Abstract:
:alpha 1-Adrenergic receptor probes, which can be radioiodinated to yield high specific activity radioligands, have been synthesized and characterized. 2-[4-(4-Amino-benzoyl)piperazin-1-yl]-4-amino-6,7-dimethoxyquin azoline (CP63,155), an arylamine analogue of the selective alpha 1-adrenergic antagonist prazosin, and its iodinated derivative, 2-[4-(4-amino-3-[125I]iodobenzoyl)piperazin-1-yl]-4-amino-6, 7-dimethoxyquinazoline [( 125I]CP63,789), bind reversibly and with high affinity (KD = 1 nM and 0.6 nM, respectively) to rat hepatic membrane alpha 1-adrenergic receptors. Conversion of [125I]CP63,789 to the aryl azide yields a photolabile derivative, 2-[4-(4-azido-3-[125I]iodobenzoyl)piperazin-1-yl]-4-amino-6, 7-dimethoxyquinazoline [( 125I]CP65,526), which prior to photolysis binds competitively and with high affinity (KD = 0.3 nM). Binding of [125I]CP63,789 and [125I]CP65,526 (prior to photolysis) is rapid and saturable. Both ligands identify similar alpha 1-adrenergic receptor binding site concentrations as the parent probe, [3H]prazosin. Specific binding by these iodinated ligands is stereoselective and inhibited by a variety of adrenergic agents with a specificity typical of the alpha 1-adrenergic receptor. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and autoradiography of [125I]CP65,526-labeled rat hepatic membranes reveal major protein species with molecular weights of 77K, 68K and 59K. Each protein binds adrenergic ligands with stereoselectivity and with a specificity typical of the alpha 1-adrenergic receptor. Inclusion of multiple protease inhibitors during membrane preparation prior to SDS-PAGE does not alter the labeling of these peptides.(ABSTRACT TRUNCATED AT 250 WORDS)
journal_name
Biochemistryjournal_title
Biochemistryauthors
Seidman CE,Hess HJ,Homcy CJ,Graham RMdoi
10.1021/bi00311a031subject
Has Abstractpub_date
1984-07-31 00:00:00pages
3765-70issue
16eissn
0006-2960issn
1520-4995journal_volume
23pub_type
杂志文章相关文献
BIOCHEMISTRY文献大全abstract::The structures of ternary complexes of human inositol monophosphatase with inhibitory Gd3+ and either D- or L-myo-inositol 1-phosphate have been determined to 2.2-2.3 A resolution using X-ray crystallography. Substrate and metal are bound identically in each active site of the phosphatase dimer. The substrate is prese...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00198a011
更新日期:1994-08-16 00:00:00
abstract::It is known that, while melittin at micromolar concentrations is unfolded under conditions of low ionic strength at neutral pH, it adopts a tetrameric alpha-helical structure under conditions of high ionic strength, at alkaline pH, or at high peptide concentrations. To understand the mechanism of the conformational tr...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00118a014
更新日期:1992-01-28 00:00:00
abstract::Studies are presented of the equilibrium binding of [3H]-d-tubocurarine (dTC) and [3H]acetylcholine (AcCh) to Torpedo postsynaptic membranes. The saturable binding of [3H]dTC is characterized by two affinities: Kd1 = 33 +/- 6 nM and Kd2 = 7.7 +/- 4.6 microM, with equal numbers of binding sites. Both components are com...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00591a032
更新日期:1979-11-27 00:00:00
abstract::Modulation of endogenous gene function, through sequence-specific recognition of double helical DNA via oligonucleotide-directed triplex formation, is a promising approach. Compared to the formation of pyrimidine motif triplexes, which require relatively low pH, purine motif appears to be the most gifted for their sta...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi1012589
更新日期:2011-05-17 00:00:00
abstract::The mechanism of chromophore biosynthesis in green fluorescent protein (GFP) is triggered by a spontaneous main chain cyclization reaction of residues 65-67. Here, we demonstrate that the initially colorless Y66L variant, designed to trap chromophore precursor states, is oxidatively modified to generate yellow chromop...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi0503798
更新日期:2005-06-14 00:00:00
abstract::Room temperature phosphorescence techniques were used to study the structural and dynamic features of the tryptophan residues in bovine alpha-crystallin. Upon excitation at 290 nm, the characteristic signature of tryptophan phosphorescence was observed with an emission maximum at 442 +/- 2 nm. The phosphorescence inte...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00439a027
更新日期:1989-06-27 00:00:00
abstract::Heparin was isolated from an unusually large human hemangioma that contained an elevated level of mast cells. Purification of multimilligram quantities of heparin from this tissue sample permitted a thorough examination of its structure and activity. Characterization of this human heparin included the following: one-d...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00164a020
更新日期:1992-12-15 00:00:00
abstract::As part of a high-throughput, structural proteomic project we have used NMR spectroscopy to determine the solution structure and ascertain the function of a previously unknown, conserved protein (MtH895) from the thermophilic archeon Methanobacterium thermoautotrophicum. Our findings indicate that MtH895 contains a ce...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi0115176
更新日期:2002-04-16 00:00:00
abstract::Chemical derivatization studies have been directed at the sulfhydryl group of D-beta-hydroxybutyrate dehydrogenase, a lipid-requiring enzyme. Reaction with N-ethylmaleimide leads to progressive and parallel loss of both enzymic activity and coenzyme binding. Both functions are lost when 1 equiv of sulfhydryl is deriva...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00564a021
更新日期:1980-11-11 00:00:00
abstract::FKBP12, a small human enzyme, aids protein folding by catalyzing cis-trans isomerization of peptidyl-prolyl bonds, and is involved in cell signaling pathways, calcium regulation, and the immune response. The underlying molecular mechanisms are not fully understood, but it is well-known that aromatic residues in the ac...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/acs.biochem.6b01157
更新日期:2017-01-10 00:00:00
abstract::The 2.15 A resolution crystal structure of arginase from Plasmodium falciparum, the parasite that causes cerebral malaria, is reported in complex with the boronic acid inhibitor 2(S)-amino-6-boronohexanoic acid (ABH) (K(d) = 11 microM). This is the first crystal structure of a parasitic arginase. Various protein const...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi100390z
更新日期:2010-07-06 00:00:00
abstract::Staphylococcal nuclease H124L is a recombinant protein produced in Escherichia coli whose sequence is identical with that of the nuclease produced by the V8 variant of Staphylococcus aureus. The enzyme-metal ion activator-nucleotide inhibitor ternary complex, nuclease H124L-thymidine 3',5'-bisphosphate-Ca2+, was inves...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00453a011
更新日期:1990-01-09 00:00:00
abstract::X-ray structural information provides the opportunity to explore quantitatively the relation between the microenvironments of heme proteins and their redox potentials. This can be done by considering the protein as a "solvent" for its redox center and calculating the difference between the electrostatic energy of the ...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00355a035
更新日期:1986-04-08 00:00:00
abstract::Molecular imaging is an important new direction in medical diagnosis; however, its success is dependent upon molecular probes that demonstrate selective tissue targeting. We report the design and chemical synthesis of a derivative of human amyloid-beta (Abeta) peptide that is capable of selectively targeting individua...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi0359574
更新日期:2004-05-25 00:00:00
abstract::Taurine/alpha-ketoglutarate (alphaKG) dioxygenase (TauD), an archetype alphaKG-dependent hydroxylase, is a non-heme mononuclear Fe(II) enzyme that couples the oxidative decarboxylation of alphaKG with the conversion of taurine to aminoacetaldehyde and sulfite. The crystal structure of taurine-alphaKG-Fe(II)TauD is kno...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi048746n
更新日期:2005-03-15 00:00:00
abstract::Glutathione S-transferase, from the malarial parasite Plasmodium falciparum (PfGST), exerts a protective role in the organism and is thus considered an interesting target for antimalarial drug development. In contrast to other GSTs, it is present in solution as a tetramer and a dimer in equilibrium, which is induced b...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi400007g
更新日期:2013-03-19 00:00:00
abstract::In aspartate aminotransferase, pyridoxal 5'-phosphate (PLP) forms a Schiff base with the epsilon-amino group of Lys258 (internal aldimine). The internal aldimine has a pKa value of 6.8. Binding of a substrate amino acid to the enzyme yields the Michaelis complex, in which PLP still forms the internal aldimine with Lys...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi981517e
更新日期:1998-10-27 00:00:00
abstract::Rapid freeze-quench (RFQ) Mössbauer and stopped-flow absorption spectroscopy were used to monitor the ferritin ferroxidase reaction using recombinant (apo) frog M ferritin; the initial transient ferric species could be trapped by the RFQ method using low iron loading (36 Fe2+/ferritin molecule). Biphasic kinetics of f...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi980847w
更新日期:1998-07-14 00:00:00
abstract::The fluorophore 4-heptadecyl-7-hydroxycoumarin was used as a probe to study the properties of phospholipid bilayers at the lipid-water interface. To this end, the steady-state fluorescence anisotropy, the differential polarized phase fluorometry, and the emission lifetime of the fluorophore were measured in isotropic ...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00324a005
更新日期:1985-01-29 00:00:00
abstract::Glutathionylation of intracellular proteins is an established physiological regulator of protein function. In multiple models, including ischemia-reperfusion of the heart, increased oxidative stress results in the glutathionylation of sarcomeric actin. We hypothesized that actin glutathionylation may play a role in th...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi900669m
更新日期:2009-08-11 00:00:00
abstract::In the absence of any external electron donor, the "peroxy" intermediate of cytochrome c oxidase (CcO-607) is converted to the ferryl form (CcO-580) and subsequently to oxidized enzyme. The rate of conversion of CcO-607 to the CcO-580 form is pH dependent between pH 3.0 and pH 7.6. A plot of the logarithm of the rate ...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi002373i
更新日期:2001-02-13 00:00:00
abstract::In the present report we studied the interaction between the skeletal muscle ryanodine receptor and the ubiquitous S100A1 Ca2+ binding protein. S100A1 did not affect equilibrium [3H]ryanodine binding to purified rabbit skeletal muscle terminal cisternae at 100 microM free [Ca2+]. At nanomolar free [Ca2+], however, S10...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi970160w
更新日期:1997-09-23 00:00:00
abstract::Stopped-flow fluorescence experiments have been carried out to study the steady-state kinetics of hydrolysis of Leu-Gly-NHNH-Dns [Dns = 5-(dimethylamino)naphthalene-1-sulfonyl] by porcine kidney cytosol leucine aminopeptidase (LAP) in 50% v/v methanol/buffer solution at ambient temperature and the pre-steady-state kin...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00414a018
更新日期:1988-07-12 00:00:00
abstract::Myosin subfragment 1 (S1) was covalently labeled with a fluorescent dye, N-[7-(dimethylamino)-4-methyl-3-coumarinyl]maleimide (DACM), and then digested by trypsin to cleave S1 heavy chain into fragments. The DACM-labeled and trypsin-treated S1 was complexed with F-actin and treated with a zero-length cross-linker, 1-e...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00262a043
更新日期:1982-09-14 00:00:00
abstract::Pyruvate decarboxylase (PDC) uses thiamine diphosphate as an essential cofactor to catalyze the formation of acetaldehyde on the pathway of ethanol synthesis. Here we report the crystallographic image of a prereaction intermediate of a bacterial pyruvate decarboxylase prepared by cocrystallizing the enzyme with pyruva...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi901864j
更新日期:2010-03-02 00:00:00
abstract::Numerous studies have concluded that the interaction of the amyloid β-peptide (Aβ) and cellular membranes contributes to the toxicity and cell death observed in the progression of Alzheimer's disease. Aggregated Aβ species disrupt membranes, leading to physical instability and ion leakage. Further, the presence of Aβ ...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi400562x
更新日期:2013-07-23 00:00:00
abstract::We have found a correlation between liposome fusion kinetics and lipid phase behavior for several inverted phase forming lipids. N-Methylated dioleoylphosphatidylethanolamine (DOPE-Me), or mixtures of dioleoylphosphatidylethanolamine (DOPE) and dioleoylphosphatidylcholine (DOPC), will form an inverted hexagonal phase ...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00435a011
更新日期:1989-05-02 00:00:00
abstract::The orientation of eukaryotic cytochromes P450, with respect to the membrane of the endoplasmic reticulum, has been investigated. There is now good evidence that the tertiary structure of these proteins is essentially the same as that of the soluble bacterial isoenzyme cytochrome P450CI, with the exception of an exten...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00215a011
更新日期:1991-01-08 00:00:00
abstract::Lysyl-5-fluoro-L-tryptophyllysine and lysyl-5-fluoro-D-tryptophyllysine were synthesized, and their interactions with double-stranded DNA were investigated as a model for protein-nucleic acid interactions. The binding to DNA was studied by monitoring various 19F NMR parameters, the fluorescence, and the optical absorb...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi00337a012
更新日期:1985-07-30 00:00:00
abstract::PI-SceI is a member of an unusual class of rare cutting homing endonucleases produced by an autocatalytic protein splicing from a precursor. To analyze the structural and functional domain organization of the endonuclease PI-SceI and to examine whether the DNA binding activity can be structurally separated from the ca...
journal_title:Biochemistry
pub_type: 杂志文章
doi:10.1021/bi980013d
更新日期:1998-06-02 00:00:00