Abstract:
:A series of novel, azacyclic ureas which are highly potent inhibitors of the HIV-1 protease (IC50 = 4.1 to < 0.5 nM) were synthesized. Aqueous solubilities of this series of compounds were improved by incorporating polar functional groups at the P1' P2 and P2' positions. These compounds also possess good anti-viral activity by inhibition of the cytopathic effect of HIV-13B in MT-4 cells in vitro.
journal_name
Biochem Biophys Res Communjournal_title
Biochemical and biophysical research communicationsauthors
Sham HL,Zhao C,Marsh KC,Betebenner DA,Lin S,Rosenbrook W Jr,Herrin T,Li L,Madigan D,Vasavanonda S,Molla A,Saldivar A,McDonald E,Wideburg NE,Kempf D,Norbeck DW,Plattner JJdoi
10.1006/bbrc.1996.1191subject
Has Abstractpub_date
1996-08-14 00:00:00pages
436-40issue
2eissn
0006-291Xissn
1090-2104pii
S0006291X96911912journal_volume
225pub_type
杂志文章abstract::Four monoclonal antibodies, M-T21, M-T32, M-T41 and UM4D4, which belong to the new CDw 60 cluster of antibodies specific for a subpopulation of human T-lymphocytes, were found to bind mainly to acetylated forms of ganglioside GD3. After O-deacetylation of the antigen, binding was reduced ("M-T"-antibodies) or abolishe...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/0006-291x(92)90450-y
更新日期:1992-09-30 00:00:00
abstract::Acute respiratory distress syndrome (ARDS) is associated with high mortality and morbidity. Early diagnosis and risk stratification in patients with ARDS should improve prognosis. Unfortunately, no clinical biomarkers are available for use in early diagnosis. Quantitative proteomics is a powerful tool for biomarker di...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2016.08.125
更新日期:2016-09-23 00:00:00
abstract::In order to establish a working cellular model for the study of post-receptor signaling events, insulin-dependent phosphatidylinositol 3' (PtdIns 3')-kinase activity was investigated in circulating mononuclear cells from normal subjects. The p85 alpha regulatory subunit of PtdIns 3'-kinase co-precipitated with activat...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1995.1494
更新日期:1995-04-06 00:00:00
abstract::Histamine H3 receptor (H3R), one of G protein-coupled receptors (GPCRs), has been known to regulate neurotransmitter release negatively in central and peripheral nervous systems. Recently, a variety of intracellular proteins have been identified to interact with carboxy (C)-termini of GPCRs, and control their intracel...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2008.02.071
更新日期:2008-05-02 00:00:00
abstract::Mouse hepatocytes were found to adhere much stronger to intact native type I collagen than to native, telopeptide-devoid collagen. Removal of telopeptides (by pepsin treatment) caused disintegration of supramolecular collagen aggregates. Similar differences in hepatocyte adhesion were observed between oligomeric and m...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1993.1827
更新日期:1993-07-15 00:00:00
abstract::This study aimed to investigate possible feedback mechanisms in the control of collagenase (matrix metalloproteinase-1) and tissue inhibitor of metalloproteinases (TIMP-1). Procollagenase, active collagenase, TIMP-1 and collagenase-TIMP complex were applied to human skin and synovial fibroblasts for 48 hours, the cell...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1994.2264
更新日期:1994-09-15 00:00:00
abstract::The effect of opioids on NO production by LPS-stimulated murine macrophages J774 has been investigated. Morphine (mu and k opioid receptor agonist), DAGO (selective mu receptor agonist) and U50-488H (selective k receptor agonist), added (10(-10)-10(-6) M) to the cells 0.5 h before activation with LPS, significantly in...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1995.2065
更新日期:1995-07-26 00:00:00
abstract::The octaheme cytochrome c3 (Mr 26000) from Desulfovibrio desulfuricans Norway was studied using cyclic voltammetry at the pyrolytic graphite electrode. The kinetics of reduction of the octaheme cytochrome c3 (Mr 26000) from D. desulfuricans Norway by the Ni-Fe-Se hydrogenase purified from the same organism was investi...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/0006-291x(91)91414-8
更新日期:1991-08-30 00:00:00
abstract::The aim of this study was to illustrate the further process of 24p3 protein after association with epididymal spermatozoa. We have previously identified a caput-initiated 24p3 protein, which interacts with the spermatozoa surface in vitro. In the present study, we investigate another role of the 24p3 protein with sper...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2004.05.091
更新日期:2004-07-09 00:00:00
abstract::Pinin (Pnn) is a nuclear speckle-associated SR-like protein. The N-terminal region of the Pnn protein sequence is highly conserved from mammals to insects, but the C-terminal RS domain-containing region is absent in lower species. The N-terminal coiled-coil domain (CCD) is, therefore, of interest not only from a funct...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2013.11.108
更新日期:2014-01-03 00:00:00
abstract::The cDNA encoding a swelling-induced chloride conductance regulatory protein, plcln, was cloned from rabbit ciliary epithelium by using a polymerase chain reaction (PCR)-based approach. The open reading frame encoding 236 amino acids possesses high amino acid identity (93/%) with the previously cloned plcln from human...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1997.7523
更新日期:1997-10-29 00:00:00
abstract::Exploring the molecular mechanisms that regulate the osteogenesis of human mesenchymal stem cells (hMSCs) will bring us more efficient methods for improving the treatment of bone-related diseases. In this study, we analyzed the effects of miR-31 on the osteogenesis of hMSCs. The overexpression of miR-31 repressed the ...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2014.02.058
更新日期:2014-03-28 00:00:00
abstract::Endo-beta-1,4-xylanase X-I is a major hydrolase produced by the aleurone tissue of germinating barley grain. It was previously reported that this cytosolic enzyme is synthesized as an inactive precursor which is proteolytically processed to active forms upon its programmed cell death dependent release. We here demonst...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2007.03.066
更新日期:2007-05-11 00:00:00
abstract::Ribosomal S6 protein kinase 4 (RSK4) was known as a novel tumor suppressor gene, and the tumor necrosis factor receptor-associated factor 4 (TRAF4) was linked to carcinogenesis. The purpose of this study is to further investigate the effect of the TRAF4 gene on cell proliferation, invasion and metastasis in vivo and e...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2018.04.164
更新日期:2018-06-07 00:00:00
abstract::Oxidative stress is involved in a multitude of pathological conditions. In the present study, cell cycle arrest was demonstrated in monolayer cultures of Chinese hamster ovary cells subjected to low-level oxidative stress induced by the addition of hydrogen peroxide. Fluorescence-activated cell sorting analysis charac...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1995.1645
更新日期:1995-05-05 00:00:00
abstract::Efonidipine is a dual L-/T- type calcium channel blocker with a slow onset of action and a long lasting effect that exibihits antihypertensive and nephroprotective effects. differs from most other DHPs which can induce reflex tachycardia. Efonidipine reduces blood pressure without decreasing cardiac output and exerts ...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2019.03.176
更新日期:2019-06-04 00:00:00
abstract::The transcriptional regulator BrlR is a member of the MerR family of multidrug transport activators in Pseudomonas aeruginosa. Recent study indicates that BrlR is a novel 3',5'-cyclic diguanylic acid (c-di-GMP) receptor and can be activated by c-di-GMP. To gain insight into BrlR function, we determined the structure o...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2017.06.033
更新日期:2017-08-19 00:00:00
abstract::The tumor necrosis factor (TNF) related apoptosis-inducing ligand (TRAIL or Apo2L) and its receptors are members of the tumor necrosis factor superfamily. TRAIL triggers apoptosis by binding to its two proapoptotic receptors DR4 and DR5, a process which is negatively regulated by binding of TRAIL to its two decoy rece...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.2000.4218
更新日期:2001-01-26 00:00:00
abstract::The appearance of Fas receptor at the surface of pancreatic beta-cells affected by progressive insulitis strongly suggests that Fas-mediated beta-cell apoptosis plays an important role in the pathogenesis of type 1 diabetes. In support of this concept, the present study has shown that islet cells from NOD mice and the...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.2001.6215
更新日期:2002-01-11 00:00:00
abstract::The molecular structures of enzyme mimics may be modified to optimize their catalytic properties. In this study, to generate artificial enzyme mimics, Watson-Crick base paired DNA duplexes were designed as scaffolds which were assembled by nucleotides modified with specific functional groups. This process allowed vari...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2013.03.106
更新日期:2013-05-10 00:00:00
abstract::The ability to identify apoptotic cells within a complex population is crucial in the research and diagnosis of normal physiology and disease states. The Cellscan mark S (CS-S) cytometer was used in this study to detect intracellular fluorescence intensity and polarization (FI and FP) in several well-established model...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1999.1934
更新日期:2000-02-05 00:00:00
abstract::To simultaneously assess the effects of exonic mutations on RNA splicing and protein functions, we report here an intron-inclusive cDNA (Intinc) expression system. As a test model, twenty-four mutations in exon 9 of the phenylalanine hydroxylase (PAH) gene were examined in an Intinc expression plasmid composed of the ...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2008.06.072
更新日期:2008-09-05 00:00:00
abstract::Although many advances have been made in the treatment of gastric cancer (GC), numerous difficulties, such as the emergence of chemo-drug resistance, continue to lead to disappointing GC prognoses. Thus, novel alternative strategies are urgently needed. The use of natural products could be a viable option to treat GC....
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2018.09.093
更新日期:2018-10-20 00:00:00
abstract::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 ma...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/0006-291x(89)92756-3
更新日期:1989-12-29 00:00:00
abstract::Growing evidences show that functionally relevant polymorphisms in various promoters alter both transcriptional activity and affinities of existing protein-DNA interactions, and thus influence disease progression in humans. We previously reported the -94G>T CFTR promoter variant in a female CF patient in whom any know...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2007.07.091
更新日期:2007-09-28 00:00:00
abstract::Transgenic (TG) mice expressing porcine GH receptor (pGHR) directed by a 762-bp proximal leptin promoter were used to analyze the capability of the promoter to drive and regulate pGHR expression in vivo. Transgene expression occurred in inguinal, retroperitoneal, and epididymal/parametrial fat depots in both male and ...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1999.1176
更新日期:1999-08-19 00:00:00
abstract::The adhesion of cancer cells to the extracellular matrix (ECM) is crucial for cell proliferation, survival, and metastasis. Thus, it is necessary to inhibit cell-ECM adhesion by blocking the activation of the associated signaling to control cancer. Here, we identify erybraedin A (EBA) as a potential Src inhibitor that...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2018.05.137
更新日期:2018-07-07 00:00:00
abstract::The 3-deoxy-octulosonic acid-containing trisaccharide was isolated from the carbohydrate material obtained after the acid hydrolysis of lipopolysaccharides of Hafnia alvei strains 2 and 1211 using gel filtration. For purification the trisaccharide fraction was rechromatographed on a Bio-Gel P2 column. On the basis of ...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1006/bbrc.1993.1929
更新日期:1993-08-16 00:00:00
abstract::The nuclear-mitochondrial stringent response was examined in isonuclear rho+, 21S rRNA-containing rho-, and rho o strains of S. cerevisiae. By 30 min after nutritional downshift, nuclear rDNA transcription falls to 15% of control levels congruently in all strains, as assayed via whole-cell RNA or by hybrid selection o...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/0006-291x(89)91727-0
更新日期:1989-10-16 00:00:00
abstract::1-4 interaction scaling factors are used in AMBER forcefields to reduce the exaggeration of short-range repulsion caused by the 6-12 Lennard-Jones potential and a nonpolarizable charge model and to obtain better agreements of small-molecule conformational energies with experimental data. However, the effects of these ...
journal_title:Biochemical and biophysical research communications
pub_type: 杂志文章
doi:10.1016/j.bbrc.2014.12.084
更新日期:2015-02-06 00:00:00