Abstract：
:The kinetics of inhibition of dialkylglycine decarboxylase by five aminophosphonate inhibitors are presented. Two of these [(R)-1-amino-1-methylpropanephosphonate and (S)-1-aminoethanephosphonate] are slow binding inhibitors. The inhibitors follow a mechanism in which a weak complex is rapidly formed, followed by slow isomerization to the tight complex. Here, the tight complexes are bound 10-fold more tightly than the weak, initial complexes. The slow onset inhibition occurs with t(1/2) values of 1.3 and 0.55 min at saturating inhibitor concentrations for the AMPP and S-AEP inhibitors, respectively, while dissociation of these inhibitor complexes occurs with t(1/2) values of 13 and 4.6 min, respectively. The X-ray structures of four of the inhibitors in complex with dialkylglycine decarboxylase have been determined to resolutions ranging from 2.6 to 2.0 A, and refined to R-factors of 14.5-19.5%. These structures show variation in the active site structure with inhibitor side chain size and slow binding character. It is proposed that the slow binding behavior originates in an isomerization from an initial complex in which the PLP pyridine nitrogen-D243 OD2 distance is approximately 2.9 A to one in which it is approximately 2.7 A. The angles that the C-P bonds make with the p orbitals of the aldimine pi system are correlated with the reactivities of the analogous amino acid substrates, suggesting a role for stereoelectronic effects in Schiff base reactivity.
journal_name
Biochemistryjournal_title
Biochemistryauthors
Liu W,Rogers CJ,Fisher AJ,Toney MDdoi
10.1021/bi026318gsubject
Has Abstractpub_date
2002-10-15 00:00:00pages
12320-8issue
41eissn
0006-2960issn
1520-4995pii
bi026318gjournal_volume
41pub_type
杂志文章相关文献
BIOCHEMISTRY文献大全abstract：:Previous studies have shown that protein 4.1 is a multifunctional protein that binds to spectrin, actin, glycophorins, the anion channel protein, and phosphatidylserine (PS). In this report, we have characterized the binding of protein 4.1 and its major proteolytic fragments to phospholipid vesicles. Pure 125I-labeled...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00402a018
更新日期：1988-01-26 00:00:00
abstract：:The enthalpies of transfer of hen egg white lysozyme from water to aqueous solutions of 1-propanol were determined by isothermal flow calorimetry at 10, 17, 25, and 40 degrees C in 0.04 M, pH 2 glycine buffer. Alcohol concentrations up to 3.4 M were employed. Four regions in the dependence of the enthalpy of transfer ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00514a016
更新日期：1981-05-26 00:00:00
abstract：:The solution conformation of the ribonuclease barnase has been determined by using 1H nuclear magnetic resonance (NMR) spectroscopy. The 20 structures were calculated by using 853 interproton distance restraints obtained from analyses of two-dimensional nuclear Overhauser spectra, 72 phi and 53 chi 1 torsion angle res...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00099a030
更新日期：1991-09-03 00:00:00
abstract：:The third intracellular loop (IL3) of G protein-coupled receptors (GPCRs) is an important contact domain between GPCRs and their G proteins. Previously, the IL3 of Ste2p, a Saccharomyces cerevisiae GPCR, was suggested to undergo a conformational change upon activation as detected by differential protease susceptibilit...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi200254h
更新日期：2011-08-16 00:00:00
abstract：:The C2 domain is a Ca2+-dependent, membrane-targeting motif originally discovered in protein kinase C and recently identified in numerous eukaryotic signal-transducing proteins, including cytosolic phospholipase A2 (cPLA2) of the vertebrate inflammation pathway. Intracellular Ca2+ signals recruit the C2 domain of cPLA...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi9717340
更新日期：1997-10-07 00:00:00
abstract：:Volumes of lipid dispersions as a function of temperature have been measured for two different kinds of binary mixtures of lecithins, (1) DMPC and DSPC and (2) DMPC and DC20PC. Emphasis was placed on DMPC-rich compositions so as to resolve ambiguities regarding solid-phase immiscibility in DMPC-DSPC mixtures. Special ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00586a032
更新日期：1979-09-18 00:00:00
abstract：:The successive high-resolution differential scanning calorimetric (DSC) thermograms for aqueous dispersions of a homologous series of mixed-chain phosphatidylcholines, C(X):C(X + 6)PC, have been recorded and analyzed. In this series of saturated mixed-chain phosphatidylcholines, the total number of carbon atoms in the...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00482a018
更新日期：1990-07-31 00:00:00
abstract：:Propeptide processing occurs in specific compartments of the secretory pathway, but how these processing-competent organelles are generated from their processing-incompetent precursor compartments is unknown. To dissect the process biochemically, we have developed a novel cell-free system reconstituting the production...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi0112762
更新日期：2001-10-30 00:00:00
abstract：:The active-site zinc in human glutathione-dependent formaldehyde dehydrogenase (FDH) undergoes coenzyme-induced displacement and transient coordination to a highly conserved glutamate residue (Glu-67) during the catalytic cycle. The role of this transient coordination of the active-site zinc to Glu-67 in the FDH catal...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi052554q
更新日期：2006-04-18 00:00:00
abstract：:Bacterial NO synthase (NOS)-like proteins such as that from Bacillus subtilis (bsNOS) share a high degree of structural homology with the oxygenase domain of mammalian NOSs (mNOSs), but biochemical studies have yet failed to establish that they are specifically capable of producing NO. To better understand the actual ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi051710q
更新日期：2006-02-07 00:00:00
abstract：:The 600-MHz proton spectrum of dethiobiotin (prepared from d-biotin with Raney nickel) was measured in order to gain information pertaining to its stereochemical homogeneity. The spectrum demonstrated clearly that the material is a 6:1 mixture of two stereoisomers. The cis compound, corresponding to the stereochemistr...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00307a002
更新日期：1984-06-05 00:00:00
abstract：:Ultraviolet absorption (UV) and circular dichroism (CD) spectra of wheat germ 5S RNA, when compared to tRNAPhe, indicate a largely base-paired and base-stacked helical structure, containing up to 36 base pairs. Fourier-transform infrared (FT-IR) spectra of tRNAPhe and wheat germ ribosomal 5S RNA have been acquired at ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00311a012
更新日期：1984-07-31 00:00:00
abstract：:The equilibrium binding of hemoglobin to isolated band 3 protein exhibited positive cooperativity [Hill coefficient = 1.65 +/- 0.1; total number of binding sites at pH 6.6 in 5 mM sodium phosphate buffer = 32 500 +/- 940 pmol/mg; Ka = (3.0 +/- 0.5) X 10(5) M-1]. The binding was reversible and ionic in nature as the bo...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00359a054
更新日期：1986-06-03 00:00:00
abstract：:The thermotropic behavior of 20 chemically related glycosphingolipids (GSLs) of high purity, containing neutral and anionic carbohydrate residues in their oligosaccharide chains, was studied by high-sensitivity differential scanning calorimetry. In general, the polar head group of GSLs appears to be one of the major d...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00326a003
更新日期：1985-02-26 00:00:00
abstract：:Central to the pathology of Alzheimer's disease (AD) is the profuse accumulation of amyloid-beta (Abeta) peptides in the brain of affected individuals, and several amyloid precursor protein (APP) transgenic (Tg) mice models have been created to mimic Abeta deposition. Among these, the PDAPP Tg mice carrying the famili...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi051213+
更新日期：2005-10-25 00:00:00
abstract：:The binding of Lens culinaris lectin to the receptors of rabbit erythrocytes was studied by a quantitative fluorometric method using the fluoresceinated conjugate. Equilibrium data showed the presence of 1.2 x 10(6) receptors/cell with an association constant varying from 8 to 3 x 10(6) M-1 over a temperature range of...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00616a022
更新日期：1978-11-14 00:00:00
abstract：:The effects of site-directed mutagenesis were used to explore the role of residues in M4 on the apparent Ki of a selective, K+-competitive inhibitor of the gastric H+,K+ ATPase, SCH28080. A double transfection expression system is described, utilizing HEK293 cells and separate plasmids encoding the alpha and beta subu...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi991837d
更新日期：2000-03-21 00:00:00
abstract：:Lysophosphatidic acid (1-acyl-sn-glycero-3-phosphate or LPA) is a phospholipid mediator displaying numerous and widespread biological activities and thought to act via G-protein-coupled receptors. Here we have studied the effects on human platelets of a number of LPA analogues, including two enantiomers of both N-palm...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi9816756
更新日期：1999-06-29 00:00:00
abstract：:The subtilisins have an extended substrate binding cleft comprising at least 8 subsites. Two pockets at the S1 and S4 sites are particularly conspicuous, and the interactions between substrate and these two pockets are very important for the substrate specificity. Phe residues have mutationally been introduced at one ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00062a016
更新日期：1993-03-23 00:00:00
abstract：:With the aid of high time resolution kinetic data extracted from a flow cytometer, we determined that there are two N-formyl peptide receptor states for human neutrophils at 4 degrees C: a low affinity and a high affinity state. Competitive binding of FMLP, FNLP, and t-BOC with FNLPNTL-FL revealed different kinetic ra...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi961088p
更新日期：1996-10-08 00:00:00
abstract：:The structural factors responsible for the extraordinary rate enhancement ( approximately 10(17)) of the reaction catalyzed by orotidine 5'-monophosphate decarboxylase (OMPDC) have not been defined. Catalysis requires a conformational change that closes an active site loop and "clamps" the orotate base proximal to hyd...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi100443a
更新日期：2010-05-04 00:00:00
abstract：:We have previously suggested that folding of the SV40 attenuator RNA 1 into two hairpin elements leads to a block of transcription elongation. Using site-directed mutagenesis, we created three templates that either strengthened or weakened the proposed hairpin structures. The mutated and wild-type templates were clone...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00150a034
更新日期：1992-09-08 00:00:00
abstract：:Immunoglobulins fragments are composed of globular domains linked by extended polypeptide segments. The molecular flexibility inherent in this arrangement allows for significant potential differences between structures observed in the crystalline state and those attained in solution. Small-angle neutron scattering mea...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00541a011
更新日期：1982-06-08 00:00:00
abstract：:The DNA binding domain of the mammalian glucocorticoid hormone receptor (GR) contains nine highly conserved cysteine residues, a conservation shared by the superfamily of steroid and thyroid hormone receptors. A fragment [150 amino acids (AA) in length] consisting of GR residues 407-556, containing within it the entir...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00491a016
更新日期：1990-10-02 00:00:00
abstract：:Phosphatase of regenerating liver 3 (PRL-3) is suggested as a biomarker and therapeutic target in several cancers. It has a well-established causative role in cancer metastasis. However, little is known about its natural substrates, pathways, and biological functions, and only a few protein substrates have been sugges...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi201095z
更新日期：2011-09-06 00:00:00
abstract：:The molecular weight of phosphophoryn, an acidic phosphoprotein unique to dentin matrix, has been difficult to determine because of a combination of neutral protease activities in this tissue and the intrinsic high charge density of the molecule. In this study, bovine dentin phosphophoryn (BDPP) was isolated by a proc...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00287a025
更新日期：1983-08-30 00:00:00
abstract：:The biosynthesis of the C ring of the antitumor antibiotic agent, tomaymycin, is proposed to proceed through five enzyme-catalyzed steps from l-tyrosine. The genes encoding these enzymes have recently been cloned and their functions tentatively assigned, but there is limited biochemical evidence supporting the assignm...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi200947w
更新日期：2011-09-06 00:00:00
abstract：:Heme oxygenases convert heme to free iron, CO, and biliverdin. Saccharomyces cerevisiae and Candida albicans express putative heme oxygenases that are required for the acquisition of iron from heme, a critical process for fungal survival and virulence. The putative heme oxygenases Hmx1 and CaHmx1 from S. cerevisiae an...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi061429r
更新日期：2006-12-12 00:00:00
abstract：:Horseradish peroxidase C binds a wide variety of small H-donor compounds such as benzohydroxamic acid (BHA) and 2-naphthohydroxamic acid (NHA). In this work, we use the Mg(II)-mesoporphyrin prosthetic group derivative as a spectroscopic probe of the active site and of the interaction with the substrates. We report on ...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi002938a
更新日期：2001-08-07 00:00:00
abstract：:Fluorescein isothiocyanate derivatization of the human lactotransferrin on Lys-264 inhibits the binding of the protein of human PHA-activated lymphocytes [Legrand, D., Mazurier, J., Maes, P., Rochard, E., Montreuil, J., & Spik, G. (1991) Biochem. J. 276, 733-738], indicating that part of the receptor-binding site is l...
journal_title：Biochemistry
pub_type： 杂志文章
doi：10.1021/bi00153a018
更新日期：1992-09-29 00:00:00
