Abstract：
:The dietary flavonoid quercetin has a broad range of biological activities, including potent antitumor activity against several types of tumors. Recently, it has been shown that quercetin inhibits cancer cells proliferation by depleting cellular microtubules and perturbing cellular microtubule functions. However, the direct interactions of quercetin with tubulin and microtubules have not been examined so far. Here, we found that quercetin inhibited polymerization of microtubules and depolymerized microtubules made from purified tubulin in vitro. The binding of quercetin with tubulin was studied using quercetin fluorescence and intrinsic tryptophan fluorescence of tubulin. Quercetin bound to tubulin at a single site with a dissociation constant of 5-7 microM, and it specifically inhibited colchicine binding to tubulin but did not bind at the vinblastine site. In addition, quercetin perturbed the secondary structure of tubulin, and the binding of quercetin stimulated the intrinsic GTPase activity of soluble tubulin. Further, quercetin stabilized tubulin against decay and protected two cysteine residues of tubulin toward chemical modification by 5,5'-dithiobis-2-nitrobenzoic acid. Our data demonstrated that the binding of quercetin to tubulin induces conformational changes in tubulin and a mechanism through which quercetin could perturb microtubule polymerization dynamics has been proposed. The data suggest that quercetin inhibits cancer cells proliferation at least in part by perturbing microtubule functions through tubulin binding.
journal_name
Biochemistryjournal_title
Biochemistryauthors
Gupta K,Panda Ddoi
10.1021/bi025952rsubject
Has Abstractpub_date
2002-10-29 00:00:00pages
13029-38issue
43eissn
0006-2960issn
1520-4995pii
bi025952rjournal_volume
41pub_type
杂志文章相关文献
BIOCHEMISTRY文献大全abstract：:The photocycle of the blue-light photoreceptor protein Photoactive Yellow Protein (PYP) was studied at reduced relative humidity (RH). Photocycle kinetics and spectra were measured in thin films of PYP in which the relative humidity was set at values between 29 and 98% RH with saturated solutions of various salts. We ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi050237d
更新日期：2005-06-28 00:00:00
abstract：:Although the importance of interactions involving both the cytosolic and transmembrane regions of SecY and SecE has been documented, no information has been available for the physical contact sites of these translocase subunits in their cytosolic domains. We now carried out site-specific cross-linking experiments to i...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi034333v
更新日期：2003-06-24 00:00:00
abstract：:Class A beta-lactamases hydrolyze penicillins and other beta-lactams via an acyl-enzyme catalytic mechanism. Ser70 is the active site nucleophile. By constructing the S70A mutant, which is unable to form the acyl-enzyme intermediate, it was possible to make stable ES complexes with various substrates. The stability of...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi9928041
更新日期：2000-05-30 00:00:00
abstract：:Lactate dehydrogenase (LDH) catalyzes the interconversion between pyruvate and lactate with nicotinamide adenine dinucleotide (NAD) as a cofactor. Using isotope-edited difference Fourier transform infrared spectroscopy on the "live" reaction mixture (LDH·NADH·pyruvate ⇌ LDH·NAD(+)·lactate) for the wild-type protein an...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi500215a
更新日期：2014-03-25 00:00:00
abstract：:The solution structure of the 63-residue heregulin-alpha (HRG-alpha) epidermal growth factor (EGF)-like domain, corresponding to residues 177-239 of HRG-alpha, has been determined to high resolution using data from two-dimensional and three-dimensional homo- and heteronuclear NMR spectroscopy. The structure is based o...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi952626l
更新日期：1996-03-19 00:00:00
abstract：:Large primary deuterium kinetic isotope effects (1° DKIEs) on enzyme-catalyzed hydride transfer may be observed when the transferred hydride tunnels through the energy barrier. The following 1° DKIEs on kcat/ Km and relative reaction driving force are reported for wild-type and mutant glycerol-3-phosphate dehydrogenas...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/acs.biochem.8b00536
更新日期：2018-07-24 00:00:00
abstract：:Activation of a growth factor receptor tyrosine kinase (RTK) is accompanied by a rapid autophosphorylation of the receptor on tyrosine residues. Receptor activation has been shown to promote the association of signal-transducing proteins containing SH2 domains (second domain of src homology). These receptor-associated...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00089a028
更新日期：1993-09-28 00:00:00
abstract：:It has been shown by genetic analysis that the external and internal invertases from Saccharomyces cerevisiae share a common structural gene [Taussig, R., & Carlson, M. (1983) Nucleic Acids Res. 11, 1943-1954]. However, the only amino acid composition of these two forms of invertase reported to date has revealed exten...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00343a014
更新日期：1985-10-22 00:00:00
abstract：:Phosphatidic (PtdOH) acid formation is recognized as an important step in numerous signaling pathways in both plants and mammals. To study the role of this lipid in signaling pathways, it is of major interest to be able to increase the amount of this lipid directly. Therefore, "caged" PtdOH was synthesized, which rele...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi0351460
更新日期：2004-04-13 00:00:00
abstract：:The class C serine beta-lactamase of Enterobacter cloacae P99 was inhibited by a series of aryl methylphosphonate monoester monoanions. The effectiveness of these inhibitors was promoted by an acylamido substituent on the methyl group and a good leaving group at phosphorus. The former preference suggests that noncoval...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00140a024
更新日期：1992-06-30 00:00:00
abstract：:Diethyl pyrocarbonate (DEP) is an electrophilic reagent that is used to modify reversibly the histidine residues of proteins. Unfortunately, the lability of the acylated histidine adduct usually does not permit the isolation and identification of the modified histidine. By use of 500-MHz proton NMR spectroscopy, it ha...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00445a004
更新日期：1989-09-19 00:00:00
abstract：:Variations for non-histones in the ADP-ribosylating activities of interphase and metaphase cells were investigated. 32P-Labeled nicotinamide adenine dinucleotide ([32P]NAD), the specific precursor for the modification, was used to radioactively label proteins. Permeabilized interphase and mitotic cells, as well as iso...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00323a017
更新日期：1985-01-15 00:00:00
abstract：:The signaling apparatus that controls bacterial chemotaxis is composed of a core complex containing chemoreceptors, the histidine autokinase CheA, and the coupling protein CheW. Site-specific spin labeling and pulsed dipolar ESR spectroscopy (PDS) have been applied to investigate the structure of a soluble ternary com...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi100055m
更新日期：2010-05-11 00:00:00
abstract：:A hallmark of penicillin-binding protein 2 (PBP2) from penicillin-resistant strains of Neisseria gonorrhoeae is insertion of an aspartate after position 345. The insertion resides on a loop near the active site and is immediately adjacent to an existing aspartate (Asp346) that forms a functionally important hydrogen b...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi5011317
更新日期：2014-12-09 00:00:00
abstract：:In mammalian cells, the incorporation of the 21st amino acid, selenocysteine, into proteins is guided by the Sec machinery. The function of this protein complex requires several protein-protein and protein-RNA interactions, leading to the incorporation of selenocysteine at UGA codons. It is guided by stem-loop structu...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/acs.biochem.6b01116
更新日期：2017-05-02 00:00:00
abstract：:The anaerobic global regulator FNR from Escherichia coli is a [4Fe-4S](2+) cluster-containing dimer that is inactivated by O(2) through disruption of the Fe-S cluster and conversion to the monomeric apoprotein. It was shown that apo-FNR is subject to ClpXP proteolysis, and two recognition sites, amino acids 5-11 and a...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi2018688
更新日期：2012-06-26 00:00:00
abstract：:A solubilized preparation of steroid 5 alpha-reductase (EC 1.3.1.30) from rat liver has been used in studies focused toward an understanding of the kinetic mechanism associated with enzyme catalysis. From the results of analyses with product and dead-end inhibitors, a preferentially ordered binding of substrates and r...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00463a025
更新日期：1990-03-20 00:00:00
abstract：:Ks values for binding of selected substrates, competitive inhibitors, and a noncompetitive inhibitor were found to be similar for alpha-chymotrypsin and N-methyl-alpha-chymotrypsin. The rates and steps of binding of a competitive inhibitor and a noncompetitive inhibitor were also found to be similar for alpha-chymotry...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00262a017
更新日期：1982-09-14 00:00:00
abstract：:Internal fatty acylation of proteins is a recognized means of modifying biological behavior. Escherichia coli hemolysin A (HlyA), a toxic protein, is transcribed as a nontoxic protein and made toxic by internal acylation of two lysine residue epsilon-amino groups; HlyC catalyzes the acyl transfer from acyl-acyl carrie...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi990138y
更新日期：1999-07-06 00:00:00
abstract：:We have mapped the interface between the two transmembrane alpha-helices in the membrane domain of the Escherichia coli enzyme leader peptidase by analyzing disulfides formed between pairs of cysteine residues introduced near their respective periplasmic ends. The interface is formed primarily from aliphatic amino aci...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00084a020
更新日期：1993-08-24 00:00:00
abstract：:Human immunodeficiency virus type 1 protease (HIV-1 PR) is an essential enzyme in the HIV-1 life cycle. As such, this protein represents a major drug target in AIDS therapy, but emerging resistance to antiretroviral inhibitor cocktails, caused by high viral mutation rates, represents a significant challenge in AIDS tr...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi100569u
更新日期：2010-05-18 00:00:00
abstract：:An aminoglycoside 3-acetyltransferase [AAC(3)], possibly a new isoenzymic species of the 3-N-acetyltransferase group, was purified to apparent homogeneity from a crude extract of Pseudomonas aeruginosa, a gentamicin-resistant clinical isolate. The method of purification was consecutive column chromatography--(i) gel f...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00534a009
更新日期：1982-03-02 00:00:00
abstract：:The early steps of the proposed mechanistic pathway for dehydroquinate synthase have been probed with a series of substrate analogues. These analogues, 3-9, are structurally prohibited from undergoing the beta-elimination of inorganic phosphate that represents the committed step in the conversion of the substrate 3-de...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00445a010
更新日期：1989-09-19 00:00:00
abstract：:The envelope glycoprotein (G protein) of vesicular stomatitis virus probably exists in the viral envelope as a trimer of identical subunits. Depending on the conditions of solubilization, G protein may dissociate into monomers. G protein solubilized with the detergent octyl glucoside was shown to exist as oligomeric f...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00462a002
更新日期：1990-03-13 00:00:00
abstract：:Phytochromes are widespread red/far-red photosensory proteins well known as critical regulators of photomorphogenesis in plants. It is often assumed that natural selection would have optimized the light sensing efficiency of phytochromes to minimize nonproductive photochemical deexcitation pathways. Surprisingly, the ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi500108s
更新日期：2014-05-06 00:00:00
abstract：:The gene 5 protein (g5p) encoded by filamentous Ff phages is an ssDNA-binding protein, which binds to and sequesters the nascent ssDNA phage genome in the process of phage morphogenesis. The g5p also binds with high affinity to DNA and RNA sequences that form G-quadruplex structures. However, sequences that would form...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi030177g
更新日期：2004-03-09 00:00:00
abstract：:The photosynthetic antenna of Chloroflexus aurantiacus includes bacteriochlorophyll (BChl) C740 and BChl a792, both of which occur in chlorosomes, and B808-866 (containing BChl a808 and BChl a866), which is membrane-located (subscripts refer to near-infrared absorption maxima in vivo). BChl a792 is thought to mediate ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00400a024
更新日期：1987-12-29 00:00:00
abstract：:Cysteine desulfurases (CDs) are pyridoxal-5'-phosphate (PLP)-dependent enzymes that cleave sulfur from cysteine via an enzyme cysteinyl persulfide intermediate. In vitro studies of these enzymes have generally employed dithiothreitol as a cosubstrate to reductively cleave the persulfide intermediate, and it has been s...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi049143e
更新日期：2004-09-28 00:00:00
abstract：:DNA-dependent synthesis of beta-galactosidase was optimized in extracts made from cells lysed by a standard French pressure cell. Extracts made at 3200 psi synthesized up to 25-fold more beta-galactosidase than extracts made at 7500 psi. beta-Galactosidase synthesis was cyclic 3', 5' AMP dependent, as expected, and in...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00624a016
更新日期：1977-03-08 00:00:00
abstract：:The gamma subunits of the 7S nerve growth factor complex (7S NGF) display arginine esteropeptidase activity. By varying the conditions of electrophoresis in acrylamide gel, it has been demonstrated that the gamma-subunit fraction of 7S NGF contains five different proteins, in contrast to the three (gamma1, gamma2, and...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00652a016
更新日期：1976-04-06 00:00:00
