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https://www.readbyqxmd.com/read/28528483/fossil-record-of-ephedra-in-the-lower-cretaceous-aptian-argentina
#1
Gabriela G Puebla, Ari Iglesias, María A Gómez, Mercedes B Prámparo
Fossil plants from the Lower Cretaceous (upper Aptian) of the La Cantera Formation, Argentina, are described. The fossils studied represent a leafy shooting system with several orders of articulated and striated axes and attached leaves with unequivocal ephedroid affinity. We also found associated remains of ovulate cones with four whorls of sterile bracts, which contain two female reproductive units (FRU). Ovulate cone characters fit well within the genus Ephedra. Special characters in the ovulate cones including an outer seed envelope with two types of trichomes, allowed us to consider our remains as a new Ephedra species...
May 20, 2017: Journal of Plant Research
https://www.readbyqxmd.com/read/28528463/facebook-advertising-to-recruit-young-urban-women-into-an-hiv-prevention-clinical-trial
#2
Rachel Jones, Lorraine J Lacroix, Eloni Porcher
Advertising via Facebook to elicit involvement in clinical trials has demonstrated promise in expanding geographic reach while maintaining confidentiality. The purpose of this study is to evaluate Facebook advertising to reach at-risk, predominately African American or Black women in higher HIV prevalence communities for an HIV prevention clinical trial, and to compare baseline characteristics to those recruited on-the-ground. Maintaining confidentiality and the practical aspects of creating and posting ads on Facebook are described...
May 20, 2017: AIDS and Behavior
https://www.readbyqxmd.com/read/28528381/metal-chelate-affinity-precipitation-with-thermo-responsive-polymer-for-purification-of-%C3%AE%C2%B5-poly-l-lysine
#3
Sipeng Li, Zhaoyang Ding, Jifu Liu, Xuejun Cao
ε-Poly-L-lysine (ε-PL) is a natural preservative for food processing industry. A thermo-responsive polymer, attached with Cu(2+) or Ni(2+), was prepared for metal-chelate affinity precipitation for purification of ε-PL. The low critical solution temperatures (LCSTs) of these polymers were close to the room temperature (31.0-35.0 °C). The optimal adsorption conditions were as follows: pH 4.0, 0 mol/L NaCl, ligand density 75.00 μmol/g, and 120 min. The ligand Cu(2+) showed a stronger affinity interaction with ε-PL and the highest adsorption amount reached 251...
May 20, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28528283/poly-vinyl-alcohol-hydroxyapatite-monolithic-in-needle-extraction-mine-device-preparation-and-examination-of-drug-affinity
#4
Monika Pietrzyńska, Michał Czerwiński, Adam Voelkel
Polymer-ceramic materials based on poly(vinyl alcohol) (PVA) and hydroxyapatite were applied as sorption material in Monolithic In-Needle Extraction (MINE) device. The presented device provides new possibilities for the examination of bisphosphonates affinity for bone and will be a helpful tool in evaluation of potential antiresorptive drugs suitability. A ceramic part of monoliths was prepared by incorporation of hydroxyapatite (HA) into the reaction mixture or by using a soaking method (mineralization of HA on the PVA)...
May 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28528273/addition-of-thiols-to-the-double-bond-of-dipeptide-c-terminal-dehydroalanine-as-a-source-of-new-inhibitors-of-cathepsin-c
#5
Paweł Lenartowicz, Maciej Makowski, Bartosz Oszywa, Kinga Haremza, Rafał Latajka, Małgorzata Pawełczak, Paweł Kafarski
Addition of thiols to double bond of glycyl-dehydroalanine and phenyl-dehydroalanine esters provided micromolar inhibitors of cathepsin C. The structure-activity studies indicated that dipeptides containing N-terminal phenylalanine exhibit higher affinity towards the enzyme. A series of C-terminal S-substituted cysteines are responsible for varying interaction with S1 binding pocket of cathepsin C. Depending on diastereomer these compounds most likely act as slowly reacting substrates or competitive inhibitors...
May 17, 2017: Biochimie
https://www.readbyqxmd.com/read/28528265/synthesis-radiolabeling-and-preclinical-evaluation-of-a-11-c-gmom-derivative-as-pet-radiotracer-for-the-ion-channel-of-the-n-methyl-d-aspartate-receptor
#6
Pieter J Klein, Robert C Schuit, Athanasios Metaxas, Johannes Am Christiaans, Esther Kooijman, Adriaan A Lammertsma, Bart Nm van Berckel, Albert D Windhorst
INTRODUCTION: Presently available PET ligands for the NMDAr ion channel generally suffer from fast metabolism. The purpose of this study was to develop a metabolically more stable ligand for the NMDAr ion channel, taking [(11)C]GMOM ([(11)C]1) as the lead compound. METHODS: [(11)C]1, its fluoralkyl analogue [(18)F]PK209 ([(18)F]2) and the newly synthesized fluorovinyloxy analogue [(11)C]7b were evaluated ex vivo in male Wistar rats for metabolic stability. In addition, [(11)C]7b was subjected to a biodistribution study and its affinity (Ki) and lipophilicity (logD7...
May 8, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/28528252/investigation-of-the-binding-affinity-in-vitamin-b12-bovine-serum-albumin-system-using-various-spectroscopic-methods
#7
Magdalena Makarska-Bialokoz
The binding affinity between vitamin B12 (VitB12) and bovine serum albumin (BSA) has been investigated in aqueous solution at pH=7.4, employing UV-vis absorption and steady-state, synchronous and three-dimensional fluorescence spectra techniques. Representative effects noted for BSA intrinsic fluorescence resulting from the interactions with VitB12 confirm the formation of π-π stacked non-covalent and non-fluorescent complexes in the system VitB12-BSA. All the determined parameters, the binding, fluorescence quenching and bimolecular quenching rate constants (of the order of 10(4)Lmol(-1), 10(3)Lmol(-1) and 10(11)Lmol(-1)s(-1), respectively), as well as Förster resonance energy transfer parameters validate the mechanism of static quenching...
May 11, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/28528024/structure-diverse-phylomer-libraries-as-a-rich-source-of-bioactive-hits-from-phenotypic-and-target-directed-screens-against-intracellular-proteins
#8
REVIEW
Paul M Watt, Nadia Milech, Shane R Stone
Phylomers are peptides derived from biodiverse protein fragments. Genetically encoded Phylomer libraries have been constructed, containing hundreds of billions of peptides derived from virtually all of the few thousand fold families found in the protein universe. They offer a rich source of high quality hits against diverse target sequences and have been used for three main purposes: firstly, to identify and validate targets in phenotypic screens; secondly, to block protein interactions with nanomolar potency binding affinities; thirdly as a source of more efficient cell penetrating peptides for the delivery of a wide range of biologics...
May 18, 2017: Current Opinion in Chemical Biology
https://www.readbyqxmd.com/read/28527988/codonopsis-lanceolata-polysaccharide-clps-inhibits-melanoma-metastasis-via-regulating-integrin-signalling
#9
Yanqiu Liu, Xiangming Zou, Guangren Sun, Yihong Bao
β1 integrin-mediated migration plays a fundamental role in melanoma metastasis. Here, we evaluated the molecular mechanisms underlying the anti-metastatic capacity of a polysaccharide fraction (CLPS) from Codonopsis lanceolata. CLPS inhibited in vivo melanoma metastasis in a B16F10 pulmonary metastasis model, impaired β1 integrin-mediated B16F10 melanoma cell migration in vitro evaluated by Transwell assay, reduced affinity between β1 integrin and ligand protein GST-FNIII9-10. Also, CLPS attenuated the adhesion-dependent formation of focal adhesion and blocked β1 integrin/FAK/paxillin signalling axis...
May 17, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28527909/binding-assay-for-characterization-of-protein-kinase-inhibitors-possessing-sub-picomolar-to-sub-millimolar-affinity
#10
Hedi Sinijarv, Shanshan Wu, Taavi Ivan, Kaido Viht, Asko Uri
High demand for inhibitors regulating the activity of protein kinases has stimulated the quest for high throughput and reliable compound screening assays. Here we introduce a method applying a non-metal photoluminescent probe ARC-Lum(Fluo) for determination of dissociation constants of competitive inhibitors of protein kinases. Employing a single probe instead of a combination of antibody and fluorescent tracer makes the assay simpler, cheaper, and more accurate than several other inhibitor-screening technologies...
May 17, 2017: Analytical Biochemistry
https://www.readbyqxmd.com/read/28527568/evolution-of-nuclear-receptors-and-ligand-signaling-toward-a-soft-key-lock-model
#11
Guillaume Holzer, Gabriel V Markov, Vincent Laudet
Nuclear receptors (NRs) are a family of ligand-regulated transcription factors that modulate a wide variety of physiological functions in a ligand-dependent manner. The first NRs were discovered as receptors of well-known hormones such as 17β-estradiol, corticosteroids, or thyroid hormones. In these cases a direct activation of the receptor transcriptional activity by a very specific ligand, with nanomolar affinity, was demonstrated, providing a strong conceptual framework to understand the mechanism of action of these hormones...
2017: Current Topics in Developmental Biology
https://www.readbyqxmd.com/read/28527467/gas-phase-anion-photoelectron-spectroscopy-and-theoretical-investigation-of-gold-acetylide-species
#12
Peng Wang, Wenjing Zhang, Xi-Ling Xu, Jinyun Yuan, Hong-Guang Xu, Weijun Zheng
We conducted gas phase anion photoelectron spectroscopy and density functional theory studies on a number of gold acetylide species, such as AuC2H, AuC2Au, and Au2C2H. Based on the photoelectron spectra, the electron affinities of AuC2H, AuC2Au, and Au2C2H are measured to be 1.54(±0.04), 1.60(±0.08), and 4.23(±0.08) eV, respectively. The highest occupied molecular orbital-lowest unoccupied molecular orbital (HOMO-LUMO) gaps of AuC2H and AuC2Au are measured to be about 2.62 and 2.48 eV, respectively. It is interesting that photoelectron spectra of AuC2H(-) and AuC2Au(-) display similar spectral features...
May 21, 2017: Journal of Chemical Physics
https://www.readbyqxmd.com/read/28527437/ab-initio-study-of-the-neutral-and-anionic-alkali-and-alkaline-earth-hydroxides-electronic-structure-and-prospects-for-sympathetic-cooling-of-oh
#13
Milaim Kas, Jérôme Loreau, Jacques Liévin, Nathalie Vaeck
We have performed a systematic ab initio study on alkali and alkaline earth hydroxide neutral (MOH) and anionic (MOH(-)) species where M = Li, Na, K, Rb, Cs or Be, Mg, Ca, Sr, Ba. The CCSD(T) method with extended basis sets and Dirac-Fock relativistic effective core potentials for the heavier atoms has been used to study their equilibrium geometries, interaction energies, electron affinities, electric dipole moment, and potential energy surfaces. All neutral and anionic species exhibit a linear shape with the exception of BeOH, BeOH(-), and MgOH(-), for which the equilibrium structure is found to be bent...
May 21, 2017: Journal of Chemical Physics
https://www.readbyqxmd.com/read/28527429/coexistence-of-light-driven-na-and-h-transport-in-a-microbial-rhodopsin-from-nonlabens-dokdonensis
#14
Hongshen Zhao, Baofu Ma, Liangliang Ji, Longjie Li, Huanhuan Wang, Deliang Chen
Ion pumping microbial rhodopsins are photochemically active membrane proteins, converting light energy into ion-motive-force for ATP synthesis. Nonlabens dokdonensis rhodopsin 2 (NdR2), was recently identified as a light-driven Na(+) pump. However, few functional studies on NdR2 have been conducted to elucidate its mechanism of ion transport. By reconstituting NdR2 into liposomes, we proved that NdR2 functions as a light-driven Na(+)/H(+) pump. As Na(+) concentration increased, the dominant H(+) pump activity switched to the Na(+) pump activity at neutral pH...
May 10, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28527406/the-relevance-of-ki-calculation-for-bi-substrate-enzymes-illustrated-by-kinetic-evaluation-of-a-novel-lysine-k-acetyltransferase-8-inhibitor
#15
Hannah Wapenaar, Thea van den Bosch, Niek G J Leus, Petra E van der Wouden, Nikolaos Eleftheriadis, Jos Hermans, Gebremedhin Solomon Hailu, Dante Rotili, Antonello Mai, Alexander Dömling, Rainer Bischoff, Hidde J Haisma, Frank J Dekker
Histone acetyltransferases (HATs) are important mediators of epigenetic post-translational modifications of histones that play important roles in health and disease. A disturbance of these modifications can result in disease states, such as cancer or inflammatory diseases. Inhibitors of HATs (HATi) such as lysine (K) acetyltransferase 8 (KAT8), could be used to study the epigenetic processes in diseases related to these enzymes or to investigate HATs as therapeutic targets. However, the development of HATi is challenged by the difficulties in kinetic characterization of HAT enzymes and their inhibitors to enable calculation of a reproducible inhibitory potency...
May 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28527150/development-of-in-silico-protocols-to-predict-structural-insights-into-the-metabolic-activation-pathways-of-xenobiotics
#16
M Kalim A Khan, Salman Akhtar, Jamal M Arif
To establish in silico model to predict the structural insight into the metabolic bioactivation pathway of xenobiotics, we considered two specific and one non-specific mammary procarcinogen [e.g., dibenzo[a,l]pyrene (DBP), 7,12-dimethylbenz[a]anthracene (DMBA), and benzo[a]pyrene (BP)]. The CYP1A1, 1B1, 2C9, 1A2 and 2B6 reported in wet-lab studies to actively metabolize DBP also showed strong binding energies (kcal/mol) of -11.50, -10.67, -10.37, -9.76 and -9.72, respectively, with inhibition constants ranging between 0...
May 19, 2017: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/28526864/a-broad-spectrum-bactericidal-lipopeptide-with-anti-biofilm-properties
#17
Ohad Meir, Fadia Zaknoon, Uri Cogan, Amram Mor
Previous studies of the oligoacyllysyl (OAK) series acyl-lysyl-lysyl-aminoacyl-lysine-amide, suggested their utility towards generating robust linear lipopeptide-like alternatives to antibiotics, although to date, none exhibited potent broad-spectrum bactericidal activity. To follow up on this premise, we produced a new analog (C14KKc12K) and investigated its properties in various media. Mechanistic studies suggest that C14KKc12K uses a non-specific membrane-disruptive mode of action for rapidly reducing viability of Gram-negative bacteria (GNB) similarly to polymyxin B (PMB), a cyclic lipopeptide used as last resort antibiotic...
May 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28526745/identification-and-characterisation-of-nanobodies-targeting-the-epha4-receptor
#18
Lies Schoonaert, Laura Rué, Bart Roucourt, Mieke Timmers, Susan Little, Lucía Chávez Gutiérrez, Maarten Dewilde, Peter Joyce, Adam Curnock, Peter Weber, Jurgen Haustraete, Gholamreza Hassanzadeh-Ghassabeh, Bart De Strooper, Ludo Van Den Bosch, Philip Van Damme, Robin Lemmens, Wim Robberecht
The ephrin receptor A4 (EphA4) is one of the receptors in the ephrin system that plays a pivotal role in a variety of cell-cell interactions, mostly studied during development. In addition, EphA4 has been found to play a role in cancer biology as well as in the pathogenesis of several neurological disorders such as stroke, spinal cord injury, multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS) and Alzheimer's disease (AD). Pharmacological blocking of EphA4 has been suggested to be a therapeutic strategy for these disorders...
May 19, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28526744/combining-properties-of-different-classes-of-pi3k%C3%AE-inhibitors-to-understand-molecular-features-that-confer-selectivity
#19
Grace Q Gong, Jackie D Kendall, James Mj Dickson, Gordon W Rewcastle, Christina M Buchanan, William A Denny, Peter R Shepherd, Jack U Flanagan
Phosphoinositide 3-kinases (PI3K) are major regulators of many cellular functions, and hyperactivation of PI3K cell signalling pathways is a major target for anticancer drug discovery. PI3Kα is the isoform most implicated in cancer, and our aim is to selectively inhibit this isoform, which may be more beneficial than concurrent inhibition of all Class I PI3Ks. We have used structure-guided design to merge high selectivity and high affinity characteristics found in existing compounds. Molecular docking including the prediction of water-mediated interactions, was used to model interactions between the ligands and the PI3Kα affinity pocket...
May 19, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28526710/gbt1118-a-potent-allosteric-modifier-of-hemoglobin-oxygen-affinity-increases-tolerance-to-severe-hypoxia-in-mice
#20
Kobina Dufu, Ozlem Yalcin, Eilleen Sy Ao-Ieong, Athiwat Hutchaleelala, Qing Xu, Zhe Li, Nicholas Vlahakis, Donna Oksenberg, Josh Lehrer-Graiwer, Pedro Cabrales
Adaptation to hypoxia requires compensatory mechanisms that affect oxygen (O2) transport and utilization. Decreased hemoglobin (Hb)-O2 affinity is considered part of the physiological adaptive process to chronic hypoxia. This manuscript explores the hypothesis that increased Hb-O2 affinity can complement acute physiological responses to hypoxia by increasing O2 uptake and delivery when compared to normal Hb-O2 affinity during acute severe hypoxia. To test this hypothesis, mice Hb-O2 affinity was increased via oral administration of 70 or 140 mg/kg GBT1118...
May 19, 2017: American Journal of Physiology. Heart and Circulatory Physiology
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