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https://www.readbyqxmd.com/read/28528134/enhancing-tumor-cell-response-to-multidrug-resistance-with-ph-sensitive-quercetin-and-doxorubicin-conjugated-multifunctional-nanoparticles
#1
Cenk Daglioglu
Classical chemotherapy uses chemotherapeutic agents as a mainstay of anticancer treatment. However, the development of multidrug resistance to chemotherapy limits the effectiveness of current cancer treatment. Nanosized bioconjugates combining a chemotherapeutic agent with a pharmacological approach may improve the curative effect of chemotherapeutic agents. Herein I addressed this issue by describing the synthesis, and testing of, pH-responsive Fe3O4@SiO2(FITC)-BTN/QUR/DOX multifunctional nanoparticles. The particles were designed to modulate resistance-mediating factors and to potentiate the efficacy of DOX against chemoresistance...
May 10, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28526350/designing-novel-bioconjugates-of-hydroxyethylcellulose-and-salicylates-for-potential-pharmaceutical-and-pharmacological-applications
#2
Khawar Abbas, Muhammad Amin, Muhammad Ajaz Hussain, Muhammad Sher, Syed Nasir Abbas Bukhari, Ibrahim Jantan, Kevin J Edgar
The present study deals with fabrication of macromolecular prodrugs (MPDs) of salicylic acid (SA) and aspirin (ASP) based on a hydrophilic cellulose ether, hydroxyethylcellulose (HEC). Degrees of substitution (DS) of SA and ASP per HEC repeating unit (HEC-RU) were achieved ranging from 0.60-2.18 and 0.53-1.50, respectively. The amphiphilic HEC-SA conjugate 2 assembled into nanowire-like structures, while HEC-ASP conjugate 6 formed nanoparticles (diameter 300-700nm) at a water/DMSO interface. After oral administration in rabbit models, conjugates 2 and 6 showed plasma half-life of 6...
May 16, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28524357/double-caging-linker-for-and-type-fluorogenic-construction-of-protein-antibody-bioconjugates-and-in-situ-quantification
#3
Shiyong Liu, Guhuan Liu, Guohai Shi, Haoyue Sheng, Yanyan Jiang, Haojun Liang
We report on in situ fluorescent quantification of the conjugation efficiency between azide-terminated synthetic polymers/ imaging probes and thiol-functionalized antibodies/proteins/peptides, by utilizing a doubly caged profluorescent and heterodifunctional core molecule (C1) as the self-sorting bridging unit. Orthogonal dual 'click' coupling of C1 with azide- and thiol-functionalized precursors leads to highly fluorescent bioconjugates, whereas single click products of C1 remain essentially nonfluorescent...
May 19, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28516168/selective-surface-pegylation-of-uio-66-nanoparticles-for-enhanced-stability-cell-uptake-and-ph-responsive-drug-delivery
#4
Isabel Abánades Lázaro, Salame Haddad, Sabrina Sacca, Claudia Orellana-Tavra, David Fairen-Jimenez, Ross S Forgan
The high storage capacities and excellent biocompatibilities of metal-organic frameworks (MOFs) have made them emerging candidates as drug-delivery vectors. Incorporation of surface functionality is a route to enhanced properties, and here we report on a surface-modification procedure-click modulation-that controls their size and surface chemistry. The zirconium terephthalate MOF UiO-66 is (1) synthesized as ∼200 nm nanoparticles coated with functionalized modulators, (2) loaded with cargo, and (3) covalently surface modified with poly(ethylene glycol) (PEG) chains through mild bioconjugate reactions...
April 13, 2017: Chem
https://www.readbyqxmd.com/read/28514167/quantum-dot-peptide-fullerene-bioconjugates-for-visualization-of-in-vitro-and-in-vivo-cellular-membrane-potential
#5
Okhil Kumar Nag, Michael H Stewart, Jeffrey R Deschamps, Kimihiro Susumu, Eunkeu Oh, Vassiliy Tsytsarev, Qinggong Tang, Alexander L Efros, Roman Vaxenburg, Bryan J Black, Yungchia Chen, Thomas J O'Shaughnessy, Stella H North, Lauren D Field, Philip E Dawson, Joseph J Pancrazio, Igor L Medintz, Yu Chen, Reha S Erzurumlu, Alan L Huston, James B Delehanty
We report the development of a quantum dot (QD)-peptide-fullerene (C60) electron transfer (ET)-based nanobioconjugate for the visualization of membrane potential in living cells. The bioconjugate is comprised of (1) a central QD electron donor, (2) a membrane-inserting peptidyl linker, and (3) a C60 electron acceptor. The photoexcited QD donor engages in ET with the C60 acceptor resulting in quenching of QD photoluminescence (PL) that tracks positively with the number of C60 moieties arrayed around the QD. The nature of the QD-capping ligand also modulates the quenching efficiency; a neutral ligand coating facilitates greater QD quenching than a negatively charged carboxylated ligand...
May 17, 2017: ACS Nano
https://www.readbyqxmd.com/read/28513734/strained-alkynes-derived-from-2-2-dihydroxy-1-1-biaryls-synthesis-and-copper-free-cycloaddition-with-azides
#6
Alessandro Del Grosso, Lavrentis-Dimitrios Galanopoulos, Cookson K C Chiu, Guy J Clarkson, Peter B O Connor, Martin Wills
A series of strained alkynes were prepared from 2,2'-dihydroxy-biaryls. Several were characterised by X-ray crystallography, revealing strained C(sp)-C(sp)-C(sp(3)) bond angles in the range of 163-167°. Their cycloadditions with azides proceed without a catalyst. Functionalised versions of these reagents have potential applications to materials synthesis and bioconjugations.
May 17, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28507710/semiconducting-polymer-dots-with-bright-narrow-band-emission-at-800-nm-for-biological-applications
#7
Dandan Chen, I-Che Wu, Zhihe Liu, Ying Tang, Haobin Chen, Jiangbo Yu, Changfeng Wu, Daniel T Chiu
The development of near-infrared (NIR) fluorescent probes is critical for in vivo exploration of the fundamental and complex processes in living systems by noninvasive fluorescence imaging techniques. Semiconducting polymer dots (Pdots) are emerging as important probes that exhibit several advantages, such as high brightness and biocompatibility. However, NIR-emitting Pdots are very rare, particularly at the center (∼800 nm) of the first optical window of biological tissues (between 650 nm and 950 nm). In this paper, we describe the synthesis of a semiconducting polymer with bright and narrow-band emission at 800 nm...
May 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28497817/rechargeable-and-led-activated-znga2o4%C3%A2-%C3%A2-cr-3-near-infrared-persistent-luminescence-nanoprobes-for-background-free-biodetection
#8
Zhihao Zhou, Wei Zheng, Jintao Kong, Yan Liu, Ping Huang, Shanyong Zhou, Zhuo Chen, Jianlin Shi, Xueyuan Chen
Persistent luminescence nanoparticles (PLNPs) have shown great promise in the field of biomedicine, but are currently limited by the challenge in the synthesis of high-quality PLNPs with bright persistent luminescence and a long afterglow time. Herein, we report a facile strategy for the synthesis of monodisperse, rechargeable and LED-activated ZnGa2O4 : Cr(3+) near-infrared (NIR) PLNPs based on a modified solvothermal liquid-solid-solution method. The as-synthesized PLNPs are not only flexible for bioconjugation, but could also circumvent the limitation of the weak persistent luminescence and short afterglow time that most PLNPs confronted owing to their rechargeable capability...
May 12, 2017: Nanoscale
https://www.readbyqxmd.com/read/28489346/metal-organic-frameworks-at-the-biointerface-synthetic-strategies-and-applications
#9
Christian Doonan, Raffaele Riccò, Kang Liang, Darren Bradshaw, Paolo Falcaro
Many living organisms are capable of producing inorganic materials of precisely controlled structure and morphology. This ubiquitous process is termed biomineralization and is observed in nature from the macroscale (e.g., formation of exoskeletons) down to the nanoscale (e.g., mineral storage and transportation in proteins). Extensive research efforts have pursued replicating this chemistry with the overarching aims of synthesizing new materials of unprecedented physical properties and understanding the complex mechanisms that occur at the biological-inorganic interface...
May 10, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28487921/triplex-hybridizing-bioconjugated-gold-nanoparticles-for-specific-y-chromosome-sequence-targeting-of-bull-spermatozoa
#10
L Gamrad, R Mancini, D Werner, D Tiedemann, U Taylor, A Ziefuß, C Rehbock, S Klein, W Kues, S Barcikowski, D Rath
Gold nanoparticles (AuNPs) are widely used in biomedical applications for drug targeting and bioimaging. This often neccesitates their functionalization with biomolecules carrying a defined biological function, yielding gold nanoparticle bioconjugates. The utilization of triplex-forming oligonucleotides (TFOs) as ligands gives access to nanoconjugates as tools for specific DNA-related nanotargeting via triplex hybridization. Since triplex hybridization with nanobioconjugates has to date not been shown on biologically relevant samples, sex-specific sperm marking may be an appropriate model system to demonstrate the opportunities of this targeting method in vitro...
May 10, 2017: Analyst
https://www.readbyqxmd.com/read/28479234/controlled-delivery-of-single-or-multiple-antigens-in-tolerogenic-nanoparticles-using-peptide-polymer-bioconjugates
#11
Ryan M Pearson, Liam M Casey, Kevin R Hughes, Leon Z Wang, Madeleine G North, Daniel R Getts, Stephen D Miller, Lonnie D Shea
Polymeric nanoparticles (NPs) have demonstrated their potential to induce antigen (Ag)-specific immunological tolerance in multiple immune models and are at various stages of commercial development. Association of Ag with NPs is typically achieved through surface coupling or encapsulation methods. However, these methods have limitations that include high polydispersity, uncontrollable Ag loading and release, and possible immunogenicity. Here, using antigenic peptides conjugated to poly(lactide-co-glycolide), we developed Ag-polymer conjugate NPs (acNPs) with modular loading of single or multiple Ags, negligible burst release, and minimally exposed surface Ag...
May 4, 2017: Molecular Therapy: the Journal of the American Society of Gene Therapy
https://www.readbyqxmd.com/read/28471005/rationally-designed-solvatochromic-fluorescent-indoline-derivatives-for-probing-mitochondrial-environment
#12
Apurba Lal Koner, Kaushik Pal
A new class of solvatochromic, robust and multifunctional fluorescent probe derived from indoline is presented. Specificity of mitochondria targeting has been achieved and utilized for probing its polarity in normal and apoptotic condition. Large Stokes-shift, high quantum yield, thermal, photochemical, pH stability, tolerance to buffer compositions and bioconjugation tool-kit makes it competent for live-cell fluorescence imaging.
May 4, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28467841/in-situ-synthesis-of-phospholipid-membranes
#13
Neal K Devaraj
Cells produce lipid membranes de novo through a complex sequence of enzymatic reactions that are difficult to reconstitute in a minimal system. We set out to take a different approach and mimic the synthesis of phospholipids using abiotic but highly selective bioconjugation reactions. Here, I outline several of our group's recent advances in exploring chemoselective reactions for stitching together lipid fragments to form membrane-forming lipids from non-membrane-forming precursors. Rapid chemical reactions can be harnessed to achieve facile de novo synthesis of lipid membranes, and spontaneous membrane formation can be applied for the reconstitution of membrane proteins, encapsulation and concentration of nanomaterials, and the study of lipid membrane remodeling...
May 12, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28463376/o-o-difluorination-of-aromatic-azide-yields-a-fast-response-fluorescent-probe-for-h2s-detection-and-for-improved-bioorthogonal-reactions
#14
Jie Zhang, Yasi Gao, Xueying Kang, Zhentao Zhu, Zhiqian Wang, Zhen Xi, Long Yi
The development of efficient bioorthogonal reactions for sensing of endogenous biomolecules and for bioconjugation should be of paramount importance in the field of chemical biology. In this work, the o,o'-difluorinated aromatic azide was firstly employed to develop a new fast-response fluorescent probe 1 for H2S detection and for bioorthogonal reactions. Compared with non- and mono-fluorinated probes, 1 showed faster reaction toward H2S, the third gasotransmitter, in buffer (pH 7.4), implying that the reaction rate could be enhanced by the dual-fluorine groups...
May 16, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28462989/developing-targeted-hybrid-imaging-probes-by-chelator-scaffolding
#15
Dominik Summer, Leo Grossrubatscher, Milos Petrik, Tereza Michalcikova, Zbynek Novy, Christine Rangger, Maximilian Klingler, Elisabeth von Guggenberg, Roland Haubner, Piriya Kaeopookum, Hubertus Haas, Clemens Decristoforo
Positron emission tomography (PET) as well as optical imaging (OI) with peptide receptor targeting probes have proven their value for oncological applications but also show restrictions depending on the clinical field of interest. Therefore the combination of both methods, particularly in a single molecule, could improve versatility in clinical routine. This proof of principle study aims to show that a chelator, Fusarinine C (FSC), can be utilized as scaffold for novel dimeric dual-modality imaging agents. Two targeting vectors (a minigastrin analogue (MG11) targeting cholecystokinin-2 receptor overexpression (CCK2R) or integrin V3 targeting cyclic pentapeptides (RGD)) and a near-infrared fluorophore (Sulfo-Cyanine7) were conjugated to FSC...
May 2, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28457140/bioconjugate-therapeutics-current-progress-and-future-perspective
#16
Feng Li, Ram I Mahato
No abstract text is available yet for this article.
May 1, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28451106/molecular-basis-for-functional-switching-of-gfp-by-two-disparate-non-native-post-translational-modifications-of-a-phenyl-azide-reaction-handle
#17
Andrew M Hartley, Harley L Worthy, Samuel C Reddington, Pierre J Rizkallah, D Dafydd Jones
Through the genetic incorporation of a single phenyl azide group into superfolder GFP (sfGFP) at residue 148 we provide a molecular description of how this highly versatile chemical handle can be used to positively switch protein function in vitro and in vivo via either photochemistry or bioconjugation. Replacement of H148 with p-azido-l-phenylalanine (azF) blue shifts the major excitation peak ∼90 nm by disrupting the H-bond and proton transfer network that defines the chromophore charged state. Bioorthogonal click modification with a simple dibenzylcyclooctyne or UV irradiation shifts the neutral-anionic chromophore equilibrium, switching fluorescence to the optimal ∼490 nm excitation...
October 1, 2016: Chemical Science
https://www.readbyqxmd.com/read/28450780/new-generation-of-electrochemical-immunoassay-based-on-polymeric-nanoparticles-for-early-detection-of-breast-cancer
#18
Fouzi Mouffouk, Sihem Aouabdi, Entesar Al-Hetlani, Hacene Serrai, Tareq Alrefae, Liaohai Leo Chen
Screening and early diagnosis are the key factors for the reduction of mortality rate and treatment cost of cancer. Therefore, sensitive and selective methods that can reveal the low abundance of cancer biomarkers in a biological sample are always desired. Here, we report the development of a novel electrochemical biosensor for early detection of breast cancer by using bioconjugated self-assembled pH-responsive polymeric micelles. The micelles were loaded with ferrocene molecules as "tracers" to specifically target cell surface-associated epithelial mucin (MUC1), a biomarker for breast and other solid carcinoma...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28450191/targeting-neuronal-nitric-oxide-synthase-by-a-cell-penetrating-peptide-tat-lk15-sirna-bioconjugate
#19
Jie Peng, Yun Rao, Xue Yang, Ji Jia, Youping Wu, Jianhua Lu, Yuanxiang Tao, Weifeng Tu
We developed a cell penetrating peptide (CPP) Tat-LK15, as a siRNA carrier to target nNOS. The feasibility, stability, efficiency and selectivity of this peptide-siRNA complex were evaluated in rat neuronal cells. We also compared the new method with conventional siRNA carrier Lipofectamine™. It was found that the CPP Tat-LK15 effectively and specifically delivered nNOS-siRNA into Rat retinal ganglia (RGC-5) cells and silenced the expression of nNOS. The CPP Tat-LK15 can conjugate with siRNA to form stable complex at a ratio of 2:1 (peptide/siRNA, w/w), which maintained stable in serum for as long as 4h...
April 24, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28450070/synthesis-of-androstene-oxime-nitrogen-mustard-bioconjugates-as-potent-antineoplastic-agents
#20
Pratap Chandra Acharya, Ranju Bansal
In the present study, synthesis and antineoplastic activity of phenylacetic acid and benzoic acid nitrogen mustard conjugates of various steroidal oximes are reported for the first time. The conjugation was achieved through a more stable oxime-ester linkage and the resulting newly synthesized conjugates were evaluated in vitro on various human cancer cell lines for cytotoxicity. The extent of their alkylating activity was investigated by the in vitro colorimetric 4-(p-nitrobenzyl)pyridine (NBP) assay. The 17E-steroidal oxime-benzoic acid mustard ester 3β-acetoxy-17E-[p-(N,N-bis(2-chloroethyl)amino)]benzoyloxyimino-androst-5-ene (8) emerged as the most potent conjugate having significant cytotoxicity on most of the NCI 60-cell lines...
April 24, 2017: Steroids
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