Tag: M.W=300-350

Wang, Yanfang published the artcileDouble Click-Functionalized siRNA Polyplexes for Gene Silencing in Epidermal Growth Factor Receptor-Positive Tumor Cells, Quality Control of 1353016-70-2, the publication is ACS Biomaterials Science & Engineering (2020), 6(2), 1074-1089, database is CAplus and MEDLINE.

Sequence-defined lipo-oligomers generated via solid-phase assisted synthesis have been developed as siRNA delivery systems for RNA-interference (RNAi) based gene silencing. Here, novel siRNA lipo-polyplexes were established, which were postmodified with monovalent or bivalent DBCO-PEG₂₄ agents terminated with peptide GE11 (YHWYGYTPQNVI) for epidermal growth factor receptor (EGFR)-targeted siRNA delivery into EGFR-pos. tumor cells. Lipo-oligomers containing eight cationizable succinoyltetraethylene-pentamine (Stp) units mediated higher siRNA nanoparticle core stability than those containing four Stp units, and the incorporation of histidines for enhanced endosomal buffer capacity resulted in an improved gene silencing efficiency. Lipo-polyplexes modified with monovalent or bivalent PEG-GE11 via the copper-free click reaction possessed significantly enhanced cellular internalization and transfection efficiency in EGF receptor-pos. human cervical KB and hepatoma Huh7 cells in comparison with the corresponding lipo-polyplexes shielded with PEG₂₄ without targeting. Furthermore, modification with the bivalent DBCO-PEG₂₄-GE11 ligand resulted in higher gene silencing efficiency than modification with the same equivalent of the monovalent DBCO-PEG₂₄-GE11 ligand.

ACS Biomaterials Science & Engineering published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C15H23BO2, Quality Control of 1353016-70-2.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Shao, Zhuzhou published the artcileBioorthogonal release of sulfonamides and mutually orthogonal liberation of two drugs, Application of Dbco-acid, the publication is Chemical Communications (Cambridge, United Kingdom) (2018), 54(100), 14089-14092, database is CAplus and MEDLINE.

Sulfonamide derivatives have been used in pharmaceutics for decades. Here we report a new approach to release sulfonamides efficiently using a bioorthogonal reaction of sulfonyl sydnonimines and dibenzoazacyclooctyne (DIBAC). The second-order rate constant of the cycloaddition reaction can be up to 0.62 M^-1s^-1, and the reactants are highly stable under physiol. conditions. Most significantly, we also discovered the mutual orthogonality between the sydnonimine-DIBAC and benzonorbornadiene-tetrazine cycloaddition pairs, which can be used for selective and simultaneous liberation of sulfonamide and primary amine drugs.

Chemical Communications (Cambridge, United Kingdom) published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C11H17BO3S, Application of Dbco-acid.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Li, Hui published the artcileWell-defined DNA-polymer miktoarm stars for enzyme-resistant nanoflares and carrier-free gene regulation, Application of Dbco-acid, the publication is Bioconjugate Chemistry (2020), 31(3), 530-536, database is CAplus and MEDLINE.

Herein, we report a star-architectured poly(ethylene glycol) (PEG)-oligonucleotide nanoconjugate of a well-defined mol. structure. Based upon fullerene C₆₀ cores, each star bears precisely 1 DNA strand and 11 polymer chains. The elevated PEG d. provides the DNA with steric selectivity: the DNA is significantly more resistant to nuclease digestion while remaining able to hybridize with a complementary sequence. The degree of resistance increases as the centers of mass for the DNA and fullerene are closer together. Such steric selectivity reduces protein-related background signals of the nanoflares synthesized from these miktoarm star polymers. Importantly, the stars improve cellular uptake and regulate gene expression as a non-cytotoxic, single-entity antisense agent without the need for a transfection carrier.

Bioconjugate Chemistry published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C19H15NO3, Application of Dbco-acid.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Liu, Chong published the artcileStrain-Promoted Click Modification of a Mesoporous Metal-Organic Framework, Application of Dbco-acid, the publication is Journal of the American Chemical Society (2012), 134(46), 18886-18888, database is CAplus and MEDLINE.

Strain-promoted click chem. was used to post-synthetically modify the pore walls of azide-functionalized mesoporous bio-MOF-100 (N₃-bio-MOF-100). The reactions proceed in high yield and produce no byproduct. This new method was used to introduce various functional groups into the MOF mesopores, including succinimidyl ester bioconjugation moieties that allow for straightforward coupling of biomols. to the pore walls.

Journal of the American Chemical Society published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C19H15NO3, Application of Dbco-acid.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Reichmuth, Andreas M. published the artcileInvestigating Complex Samples with Molograms of Low-Affinity Binders, Recommanded Product: Dbco-acid, the publication is ACS Sensors (2021), 6(3), 1067-1076, database is CAplus and MEDLINE.

In vitro diagnostics relies on the quantification of minute amounts of a specific biomol., called biomarker, from a biol. sample. The majority of clin. relevant biomarkers for conditions beyond infectious diseases are detected by means of binding assays, where target biomarkers bind to a solid phase and are detected by biochem. or phys. means. Nonspecifically bound biomols., the main source of variation in such assays, need to be washed away in a laborious process, restricting the development of widespread point-of-care diagnostics. Here, we show that a diffractometric assay provides a new, label-free possibility to investigate complex samples, such as blood plasma. A coherently arranged sub-micron pattern, i.e., a peptide mologram, is created to demonstrate the insensitivity of this diffractometric assay to the unwanted masking effect of nonspecific interactions. In addition, using an array of low-affinity binders, we also demonstrate the feasibility of mol. profiling of blood plasma in real time and show that individual patients can be differentiated based on the binding kinetics of circulating proteins.

ACS Sensors published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C19H15NO3, Recommanded Product: Dbco-acid.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Wang, Wentao published the artcileMultifunctional and High Affinity Polymer Ligand that Provides Bio-Orthogonal Coating of Quantum Dots, Synthetic Route of 1353016-70-2, the publication is Bioconjugate Chemistry (2016), 27(9), 2024-2036, database is CAplus and MEDLINE.

The authors detail the design of hydrophilic metal-coordinating ligands and their use for the effective coating of luminescent quantum dots. The ligand design exploits the specific, reagent-free nucleophilic addition reaction of amine-modified mols. toward maleic anhydride to introduce several lipoic acid metal-anchors, hydrophilic zwitterion moieties and specific reactive groups along a poly(isobutylene-alt-maleic anhydride) (PIMA) chain. Tunable reactive groups tested in this study include azide, biotin, carboxyl, and amine. Cap exchange with these multi-lipoic acid ligands via a photochem. ligation strategy yields homogeneous QD dispersions that are colloidally stable over several biol.-relevant conditions and for extended periods of time. The zwitterionic coating yields compact nanoparticle size and imparts non-sticky surface properties onto the QDs, preventing protein absorption. The introduction of a controllable number of reactive groups allows conjugation of the QDs to biomols. via bio-orthogonal coupling chemistries including: (1) attachment of the neurotransmitter dopamine to QDs via amine-isothiocyanate reaction to produce a platform capable of probing interactions with cysteine in proteins, based on charge transfer interactions; (2) self-assembly of biotinylated QDs with streptavidin-dye; (3) ligation of azide-functionalized QDs to cyclooctyne-modified transferrin via copper-free click chem. for intracellular delivery. This ligand design strategy can be used to prepare an array of metal-coordinating ligands adapted for coating other inorganic nanoparticles, including magnetic and plasmonic nanomaterials.

Bioconjugate Chemistry published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C8H11BO2, Synthetic Route of 1353016-70-2.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Sun, Lina published the artcileMetabolic labeling of HIV-1 envelope glycoprotein gp120 to elucidate the effect of gp120 glycosylation on antigen uptake, Product Details of C19H15NO3, the publication is Journal of Biological Chemistry (2018), 293(39), 15178-15194, database is CAplus and MEDLINE.

The glycan shield on the envelope glycoprotein gp120 of HIV-1 has drawn immense attention as a vulnerable site for broadly neutralizing antibodies and for its significant impact on host adaptive immune response to HIV-1. Glycosylation sites and glycan composition/structure at each site on gp120 along with the interactions of gp120 glycan shield with broadly neutralizing antibodies have been extensively studied. However, a method for directly and selectively tracking gp120 glycans has been lacking. Here, we integrate metabolic labeling and click chem. technol. with recombinant gp120 expression to demonstrate that gp120 glycans could be specifically labeled and directly detected. Selective labeling of gp120 by N-azidoacetylmannosamine (ManNAz) and N-azidoacetylgalactosamine (GalNAz) incorporation into the gp120 glycan shield was characterized by MS of tryptic glycopeptides. By using metabolically labeled gp120, we investigated the impact of gp120 glycosylation on its interaction with host cells and demonstrated that oligomannose enrichment and sialic acid deficiency drastically enhanced gp120 uptake by bone marrow-derived dendritic cells. Collectively, our data reveal an effective labeling and detection method for gp120, serving as a tool for functional characterization of the gp120 glycans and potentially other glycosylated proteins.

Journal of Biological Chemistry published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C23H20BN, Product Details of C19H15NO3.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

David, Tomas published the artcileImproved Conjugation, 64-Cu Radiolabeling, in Vivo Stability, and Imaging Using Nonprotected Bifunctional Macrocyclic Ligands: Bis(Phosphinate) Cyclam (BPC) Chelators, Application In Synthesis of 1353016-70-2, the publication is Journal of Medicinal Chemistry (2018), 61(19), 8774-8796, database is CAplus and MEDLINE.

Bifunctional derivatives of Bis(Phosphinate)-bearing Cyclam (BPC) chelators bearing carboxylate, amine, isothiocyanate, azide or cyclooctyne in BP-side chain were synthesized. Conjugations required no protection of phosphinate or ring secondary amine groups. The ring amines were not reactive (proton protected) at pH < ∼8. For isothiocyanate coupling, oligopeptide N-terminal α-amines were more suitable than alkyl amines, e.g. Lys ω-amine (pKa ∼7.5-8.5 and ∼10-11, resp.) due to lower basicity. The Cu-64 labeling was efficient at room temperature (specific activity ∼100 GBq/μmol; 25°C, pH 6.2, ∼100 ligand equivalent, 10 min). A representative Cu-64-BPC was tested in-vivo showing fast clearance and no non-specific radioactivity deposition. The monoclonal anti-PSCA antibody 7F5 conjugates with thiocyanate BPC derivative or NODAGA were radiolabeled and studied in PC-3-PSCA tumor bearing mice by PET. The radiolabeled BPC conjugate was accumulated in the prostate tumor with low off-target uptake, unlike Cu-64-labeled NODAGA-antibody conjugate. The BPC chelators have a great potential for theranostic applications of Cu-64/Cu-67 matched pair.

Journal of Medicinal Chemistry published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C19H15NO3, Application In Synthesis of 1353016-70-2.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Shoaib, Muhammad M. published the artcileControlled degradation of low-fouling poly(oligo(ethylene glycol)methyl ether methacrylate) hydrogels, Formula: C19H15NO3, the publication is RSC Advances (2019), 9(33), 18978-18988, database is CAplus and MEDLINE.

Degradable low-fouling hydrogels are ideal vehicles for drug and cell delivery. For each application, hydrogel degradation rate must be re-optimized for maximum therapeutic benefit. We developed a method to rapidly and predictably tune degradation rates of low-fouling poly(oligo(ethylene glycol)methyl ether methacrylate) (P(EG)_xMA) hydrogels by modifying two interdependent variables: (1) base-catalyzed crosslink degradation kinetics, dependent on crosslinker electronics (electron withdrawing groups (EWGs)); and, (2) polymer hydration, dependent on the mol. weight (M_W) of poly(ethylene glycol) (PEG) pendant groups. By controlling PEG MW and EWG strength, P(EG)_xMA hydrogels were tuned to degrade over 6 to 52 d. A 6-member P(EG)_xMA copolymer library yielded slow and fast degrading low-fouling hydrogels suitable for short- and long-term delivery applications. The degradation mechanism was also applied to RGD-functionalized poly(carboxybetaine methacrylamide) (PCBMAA) hydrogels to achieve slow (∼50 d) and fast (∼13 d) degrading low-fouling, bioactive hydrogels.

RSC Advances published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C9H8O4, Formula: C19H15NO3.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Black, Jacob W. published the artcileAn Optical Tweezers Platform for Single Molecule Force Spectroscopy in Organic Solvents, Application of Dbco-acid, the publication is Nano Letters (2017), 17(11), 6598-6605, database is CAplus and MEDLINE.

Observation at the single mol. level was a revolutionary tool for mol. biophysics and materials science, but single mol. studies of solution-phase chem. are less widespread. The authors develop an exptl. platform for solution-phase single mol. force spectroscopy in organic solvents. This optical-tweezer-based platform was designed for broad chem. applicability and uses optically trapped core-shell microspheres, synthetic polymer tethers, and click chem. linkages formed in situ. Stable optical trapping of the core-shell microspheres in 10 different solvents was observed, as was single mol. link formation in 4 different solvents. These experiments demonstrate how to use optical tweezers for single mol. force application in the study of solution-phase chem.

Nano Letters published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C19H15NO3, Application of Dbco-acid.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider