- Polymer vesicles containing small vesicles within interior aqueous compartments and pH-responsive transmembrane channels
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(Figure Presented) Multivesicle assemblies with pH-responsive transmembrane channels in the vesicle walls (see picture) were made by two-step double emulsion of copolymers comprising acrylic acid and acrylate of 1,2-distearoyl-rac-glycerol. These assemblies mimic eukaryotic cells, which contain functional organelles within the cell walls.
- Chiu, Hsin-Cheng,Lin, Yue-Wen,Huang, Yi-Fong,Chuang, Chih-Kai,Chern, Chorng-Shyan
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- Affinity chromatography with collapsibly tethered ligands
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We introduce a novel affinity chromatography mode in which affinity ligands are secured to the media surface via collapsible tethers. In traditional affinity chromatography, the immobilized ligands act passively, and their local concentration is static. In collapsibly tethered affinity chromatography, the ligand can move dynamically in response to external stimuli, a design that enables marked changes in both the local concentration of the ligand and its surrounding environment without exchange of solvent. Using the thermoresponsive polymer poly(N-isopropylacrylamide) (PIPAAm) as a scaffold for ligand and hapten attachment, we were able to achieve controlled mobility and microenvironment alteration of the affinity ligand Ricinus communis agglutinin (RCA120). The glycoprotein target, asialotransferrin, was loaded onto a column in which PIPAAm was partially substituted with both RCA120 and lactose. At 5 °C, the column retained the glycoprotein, but released most (95%) of the asialotransferrin upon warming to 30 °C. This temperature-induced elution was much greater than can be explained by temperature dependency of sugar recognition by RCA120. The simplest explanation is that upon thermally induced dehydration and collapse of the PIPAAm chains, coimmobilized RCA120 ligand and lactose hapten are brought into closer proximity to each other, enabling immobilized lactose to displace affinity-bound asislotransferrin from the immobilized RCA120 lectin.
- Yamanaka, Hidenori,Yoshizako, Kimihiro,Akiyama, Yoshikatsu,Sota, Hiroyuki,Hasegawa, Yukio,Shinohara, Yasuro,Kikuchi, Akihiko,Okano, Teruo
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- Elaboration of densely functionalized polylactide nanoparticles from N-acryloxysuccinimide-based block copolymers
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Poly(N-acryloxysuccinimide) (PNAS) and poly(N-acryloxysuccinimide-co-N- vinylpyrrolidone) (P(NAS-co-NVP)) of adjustable molecular weights and narrow polydispersities were prepared by nitroxide-mediated polymerization (NMP) in N,N-dimethylformamide in the presence of free SG1 (N-tert-butyl-N-1- diethylphosphono-(2,2-dimethylpropyl) nitroxide), with MAMA-SG1 (N-(2-methylpropyl)-N-(1-diethylphosphono-2,2-dimethylpropyl) -O-(2-carboxylprop-2-yl)hydroxylamine) alkoxyamine as initiator. The reactivity ratios of NAS and NVP were determined to be rNAS = 0.12 and r NVP = 0, indicating a strong alternating tendency for the P(NAS-co-NVP) copolymer. NAS/NVP copolymerization was then performed from a SG1-functionalized poly(D,L-lactide) (PLA-SG1) macro-alkoxyamine as initiator, leading to the corresponding PLA-b-P(NAS-co-NVP) block copolymer, with similar NAS and NVP reactivity ratios as mentioned above. The copolymer was used as a surface modifier for the PLA diafiltration and nanoprecipitation processes to achieve nanoparticles in the range of 450 and 150 nm, respectively. The presence of the functional/hydrophilic P(NAS-co-NVP) block, and particularly the N-succinimidyl (NS) ester moieties at the particle surface, was evidenced by ethanolamine derivatization and zeta potential measurements.
- Handke, Nadege,Trimaille, Thomas,Luciani, Elsa,Rollet, Marion,Delair, Thierry,Verrier, Bernard,Bertin, Denis,Gigmes, Didier
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- Synthesis of Comblike Poly(butyl methacrylate) Using Reversible Addition-Fragmentation Chain Transfer and an Activated Ester
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Comblike polymers of poly(n-butyl methacrylate) were prepared using an activated ester-type comonomer (N-acryloxysuccinimide, NAS) to generate branch points. The conventional solution free-radical copolymerization kinetics of n-butyl methacrylate (BMA) and NAS were first investigated by following individual monomer consumption rates by 1H NMR spectrometry and reactivity ratios of BMA and NAS determined using the terminal model. The reactivity ratios so obtained are both close to 0.2; the joint confidence interval is also determined. Reversible addition - fragmentation chain transfer (RAFT) was then used to grow polymers with controlled backbone and branch chain length. Because both reactivity ratios have similar values, this implies that the copolymer will have a random distribution of NAS and hence of branch points. RAFT-mediated polymerization was first used to synthesize linear poly(BMA-co-NAS) chains. Primary hydroxy-functionalized RAFT agents were then immobilized on this linear poly(BMA-co-NAS) through nucleophilic substitution on the activated ester units of the NAS. From these immobilized RAFT agents, branches were grown upon addition of a further aliquot of monomer (BMA) and initiator (AIBN). The amount of NAS in the starting BMA/NAS composition was varied without adversely affecting the uniformity of the NAS distribution along the resulting linear poly(BMA-co-NAS) backbone. This results in branched polymers whose molecular weight, branching density, and degree of polymerization of branches are all relatively narrow and controlled.
- Vosloo, Johannes J.,Tonge, Matthew P.,Fellows, Christopher M.,D'Agosto, Franck,Sanderson, Ronald D.,Gilbert, Robert G.
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- Thermo-responsive shell cross-linked PMMA-b-P(NIPAAm-co-NAS) micelles for drug delivery
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Thermo-responsive amphiphilic poly(methyl methacrylate)-b-poly(N- isopropylacrylamide-co-N-acryloxysuccinimide) (PMMA-b-P(NIPAAm-co-NAS)) block copolymer was synthesized by successive RAFT polymerizations. The uncross-linked micelles were facilely prepared by directly dissolving the block copolymer in an aqueous medium, and the shell cross-linked (SCL) micelles were further fabricated by the addition of ethylenediamine as a di-functional cross-linker into the micellar solution. Optical absorption measurements showed that the LCST of uncross-linked and cross-linked micelles was 31.0 °C and 40.8 °C, respectively. Transmission electron microscopy (TEM) showed that both uncross-linked and cross-linked micelles exhibited well-defined spherical shape in aqueous phase at room temperature, while the SCL micelles were able to retain the spherical shape with relatively smaller dimension even at 40 °C due to the cross-linked structure. In vitro drug release study demonstrated a slower and more sustained drug release behavior from the SCL micelles at high temperature as compared with the release profile of uncross-linked micelles, indicating the great potential of SCL micelles developed herein as novel smart carriers for controlled drug release.
- Chang, Cong,Wei, Hua,Wu, De-Qun,Yang, Bin,Chen, Ni,Cheng, Si-Xue,Zhang, Xian-Zheng,Zhuo, Ren-Xi
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- Semiconductor nanocrystals with multifunctional polymer ligands
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In this letter, we describe the preparation of a versatile polymer ligand, which can be attached to CdSe/ZnS semiconductor nanocrystals via a phase transfer reaction. The ligand is based on a chain of reactive esters, which can, in principle, be substituted by any compound containing amino-functionalities. The polymer/nanocrystal complexes are characterized in terms of structure and photostability. Copyright
- Potapova, Inga,Mruk, Ralf,Prehl, Sabine,Zentel, Rudolf,Basche, Thomas,Mews, Alf
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- Effective inhibitors of hemagglutination by influenza virus synthesized from polymers having active ester groups. Insight into mechanism of inhibition
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Highly effective sialic acid-containing inhibitors of influenza virus X- 31 were synthesized using poly[N-(acryoyloxy)succinimide] (pNAS), a polymer preactivated by incorporation of active ester groups. Polymers containing two and three different components were prepared by sequential reaction of pNAS with two and three amines, respectively. This preparation of co- and terpolymers was synthetically more efficient than methods involving copolymerization of different monomers and gave polymers that were more easily compared than those generated by copolymerization. Polymers in this study (prepared from a single batch of pNAS) had a constant degree of polymerization (DP ? 2000) and probably had a distribution of components that was more random than analogous polymers prepared by copolymerization. Use of C-glycosides of sialic acid made it possible to investigate inhibition by different polymers at temperatures ranging from 4 to 36°C without artifacts due to the hydrolytic action of neuraminidase. The inhibitors were, in general, more effective at 36 °C than at 4 °C. The hemagglutination (HAI) assay was used to measure the value of the inhibition constant K(i)/(HAI) each polymer. The value of K(i)/(HAI) for the two-component polymer containing 20% sialic acid on a polyacrylamide backbone at 4 °C was 4 nM (in terms of the sialic acid moieties present in solution) and was approximately 50-fold more effective than the best inhibitors previously described and 25-fold more effective than the best naturally occurring inhibitor. The most effective inhibitor synthesized in this work contained 10% benzyl amine and 20% sialic acid on a polyacrylamide backbone, and its value of K(i)/(HAI) was 600 pM at 36 °C. Approximately 100 polymers that differed in one or two components were assayed to distinguish between two limiting mechanisms for inhibition of the interaction between the surfaces of virus and erythrocytes: high-affinity binding through polyvalency, and steric stabilization. The results suggest that both mechanisms play an important role. The system comprising polyvalent inhibitors of agglutination of erythrocytes by influenza provides a system that may be useful as a model for inhibitors of other pathogen-host interactions, a large number of which are themselves polyvalent.
- Mammen,Dahmann,Whitesides
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- Temperature-Switchable Glycopolymers and Their Conformation-Dependent Binding to Receptor Targets
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The temperature-dependent binding of copolymers from poly(N-isopropylacrylamide) (PNIPAM) and mannose ligands to Escherichia coli and concanavalin A (ConA) is determined. Through polymer analogous reactions using poly(N-acryloxysuccinimide) and amine-linked mannose residues with different linkers, glycopolymers are prepared with the variation of the mannose density. Quantitative adhesion inhibition assays show the inhibitory potential of the glycopolymers as a function of the mannose/NIPAM ratio and linker type above and below their lower critical solution temperature (LCST). Intriguingly, opposite temperature effects on the binding to E. coli and ConA are observed. While the E. coli inhibition is stronger above the LCST, the ConA inhibition is, in overall, weaker at elevated temperatures. When going beyond the LCST, the polymers undergo a coil-to-globule transition, forming microphases with surface-enriched hydrophilic sugar moieties exhibiting increased E. coli inhibition through steric shielding. However, the formation of such microphases above the LCST renders a fraction of carbohydrate ligands inaccessible,and the polymers remaining in the solution phase then have coil sizes below the minimum binding site spacing of the ConA receptor, explaining reduced ConA inhibition. Overall, these results suggest that the coil-to-globule transition of glycopolymers may induce lower or higher inhibitory potentials due to the adverse effects of steric shielding and carbohydrate ligand accessibility.
- Paul, Tanja J.,Strzelczyk, Alexander K.,Feldhof, Melina I.,Schmidt, Stephan
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- Efficient Amino-Sulfhydryl Stapling on Peptides and Proteins Using Bifunctional NHS-Activated Acrylamides
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Widely used reagents in the peptide functionalization toolbox, Michael acceptors and N-hydroxysuccinimide (NHS) activated esters, are combined in NHS-activated acrylamides for efficient chemoselective amino-sulfhydryl stapling on native peptides and proteins. NHS-activated acrylamides allow for a fast functionalization of N-terminal cysteines (k2=1.54±0.18×103 M?1 s?1) under dilute aqueous conditions, enabling selectivity over other nucleophilic amino acids. Additionally, the versatility of these new bioconjugation handles was demonstrated in the cross-linking of in-chain or C-terminal cysteines with nearby lysine residues. NHS-activated acrylamides are compatible with the use of other cysteine selective reagents, allowing for orthogonal dual-modifications. This strategy was successfully applied to the late-stage functionalization of peptides and proteins with a PEG unit, fluorescent probe, and cytotoxic agent. The level of molecular control offered by NHS-activated acrylamides is expected to promote amino-sulfhydryl stapling technology as a powerful strategy to design functional bioconjugates.
- Silva, Maria J. S. A.,Faustino, Hélio,Coelho, Jaime A. S.,Pinto, Maria V.,Fernandes, Adelaide,Compa?ón, Ismael,Corzana, Francisco,Gasser, Gilles,Gois, Pedro M. P.
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supporting information
p. 10850 - 10857
(2021/04/15)
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- Modified Polyvinylchloride Surface with Antibacterial and Antifouling Functions
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Disclosed are materials having an antifouling and a biocidal property. The materials include a polyvinylchloride plastic covalently linked to a polymer, where the polymer includes an antifouling component and a biocidal component.
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Paragraph 0021
(2020/08/12)
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- A GENETICALLY ENCODED, PHAGE-DISPLAYED CYCLIC PEPTIDE LIBRARY AND METHODS OF MAKING THE SAME
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Embodiments of the present disclosure pertain to methods of selecting cyclic peptides that bind to a target by transforming a phage display library with a plurality of nucleic acids into bacterial host cells, where the nucleic acids include phage coat protein genes with a combinatorial region that encodes at least one cysteine and at least one non-canonical amino acid. The transformation results in the production of phage particles with phage coat proteins where the cysteine and the non-canonical amino acid couple to one another to form a cyclic peptide library. Phage particles are then screened against the desired target to select bound cyclic peptides. Amino acid sequences of the selected cyclic peptides are then identified. Additional embodiments pertain to methods of constructing a phage display library that encodes the cyclic peptides. Further embodiments of the present disclosure pertain to the produced cyclic peptides, phage display libraries and phage particles.
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Paragraph 0094; 00117-00119; 00158; 00163
(2020/12/07)
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- A Genetically Encoded, Phage-Displayed Cyclic-Peptide Library
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Superior to linear peptides in biological activities, cyclic peptides are considered to have great potential as therapeutic agents. To identify cyclic-peptide ligands for therapeutic targets, phage-displayed peptide libraries in which cyclization is achieved by the covalent conjugation of cysteines have been widely used. To resolve drawbacks related to cysteine conjugation, we have invented a phage-display technique in which its displayed peptides are cyclized through a proximity-driven Michael addition reaction between a cysteine and an amber-codon-encoded N?-acryloyl-lysine (AcrK). Using a randomized 6-mer library in which peptides were cyclized at two ends through a cysteine–AcrK linker, we demonstrated the successful selection of potent ligands for TEV protease and HDAC8. All selected cyclic peptide ligands showed 4- to 6-fold stronger affinity to their protein targets than their linear counterparts. We believe this approach will find broad applications in drug discovery.
- Wang, Xiaoshan Shayna,Chen, Peng-Hsun Chase,Hampton, J. Trae,Tharp, Jeffery M.,Reed, Catrina A.,Das, Sukant K.,Wang, Duen-Shian,Hayatshahi, Hamed S.,Shen, Yang,Liu, Jin,Liu, Wenshe Ray
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supporting information
p. 15904 - 15909
(2019/10/28)
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- N?-Acryloyllysine Piperazides as Irreversible Inhibitors of Transglutaminase 2: Synthesis, Structure-Activity Relationships, and Pharmacokinetic Profiling
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Transglutaminase 2 (TGase 2)-catalyzed transamidation represents an important post-translational mechanism for protein modification with implications in physiological and pathophysiological conditions, including fibrotic and neoplastic processes. Consequently, this enzyme is considered a promising target for the diagnosis of and therapy for these diseases. In this study, we report on the synthesis and kinetic characterization of N?-acryloyllysine piperazides as irreversible inhibitors of TGase 2. Systematic structural modifications on 54 new compounds were performed with a major focus on fluorine-bearing substituents due to the potential of such compounds to serve as radiotracer candidates for positron emission tomography. The determined inhibitory activities ranged from 100 to 10?000 M-1 s-1, which resulted in comprehensive structure-activity relationships. Structure-activity correlations using various substituent parameters accompanied by covalent docking studies provide an advanced understanding of the molecular recognition for this inhibitor class within the active site of TGase 2. Selectivity profiling of selected compounds for other transglutaminases demonstrated an excellent selectivity toward transglutaminase 2. Furthermore, an initial pharmacokinetic profiling of selected inhibitors was performed, including the assessment of potential membrane permeability and liver microsomal stability.
- Wodtke, Robert,Hauser, Christoph,Ruiz-Gómez, Gloria,J?ckel, Elisabeth,Bauer, David,Lohse, Martin,Wong, Alan,Pufe, Johanna,Ludwig, Friedrich-Alexander,Fischer, Steffen,Hauser, Sandra,Greif, Dieter,Pisabarro, M. Teresa,Pietzsch, Jens,Pietsch, Markus,L?ser, Reik
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supporting information
p. 4528 - 4560
(2018/05/07)
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- An Oxygen-Tolerant PET-RAFT Polymerization for Screening Structure–Activity Relationships
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The complexity of polymer–protein interactions makes rational design of the best polymer architecture for any given biointerface extremely challenging, and the high throughput synthesis and screening of polymers has emerged as an attractive alternative. A porphyrin-catalysed photoinduced electron/energy transfer–reversible addition-fragmentation chain-transfer (PET-RAFT) polymerisation was adapted to enable high throughput synthesis of complex polymer architectures in dimethyl sulfoxide (DMSO) on low-volume well plates in the presence of air. The polymerisation system shows remarkable oxygen tolerance, and excellent control of functional 3- and 4-arm star polymers. We then apply this method to investigate the effect of polymer structure on protein binding, in this case to the lectin concanavalin A (ConA). Such an approach could be applied to screen the structure–activity relationships for any number of polymer–protein interactions.
- Gormley, Adam J.,Yeow, Jonathan,Ng, Gervase,Conway, órla,Boyer, Cyrille,Chapman, Robert
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supporting information
p. 1557 - 1562
(2018/01/15)
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- Efficient Construction of Well-Defined Multicompartment Porous Systems in a Modular and Chemically Orthogonal Fashion
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A microfluidic assembly approach was developed for efficiently producing hydrogel spheres with reactive multidomains that can be employed as an advantageous platform to create spherical porous networks in a facile manner with well-defined multicompartments and spatiotemporally controlled functions. This strategy allows for not only large scale fabrication of various robust hydrogel microspheres with controlled size and porosity, but also the domains embedded in hydrogel network could be introduced in a modular manner. Additionally, the number of different domains and their ratio could be widely variable on demand. More importantly, the reactive groups distributed in individual domains could be used as anchor sites to further incorporate functional units in an orthogonal fashion, leading to well-defined multicompartment systems. The strategy provides a new and efficient route to construct well-defined functional multicompartment systems with great flexibility and extendibility.
- Gao, Ning,Tian, Tian,Cui, Jiecheng,Zhang, Wanlin,Yin, Xianpeng,Wang, Shiqiang,Ji, Jingwei,Li, Guangtao
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supporting information
p. 3880 - 3885
(2017/03/27)
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- POLYMER BACKBONE ELEMENT TAGS
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Element tags based on novel metal-polymer conjugates are provided for elemental analysis of analytes, including ICP-MS. A polymer backbone is functionalized to irreversibly bind metals that are selected prior to use by the user. The polymer is further functionalized to attach a linker which allows for attachment to antibodies or other affinity reagents. The polymer format allows attachment of many copies of a given isotope, which linearly improves sensitivity. The metal-polymer conjugate tags enable multiplexed assay in two formats : bulk assay, where the average biomarker distribution in the sample is diagnostic, and single cell format to distinguish a rare (for example a diseased) cell in a complex sample (for example, blood).
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Paragraph 0098
(2016/01/29)
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- CARBOHYDRATE LIGANDS THAT BIND TO IGM ANTIBODIES AGAINST MYELIN-ASSOCIATED GLYCOPROTEIN
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The invention relates to carbohydrate ligands presenting the minimal Human Natural Killer-1 (HNK-1) epitope that bind to anti-MAG (myelin-associated glycoprotein) IgM antibodies, and their use in diagnosis as well as for the treatment of anti-MAG neuropathy. In particular, the invention relates to disaccharides of formula (I) and (II) wherein Z is optionally substituted phenyl, heteroaryl, arylcarbonyl, or heteroarylmethyl, and to therapeutically acceptable polymers comprising a multitude of substituents of formula (I) and/or formula (II), wherein Z is a bifunctional linker connecting the disaccharides to the polymer backbone.
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Page/Page column 48
(2015/10/05)
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- Conducting polymer nanoparticles decorated with collagen mimetic peptides for collagen targeting
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We report on the formation of conducting polymer nanoparticles (CPNs), stabilized by a collagen mimetic peptide (CMP)-polymer amphiphile. CPNs ranging from ~15 to 40 nm were readily accessible upon modifying the amphiphile concentration. Surface presentation of CMPs on CPN precluded intra-/inter-particle trimerization, while preserving their ability to target collagen without pre-activation.
- Santos, Jos Luis,Li, Yang,Culver, Heidi R.,Yu, Michael S.,Herrera-Alonso, Margarita
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supporting information
p. 15045 - 15048
(2015/02/19)
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- Continuous recycling of homogeneous Pd/Cu catalysts for cross-coupling reactions
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Given the importance of homogeneous catalysts recycling in organic chemistry, we have developed a unique microfluidic loop system for automated continuous recirculation of a soluble polymer supported metal catalyst for novel isocyanide cross-coupling reactions under thermomorphic multicomponent solvent (TMS) conditions. Our system provides an innovative approach for the chemical library synthesis of quinazolinone derivatives as well as an important intermediate of Merck's LTD4 antagonist "Singulair" with efficient continuous homogeneous catalyst recycling.
- Sharma, Siddharth,Basavaraju,Singh, Ajay K.,Kim, Dong-Pyo
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supporting information
p. 3974 - 3977
(2014/08/18)
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- Design and synthesis of novel DOTA(Gd3+)-polymer conjugates as potential MRI contrast agents
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Conventional low molecular weight gadolinium based Magnetic Resonance Imaging (MRI) contrast agents such as Magnevist are very useful for imaging tissues. However, at the high magnetic fields used in modern MRI equipments, their relaxivity (contrasting efficiency) is rather poor. The grafting of the gadolinium complex onto macromolecules is a way to enhance their relaxivity provided that the rotational motion of the complex is decreased significantly. Here we report the design of novel Gd3+ based MRI contrast agents with improved relaxivity and potential long blood circulation life-time. We investigate the grafting of 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid, 1,4,7-tris(1,1-dimethylethyl) ester (DO3AtBu-NH2; a precursor of Gd3+ ligand) onto well-defined functional copolymers bearing activated esters (succinimidyl esters) and poly(ethylene oxide) (PEO) chains required for stealthiness. The tert-butyl groups of grafted DO3AtBu-NH 2 are then deprotected by trifluoroacetic acid followed by complexation of Gd3+. Addition of free DOTA at the end of the reaction is necessary to leave the pure and stable water soluble macrocontrast agent. Importantly it shows a relaxivity at high frequencies that is 300% higher than that of the ungrafted gadolinium complex. These novel functional copolymers are therefore promising candidates as macromolecular contrast agents for MRI applications.
- Grogna, Mathurin,Cloots, Rudi,Luxen, Andre,Jerome, Christine,Desreux, Jean-F.,Detrembleur, Christophe
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experimental part
p. 12917 - 12926
(2011/12/21)
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- Compact biocompatible quantum dots via RAFT-mediated synthesis of imidazole-based random copolymer ligand
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We present a new class of polymeric ligands for quantum dot (QD) water solubilization to yield biocompatible and derivatizable QDs with compact size (10-12 nm diameter), high quantum yields (>50%), excellent stability across a large pH range (pH 5-10.5), and low nonspecific binding. To address the fundamental problem of thiol instability in traditional ligand exchange systems, the polymers here employ a stable multidentate imidazole binding motif to the QD surface. The polymers are synthesized via reversible addition-fragmentation chain transfer-mediated polymerization to produce molecular weight controlled monodisperse random copolymers from three types of monomers that feature imidazole groups for QD binding, polyethylene glycol (PEG) groups for water solubilization, and either primary amines or biotin groups for derivatization. The polymer architecture can be tuned by the monomer ratios to yield aqueous QDs with targeted surface functionalities. By incorporating amino-PEG monomers, we demonstrate covalent conjugation of a dye to form a highly efficient QD-dye energy transfer pair as well as covalent conjugation to streptavidin for high-affinity single molecule imaging of biotinylated receptors on live cells with minimal nonspecific binding. The small size and low serum binding of these polymer-coated QDs also allow us to demonstrate their utility for in vivo imaging of the tumor microenvironment in live mice.
- Liu, Wenhao,Greytak, Andrew B.,Lee, Jungmin,Wong, Cliff R.,Park, Jongnam,Marshall, Lisa F.,Jiang, Wen,Curtin, Peter N.,Ting, Alice Y.,Nocera, Daniel G.,Fukumura, Dai,Jain, Rakesh K.,Bawendi, Moungi G.
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experimental part
p. 472 - 483
(2010/03/25)
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- Rapid isolation of novel FK506 binding proteins from multiple organisms using gDNA and cDNA T7 phage display
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Reverse chemical proteomics using T7 phage display is a powerful technique for identifying cellular receptors of biologically active small molecules. However, to date this method has generally been limited to cDNA libraries constructed from mRNA isolated from eukaryotes. In this paper, we describe the construction of the first prokaryotic T7 phage display libraries from randomly digested Pseudomonas stutzeri and Vibrio fischeri gDNA, as well as a plant cDNA library from Arabidopsis thaliana. We also describe the use of T7 phage display to identify novel proteins from environmental DNA samples using biotinylated FK506 as a model affinity probe.
- Piggott, Andrew M.,Kriegel, Alison M.,Willows, Robert D.,Karuso, Peter
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experimental part
p. 6841 - 6850
(2010/01/06)
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- 3D small-molecule microarrays
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A PEG based 3D hydrogel slide was developed specifically for small-molecule microarraying purposes, which displayed improved loading capacity, signal sensitivity and spot morphology compared with a commercially available slide and comparative 2D slide. The Royal Society of Chemistry 2009.
- Marsden, David M.,Nicholson, Rebecca L.,Ladlow, Mark,Spring, David R.
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supporting information; experimental part
p. 7107 - 7109
(2010/03/25)
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- Soluble polymer-supported catalysts containing azo dyes
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(equation presented) Azo benzene derivatives were incorporated into soluble polymer-bound catalysts by two different approaches. The first was to attach the dye to the polymer-bound catalysts, using the dye as an innocent spectator to study the phase preference, concentration, and recoverability of a catalyst. The second approach used an azo dye as a ligand to form an effective soluble polymer-bound Pd(II) catalyst for Heck reactions.
- Bergbreiter, David E.,Osburn, Philip L.,Li, Chunmei
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p. 737 - 740
(2007/10/03)
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- Process for the preparation of carboxylic acid succinimidyl esters
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A process for the preparation of carboxylic acid succinimidyl esters by reaction of N-hydroxysuccinimide with a carboxylic acid and a halophosphoric acid ester of the formula STR1 is desired, in which R1 and R2 are identical or different and are a C2 - to C6 -alkyl radical or a phenyl radical, or R1 and R2 The process is carried out in the presence of a base in a diluent at a temperature of 0° C. up to 100° C. with isolation of the corresponding carboxylic acid succinimidyl ester.
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- One-pot formation of succinimidyl esters by the system chlorophosphate/hydroxysuccinimide/base
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Succinimidyl esters of various carboxylic acids are formed in high yield at ambient to slightly elevated temperature by the system chlorophosphate/hydroxysuccinimide/base.
- Poechlauer, Peter,Hendel, Wolfram
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p. 3489 - 3494
(2007/10/03)
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