ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDicationic Diarylfurans as Anti-Pneumocystis carinii AgentsDavid W. Boykin, Arvind Kumar, Jaroslaw Spychala, Min Zhou, Richard J. Lombardy, David Wilson, Christine C. Dykstra, Susan K. Jones, James E. Hall, and Cite this: Med. Chem. 1995, 38, 6, 912–916Publication Date (Print):March 1, 1995Publication History Published online1 May 2002Published inissue 1 March...

Adenosine kinase catalyzes the phosphorylation of adenosine to AMP and hence is a potentially important regulator extracellular concentrations. Despite extensive characterization kinetic properties enzyme, its primary structure has never been elucidated. Full-length cDNA clones encoding catalytically active were obtained from lymphocyte, placental, liver libraries. Corresponding mRNA species 1.3 1.8 kb noted on Northern blots all tissues examined attributable alternative polyadenylylation...

Abstract A human placental soluble high Km 5'-nucleotidase has been separated from low and nonspecific phosphatase by AMP-Sepharose affinity chromatography. The enzyme was purified 8000-fold to a specific activity of 25.6 mumol/min/mg. subunit molecular mass is 53 kDa, the native 210 suggesting tetrameric structure. Soluble most active with IMP GMP their deoxy derivatives. hydrolyzed 15 times faster than AMP. virtually absolute requirement for magnesium ions regulated them. Purine nucleoside...

Deoxycytidine kinase (NTP:deoxycytidine 5'-phosphotransferase, EC 2.7.1.74) is an enzyme that catalyzes phosphorylation of deoxyribonucleosides and a number nucleoside analogs are important in antiviral cancer chemotherapy. Deficiency this activity associated with resistance to these agents, whereas increased activation such compounds cytotoxic triphosphate derivatives. To characterize the regulation expression gene, we have isolated genomic clones encompassing its entire coding 5' flanking...

ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTDesign and Synthesis of RNA-Specific Groove-Binding Cations: Implications for Antiviral Drug DesignAdrian W. McConnaughie, Jaroslaw Spychala, Min Zhao, David Boykin, WilsonCite this: J. Med. Chem. 1994, 37, 8, 1063–1069Publication Date (Print):April 1, 1994Publication History Published online1 May 2002Published inissue 1 April 1994https://pubs.acs.org/doi/10.1021/jm00034a004https://doi.org/10.1021/jm00034a004research-articleACS PublicationsRequest...

Upregulated expression of eN has been found in the highly invasive human melanoma cell lines but neither melanocytes nor primary tumor cells. Membrane proteins associated with adhesion and metastasis: α5-, β1-, β3-integrins, CD44 were elevated gradually accordance increasing metastatic potential. αv-integrin was seen mostly aggressive melanomas. The correlated a number metastasis-related markers thus may have function process. activity went parallel its amount all Concanavalin A strongly...

Abstract We have previously synthesized a 2,5-diphenylfuranamidine dication (4) and presented evidence that this compound binds to AT sequences in DNA by minor-groove interaction mode but GC intercalation (1,2). To probe these sequence-dependent binding modes more detail, particularly obtain additional for the rich sequences, we studied complexes of 1–3 which furan ring 4 replaced 2,6-substituted pyridine (1), pyrimidine (2), or triazine (3) systems. The three compounds with six-membered...

Adenosine has potent immunosuppressive activity. Since the source of adenosine and mechanism its release in immune system is largely unknown may vary according to cell type, we have evaluated relationship between metabolism enzymatic activities mRNA levels adenosine-metabolizing enzymes myeloid lymphoid lines. Induction HL-60 differentiation along macrophage lineage by PMA resulted a reduction deaminase (ADA), kinase (AK), inosine monophosphate-specific cytosolic 5'-nucleotidase an elevation...

Abstract The Pinner synthesis was applied to the preparation of 4-(cyclic amidino)phenols in high yields from readily available 4-hydroxybenzimidic acid methyl ester hydrochloride and diaminoalkanes. An alternative attempt made convert 4-(hydroxy)thiobenzamide 4-(1,4,5,6-tetrahydro-5-hydroxy-2-pyrimidiyl)phenol. A procedure for 3,6-bis(4-hydroxyphenyl)- 1,2,4,5-tetrazine is reported here. syntheses 2,4-bis[4-(4,5-dihydro-lH-imidazol-2-yl)phenoxy]pyrimidine...

Abstract 1-[(Cyclic amidino)methyl]thymines have been conveniently synthesized from thymine in a three-step procedure via 1-cyanomethyl- and 1-[(thiocarbamoyl) methyl]thymines. The above synthetic intermediates were obtained good yields by improved methods.

Abstract N2-Arylisocytosines were obtained in good yields varying from 59 to 96% by a simple two-step process starting 2-thiouracil via readily accessible 2-(methylthio)pyrimidin-4(3H)-one.

Three distinct 5'-phosphomonoesterase activities were isolated from soluble fractions of human placenta, cultured T and B lymphoblasts, rat liver using 5'-AMP-sepharose 4B affinity chromatography. We define these as "low-Km" 5'-nucleotidase, "high-Km" nonspecific phosphatase. High-Km 5'-nucleotidase was eluted with 0.5 M NaCl, low-Km 10 mM ADP, phosphatase not retained on the column. have found significant variability in relative content high- to tissues studied ratios ranging 5.5 264. The...

Results concerning the electronic structure of five cytosine derivatives obtained by NMR- NQR double resonance technique on nitrogen nuclei are reported. spectra were taken at 120 K. The influence substitution 4-N position ring was analysed NQR. According to results study, amine group, which acts as a π electron acceptor in most molecular systems, phenylcytosine and naphthylcytosine becomes an donor, while aromatic rings, usually compensate for density changes cytosine, act acceptors. When...

Abstract The mass fragmentation of 4‐arylaminocytosine derivatives was investigated and it found that the ortho effect is mainly responsible for strong stabilization even‐electron ions formed during fragmentation. in this class compounds completely eliminates other possible patterns. This disappears when aryl substituent separated from 4‐amino group cytosine moiety by a methylene group.

The turnover of the adenine nucleotide pool, pathway degradation AMP and occurrence recycling adenosine were investigated in isolated chicken hepatocytes, which adenylates had been labelled by prior incubation with [14C]adenine. Under physiological conditions, 85% IMP synthesized ‘de novo’ (approx. 37 nmol/min per g cells) was catabolized directly via inosine into uric acid, 14% converted nucleotides. latter found to turn over at rate approx. 5 tissue. Inhibition deaminase 1...