting a possibility that wild soybeans contain storage proteins with properties different from and better than those of cultivated soybeans. To identify a wild soybean ...

PubMed

67
Synthesis and bioassay of improved mosquito repellents predicted from chemical structure
2008-05-27

Mosquito repellency data on acylpiperidines derived from the U.S. Department of Agriculture archives were modeled by using molecular descriptors calculated by CODESSA PRO software. An artificial neural network model was developed for the correlation of these archival results and used to predict the repellent activity of novel compounds of similar structures. A series of 34 ...

PubMed Central

68
Synthesis and Structure-Activity Relationships of Constrained Heterocyclic Analogues of Combretastatin A4.
2011-07-01

A series of combretastatin A4 (CA4) analogues with a lactam or lactone ring fused to the trimethoxyphenyl or the B-phenyl moiety were synthesized in an efficient and stereoselective manner by using a domino Heck-Suzuki-Miyaura coupling reaction. The vascular-disrupting potential of these conformationally restricted CA4 analogues was assessed by various ...

PubMed

69
Cyclization of N-alkylazinium cations with bifunctional nucleophiles. 15. Isomerization of thiazolo(4,5-b)quinoxalines in the presence of acids
1985-09-01

4-Alkyl-2-phenyl-3a,4,9,9a-tetrahydrothioazolo(4,5-b)quinoxalines undergo isomerization in chloroform in the presence of acids to the regioisomeric (with respect to them) 9-alkyl-substituted derivatives. Under the same conditions 2,4-dimethyl-3a,4-9,9a-tetrahydrothiazolo (4,5-b)quinoxaline ...

Energy Citations Database

70
Characterization of human liver cytochrome P450 enzymes involved in the metabolism of rutaecarpine.
2005-11-28

Rutaecarpine has recently been characterized to have an anti-inflammatory activity through cyclooxygenase-2 inhibition. The incubation of rutaecarpine with human liver microsomes in the presence of NADPH generated six isobaric mono-hydroxylated metabolites. The specific cytochrome P450 (CYP) isozymes responsible for rutaecarpine metabolites were identified using the combination of chemical ...

PubMed

71
BOL20104.TAB

(6 4a1a $1 7Eo* 4a1a 4a1a 4a1a RM 4a1a 4a1a h.86 4a1a 4a1a 4a1a 4a1a M'4a1a ..... 4a1a GQ4a1a G#4a1a ...

NASA Website

72
44 CFR Appendix A(4) to Part 61 - Appendix A(4) to Part 61
2010-10-01

... Emergency Management and Assistance 1 2010-10-01 2010-10-01 false Appendix A(4) to Part 61 A(4) Appendix A(4) to Part 61 Emergency Management and Assistance FEDERAL EMERGENCY MANAGEMENT AGENCY,...

Code of Federal Regulations, 2010

73
26 CFR 1.401(a)(4)-1 - Nondiscrimination requirements of section 401(a)(4).
2011-04-01

...5 2011-04-01 2011-04-01 false Nondiscrimination requirements of section 401(a)(4). 1.401(a)(4)-1 Section 1.401(a)(4)-1 Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF THE TREASURY...

Code of Federal Regulations, 2011

74
26 CFR 1.1313(a)-4 - Agreement pursuant to section 1313(a)(4) as a determination.
2011-04-01

...Internal Revenue 11 2011-04-01 2011-04-01 false Agreement pursuant to section 1313(a)(4) as a determination. 1.1313(a)-4 Section 1.1313(a)-4 Internal Revenue INTERNAL REVENUE SERVICE, DEPARTMENT OF...

Code of Federal Regulations, 2011

75
[Azoles. 34. Nitroimidazole derivatives and their antibacterial and fungicidal action].
1992-04-01

Nitroimidazole derivatives 4a-4c, 5a-5c, 8a-8c and 9a-9c were synthesized by treating 4,5-dinitro- and 2-methyl-4,5-dinitroimidazole (1,2) or their silver salts [1.Ag,, 2.Ag) with chlorosubtituted phenacyl bromides 3a-3c, diethyl sulphate or ethyl iodide, allyl iodide and ethyl chloro-, azo- or bromoacetate. 2,4(5)-dinitroimidazole ...

PubMed

76
Expression Patterns of Cancer-Testis Antigens in Human Embryonic Stem Cells and Their Cell Derivatives Indicate Lineage Tracks
2011-07-18

Pluripotent stem cells can differentiate into various lineages but undergo genetic and epigenetic changes during long-term cultivation and, therefore, require regular monitoring. The expression patterns of cancer-testis antigens (CTAs) MAGE-A2, -A3, -A4, -A6, -A8, -B2, and GAGE were examined in undifferentiated human embryonic stem (hES) cells, their ...

PubMed Central

77
Modulation of the spectroscopic property of Bodipy derivates through tuning the molecular configuration.
2011-03-08

A series of six Bodipy derivatives, namely 4,4-difluoro-8-(4-amidophenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene (1), 4,4-difluoro-8-(4-methylphenyl)-1,3,5,7-tetramethyl-4-bora-3a,4a-diaza-s-indacene (2), ...

PubMed

78
Stahara, S. S. - NASA Technical Reports Server

Mar 1, 2011 ... Hacking, C. A. (4) [x] : Vanderveen, A. A. (4) [x] : Striepe, Scott A. (4) [x] : Sagan, C. (3) [x] : Pritchard, E. B. (3) [x] ...

NASA Website

79
A-4F Blue Angel Flight Usage Data - 1976
1977-10-15

... NADC-77287-60 I' A-4F BLUE ANGEL FLIGHT USAGE DATA - 1976 ... "'LE (FRE A-4F Blue Angel Flight Usage Data 197 Final "p~t, 6 UTH ...

DTIC Science & Technology

80
38 CFR 18a.4 - Duties of the Director, Contract Compliance Service.
2010-07-01

...Section 18a.4 Pensions, Bonuses, and Veterans' Relief DEPARTMENT OF VETERANS AFFAIRS (CONTINUED) DELEGATION OF RESPONSIBILITY IN CONNECTION WITH TITLE VI, CIVIL RIGHTS ACT OF 1964 § 18a.4 Duties of the Director, Contract...

Code of Federal Regulations, 2010

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81
38 CFR 18a.4 - Duties of the Director, Contract Compliance Service.
2009-07-01

...Section 18a.4 Pensions, Bonuses, and Veterans' Relief DEPARTMENT OF VETERANS AFFAIRS (CONTINUED) DELEGATION OF RESPONSIBILITY IN CONNECTION WITH TITLE VI, CIVIL RIGHTS ACT OF 1964 § 18a.4 Duties of the Director, Contract...

Code of Federal Regulations, 2010

82
p73 G4C14-A4T14 polymorphism and cancer risk: a meta-analysis based on 27 case-control studies.
2011-04-18

p73 G4C14-A4T14 polymorphism has been hypothesised to be associated with the risk of cancer development by many epidemiological studies, however, the available results were conflicting. To derive a more precise estimation of association between the p73 G4C14-A4T14 polymorphism and risk of ...

PubMed

83
What Formyl Peptide Receptors, if Any, Are Triggered by Compound 43 and Lipoxin A(4) ?
2011-09-01

In this study, we determined receptor preferences for compound 43, a nitrosylated pyrazolone derivative, and the eicosanoid lipoxin A(4) (LXA(4) ), potent anti-inflammatory mediators in many experimental in vivo models. Their effects have been suggested to be mediated through binding to formyl peptide receptor (FPR)2 [earlier known as ...

PubMed

84
Mycolic Acid Modification by the mmaA4 Gene of M. tuberculosis Modulates IL-12 Production
2008-06-06

Mycobacterium tuberculosis has evolved many strategies to evade elimination by the host immune system, including the selective repression of macrophage IL-12p40 production. To identify the M. tuberculosis genes responsible for this aspect of immune evasion, we used a macrophage cell line expressing a reporter for IL-12p40 transcription to screen a transposon library of M. tuberculosis for mutants ...

PubMed Central

85
CP violation and FCNC in a warped A4 flavor model
2011-06-01

We recently proposed a spontaneous A4 flavor symmetry breaking scheme implemented in a warped extra dimensional setup to explain the observed pattern of quark and lepton masses and mixings. The quark mixing is absent at leading order in the VEV expansion and it is induced at next-to-leading order by bulk A4 flavons ...

NASA Astrophysics Data System (ADS)

86
Doxyfile - NASA

... Catalan, Chinese, Chinese-Traditional, Croatian, Czech, Danish, # Dutch, Finnish, ..... Possible values are: a4, a4wide, letter, legal and # executive. ...

NASA Website

87
Commissioning (Phases 4, 4A, 4B)
1997-09-01

... Accession Number : ADA338342. Title : Commissioning (Phases 4, 4A, 4B). Descriptive Note : Final technical rept. Corporate ...

DTIC Science & Technology

88
A4SPECTRA - HEAO 1 A4 Spectra - HEASARC - NASA

Oct 12, 2005 ... The experiment consisted of a collection of collimated sodium iodide scintillators, two of which the Low Energy detectors (LED, LED-3 and ...

NASA Website

89
N-dealkylation of arylpiperazine derivatives: disposition and metabolism of the 1-aryl-piperazines formed.
2007-08-01

In recent years several arylpiperazine derivatives have reached the stage of clinical application, mainly for the treatment of depression, psychosis or anxiety. Examples are the pyrimidinylpiperazine buspirone, the chlorophenylpiperazine derivatives nefazodone and trazodone, the dichlorophenylpiperazine aripiprazole and the benzisothiazolyl ...

PubMed

90
Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivatives.
2011-06-01

A series of 6-aryl-5-cyano-2-thiouracil derivatives (1a-d) was synthesized by the reaction of ethyl cyanoacetate with thiourea and aldehydes. These products were used as intermediate compounds for the synthesis of a number of thiouracil derivatives (2a-d to 10a-d). All compounds were screened for antibacterial and antifungal activities. Some of the ...

PubMed

91
Significance of lipid mediators in corneal injury and repair
2010-05-01

Corneal injury induces an inflammatory reaction and damages the sensory nerves that exert trophic influences in the corneal epithelium. Alterations in normal healing disrupt the integrity and function of the tissue with undesirable consequences, ranging from dry eye and loss of transparency to ulceration and perforation. Lipids play important roles in this complex process. Whereas lipid mediators ...

PubMed Central

92
[111In]5-[(3aR,6S,6aS)-2-Oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d] imidazol-6-yl]pentanoic acid

pentaacetic acid (DTPA) and ethylene diamine tetraacetic acid (EDTA) derivatives of biotin (10). The two-biotin was also described by Lazzeri et al. (9). Briefly, DTPA- conjugated biotin was purchased commercially and diluted in 0.05 M acetate buffer (pH 5.5). Aliquots of DTPA-biotin were stored at 4�C until required

E-print Network

93
Thermodynamics of apparent horizon in modified FRW universe with power-law corrected entropy
2011-08-01

We derive the modified Friedmann equation corresponding to the power-law corrected entropy-area relation {S_A} = A/4[ {1 - {K_? }{A^{1 - ? /2}}} ] which is motivated by the entanglement of quantum fields in and out of the apparent horizon. We consider a non-flat modified FRW universe containing an interacting viscous dark energy with ...

NASA Astrophysics Data System (ADS)

94
The BDNF Val66Met polymorphism is associated with rumination in healthy adults
2009-08-01

This study examined associations between the tendency to ruminate and two polymorphisms: the Val66Met polymorphism in the brain-derived neurotrophic factor (BDNF) gene and 5-HTTLPR polymorphism in the serotonin transporter gene (SLC6A4). Participants were a homogenous group of healthy, unmedicated, never depressed individuals with few ...

PubMed Central

95
Structure and vibrational spectroscopy investigation of 2-(4-chlorophenyliminomethyl)-8-hydroxyquinoline.
2011-06-29

2-(4-Chlorophenyliminomethyl)-8-hydroxyquinoline was synthesized and crystal data was obtained in the orthorhombic space group P-1, with Z=4. Unit cell parameters a=4.744(7)?, b=9.981(15)?, c=27.27(4)? and V=12915(3)?(3). In this paper the structural properties and vibrational frequencies of 8-hydroxyquinoline derivative, 2CP8HQ, are ...

PubMed

96
Reactions of imidic acid derivatives with nucleophilic reagents. Bifunctional catalysis of the arylaminolysis of aryl n-phenyl-sulfonylbenzimidates in chlorobenzene
1987-10-20

The kinetics of the reaction of aryl N-phenylsulfonylbenzimidates PhC(OArX)=NSO/sub 2/Ph (I,X=4-NO/sub 2/ (a), 4-N=NC/sub 6/H/sub 5/ (b)) with aniline in chlorobenzene at 25/sup 0/C are characterized by first-order in the imidate and third (compound (Ib)) and fourth (compound (Ia)) order in the arylamine. The reaction is accelerated by phenols, pyridines, ...

Energy Citations Database

97
Quasinormal modes for doubly rotating black holes
2011-06-01

Based on the work of Chen, L�, and Pope, we derive expressions for the D?6 dimensional metric for Kerr-anti-de Sitter black holes with two independent rotation parameters and all others set equal to zero: a1?0, a2?0, a3=a4=?=0. The Klein-Gordon equation is then explicitly separated on this background. For D?6 this separation results ...

NASA Astrophysics Data System (ADS)

98
Possible resolution of the lattice Gribov ambiguity
1990-04-15

The Gribov ambiguity in lattice gauge theory is discussed. The Landau gauge and the finite-temperature temporal gauge ({partial derivative}{sub 4}{ital A4}=0) are formulated as maximization conditions on the lattice. This formulation is shown to eliminate Gribov copies from the temporal gauge. The possibility that it also eliminates ...

Energy Citations Database

99
Physical interpretation of the spectrum of black hole quasinormal modes.
2008-04-08

When a classical black hole is perturbed, its relaxation is governed by a set of quasinormal modes with complex frequencies omega=omega R +i omega I. We show that this behavior is the same as that of damped harmonic oscillators whose real frequencies are (omega R2+omega I 2)1/2, rather than simply omega R. Since, for highly excited modes, omega I>>omega R, this observation changes ...

PubMed

100
Micelles catalyzed chemoselective synthesis 'in water' and biological evaluation of oxygen containing hetero-1,4-naphthoquinones as potential antifungal agents.
2011-08-31

Various oxygen containing 1,4-naphthoquinone derivatives have been synthesized chemoselectively by an economical, viable green methodology approach using water as solvent with or without surfactants such as Triton X-100, SDS, LD (laundry detergent), and TBAB, a phase transfer catalyst and evaluated for their in vitro antifungal and antibacterial activity. The antifungal ...

PubMed

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101
Ionic liquid promoted synthesis, antibacterial and in vitro antiproliferative activity of novel ?-aminophosphonate derivatives.
2011-02-15

Ionic liquid ethyl ammonium nitrate is used as an excellent catalyst and solvent for three-component one-pot reaction of an aldehydes, amines and diethylphosphite to form novel ?-aminophosphonates at room temperature. Among the various catalysts, the preparation of ethyl ammonium nitrate is an environmental friendly, cost effective and recyclable catalyst. Compounds 4b, 4c, 4d, 4f and 4j were ...

PubMed

102
Highly enantioselective nitroaldol reactions catalyzed by copper(II) complexes derived from substituted 2-(pyridin-2-yl)imidazolidin-4-one ligands.
2011-05-13

Ten optically pure substituted 2-(pyridin-2-yl)imidazolidin-4-ones, 1a-d, 2a-4a, and 2b-4b, were prepared and characterized. The absolute configurations of individual ligands were determined by X-ray analysis or NOESY experiments. The Cu(II) complexes of the respective ligands were studied as enantioselective catalysts of the nitroaldol (Henry) reaction of ...

PubMed

103
Glycosylation via mixed disulfide formation using glycosylthio-phthalimides and -succinimides as glycosylsulfenyl-transfer reagents.
2011-04-24

The silver salts of tetra-O-acetyl ?- or -?-d-glycopyranosyl thiols 1a-4a react smoothly with N-bromophthalimide and N-bromosuccinimide to furnish glycosylthio-phthalimide (1b-4b) and -succinimide (1c-3c) derivatives. Reactions of these reagents with aliphatic, aromatic, and glycosyl thiols as well as with cysteine and glutathione ...

PubMed

104
Glomerular basement membrane composition and the filtration barrier.
2011-02-15

The glomerular basement membrane (GBM) is an especially thick basement membrane that contributes importantly to the kidney's filtration barrier. The GBM derives from the fusion of separate podocyte and endothelial cell basement membranes during glomerulogenesis and consists primarily of laminin-521 (?5?2?1), collagen ?3?4?5(IV), nidogens-1 and -2, and agrin. Of these nine ...

PubMed

105
Diastereo- and Enantioselective anti-Alkoxyallylation Employing Allylic gem-Dicarboxylates as Allyl Donors via Iridium Catalyzed Transfer Hydrogenation
2010-02-17

Enantioselective transfer hydrogenation of gem-dibenzoate 1e in the presence of aromatic, ?, ?-unsaturated or aliphatic aldehydes 2a�2i mediated by isopropanol and employing a cyclometallated iridium C,O-benzoate derived from allyl acetate, 4-cyano-3-nitrobenzoic acid and (R)-SEGPHOS delivers products of alkoxyallylation 3a�3i, 4a, ...

PubMed Central

106
Constituents from the leaves of Phellodendron amurense and their antioxidant activity.
2006-09-01

Three new coumarins, phellodenols F-H (1-3) and a new glutaric acid derivative, phellodendric acid-A (4) were isolated from the leaves of Phellodendron amurense together with twenty-nine known compounds. Extensive 1D and 2D NMR experiments and other spectroscopic studies were employed to determine the structures of 1-4. The isolated ...

PubMed

107
Charon Phages: Safer Derivatives of Bacteriophage Lambda for DNA Cloning
1977-04-01

The Charon ? bacteriophages have been developed as vectors for cloning. Their construction incorporates mutations that make them simple to use and also greatly increases their safety for the biological containment of cloned recombinant DNA. Three of the Charon vector phages, 3A, 4A, and 16A, have been certified for use as EK2 vector-host systems, when ...

NASA Astrophysics Data System (ADS)

108
Bolide physical theory with application to PN and EN fireballs
2001-11-01

Using data on 22 "precise bolides" with up to 882 individual points on their trajectories and using data on 29 "bright bolides" and on 10 artificial meteors we tried to derive the dependence of the ablation and shape-density coefficients, and of the luminous efficiency on various time dependent parameters. The only significant dependence we found was that on v?-v (the ...

NASA Astrophysics Data System (ADS)

109
A Simple Photoelectrochemical Cell Using Fe+++/Fe++(aq) As Redox Couple
2010-12-01

We report a simple photoelectrochemical cell (PEC) using a derivative of borondipyrromethane (BODIPY), that is, (4,4-difluoro-1,3,5,7,8-pentamethyl-2,6-diethyl-4-bora-3a,4a-diaza-s-indecene) as dye sensitizer and an aqueous electrolyte containing Ferric/ferrous redox couple (F+++/Fe++). Under white light illumination of intensity ~1 ...

NASA Astrophysics Data System (ADS)

110
A Compact Quasi-axisymmetric Stellarator Reactor
2003-10-20

We report the progress made in assessing the potential of compact, quasi-axisymmetric stellarators as power-producing reactors. Using an aspect ratio A=4.5 configuration derived from NCSX and optimized with respect to the quasi-axisymmetry and MHD stability in the linear regime as an example, we show that a reactor of 1 GW(e) maybe ...

Energy Citations Database

111
Summary Report on Federal Laboratory Technology Transfer

.......................................................................................... A-4 A.2 Actinium (235 U) Decay Series

E-print Network

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