Abstract：
:Microtubules are made up of tubulin protein and play a very important part in numerous cellular events of eukaryotic cells, which is why they are seen as attractive targets for tumor chemotherapy. BNC105, a known vascular targeting agent, has entered in phase II clinical trials. It has previously been confirmed that BNC105 is an effective microtubule targeting agent for various cancers. BNC105 exhibits selectivity for tumor cells, elicits vascular disrupting effects, and inhibits tumor growth. However, the molecular mechanism of BNC105 is still elusive. Herein, the crystal structure of BNC105 in complex with tubulin protein is revealed, demonstrating the its interaction with the colchicine binding site. In order to thoroughly evaluate its molecular mechanism from a structural-activity-relationship standpoint, the binding mode of tubulin to BNC-105 is compared with colchicine, CA-4 and other BNC-105 derivatives. Our study not only confirms the detailed interactions of the BNC105-tubulin complex, but also offer substantial structural foundation for the design and development of novel benzo[b]furan derivatives as microtubule targeting agents.
journal_name
Biochem Biophys Res Communjournal_title
Biochemical and biophysical research communicationsauthors
Wang T,Wu C,Wang C,Zhang G,Arnst KE,Yao Y,Zhang Z,Wang Y,Pu D,Li Wdoi
10.1016/j.bbrc.2019.12.083subject
Has Abstractpub_date
2020-02-18 00:00:00eissn
0006-291Xissn
1090-2104pii
S0006-291X(20)30008-5pub_type
杂志文章abstract：:Capsaicin has been reported to regulate blood glucose levels and to ameliorate insulin resistance in obese mice. This study demonstrates that capsaicin increases glucose uptake directly by activating AMP-activated protein kinase (AMPK) in C2C12 muscle cells, which manifested as an attenuation of glucose uptake when co...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2013.08.027
更新日期：2013-09-13 00:00:00
abstract：:Ca2+/calmodulin-dependent protein kinases are implicated in regulating the Ca2+ signaling involved in T cell activation and in thymocyte selection. One of the earliest events in signaling through the T cell antigen receptor is activation of the protein tyrosine kinase p56lck. Following T cell activation or signaling t...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1994.1010
更新日期：1994-01-14 00:00:00
abstract：:The trans-translation system in bacteria promotes recycling of stalled ribosomes and targets incomplete peptides for proteolysis. In Escherichia coli, loss of trans-translation function has little effect on growth under normal laboratory conditions. Among the subtle phenotypes of tmRNA-deficient mutants is the inabili...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2007.03.142
更新日期：2007-05-25 00:00:00
abstract：:The hepatic microsomal monooxygenase system was studied in hypophysectomized male rats exposed for 24 or 48 h to PB and/or TPA, an activator of kinase C. TPA attenuated basal and PB-induced levels of P450, aniline hydroxylase (ANH), ethylmorphine demethylase (EDM) and cytochrome c reductase. Hence, PB may effect induc...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/s0006-291x(88)81155-0
更新日期：1988-06-16 00:00:00
abstract：:With the development of a culture method for stratified squamous epithelial cells, tissue-engineered epithelial cell sheets have been successfully applied as clinical cell grafts. However, the implementation of these cell sheets without the use of any animal-derived materials is highly desirable. In this study, Rho-as...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2015.02.120
更新日期：2015-05-01 00:00:00
abstract：:Analysis of a 67 kDa lipid-dependent Ca(2+)-binding protein from avian matrix vesicles revealed amino acid sequences homologous to mammalian annexin VI. PCR methods were used to identify a clone from an avian cDNA library that contained a full length copy of the 67-kDa annexin cDNA. This was restriction mapped, subclo...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1993.2515
更新日期：1993-12-15 00:00:00
abstract：:This report describes the in vivo phosphorylation of isocitrate lyase and examines the possible consequences to the control of the Kreb's cycle and glyoxylate bypass. NADP-specific isocitrate dehydrogenase from E. coli was the first bacterial protein whose enzymic activity was shown to be modulated by reversible phosp...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/s0006-291x(88)81177-x
更新日期：1988-06-16 00:00:00
abstract：:Bovine brain-derived growth factor (BDGF) is a approximately 16-17 kD polypeptide mitogen with a broad spectrum of cell specificity. Using a highly specific mouse polyclonal anti-BDGF antiserum for indirect immunoperoxidase and immunofluorescent stainings, BDGF was found to be specifically localized in the neurons of ...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/s0006-291x(87)80478-3
更新日期：1987-04-14 00:00:00
abstract：:Overexpression in Escherichia coli of the fdx4 gene from Aquifex aeolicus has allowed isolation and characterization of the first hyperthermophilic [2Fe-2S](Scys)(4) protein, a homodimer of M = 2 x 12.4 kDa with one [2Fe-2S] cluster per subunit. This protein is undamaged by heating to 100 degrees C for at least three ...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1999.1138
更新日期：1999-08-11 00:00:00
abstract：:Serine palmitoyltransferase long chain-1 (SPTLC1), which is the rate-limiting enzyme for sphingolipid biosynthesis, has been indicated to be essential for carcinoma cell survival and proliferation in recent, but its role in the regulation of renal cell carcinoma (RCC) remains unknown. In the present study, we found th...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2019.09.073
更新日期：2019-11-26 00:00:00
abstract：:The present study characterizes constitutively expressed rat testicular interleukin-1alpha (IL-1alpha) proteins. IL-1 bioactivity of crude testis protein was completely neutralized by IL-1alpha antiserum, IL-1 receptor antagonist, and soluble type I IL-1 receptor. Upon non-denaturating gel permeation chromatography, b...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/s0006-291x(02)02239-8
更新日期：2002-09-27 00:00:00
abstract：:Agmatine, a putative endogenous ligand of imidazoline receptors, suppresses cardiovascular function by inhibiting peripheral sympathetic tone. However, the molecular identity of imidazoline receptor subtypes and its cellular mechanism underlying the agmatine-induced sympathetic suppression remains unknown. Meanwhile, ...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2016.06.086
更新日期：2016-08-26 00:00:00
abstract：:We have analyzed heteroplasmy of mitochondrial DNA in clonal cultures from two patients with Kearns-Sayre syndrome, and have found that individual muscle or fibroblast clones contained either a mixed (i.e. heteroplasmic) population of normal and deleted mitochondrial DNAs, or only normal mitochondrial DNAs (i.e. homop...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(89)92499-6
更新日期：1989-04-28 00:00:00
abstract：:Spin-trapping of superoxide ion, O2-, which is produced from two different sources (OH(-)-DMSO and xanthine-xanthine oxidase systems), was investigated by use of a water-soluble, notroso-aromatic spin trap, sodium 3,5-dibromo-4-nitrosobenzene-sulfonate (DBNBS). It was found that O2- from all sources was easily trapped...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(86)90491-2
更新日期：1986-04-29 00:00:00
abstract：:In humans, mutations in the gene encoding cereblon (CRBN) are associated with mental retardation. Although CRBN has been investigated in several cellular contexts, its function remains unclear. Here, we demonstrate that CRBN plays a role in regulating the ubiquitin-proteasome system (UPS). Heterologous expression of C...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2012.09.108
更新日期：2012-10-26 00:00:00
abstract：:Animals and plants respond to bacterial infections and environmental stresses by inducing overlapping repertoires of defense genes. How the signals associated with infection and abiotic stresses are differentially integrated within a whole organism remains to be fully addressed. We show that the transcription of a Cae...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2007.08.190
更新日期：2007-11-16 00:00:00
abstract：:Septins, a conserved family of GTPases, are heteropolymeric filament-forming proteins that associate with the cell membrane and cytoskeleton and serve essential functions in cell division and morphogenesis. Their roles in fungal cell wall chitin deposition, septation, cytokinesis, and sporulation have been well establ...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2011.01.017
更新日期：2011-02-11 00:00:00
abstract：:Protein Z was purified from rabbit liver cytosol by affinity chromatography on oleic acid-agarose and preparative sodium dodecyl sulfate-polyacrylamide gel electrophoresis. After removal of sodium dodecyl sulfate, the renatured protein was found to bind heme and bilirubin with a Kd of approximately 1 microM which prod...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(85)91172-6
更新日期：1985-10-30 00:00:00
abstract：:miRNAs are approximately 21nt non-coding RNAs and play important roles in plant development and response to stress. Symbiotic nitrogen fixation (SNF) is agronomically important for reducing the need of nitrogen fertilizers. The soybean root nodule is the place where SNF takes place. To identify miRNAs that are possibl...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2008.11.140
更新日期：2009-01-23 00:00:00
abstract：:The effect of several agents known to interact with muscarinic acetylcholine receptors on the release of choline from slices of rat corpus striatum into the incubation medium has been investigated. The amount of released choline was increased if choline, acetylcholine, or oxotremorine had been added to the incubation ...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/s0006-291x(84)80206-5
更新日期：1984-05-16 00:00:00
abstract：:We have previously observed that extracellular Mg2+ influences the phosphofructokinase (PFK) activity of intact Ehrlich Ascites tumour cells (EATC). In this study we have investigated the mechanism by which Mg2+ modulates this key glycolytic enzyme in EATC made permeable to the cation by either digitonin or dextran su...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(91)91917-2
更新日期：1991-09-16 00:00:00
abstract：:Alkaline elastase YaB, produced by alkalophilic Bacillus YaB, is an extracellular serine protease having 55% homology to subtilisin BPN' and thus could be called subtilisin YaB. It is synthesized as a 378-amino acid preproenzyme and secreted into the culture medium as a 265-amino acid mature protease. To examine if th...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1006/bbrc.1996.0256
更新日期：1996-02-15 00:00:00
abstract：:Gastrointestinal (GI) anthrax, caused by the bacterial infection of Bacillus anthracis, posts a significant bioterrorism threat by its relatively high mortality rate in humans. Different from inhalational anthrax by the route of infection, accumulating evidence indicates the bypass of vegetative bacteria across GI epi...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2010.02.091
更新日期：2010-04-02 00:00:00
abstract：:Incubation of primary neuronal cultures prepared from the brains of neonatal rats with 50 microM epinephrine resulted in the transient redistribution of protein kinase C from the cytosol to the particulate fraction. This effect occurred after 1 and 5 min of incubation and resulted in a decrease in cytosolic protein ki...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(90)91906-9
更新日期：1990-01-15 00:00:00
abstract：:Vascular pericytes and smooth muscle cells surround many blood vessels of the body. Their primary roles include vessel stabilization and regulation of the blood flow. The high degree of heterogeneity among these cells is dictated by (1) differences in their developmental origin and (2) their location in the vascular b...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2019.03.143
更新日期：2019-05-21 00:00:00
abstract：:Pseudohypoaldosteronism type II (PHAII), an autosomal dominant disorder characterized by hypertension, hyperkalemia, and hyperchloremic acidosis, is reportedly due to mutations in WNK1 and WNK4 kinase genes. However, the pathogenesis of the disease remains unknown. Mutations in the WNK1 gene are the deletions in the f...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2006.08.101
更新日期：2006-10-20 00:00:00
abstract：:In this study, acetosyringone was identified as one of the major extracellular phenolics in tobacco suspension cells and was shown to have bioactive properties that influence early events in plant-bacterial pathogenesis. In our model system, tobacco cell suspensions treated with bacterial isolate Pseudomonas syringae ...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2004.12.153
更新日期：2005-03-04 00:00:00
abstract：:An intein is a polypeptide that interrupts the functional domains of a protein, called the exteins. The intein can facilitate its own excision from the exteins, concomitant with the ligation of the exteins, in a process called protein splicing. The alpha subunit of the ribonucleotide reductase of the extreme thermophi...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2009.06.145
更新日期：2009-09-11 00:00:00
abstract：:Translation initiation factor 5B (IF5B) is required for initiation of protein synthesis. The solution structure of archaeal IF5B (aIF5B) was analysed by small-angle X-ray scattering (SAXS) and dynamic light scattering (DLS) and was indicated to be in both monomeric and dimeric form. Sedimentation equilibrium (SE) anal...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/j.bbrc.2011.11.012
更新日期：2011-12-09 00:00:00
abstract：:Using minimum energy calculations and molecular dynamics techniques the preferred conformational states of LHRH and its analogues have been reported to involve a modified beta-bend between residues 5 to 8. Based on some of these models cyclic peptide analogues of LHRH antagonists were synthesised using solid phase pep...
journal_title：Biochemical and biophysical research communications
pub_type： 杂志文章
doi：10.1016/0006-291x(89)92224-9
更新日期：1989-03-31 00:00:00
