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Search for "targeting" in Full Text gives 226 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.
Exploring mechanochemistry to turn organic bio-relevant molecules into metal-organic frameworks: a short review
Beilstein J. Org. Chem. 2017, 13, 2416–2427, doi:10.3762/bjoc.13.239
- mechanochemical processes towards attaining metallopharmaceuticals, metallodrugs and MOFs synthesized within our group [49], and another on the design, screening, and characterization of BioMOFs in general [110]. To the best of our knowledge, this is the first short review targeting on the mechanochemical
Phosphonic acid: preparation and applications
Beilstein J. Org. Chem. 2017, 13, 2186–2213, doi:10.3762/bjoc.13.219
- bone targeting, for the design of supramolecular or hybrid materials, for the functionalization of surfaces, for analytical purposes, for medical imaging or as phosphoantigen. These applications are covering a large panel of research fields including chemistry, biology and physics thus making the
- 14, Figure 4), was assessed to complex indium [86] or terbium [87] with the aim to develop bone targeting and dosimetry. It was also employed to complex 89Y and applied as pH sensitive NMR probe [88], or as organic precursor of crystalline manganese, nickel [89] or lanthanide-containing hybrid
- develop bone targeting which was assessed for therapy [96] and imaging [97][98]. Finally, the phosphonic acid group was also employed to immobilize organic or organometallic molecules on the surface of metal oxide [99][100] (Al2O3 [101], TiO2 [102][103], SnO2 [104], Fe3O4 [105], ZnO [106]), CdSe quantum
18-Hydroxydolabella-3,7-diene synthase – a diterpene synthase from Chitinophaga pinensis
Beilstein J. Org. Chem. 2017, 13, 1770–1780, doi:10.3762/bjoc.13.171
- synthases in plants are targeted to the mitochondria [27], we decided to attempt the expression of HdS with mitochondrial targeting (HdS-mit). A construct without targeting signal (HdS; resulting in cytoplasmic localisation) and an empty vector were used as controls. A p19 construct [28] was co-infiltrated
- targeting to the mitochondria resulted in the production of the same diterpene alcohol. Although the mitochondria of N. benthamiana also produce FPP [32], again no germacrene D was detected. Taken together, these experiments demonstrate that the expression of one and the same terpene synthase in different
- of GC–MS analyses of N. benthamiana leaf extracts. A) HdS-mit (HdS expressed with mitochondrial targeting signal) showing the production of 3 in planta, B) HdS (expression without targeting signal) and C) empty vector. Germacrene A (1) and its Cope rearrangement to β-elemene (2). Product obtained
The chemistry and biology of mycolactones
Beilstein J. Org. Chem. 2017, 13, 1596–1660, doi:10.3762/bjoc.13.159
- relies on the experience of local health professionals. Subsequent laboratory testing to confirm the clinical diagnosis might then be performed by 1) direct smear examination for acid-fast bacilli; 2) in vitro culture; 3) polymerase chain reaction (PCR), targeting the genomic region IS2404; and 4
- accompanied by macroscopic or ultrastructural signs of nerve destruction and hypoesthesia. Subsequent experiments revealed that mycolactone exposure caused hyperpolarization of neurons derived from PC12 cells that was mediated by the TRAAK potassium channel. Finally, screening of a siRNA library targeting
Synthesis of oligonucleotides on a soluble support
Beilstein J. Org. Chem. 2017, 13, 1368–1387, doi:10.3762/bjoc.13.134
- in the development of therapeutic oligonucleotides targeting either pre-mRNA [24][25], mature mRNA [26][27][28] or noncoding microRNA [29][30] have even increased this interest. It has been repeatedly argued that (i) the synthesis in solution could be carried out with a smaller excess of building
BODIPY-based fluorescent liposomes with sesquiterpene lactone trilobolide
Beilstein J. Org. Chem. 2017, 13, 1316–1324, doi:10.3762/bjoc.13.128
- theranostic applications. Keywords: BODIPY conjugates; cancer targeting; drug delivery; liposomes; natural compounds; sesquiterpene lactone trilobolide; Introduction Targeted (smart) drug delivery is a method for specific delivering of an active compound preferentially to some cells or tissues in the human
- body. This approach has become the key issue for surpassing the bottleneck of drug discovery. With the advent of new technologies and deeper understanding of the biological processes, the concept of specific targeting has become one of the most attractive directions in the field of biomedicine
- . Specific drug targeting can be achieved by using, for example, antibodies, peptides, polyethylene glycol polymers, and last but not least, liposomes, which have been nowadays extensively investigated [1][2]. In general, liposomes are employed in order to enhance the therapeutic index of an applied drug by
Aqueous semisynthesis of C-glycoside glycamines from agarose
Beilstein J. Org. Chem. 2017, 13, 1222–1229, doi:10.3762/bjoc.13.121
- recently envisaged that its substituted C-threofuranose ring could serve as an excellent scaffold to build muscarine analogues [11]. Cholinergic agents targeting muscarinic acetylcholine receptors (mAChRs) have historically served for diverse applications in medicine [12][13] and recently regained interest
Total syntheses of the archazolids: an emerging class of novel anticancer drugs
Beilstein J. Org. Chem. 2017, 13, 1085–1098, doi:10.3762/bjoc.13.108
- development and SAR studies [49][55][56][57][58] and the group of O’Neil has been targeting dihydroarchazolid B (3) as a potentially equipotent structurally simplified derivative [45][46][48]. This review covers the various tactics and strategies, employed by the Menche, Trauner and O’Neil group in archazolid
Glyco-gold nanoparticles: synthesis and applications
Beilstein J. Org. Chem. 2017, 13, 1008–1021, doi:10.3762/bjoc.13.100
- : gold nanoparticles; glyco nanoparticles; glyconanomaterials; immunology; targeting; Introduction Carbohydrates are well recognized as crucial biomolecules for their capability to produce an enormous number of biocodes which are translated into their ability to promote or suppress a plethora of
- molecules displayed on the metallic surface. In particular, an in vitro study performed by Mitragotri and co-workers reported that the endothelial targeting specificity could be enhanced by modulating the NP shape. By using a microfluidic synthetic vascular network the authors demonstrated that rod-shaped
- [45][56][57][58]. Prosperi and co-workers coated dodecanthiol AuNPs with manno-calixarenes exploiting hydrophobic interactions, obtaining an efficient targeting against cancer cells [56]. Similarly, a reversible addition−fragmentation chain transfer (RAFT) polymerization approach has been exploited
Opportunities and challenges for the sustainable production of structurally complex diterpenoids in recombinant microbial systems
Beilstein J. Org. Chem. 2017, 13, 845–854, doi:10.3762/bjoc.13.85
- ]. Different approaches of terpene product increase involved targeting specific elements of the MEP pathway [28] or introducing heterologous MEV pathway from yeast [82][83]. A high level of taxadiene production in E. coli was achieved by Ajikumar and co-workers through overexpression of bottleneck enzymes of
Highly bulky and stable geometry-constrained iminopyridines: Synthesis, structure and application in Pd-catalyzed Suzuki coupling of aryl chlorides
Beilstein J. Org. Chem. 2017, 13, 213–221, doi:10.3762/bjoc.13.24
- industrial point of view [5]. Targeting the handling and applicability of palladium catalysts, various species have been developed through the use of diversified ligands [6][7][8][9][10][11][12]. Typical ligands that successfully enhanced the reactivity of palladium species towards the oxidative addition of
Synthesis of multi-lactose-appended β-cyclodextrin and its cholesterol-lowering effects in Niemann–Pick type C disease-like HepG2 cells
Beilstein J. Org. Chem. 2017, 13, 10–18, doi:10.3762/bjoc.13.2
- -cyclodextrin (HP-β-CD). HP-β-CD is effective in the treatment of hepatosplenomegaly in NPC disease, albeit at a very high dose. One of the methods to reduce the required dose of HP-β-CD for treatment of NPC is to actively targeting hepatocytes with β-cyclodextrin (β-CD). The aim of the present study was to
- synthesized a novel multi-lactose-appended β-CD (multi-Lac-β-CD) to enhance the targeting ability to ASGPR, and evaluated its cholesterol-lowering effect in NPC-like HepG2 cells. Results and Discussion Synthesis of multi-Lac-β-CD In the present study, we fabricated multi-Lac-β-CD (5) to obtain a hepatocyte
- loss in cats [20][21]. Therefore, the targeting technique is one of promising approaches to reduce the dose of CDs. Importantly, the multi-Lac-β-CD (DSL5.6) showed more potent cholesterol-lowering effects in NPC-like HepG2 cells than HP-β-CD. Accordingly, multi-Lac-β-CD (DSL5.6) may attenuate the risk
Versatile synthesis of end-reactive polyrotaxanes applicable to fabrication of supramolecular biomaterials
Beilstein J. Org. Chem. 2016, 12, 2883–2892, doi:10.3762/bjoc.12.287
- click reactions, including ligand molecules for active targeting, radioactive molecules for in vivo imaging, hydrophobic polymers for the surface immobilization of PRXs, and hydrophilic polymers for acquiring water solubility. Accordingly, the azide group-terminated end-reactive 4a and 4b are expected
Synthesis of spiro[isoindole-1,5’-isoxazolidin]-3(2H)-ones as potential inhibitors of the MDM2-p53 interaction
Beilstein J. Org. Chem. 2016, 12, 2793–2807, doi:10.3762/bjoc.12.278
- preventing its mutation. Normally, p53 is found at low levels because of its continuous proteasomal degradation promoted by MDM2. MDM2 inhibits p53 activity in two ways: i) by targeting p53 into the region of interaction with CBP/p300, thus preventing its transcriptional activity, and ii) by exporting p53
Chemical probes for competitive profiling of the quorum sensing signal synthase PqsD of Pseudomonas aeruginosa
Beilstein J. Org. Chem. 2016, 12, 2784–2792, doi:10.3762/bjoc.12.277
- selectively targeting the active site of an enzyme and a reporter group that allows in-gel imaging and/or affinity enrichment of target enzymes [22]. We thus synthesized a small library of chemical probes with electrophilic α-chloroacetamide, α,β-unsaturated amide, and α,β-unsaturated ketone moieties as
- site cysteine was replaced by alanine. The purified mutant PqsD C112A exhibited only low background labeling for some probes but not comparable to labelling of the wild type protein by CA1–3, indicating that the probes were selectively targeting the active site (Figure 3A). Concentration series with a
- underlining the selectivity of our probes (Figure 3C). These results indicate that probes CA1–3 are specific and covalently bind to Cys112 of PqsD and are thus, to the best of our knowledge, the first account of activity-based probes targeting and selectively labelling the active site of PqsD. Interestingly
Computational methods in drug discovery
Beilstein J. Org. Chem. 2016, 12, 2694–2718, doi:10.3762/bjoc.12.267
- -throughput screening has been used to identify inhibitors of protein kinase CK2 targeting its ATP binding site [165]. CK2 is an important target in developing antitumor drugs. About 400,000 compounds have been screened, from which 12 hits were selected for evaluations using in vitro assays. Out of these hits
A self-assembled cyclodextrin nanocarrier for photoreactive squaraine
Beilstein J. Org. Chem. 2016, 12, 2535–2542, doi:10.3762/bjoc.12.248
- for the CDV without affecting its photochemistry. In addition, it is expected that the aggregation of squaraine will be supressed by immobilization at the CDV surface. Ultimately, the photoactive squaraine can be combined with other functional guests, such as targeting units and tracers, to further
- squaraines on the vesicle surface. In short, the self-assembled nanosystem has several advantageous properties to be used as a PDT system. We envision that the photoactive squaraine can be combined with other functional guests, such as targeting units and tracers, to enhance the potential of the nanocarrier
Efficient mechanochemical synthesis of regioselective persubstituted cyclodextrins
Beilstein J. Org. Chem. 2016, 12, 2364–2371, doi:10.3762/bjoc.12.230
- drug targeting hosts [7][8], can be problematic as they require sophisticated, efficient and yet simple methods which lead to acceptable purity and impurity profiles. Furthermore, the special structural properties of selectively substituted CDs mean that their syntheses are not always environmentally
Potent triazine-based dehydrocondensing reagents substituted by an amido group
Beilstein J. Org. Chem. 2016, 12, 1897–1903, doi:10.3762/bjoc.12.179
- ], a crown-ether-based cyclotransferase [8], membrane fusion of small unilamellar vesicles to form giant unilamellar vesicles [9], modular methods for the affinity labeling of targeting proteins [10][11][12], and reaction acceleration on micelle interfaces [13][14]. Thus, various types of molecular
Organic chemistry meets polymers, nanoscience, therapeutics and diagnostics
Beilstein J. Org. Chem. 2016, 12, 1638–1646, doi:10.3762/bjoc.12.161
- protein (GFP). It worked even better than we hoped, with complete cytosolar distribution of the GFP observed (Figure 4) [63]. This ability to "dump" proteins into cells is unprecedented, allowing us to deliver proteins capable of intracellular localization – the next frontier of targeting [64]. We also
Discovery of an inhibitor of the production of the Pseudomonas aeruginosa virulence factor pyocyanin in wild-type cells
Beilstein J. Org. Chem. 2016, 12, 1428–1433, doi:10.3762/bjoc.12.137
- potential of targeting virulence factors [8][9][34]. There is some evidence suggesting that 4 reduces the level of pyocyanin production by disrupting OdDHL-dependent activation of LasR; that it, compound 4, may be a LasR antagonist and an inhibitor of LasR-based quorum sensing. This could have interesting
Towards potential nanoparticle contrast agents: Synthesis of new functionalized PEG bisphosphonates
Beilstein J. Org. Chem. 2016, 12, 1366–1371, doi:10.3762/bjoc.12.130
- , F-93017 Bobigny, France ICG Montpellier-UMR 5253, Equipe AM2N, ENSCM, 8, Rue de l’Ecole Normale, F-34296 Montpellier Cedex 5, France 10.3762/bjoc.12.130 Abstract The use of nanotechnologies for biomedical applications took a real development during these last years. To allow an effective targeting
Application of Cu(I)-catalyzed azide–alkyne cycloaddition for the design and synthesis of sequence specific probes targeting double-stranded DNA
Beilstein J. Org. Chem. 2016, 12, 1348–1360, doi:10.3762/bjoc.12.128
The synthesis of functionalized bridged polycycles via C–H bond insertion
Beilstein J. Org. Chem. 2016, 12, 985–999, doi:10.3762/bjoc.12.97
- . Conclusion Many of the early examples of bridged-polycycle synthesis via C–H bond insertion arose from strategies targeting the total synthesis of natural products. The results of these early efforts led to useful reaction conditions, a better understanding of stereoelectronic effects involved in the
A cross-metathesis approach to novel pantothenamide derivatives
Beilstein J. Org. Chem. 2016, 12, 963–968, doi:10.3762/bjoc.12.95
- if 16 was targeting CoA biosynthesis as reported for other pantothenamides, the IC50 was also measured in the presence of excess pantothenate (100 µM), in the presence or absence of pantetheinase. The dramatic loss of activity observed confirms that compound 16 acts on the CoA biosynthesis
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