Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative.


:A novel 6-substituted acyclouridine derivative, 1-[(2-hydroxy-ethoxy) methyl]-6-phenylthiothymine (HEPT), has proved to be a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) in vitro. HEPT inhibits HIV-1 replication in various T4 cell cultures as well as peripheral blood lymphocytes and macrophages. The 50% antiviral effective concentration for HIV-1 (HTLV-IIIB) in MT-4 cells is 7.0 microM, while the 50% cytotoxic concentration for mock-infected MT-4 cells is 740 microM. Although HEPT is inhibitory to various strains of HIV-1, it has no effect on the replication of other retroviruses including HIV type 2. In contrast with the dideoxynucleoside (i.e. azidothymidine) 5'-triphosphates, the triphosphate of HEPT does not interact with HIV-1 reverse transcriptase. The mechanism of action of HEPT remains subject of further study.


Baba M,Tanaka H,De Clercq E,Pauwels R,Balzarini J,Schols D,Nakashima H,Perno CF,Walker RT,Miyasaka T




Has Abstract


1989-12-29 00:00:00














  • Influence of divalent cations on the cytoskeletal dynamics of K562 cells determined by nano-scale bead tracking.

    abstract::Cytoskeletal reorganization processes can be analyzed by studying the nanometer-scale spontaneous motion of beads bound to the cytoskeleton. The bead motion is determined by force fluctuations within the cytoskeletal network that originates from myosin motor activity and dynamic restructuring of cytoskeletal filaments...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Alonso JL,Goldmann WH

    更新日期:2012-05-04 00:00:00

  • Tissue transglutaminase-induced down-regulation of matrix metalloproteinase-9.

    abstract::Tissue transglutaminase (TGase 2) has been reported to have multiple functions in addition to its function as a biological adhesive. To identify its roles, we investigated the effects of TGase 2 on gelatinase activity. The MMP-9 activity of certain cell lines was significantly inhibited with retinoic acid treatment, a...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Ahn JS,Kim MK,Hahn JH,Park JH,Park KH,Cho BR,Park SB,Kim DJ

    更新日期:2008-11-28 00:00:00

  • Deltoid human muscle mtDNA is extensively rearranged in old age subjects.

    abstract::Extra long PCR analysis of mitochondrial DNA (mtDNA) isolated from skeletal muscle of humans of different ages revealed three phenomena: (i) the amount of normal length mtDNA (16.5 kb) was progressively reduced with age, such that the cells of old age individuals (about 90 years) contained little, or undetectable amou...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Kovalenko SA,Kopsidas G,Kelso JM,Linnane AW

    更新日期:1997-03-06 00:00:00

  • The N-terminal cleavage site of PrPSc from BSE differs from that of PrPSc from scrapie.

    abstract::Heterogeneity in transmissible spongiform encephalopathy is thought to have derived from conformational variation in an abnormal isoform of the prion protein (PrPSc). To characterize PrPSc in bovine spongiform encephalopathy (BSE) and scrapie, we analyzed the newly generated N-terminus of PrPSc isoforms by digestion w...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Hayashi HK,Yokoyama T,Takata M,Iwamaru Y,Imamura M,Ushiki YK,Shinagawa M

    更新日期:2005-03-25 00:00:00

  • Deletion and transfection analysis of the p15/MTS2 gene in malignant gliomas.

    abstract::We have investigated the status of the MTS2 gene, encoding the cyclin-dependent kinase (CDK) inhibitor p15, in 32 glioblastomas. Semi-quantitative PCR identified 7 tumors in which the amplified material was 18.6% of controls and 7 in which was 48.0%, suggesting the occurrence of homozygous and hemizygous deletions, re...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Tenan M,Benedetti S,Finocchiaro G

    更新日期:1995-12-05 00:00:00

  • Characterization of the platelet-derived growth factor beta-receptor kinase activity by use of synthetic peptides.

    abstract::Synthetic peptides derived from the sequence surrounding tyrosine-857 in the human platelet-derived growth factor (PDGF) beta-receptor were used to elucidate the requirement for length and presence of negative and positively charged amino acids in substrates of the PDGF beta-receptor protein tyrosine kinase. The measu...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Rönnstrand L,Sorokin A,Engström U,Heldin CH

    更新日期:1990-03-30 00:00:00

  • LncRNA snaR upregulates GRB2-associated binding protein 2 and promotes proliferation of ovarian carcinoma cells.

    abstract:BACKGROUND:The functionality of lncRNA snaR has only been characterized in breast cancer and colon cancer. The aim of the current study is to explore the involvement of lncRNA snaR in ovarian carcinoma (OC). MATERIALS AND METHODS:Expression of lncRNA snaR and GRB2-associated binding protein 2 (GAB2) in plasma of both ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Huang Y,Hu Y,Jin Z,Shen Z

    更新日期:2018-09-10 00:00:00

  • Visualization of antigenic proteins blotted onto nitrocellulose using the immuno-gold-staining (IGS) method.

    abstract::A new and simple method for the detection of antigenic proteins blotted onto nitrocellulose was developed. After transfer of spinach stromal proteins and purified phosphoribulokinase immunolabeling was performed with phosphoribulokinase antiserum, followed by a) Protein A-labeled colloidal gold particles, and b) by ho...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Surek B,Latzko E

    更新日期:1984-05-31 00:00:00

  • Effects of hyperthyroidism on expression of a phosphoenolpyruvate carboxykinase/bovine growth hormone gene in transgenic mice.

    abstract::Thyroid hormone (T3) responsiveness of the PEPCK promoter in vivo was examined in both PEPCK/bGH(460) and PEPCK/bGH(335) mouse lines. Transgenic and non-transgenic littermates were treated with methimazole or PTU for 6 or 4 weeks, respectively, then treated +/- T3 for 10 days. In PEPCK/bGH(460) and PEPCK/bGH(355) tran...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Xu C,McGrane MM

    更新日期:1996-01-17 00:00:00

  • Baculovirus-mediated high level expression of a mammalian DNA methyltransferase.

    abstract::The murine C-5 cytosine DNA methyltransferase (MTase, E.C. containing a hexahistidine affinity leader peptide has been expressed at levels which are at least 50-fold higher than previously reported. The recombinant enzyme has activity levels similar to the wild-type enzyme. The recombinant polypeptide binds t...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Glickman JF,Reich NO

    更新日期:1994-11-15 00:00:00

  • Moderate hearing loss associated with a novel KCNQ4 non-truncating mutation located near the N-terminus of the pore helix.

    abstract::Genetic mutation is one of the causative factors for idiopathic progressive hearing loss. A patient with late-onset, moderate, and high-frequency hearing loss was found to have a novel, heterozygous KCNQ4 mutation, c.806_808delCCT, which led to a p.Ser260del located between S5 and the pore helix (PH). Molecular modeli...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Watabe T,Matsunaga T,Namba K,Mutai H,Inoue Y,Ogawa K

    更新日期:2013-03-15 00:00:00

  • Thyroid hormone binding protein contains glycosylation site binding protein activity.

    abstract::Several lines of evidence provided by other workers indicate that within the same species thyroid hormone binding protein, the beta-subunit of prolyl hydroxylase, and protein disulfide isomerase are the same protein. We sought to determine if glycosylation site binding protein, a lumenal protein of the endoplasmic ret...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Kimura H,Noiva R,Mizunaga T,Yamauchi K,Horiuchi R,Cheng SY,Lennarz WJ

    更新日期:1990-08-16 00:00:00

  • Is the idea of a fast block to polyspermy based on artifact?

    abstract::This purpose of this review is to look at the experimental evidence, both kinetic and electrophysiological, that led to the hypothesis of a fast electrical block to polyspermy in sea urchin eggs. The idea of a fast partial block, forwarded in the 1950's, that would reduce the receptivity of the egg surface by 1/20th f...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章,评审


    authors: Dale B

    更新日期:2014-08-01 00:00:00

  • Suppression of HPV E6 and E7 expression by BAF53 depletion in cervical cancer cells.

    abstract::Deregulation of the expression of human papillomavirus (HPV) oncogenes E6 and E7 plays a pivotal role in cervical carcinogenesis because the E6 and E7 proteins neutralize p53 and Rb tumor suppressor pathways, respectively. In approximately 90% of all cervical carcinomas, HPVs are found to be integrated into the host g...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Lee K,Lee AY,Kwon YK,Kwon H

    更新日期:2011-08-26 00:00:00

  • Interpretation of field potentials measured on a multi electrode array in pharmacological toxicity screening on primary and human pluripotent stem cell-derived cardiomyocytes.

    abstract::Multi electrode arrays (MEAs) are increasingly used to detect external field potentials in electrically active cells. Recently, in combination with cardiomyocytes derived from human (induced) pluripotent stem cells they have started to become a preferred tool to examine newly developed drugs for potential cardiac toxi...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Tertoolen LGJ,Braam SR,van Meer BJ,Passier R,Mummery CL

    更新日期:2018-03-18 00:00:00

  • Molecular cloning of cDNA for human poly(ADP-ribose) polymerase and expression of its gene during HL-60 cell differentiation.

    abstract::Human placental poly(ADP-ribose) polymerase was purified and the NH2-terminal amino acid sequences of 16 KDa and 40 KDa chymotryptic peptides were determined. Screening of a lambda gt11 cDNA library of normal human placenta with a 51-mer oligodeoxyribonucleotide yielded one clone with a 1.8 Kb insert and two clones wi...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Suzuki H,Uchida K,Shima H,Sato T,Okamoto T,Kimura T,Miwa M

    更新日期:1987-07-31 00:00:00

  • The 6H1 orphan receptor, claimed to be the p2y5 receptor, does not mediate nucleotide-promoted second messenger responses.

    abstract::An orphan G protein-coupled receptor, termed 6H1, with approximately 30% sequence identity to P2Y receptors has been proposed to be a P2Y receptor (p2y5) based solely on a radioligand binding assay with [35S]dATP alphaS [Webb et al. (1997) Biochem. Biophys. Res. Commun. 219:105-110]. Previous work in our laboratory ha...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Li Q,Schachter JB,Harden TK,Nicholas RA

    更新日期:1997-07-18 00:00:00

  • Sugarcane Elongin C is involved in infection by sugarcane mosaic disease pathogens.

    abstract::Sugarcane (Saccharum sp. hybrid) provides the main source of sugar for humans. Sugarcane mosaic disease (SMD) is a major threat to sugarcane production. Currently, control of SMD is mainly dependent on breeding resistant cultivars through hybridization, which is time-consuming. Understanding the mechanism of viral inf...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Zhai Y,Deng Y,Cheng G,Peng L,Zheng Y,Yang Y,Xu J

    更新日期:2015-10-23 00:00:00

  • Variable allelic expression of imprinted genes in human pluripotent stem cells during differentiation into specialized cell types in vitro.

    abstract::Genomic imprinting is an epigenetic phenomenon by which a subset of genes is asymmetrically expressed in a parent-of-origin manner. However, little is known regarding the epigenetic behaviors of imprinted genes during human development. Here, we show dynamic epigenetic changes in imprinted genes in hESCs during in vit...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Park SW,Kim J,Park JL,Ko JY,Im I,Do HS,Kim H,Tran NT,Lee SH,Kim YS,Cho YS,Lee DR,Han YM

    更新日期:2014-04-04 00:00:00

  • Single-stranded DNA binding and methylation by EcoP1I DNA methyltransferase.

    abstract::EcoP1I methyltransferase (M.EcoP1I) belongs to the type III restriction-modification system encoded by prophage P1 that infects Escherichia coli. Binding of M.EcoP1I to double-stranded DNA and single-stranded DNA has been characterized. Binding to both single- and double-stranded DNA could be competed out by unlabeled...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Sistla S,Krishnamurthy V,Rao DN

    更新日期:2004-01-30 00:00:00

  • Quinolone antibiotics inhibit eucaryotic DNA polymerase alpha and beta, terminal deoxynucleotidyl transferase but not DNA ligase.

    abstract::DNA polymerases alpha and beta, Terminal deoxynucleotidyl Transferase and DNA ligases from chicken thymus were purified to homogeneity. Quinolone antibiotics (nalidixic acid, oxolinic acid and pefloxacin ) known to inhibit DNA replication were tested for their effects on these enzymes. DNA ligase activity was not affe...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Rusquet R,Bonhommet M,David JC

    更新日期:1984-06-29 00:00:00

  • Regulated expression of 5'-deleted mouse GLUT4 minigenes in transgenic mice: effects of exercise training and high-fat diet.

    abstract::Fourteen kb murine GLUT4 minigene (= -7395 GLUT4) contains DNA sequence that confers tissue specific, exercise-induced up-regulation of the GLUT4 gene in skeletal muscle and high-fat diet induced-down-regulation in white adipose tissue. To identify the DNA sequences required for regulated expression, we generated GLUT...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Tsunoda N,Cooke DW,Ikemoto S,Maruyama K,Takahashi M,Lane MD,Ezaki O

    更新日期:1997-10-20 00:00:00

  • Rapid purification of inositol monophosphate phosphatase from beef brain.

    abstract::A procedure is described for preparation of homogeneous inositol monophosphate phosphatase (EC from beef brain in less than 2 days with an overall recovery of 15-25%. This enzyme, an essential part of the inositol phospholipid cycle in brain, is a proposed site of action of lithium ions in manic-depressive d...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Meek JL,Rice TJ,Anton E

    更新日期:1988-10-14 00:00:00

  • Mechanistic insights into human pre-mRNA splicing of human ultra-short introns: potential unusual mechanism identifies G-rich introns.

    abstract::It is unknown how very short introns (<65 nt; termed 'ultra-short' introns) could be spliced in a massive spliceosome (>2.7 MDa) without steric hindrance. By screening an annotated human transcriptome database (H-InvDB), we identified three model ultra-short introns: the 56-nt intron in the HNRNPH1 (hnRNP H1) gene, th...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Sasaki-Haraguchi N,Shimada MK,Taniguchi I,Ohno M,Mayeda A

    更新日期:2012-06-29 00:00:00

  • Biochemical characterization of Drosophila melanogaster acetylcholinesterase expressed by recombinant baculoviruses.

    abstract::Recombinant baculoviruses expressing full length and 3' truncated forms of c-DNA encoding the Drosophila melanogaster acetylcholinesterase (AChE) were constructed. Biochemical analyses showed that full length recombinant protein was enzymatically active and anchored to the cell membrane via a glycolipidic residue. DTT...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Chaabihi H,Fournier D,Fedon Y,Bossy JP,Ravallec M,Devauchelle G,Cérutti M

    更新日期:1994-08-30 00:00:00

  • Abnormal methylation of PIK3AP1 was involved in regulating the immune inflammatory response of GES-1 cells induced by Helicobacter pylori.

    abstract::Gastric epithelial cells (GES-1) stimulated by Helicobacter pylori (H. pylori) would affect the expression of related genes and induce the immune response of the cells. Abnormal methylation of DNA was one of the main causes. The aim of this study was to investigate phosphoinositol-3-kinase adaptor protein 1(PIK3AP1), ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Zhang A,Yan S,Cao M,Wu D,Zhou J,Yu Z,Wu M,Liu Y,Lu S,Hu G,Zhao J

    更新日期:2020-03-26 00:00:00

  • Cholesterol secoaldehyde induces apoptosis in J774 macrophages via mitochondrial pathway but not involving reactive oxygen species as mediators.

    abstract::Cholesterol secoaldehyde (3beta-hydroxy-5-oxo-5,6-secocholestan-6-al or ChSeco) is an oxysterol known to be formed in reactions of ozone with cholesterol and also when cholesterol-5alpha-hydroperoxide undergoes Hock cleavage. In view of its widespread occurrence and atherogenic potential, we examined the effects of Ch...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Gao X,Raghavamenon AC,D'Auvergne O,Uppu RM

    更新日期:2009-11-13 00:00:00

  • Tensile forces attenuate estrogen-stimulated collagen synthesis in the ACL.

    abstract::The purpose of this study was to examine whether mechanical tensile forces affect estrogen regulation of collagen synthesis of anterior cruciate ligament fibroblasts at the mRNA level. Estrogen was studied at three physiologic levels, 10(-11), 10(-10), and 10(-9)M. The results revealed that estrogen alone stimulated T...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Lee CY,Smith CL,Zhang X,Hsu HC,Wang DY,Luo ZP

    更新日期:2004-05-14 00:00:00

  • Thrombin and ionomycin can raise platelet cytosolic Ca2+ to micromolar levels by discharge of internal Ca2+ stores: studies using fura-2.

    abstract::In the presence of 1 mM EGTA, the addition of the calcium ionophore ionomycin to human platelets loaded with 30 microM fura-2 could elevate [Ca2+]i from less than 100 nM to a maximum of greater than 3 microM, presumably by discharge of Ca2+ from internal stores. Under the same conditions thrombin could maximally incre...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Pollock WK,Rink TJ

    更新日期:1986-08-29 00:00:00

  • Glycogen Synthase Kinase 3 (GSK-3) influences epithelial barrier function by regulating occludin, claudin-1 and E-cadherin expression.

    abstract::The Apical Junctional Complex (AJC) encompassing the tight junction (TJ) and adherens junction (AJ) plays a pivotal role in regulating epithelial barrier function and epithelial cell proliferative processes through signaling events that remain poorly characterized. A potential regulator of AJC protein expression is Gl...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Severson EA,Kwon M,Hilgarth RS,Parkos CA,Nusrat A

    更新日期:2010-07-02 00:00:00