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关键词:'53787'
显示 1-30 共 44 条结果 关于 "53787" 范围 论文
Kimberly A Reynolds et al.
Journal of computer-aided molecular design, 23(5), 273-288 (2009-01-17)
The new beta(2) Adrenoceptor (beta(2)AR) crystal structures provide a high-resolution snapshot of receptor interactions with two particular partial inverse agonists, (-)-carazolol and timolol. However, both experimental and computational studies of GPCR structure are significantly complicated by the existence of multiple
Determination of tranquilisers and carazolol residues in animal tissue using high-performance liquid chromatography with electrochemical detection.
Rose MD and Shearer G
Journal of Chromatography A, 624(1-2), 471- 477 (1992)
Elena Navarro et al.
Frontiers in veterinary science, 8, 574250-574250 (2021-03-09)
Many factors can lead to an inadequate development of piglets during their first days of life, including poor maternal behavior, which can be due to pain caused by farrowing, and reduced colostrum ingestion. This study investigates the action of meloxicam
Jian-Qiao Cheng et al.
Molecules (Basel, Switzerland), 24(4) (2019-03-03)
This paper presents an application of high performance liquid chromatography coupled with quadrupole orbitrap high-resolution mass spectrometry (HPLC-Q-Orbitrap HRMS) for the analysis of 27 β-blockers and metabolites in milk powder. Homogenized milk power samples were extracted by acetonitrile and purified
Vsevolod Katritch et al.
Journal of molecular recognition : JMR, 22(4), 307-318 (2009-04-09)
The 2.4 A crystal structure of the beta(2)-adrenergic receptor (beta(2)AR) in complex with the high-affinity inverse agonist (-)-carazolol provides a detailed structural framework for the analysis of ligand recognition by adrenergic receptors. Insights into agonist binding and the corresponding conformational
Iwona Zawadzka et al.
Roczniki Panstwowego Zakladu Higieny, 60(1), 19-23 (2009-07-08)
The method is presented to analyze azaperone and carazolol in pigs kidney. Samples were extracted with acetonitryle. The determination was performed by LC-ESI-MS/MS. The LC was equipped with column Luna C18 Phenomenex. Haloperidol was used as internal standards. The method
Arun K Shukla et al.
Molecular pharmacology, 73(5), 1333-1338 (2008-02-02)
Two recently determined crystal structures of the human beta2-adrenergic receptor (beta2AR) provide a long-awaited advance in the field of G protein-coupled receptor research. The beta2AR is only the second member of this, the largest family of receptors encoded in the
Bruno Bard et al.
Journal of medicinal chemistry, 52(10), 3416-3419 (2009-04-29)
RPLC gains acceptance in pharmaceutical research for the rapid determination of lipophilicity but remains limited for the determination of partition coefficients of moderate to strong basic compounds under their neutral form because stationary phases are not compatible with high pH
Karin A Stephenson et al.
Journal of medicinal chemistry, 51(16), 5093-5100 (2008-07-29)
An efficient and general method has been developed for fluorine-18 labeling of beta-blockers that possess the propanolamine moiety. A new synthetically versatile intermediate, 3-(1-(benzyloxy)propan-2-yl)-2-oxooxazolidin-5-yl)methyl 4-methylbenzenesulfonate (13), was prepared and can be conjugated to any phenoxy core. To demonstrate the synthetic
Wanhui Hu et al.
FEBS letters, 593(10), 1113-1121 (2019-04-07)
Large membrane proteins such as G protein-coupled receptors (GPCRs) are difficult for NMR study due to severe signal overlaps and unfavorable relaxation properties. We used a trimethylsilyl (TMS) group as a reporter group for 1 H NMR study of conformational
Biochemistry. Signaling across the cell membrane.
Rama Ranganathan
Science (New York, N.Y.), 318(5854), 1253-1254 (2007-11-24)
Ting Wang et al.
Journal of molecular biology, 392(4), 1102-1115 (2009-08-12)
The recently determined crystal structure of the human beta(2)-adrenergic (beta(2)AR) G-protein-coupled receptor provides an excellent structural basis for exploring beta(2)AR-ligand binding and dissociation process. Based on this crystal structure, we simulated ligand exit from the beta(2)AR receptor by applying the
Michael Zocher et al.
Structure (London, England : 1993), 20(8), 1391-1402 (2012-07-04)
G protein-coupled receptors (GPCRs) are a class of versatile proteins that transduce signals across membranes. Extracellular stimuli induce inter- and intramolecular interactions that change the functional state of GPCRs and activate intracellular messenger molecules. How these interactions are established and
Jinmei Wei et al.
Journal of the science of food and agriculture, 95(3), 598-606 (2014-06-21)
The use of xenobiotic compounds in animal husbandry has given rise to consumer anxieties regarding residual risk and food safety. Thus, animal tissues have become main samples for residue analysis and food safety for sedatives. In this study, a rapid
Simone Moretti et al.
Analytica chimica acta, 1032, 56-67 (2018-08-26)
A multiclass screening method to detect fifty-three forbidden substances by liquid-chromatography coupled to hybrid high-resolution mass spectrometry (LC-Q-Orbitrap) was developed and validated in bovine bile and urine. Eight classes of compounds were included in the method's scope (β-agonists, corticosteroids, nitroimidazoles
Mayako Michino et al.
Proteins, 78(10), 2189-2201 (2010-06-15)
Building reliable structural models of G protein-coupled receptors (GPCRs) is a difficult task because of the paucity of suitable templates, low sequence identity, and the wide variety of ligand specificities within the superfamily. Template-based modeling is known to be the
Graham M West et al.
Structure (London, England : 1993), 19(10), 1424-1432 (2011-09-06)
Mechanism of G protein-coupled receptor (GPCR) activation and their modulation by functionally distinct ligands remains elusive. Using the technique of amide hydrogen/deuterium exchange coupled with mass spectrometry, we examined the ligand-induced changes in conformational states and stability within the beta-2-adrenergic
Sid Topiol et al.
Biochemical pharmacology, 78(1), 11-20 (2009-05-19)
G-protein-coupled receptor (GPCR) proteins [Lundstrom KH, Chiu ML, editors. G protein-coupled receptors in drug discovery. CRC Press; 2006] are the single largest drug target, representing 25-50% of marketed drugs [Overington JP, Al-Lazikani B, Hopkins AL. How many drug targets are
Daniel M Rosenbaum et al.
Nature, 469(7329), 236-240 (2011-01-14)
G-protein-coupled receptors (GPCRs) are eukaryotic integral membrane proteins that modulate biological function by initiating cellular signalling in response to chemically diverse agonists. Despite recent progress in the structural biology of GPCRs, the molecular basis for agonist binding and allosteric modulation
Yveline Henchoz et al.
Journal of medicinal chemistry, 51(3), 396-399 (2008-01-15)
Accurate determinations of lipophilicity indices benefit from recent advances in chromatographic sciences such as the launch of ultraperformance liquid chromatography (UPLC). The fast strategy presented here emerges as a powerful method suitable for high-throughput log P measurements of therapeutic compounds
Michael P Bokoch et al.
Nature, 463(7277), 108-112 (2010-01-08)
G-protein-coupled receptors (GPCRs) are seven-transmembrane proteins that mediate most cellular responses to hormones and neurotransmitters. They are the largest group of therapeutic targets for a broad spectrum of diseases. Recent crystal structures of GPCRs have revealed structural conservation extending from
Tomonaga Ozawa et al.
Bioorganic & medicinal chemistry, 19(17), 5231-5237 (2011-08-09)
We examined CH/π hydrogen bonds using an ab initio fragment molecular orbital (FMO) method, combined with the CHPI program, to evaluate complexes of active (bound with agonist 1) and inactive (bound with inverse agonist 2) β2 adrenergic receptor (β(2)AR) states.
Xiangyu Liu et al.
Nature, 548(7668), 480-484 (2017-08-17)
G-protein-coupled receptors (GPCRs) pose challenges for drug discovery efforts because of the high degree of structural homology in the orthosteric pocket, particularly for GPCRs within a single subfamily, such as the nine adrenergic receptors. Allosteric ligands may bind to less-conserved
Punita Kumari et al.
Nature communications, 7, 13416-13416 (2016-11-09)
G Protein-coupled receptors (GPCRs) constitute the largest family of cell surface receptors and drug targets. GPCR signalling and desensitization is critically regulated by β-arrestins (βarr). GPCR-βarr interaction is biphasic where the phosphorylated carboxyl terminus of GPCRs docks to the N-domain
Structural biology: a receptor unlocked.
Stephen R Sprang
Nature, 450(7168), 355-356 (2007-11-16)
Søren G F Rasmussen et al.
Nature, 469(7329), 175-180 (2011-01-14)
G protein coupled receptors (GPCRs) exhibit a spectrum of functional behaviours in response to natural and synthetic ligands. Recent crystal structures provide insights into inactive states of several GPCRs. Efforts to obtain an agonist-bound active-state GPCR structure have proven difficult
Tony Warne et al.
Nature, 454(7203), 486-491 (2008-07-03)
G-protein-coupled receptors have a major role in transmembrane signalling in most eukaryotes and many are important drug targets. Here we report the 2.7 A resolution crystal structure of a beta(1)-adrenergic receptor in complex with the high-affinity antagonist cyanopindolol. The modified
Betablockers at work: the crystal structure of the beta2-adrenergic receptor.
Felix Hausch
Angewandte Chemie (International ed. in English), 47(18), 3314-3316 (2008-03-19)
Natalia Casado et al.
Talanta, 165, 223-230 (2017-02-06)
A SBA-15 type mesoporous silica was synthesized and bi-functionalized with octadecylsilane (C18) or octylsilane (C8), and sulfonic acid (SO
Mehmet Can Gündüz et al.
Animal reproduction science, 118(1), 32-36 (2009-07-10)
The effect of carazolol on the ease of penetrating the cervix during artificial insemination, lambing rate and litter size was studied using 1.5-4.0-year old Kivircik ewes in an incomplete 3 x 2 x 2 experimental design. All of the ewes
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