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Click chemistry

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https://www.readbyqxmd.com/read/29786944/design-synthesis-and-evaluation-of-a-novel-series-of-inhibitors-reversing-p-glycoprotein-mediated-multidrug-resistance
#1
Hesham Ghaleb, Huilan Li, Mutta Kairuki, Qianqian Qiu, Xinzhou Bi, Chunxia Liu, Chen Liao, Jieming Li, Kamal Hezam, Wenlong Huang, Hai Qian
Multidrug resistance (MDR) is still the main barrier to attaining effective results with chemotherapy. Discovery of new chemo-reversal agents is needed to overcome MDR. Our study focused on a better way to obtain novel drugs with triazole rings that have an MDR-reversal ability through click chemistry. Among 20 developed compounds, compound 19 had a minimal cytotoxic effect compared to tariquidar and verapamil (VRP) and showed a higher reversal activity than VRP through increased accumulation in K562/A02 cells...
May 22, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29784475/post-fabrication-qac-functionalized-thermoplastic-polyurethane-for-contact-killing-catheter-applications
#2
Zachary K Zander, Peiru Chen, Yen-Hao Hsu, Nathan Z Dreger, Laura Savariau, Willie C McRoy, Alec E Cerchiari, Sean D Chambers, Hazel A Barton, Matthew L Becker
The use of catheters is ubiquitous in medicine and the incidence of infection remains unacceptably high despite numerous advances in functional surfaces and drug elution. Herein we report the use of a thermoplastic polyurethane containing an allyl ether side-chain functionality (allyl-TPU) that allows for rapid and convenient surface modification with antimicrobial reagents, post-processing. This post-processing functionalization affords the ability to target appropriate TPU properties and maintain the functional groups on the surface of the device where they do not affect bulk properties...
May 11, 2018: Biomaterials
https://www.readbyqxmd.com/read/29783836/a-y-shaped-three-arm-structure-for-probing-bivalent-interactions-between-protein-receptor-ligand-using-afm-and-spr
#3
Subhadip Senapati, Sudipta Biswas, Saikat Manna, Robert Ros, Stuart Lindsay, Peiming Zhang
The goal of this research was to develop linkage chemistry for the study of bivalent interactions between a receptor and its ligand using atomic force microscopy (AFM) and surface plasmon resonance (SPR). We conceived a three-arm structure composed of flexible chains connected to a large rigid core with orthogonal functional groups at their ends for formation and attachment (or immobilization) of bivalent ligands. To demonstrate the principle, we chose the well-known biotin-streptavidin interaction as a model system...
May 21, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/29781014/cat-elcca-catalyzing-drug-discovery-through-click-chemistry
#4
Amanda L Garner
Click chemistry has emerged as a powerful tool in our arsenal for unlocking new biology. This includes its utility in both chemical biology and drug discovery. An emerging application of click chemistry is in the development of biochemical assays for high-throughput screening to identify new chemical probes and drug leads. This Feature Article will discuss the advancements in click chemistry that were necessary for the development of a new class of biochemical assay, catalytic enzyme-linked click chemistry assay or cat-ELCCA...
May 21, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29780504/gene-specific-loci-quantitative-and-single-base-resolution-analysis-of-5-formylcytosine-by-compound-mediated-polymerase-chain-reaction
#5
Yafen Wang, Chaoxing Liu, Xiong Zhang, Wei Yang, Fan Wu, Guangrong Zou, Xiaocheng Weng, Xiang Zhou
5-Formylcytosine (5fC) is known as one of the key players in the process of active DNA demethylation and displays essential epigenetic functions in mammals. In spite of the blooming development of whole genome sequencing methods for this modified cytosine base, the easily operated gene specific-loci detection of 5fC has rarely been reported. Herein, we present a compound-mediated analysis of the content and site of 5fC by the polymerase chain reaction (PCR) assay. The molecule, namely azi-BP, which can selectively label 5fC and form a huge group through a click chemistry reaction, hindering the amplification activity of Taq DNA polymerase, acts as a "roadblock" and enables the quantitative analysis of 5fC by quantitative polymerase chain reaction (qPCR)...
April 21, 2018: Chemical Science
https://www.readbyqxmd.com/read/29780463/simultaneous-multiple-single-nucleotide-polymorphism-detection-based-on-click-chemistry-combined-with-dna-encoded-probes
#6
Qian-Yu Zhou, Fang Yuan, Xiao-Hui Zhang, Ying-Lin Zhou, Xin-Xiang Zhang
Single nucleotide polymorphisms (SNPs) are emerging as important biomarkers for disease diagnosis, prognostics and disease pathogenesis. As one type of disease is always connected to several SNP sites, there is great demand for a reliable multiple SNP detection method. Herein, we mimicked a ligation reaction based on DNA ligase and originally utilized an enzyme-free DNA template-directed click reaction for SNP detection. With 5'-alkyne and 3'-azide groups labelled on two oligonucleotide probes, the target DNA-directed Cu(i)-catalyzed alkyne-azide cycloaddition (CuAAC) click reaction produced a new DNA strand with a triazole backbone, as a mimic of a DNA phosphodiester linkage...
April 7, 2018: Chemical Science
https://www.readbyqxmd.com/read/29779862/replenishable-drug-depot-to-combat-post-resection-cancer-recurrence
#7
Yevgeny Brudno, Matthew J Pezone, Tracy K Snyder, Oktay Uzun, Christopher T Moody, Michael Aizenberg, David J Mooney
Local drug presentation made possible by drug-eluting depots has demonstrated benefits in a vast array of diseases, including in cancer, microbial infection and in wound healing. However, locally-eluting depots are single-use systems that cannot be refilled or reused after implantation at inaccessible sites, limiting their clinical utility. New strategies to noninvasively refill drug-eluting depots could dramatically enhance their clinical use. In this report we present a refillable hydrogel depot system based on bioorthogonal click chemistry...
May 6, 2018: Biomaterials
https://www.readbyqxmd.com/read/29779667/terminal-alkyne-biosynthesis-in-marine-microbes
#8
Xuejun Zhu, Wenjun Zhang
The terminal alkyne is a readily derivatized functionality valued for its diverse applications in material synthesis, pharmaceutical science, and chemical biology. The synthetic biology routes to terminal alkynes are highly desired and yet underexplored. Some marine natural products contain a terminal alkyne functionality, and the discovery of the biosynthetic gene clusters for jamaicamide B and carmabin A marked the beginning of a new era in the understanding and engineering of terminal alkyne biosynthesis...
2018: Methods in Enzymology
https://www.readbyqxmd.com/read/29775058/multiple-click-selective-trna-synthetases-expand-mammalian-cell-specific-proteomics
#9
Andrew C Yang, Haley du Bois, Niclas Olsson, David Gate, Benoit Lehallier, Daniela Berdnik, Kyle D Brewer, Carolyn R Bertozzi, Joshua E Elias, Tony Wyss-Coray
Bio-orthogonal tools enable cell-type-specific proteomics, a prerequisite to understanding biological processes in multicellular organisms. Here we report two engineered aminoacyl-tRNA synthetases for mammalian bio-orthogonal labeling: a tyrosyl ( ScTyrY34G ) and a phenylalanyl ( MmPheT412G ) tRNA synthetase that incorporate azide-bearing noncanonical amino acids specifically into the nascent proteomes of host cells. Azide-labeled proteins are chemoselectively tagged via azide-alkyne cycloadditions with fluorophores for imaging or affinity resins for mass spectrometric characterization...
May 18, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29774654/a-photoactivatable-%C3%AE-5%C3%AE-1-specific-integrin-ligand
#10
Aranzazu Del Campo, Roshna V Nair, Aleeza Farrukh
The integrin α5β1 is overexpressed in colon, breast, ovarian, lung and brain tumors and has been identified as key component in mechanosensing. In order to study how dynamic changes of α5β1 engagement affect cellular behaviour, photoactivatable derivatives of α5β1 specific ligands are presented in this article. A photoremovable protecting group (PRPG) was introduced into the ligand structure at a relevant position for integrin recognition. The presence of the chromophore temporally inhibited ligand bioactivity...
May 18, 2018: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/29772166/pixel-counting-of-fluorescence-spots-triggered-by-dna-walkers-for-ultrasensitive-quantification-of-nucleic-acid
#11
Longyi Zhu, Qihui Liu, Bangyu Yang, Huangxian Ju, Jianping Lei
A pixel counting strategy is designed based on DNA walker-triggered fluorescence spots for ultrasensitive detection of nucleic acid. The two-dimensional DNA walker was constructed by hybridization of the dye-labeled hairpin structure (hDNA) as track and swing strand (sDNA) as DNAzyme with two types of capture DNAs covalently modified by click chemistry on glass slide. Introduction of target DNA unlocked the sDNA via strand displacement to form the activated DNAzyme, and the latter cut nearby hDNA with Mn2+ as cofactor, resulting in fluorescence recovery of dye-labeled hDNA on the substrate due to the separation from the quencher...
May 17, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29767952/laser-cleavable-probes-based-cell-surface-engineering-for-in-situ-sialoglycoconjugates-profiling-by-ldi-mass-spectrometry
#12
Jie Sun, Huihui Liu, Lingpeng Zhan, Caiqiao Xiong, Xi Huang, Jinjuan Xue, Zongxiu Nie
Cell-surface sialoglycoconjugates (sialoglycoproteins & sialoglycolipids) play important roles in cell-cell interactions and related tumor metastasis process. Although there have been some analytical methods to evaluate the sialoglycoconjugates, an effective method providing both qualitative and quantitative information is still deficient. Here we establish an extraction-free, sensitive and high-throughput platform to realize in-situ detection of the cell-surface sialoglycoconjugates on various cell lines, e...
May 16, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29766153/a-bioorthogonal-turn-on-fluorescent-strategy-for-the-detection-of-lysine-acetyltransferase-activity
#13
Maomao He, Zhen Han, Jing Qiao, Liza Ngo, May P Xiong, Y George Zheng
Lysine acetylation plays vital roles in the regulation of fundamental cellular processes, which is mediated by lysine acetyltransferases (KATs). Developing chemical biology probes for KAT activity detection is of important value in providing improved understanding of their biological functions. We reported a panel of "turn-on" fluorescent probes for sensitive and selective detection of KAT enzymatic activity through a simple mix-and-read format. Combined with bioorthogonal substrate labelling and click chemistry, these probes produced strong "turn-on" fluorescent signals in response to KAT-mediated acylation process...
May 16, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29763554/template-catalyzed-disulfide-conjugation-of-monoclonal-antibodies-using-a-natural-amino-acid-tag
#14
Jeremy D King, Yuelong Ma, Yi-Chui Kuo, Krzysztof P Bzymek, Leah H Goodstein, Kassondra Meyer, Roger E Moore, Desiree Crow, David Colcher, Gagandeep Singh, David A Horne, John C Williams
The high specificity and favorable pharmacological properties of monoclonal antibodies (mAbs) have prompted significant interest in re-engineering this class of molecules to add novel functionalities for enhanced therapeutic and diagnostic potential. Here, we used the high affinity, meditope-Fab interaction to template and drive the rapid, efficient, and stable site-specific formation of a disulfide bond. We demonstrate that this template-catalyzed strategy provides a consistent and reproducible means to conjugate fluorescent dyes, cytotoxins, or "click" chemistry handles to meditope-enabled mAbs (memAbs) and memFabs...
May 15, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29759208/polarity-tuned-perphenylcarbamoylated-cyclodextrin-separation-materials-for-achiral-and-chiral-differentiation
#15
Xiaoxuan Li, Jia Li, Qing Kang, Yong Wang
Phenylcarbamoyls are known to remarkably accentuate cyclodextrin's enantioselectivities. In this work, by inducing electron-donating methoxyl or electron-withdrawing bromine/trifluoromethyl moieties, three novel cyclodextrin enantioseparation materials including per(4-trifluoromethoxy) phenylcarbamoylated-β-CD CSP (CSP1), per(4-bromo)phenylcarbamoylated-β-CD CSP (CSP2) and per(4-methoxy)phenylcarbamoylated-β-CD CSP (CSP3) were prepared via thiol-ene click chemistry. The polarity tuning decorations are found to significantly influence the CSPs' achiral and chiral separation performance...
August 1, 2018: Talanta
https://www.readbyqxmd.com/read/29746551/a-multi-chamber-microfluidic-intestinal-barrier-model-using-caco-2-cells-for-drug-transport-studies
#16
Hsih-Yin Tan, Sofie Trier, Ulrik L Rahbek, Martin Dufva, Jörg P Kutter, Thomas L Andresen
This paper presents the design and fabrication of a multi-layer and multi-chamber microchip system using thiol-ene 'click chemistry' aimed for drug transport studies across tissue barrier models. The fabrication process enables rapid prototyping of multi-layer microfluidic chips using different thiol-ene polymer mixtures, where porous Teflon membranes for cell monolayer growth were incorporated by masked sandwiching thiol-ene-based fluid layers. Electrodes for trans-epithelial electrical resistance (TEER) measurements were incorporated using low-melting soldering wires in combination with platinum wires, enabling parallel real-time monitoring of barrier integrity for the eight chambers...
2018: PloS One
https://www.readbyqxmd.com/read/29738228/enhanced-tumor-retention-effect-by-click-chemistry-for-improved-cancer-immunochemotherapy
#17
Ling Mei, Yayuan Liu, Jingdong Rao, Xian Tang, Man Li, Zhirong Zhang, Qin He
Due to the limited drug concentration in tumor tissues and inappropriate treatment strategies, tumor recurrence and metastasis are critical challenges for effectively treating malignancies. A key challenge for effective delivery of nanoparticles is to reduce reticuloendothelial system uptake and to maximize the enhanced permeability and retention effect. Herein, we demonstrated that Cu(I)-catalyzed click chemistry triggered the aggregation of azide/alkyne-modified micelles, enhancing micelles accumulation in tumor tissues...
May 8, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29733585/clickable-and-high-sensitivity-metal-containing-tags-for-mass-cytometry
#18
Bedilu Allo, Xudong Lou, Alexandre Bouzekri, Olga I Ornatsky
Mass cytometry is a highly multiplexed single-cell analysis platform that uses metal tagged reagents to identify multiple cellular biomarkers. Current metal-tagged reagent preparation employs thiol-maleimide chemistry to covalently couple maleimide-functionalized metal-chelating polymers (MCPs) with antibodies (Abs), a process that requires partial reduction of the Ab to form reactive thiol groups. However, some classes of Abs (for example, IgM) as well as biomolecules lacking cysteine residues has been challenging to label using this method...
May 7, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29731606/clickable-prodrugs-bearing-potent-and-hydrolytically-cleavable-nicotinamide-phosphoribosyltransferase-inhibitors
#19
Keivan Sadrerafi, Emilia O Mason, Mark W Lee
Purpose: Our previous study indicated that carborane containing small-molecule 1-(hydroxymethyl)-7-(4'-( trans -3″-(3'″-pyridyl)acrylamido)butyl)-1,7-dicarbadodecaborane (hm-MC4-PPEA), was a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt). Nampt has been shown to be upregulated in most cancers and is a promising target for the treatment of many different types of cancers, including breast cancers. Patients and methods: To increase the selectivity of hm-MC4-PPEA toward cancer cells, three prodrugs were synthesized with different hydrolyzable linkers: ester, carbonate, and carbamate...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29727181/a-new-formulation-for-the-delivery-of-oligonucleotides-using-clickable-sirna-polyisoprenoid-conjugated-nanoparticles-application-to-cancers-harboring-fusion-oncogenes
#20
Liliane Massaad-Massade, Suzan Boutary, Marie Caillaud, Céline Gracia, Beatrice Parola, Soukaina Bel Gnaouiya, Barbara Stella, Silvia Arpicco, Eric Buchy, Didier Desmaêle, Patrick Couvreur, Giorgia Urbinati
The aim of the present study is to take advantage of the unique property of polyisoprenoid chains to adopt a compact molecular conformation and to use these natural and biocompatible lipids as nanocarriers of drugs to deliver siRNA. A new chemical strategy is here applied to conjugate squalene (SQ) and solanesol (SOLA) to siRNA consisting in an activated variant of the azide-alkyne Huisgen cycloaddition also known as copper-free (Cu-free) click chemistry. We conjugated siRNA against TMPRSS2-ERG, a fusion oncogene found in more than 50% of prostate cancers to SQ or SOLA...
May 4, 2018: Bioconjugate Chemistry
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