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https://www.readbyqxmd.com/read/29334588/molecular-wire-effects-in-phenyleneethynylene-oligomers-surprising-insights
#1
Uwe Heiko Bunz, Marcel Hergert, Markus Bender, Kai Seehafer
We report the synthesis and quenching behavior of a series of water soluble, carboxylate-carrying phenyleneethynylene oligomers - monomer to tetramer - and their polymers and investigate their quenching behavior with different test analytes (paraquat, lead salts, mercury salts, picric acid, methylpyridinium iodide) in water and compare the results to that of the conjugated polymer. We find significant but analyte-dependent enhancement effects. For monovalent quenchers only the molecular wire effect applies but for divalent quenchers multivalency effects are also important...
January 15, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29334584/in-vitro-and-in-vivo-metabolite-identification-of-a-novel-benzimidazole-compound-zln005-by-lc-ms-ms
#2
Wenchao Sun, Khoa Dinh Nguyen, William L Fitch, Samuel D Banister, Hongxiang Tang, Xiaolan Zhang, Lewis Yu, Edgar G Engleman, Jayakumar Rajadas
RATIONALE: A novel benzimidazole compound ZLN005 was previously identified as a transcriptional activator of peroxisome proliferator-activated receptor γ coactivator 1α (PGC-1α) in certain metabolic tissues. Upregulation of PGC-1α by ZLN005 has been shown to have beneficial effect in a diabetic mouse model and in a coronary artery disease model in vitro. ZLN005 could also have therapeutic potential in neurodegenerative diseases involving down-regulation of PGC-1α. Given the phenotypic efficacy of ZLN005 in several animal models of human disease, its metabolic profile was investigated to guide the development of novel therapeutics using ZLN005 as the lead compound...
January 15, 2018: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/29334461/enhanced-proton-loss-from-neutral-free-radicals-towards-carbon-centered-superacids
#3
John C Walton
Radical centers close to protons are known to enhance their dissociation. Investigation of the generality of this Radical Enhanced Deprotonation (RED-shift) phenomenon and the kinds of structures in which it operates are reported. The pKas for sulfinic, sulfonic, pentan-2,4-dione and Meldrum's acid species, with adjacent radicals centered on C-, N- and O-atoms, were computed by a DFT method from free energies of deprotonation. All series showed significant RED-shifts that increased with the electronegativity of the radical center...
January 15, 2018: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/29334378/supermultiplexed-optical-imaging-and-barcoding-with-engineered-polyynes
#4
Fanghao Hu, Chen Zeng, Rong Long, Yupeng Miao, Lu Wei, Qizhi Xu, Wei Min
Optical multiplexing has a large impact in photonics, the life sciences and biomedicine. However, current technology is limited by a 'multiplexing ceiling' from existing optical materials. Here we engineered a class of polyyne-based materials for optical supermultiplexing. We achieved 20 distinct Raman frequencies, as 'Carbon rainbow', through rational engineering of conjugation length, bond-selective isotope doping and end-capping substitution of polyynes. With further probe functionalization, we demonstrated ten-color organelle imaging in individual living cells with high specificity, sensitivity and photostability...
January 15, 2018: Nature Methods
https://www.readbyqxmd.com/read/29334375/a-small-molecule-inhibitor-of-the-ubiquitin-activating-enzyme-for-cancer-treatment
#5
Marc L Hyer, Michael A Milhollen, Jeff Ciavarri, Paul Fleming, Tary Traore, Darshan Sappal, Jessica Huck, Judy Shi, James Gavin, Jim Brownell, Yu Yang, Bradley Stringer, Robert Griffin, Frank Bruzzese, Teresa Soucy, Jennifer Duffy, Claudia Rabino, Jessica Riceberg, Kara Hoar, Anya Lublinsky, Saurabh Menon, Michael Sintchak, Nancy Bump, Sai M Pulukuri, Steve Langston, Stephen Tirrell, Mike Kuranda, Petter Veiby, John Newcomb, Ping Li, Jing Tao Wu, Josh Powe, Lawrence R Dick, Paul Greenspan, Katherine Galvin, Mark Manfredi, Chris Claiborne, Benjamin S Amidon, Neil F Bence
The ubiquitin-proteasome system (UPS) comprises a network of enzymes that is responsible for maintaining cellular protein homeostasis. The therapeutic potential of this pathway has been validated by the clinical successes of a number of UPS modulators, including proteasome inhibitors and immunomodulatory imide drugs (IMiDs). Here we identified TAK-243 (formerly known as MLN7243) as a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE), the primary mammalian E1 enzyme that regulates the ubiquitin conjugation cascade...
January 15, 2018: Nature Medicine
https://www.readbyqxmd.com/read/29334371/cooperative-targeting-of-melanoma-heterogeneity-with-an-axl-antibody-drug-conjugate-and-braf-mek-inhibitors
#6
Julia Boshuizen, Louise A Koopman, Oscar Krijgsman, Aida Shahrabi, Elke Gresnigt- van den Heuvel, Maarten A Ligtenberg, David W Vredevoogd, Kristel Kemper, Thomas Kuilman, Ji-Ying Song, Nora Pencheva, Jens Thing Mortensen, Marnix Geukes Foppen, Elisa A Rozeman, Christian U Blank, Maarten L Janmaat, David Satijn, Esther C W Breij, Daniel S Peeper, Paul W H I Parren
Intratumor heterogeneity is a key factor contributing to therapeutic failure and, hence, cancer lethality. Heterogeneous tumors show partial therapy responses, allowing for the emergence of drug-resistant clones that often express high levels of the receptor tyrosine kinase AXL. In melanoma, AXL-high cells are resistant to MAPK pathway inhibitors, whereas AXL-low cells are sensitive to these inhibitors, rationalizing a differential therapeutic approach. We developed an antibody-drug conjugate, AXL-107-MMAE, comprising a human AXL antibody linked to the microtubule-disrupting agent monomethyl auristatin E...
January 15, 2018: Nature Medicine
https://www.readbyqxmd.com/read/29334247/development-of-fisetin-loaded-folate-functionalized-pluronic-micelles-for-breast-cancer-targeting
#7
Atmaram Pawar, Srishti Singh, S Rajalakshmi, Karimunnisa Shaikh, C Bothiraja
The natural flavonoid fisetin (FS) has shown anticancer properties but its in-vivo administration remains challenging due to its poor aqueous solubility. The aim of the study was to develop FS loaded pluronic127 (PF)-folic acid (FA) conjugated micelles (FS-PF-FA) by the way of increasing solubility, bioavailability and active targetability of FS shall increase its therapeutic efficacy. FA-conjugated PF was prepared by carbodiimide crosslinker chemistry. FS-PF-FA micelles were prepared by thin-film hydration method and evaluated in comparison with free FS and FS loaded PF micelles (FS-PF)...
January 15, 2018: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29334189/a-multifunctional-micellar-nanoplatform-with-ph-triggered-cell-penetration-and-nuclear-targeting-for-effective-cancer-therapy-and-inhibition-to-lung-metastasis
#8
Yuting Jing, Xiang Xiong, Yang Ming, Jingya Zhao, Xing Guo, Guang Yang, Shaobing Zhou
The enhancement of cellular internalization and subsequent achievement of a nuclear targeting of nanocarriers play an important role in maximizing the therapeutic potency and minimizing the side effects of encapsulated drugs. Herein, a multifunctional micellar nanoplatform simultaneously with high cell penetration and nuclear targeting through pH-triggered surface charge reversal is presented. The miscellar system is constructed from poly(ethylene glycol)-poly(ε-caprolactone) with 2,3-dimethylmaleic anhydride-Tat decoration (PECL/DA-Tat)...
January 15, 2018: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/29334163/isomerically-pure-star-shaped-triphenylene-perylene-hybrids-involving-highly-extended-%C3%AF-conjugation
#9
Edurne Nuin, Vicent Lloret, Konstantin Amsharov, Frank Hauke, Gonzalo Abellán, Andreas Hirsch
The synthesis and characterization of a new type of a highly conjugated heterocyclic π-chromophore, consisting of a central triphenylene core fused with three perylene-monoimide units (star-shaped molecule) is described. By judicious bay-functionalization with tert-butylphenoxy substituents, aggregation was completely prevented in common organic solvents, allowing for a straightforward purification and, for the very first time, the complete separation of the constitutional isomers by HPLC. Both isomers can be easily distinguished by means of several conventional spectroscopic techniques...
January 15, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29334159/a-gold-iii-pincer-ligand-scaffold-for-the-synthesis-of-binuclear-and-bioconjugated-complexes-synthesis-and-anticancer-potential
#10
Bertrand Benoît, Maria A O'Connell, Zöe A E Waller, Manfred Bochmann
Cyclometalated (C^N^C)Au(III) complexes bearing functionalized N-heterocyclic carbene (NHC) ligands provide a high-yielding, modular route to bioconjugated and binuclear complexes. That methodology has been applied to the synthesis of bioconjugated complexes presenting biotin and 17α-ethynylestradiol vectors, as well as to the synthesis of bimetallic Au(III)/Au(I) complexes. The in vitro antiproliferative activities of these compounds against various cancer cells lines depend on the linker length, with the longer linker being the most potent...
January 15, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29334085/spycatcher-spytag-mediated-in-situ-labelling-of-progeny-baculovirus-with-quantum-dots-for-tracking-viral-infection-in-living-cells
#11
Xianliang Ke, Yuan Zhang, Fangliang Zheng, Yan Liu, Zhenhua Zheng, Yi Xu, Hanzhong Wang
A non-invasive labelling strategy is proposed to label baculovirus via genetic insertion of a SpyTag into the viral glycoprotein, followed by specific conjugation with the SpyCatcher protein on modified quantum dots (QDs) through an isopeptide bond. The labelling method is convenient and efficient and shows little attenuation of viral infectivity. Therefore, it is a biologically compatible technique for tracking viral infection.
January 15, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29333849/asymmetric-conjugate-addition-of-%C3%AE-cyanoketones-to-enones-using-diaminomethylenemalononitrile-organocatalyst
#12
Kosuke Nakashima, Yuta Noda, Shin-Ichi Hirashima, Yuji Koseki, Tsuyoshi Miura
A diaminomethylenemalononitrile organocatalyst efficiently catalyzed the asymmetric conjugate addition of α-cyanoketones to vinyl ketones to give the corresponding 1,5-dicarbonyl compounds, which bear an all-carbon quaternary stereogenic center, with high enantioselectivities. This report is the first example of the asymmetric conjugate addition of α-cyanoketones to vinyl ketones using an organocatalyst.
January 15, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29333698/design-of-enzyme-micelles-with-controllable-concavo-convex-micromorphologies-for-highly-enhanced-stability-and-catalytical-activity
#13
Tao Chen, Yuanhong Xu, Wenrong Yang, Aihua Li, Yao Wang, Jing Sun, Jingquan Liu
Concavo-convex micelles with controllable sizes and nanostructures are prepared via self-assembling polymer-enzyme (e.g., shellac enzyme) conjugates with heterogeneous polymer chains, which exhibit higher enzyme stability (300%) and bioactivity (760%) comparing with the well-defined ones. The applied amphiphilic and negatively charged copolymer, poly (methyl methacrylate)-block-poly (sodium p-styrene sulfonate), is synthesized via reversible addition-fragmentation chain transfer polymerization to modify shellac enzyme and immobilize the enzyme bioactivity inducer by covalent conjugation and electrostatic attraction, respectively...
January 15, 2018: Macromolecular Bioscience
https://www.readbyqxmd.com/read/29333658/in-situ-shrna-synthesis-on-dna-polylactide-nanoparticles-to-treat-multidrug-resistant-breast-cancer
#14
Qianqian Ni, Fuwu Zhang, Yunlei Zhang, Guizhi Zhu, Zhe Wang, Zhaogang Teng, Chunyan Wang, Bryant C Yung, Gang Niu, Guangming Lu, Longjiang Zhang, Xiaoyuan Chen
Nanomedicine has shown unprecedented potential for cancer theranostics. Nucleic acid (e.g., DNA and RNA) nanomedicines are of particular interest for combination therapy with chemotherapeutics. However, current nanotechnologies to construct such nucleic acid nanomedicines, which rely on chemical conjugation or physical complexation of nucleic acids with chemotherapeutics, have restrained their clinical translation due to limitations such as low drug loading efficiency and poor biostability. Herein, in situ rolling circle transcription (RCT) is applied to synthesize short hairpin RNA (shRNA) on amphiphilic DNA-polylactide (PLA) micelles...
January 15, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29333630/efficient-supercapacitor-energy-storage-using-conjugated-microporous-polymer-networks-synthesized-from-buchwald-hartwig-coupling
#15
Yaozu Liao, Haige Wang, Meifang Zhu, Arne Thomas
Supercapacitors have received increasing interest as energy storage devices due to their rapid charge-discharge rates, high power densities, and high durability. In this work, novel conjugated microporous polymer (CMP) networks are presented for supercapacitor energy storage, namely 3D polyaminoanthraquinone (PAQ) networks synthesized via Buchwald-Hartwig coupling between 2,6-diaminoanthraquinone and aryl bromides. PAQs exhibit surface areas up to 600 m2 g-1 , good dispersibility in polar solvents, and can be processed to flexible electrodes...
January 15, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29333575/a-phase-1-dose-escalation-study-of-pf-06664178-an-anti-trop-2-aur0101-antibody-drug-conjugate-in-patients-with-advanced-or-metastatic-solid-tumors
#16
Gentry T King, Keith D Eaton, Brandon R Beagle, Christopher J Zopf, Gilbert Y Wong, Heike I Krupka, Steven Y Hua, Wells A Messersmith, Anthony B El-Khoueiry
Purpose and Methods Trop-2 is a glycoprotein over-expressed in many solid tumors but at low levels in normal human tissue, providing a potential therapeutic target. We conducted a phase 1 dose-finding study of PF-06664178, an antibody-drug conjugate that targets Trop-2 for the selective delivery of the cytotoxic payload Aur0101. The primary objective was to determine the maximum tolerated dose and recommended phase 2 dose. Secondary objectives included further characterization of the safety profile, pharmacokinetics and antitumor activity...
January 15, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29333553/microwave-assisted-synthesis-of-tempo-labeled-hydrogels-traceable-with-mri
#17
Emanuele Mauri, Edoardo Micotti, Arianna Rossetti, Lucio Melone, Simonetta Papa, Giulia Azzolini, Stefano Rimondo, Pietro Veglianese, Carlo Punta, Filippo Rossi, Alessandro Sacchetti
Polymer functionalization strategies have recently attracted considerable attention for several applications in biomaterials science. In particular, technological advancements in medical imaging have focused on the design of polymeric matrices to improve non-invasive approaches and diagnostic accuracy. In this scenario, the use of microwave irradiation of aqueous solutions containing appropriate combinations of polymers is gaining increasing interest in the synthesis of sterile hydrogels without using monomers, eliminating the need to remove unreacted species...
January 15, 2018: Soft Matter
https://www.readbyqxmd.com/read/29333473/charge-migration-and-charge-transfer-in-molecular-systems
#18
REVIEW
Hans Jakob Wörner, Christopher A Arrell, Natalie Banerji, Andrea Cannizzo, Majed Chergui, Akshaya K Das, Peter Hamm, Ursula Keller, Peter M Kraus, Elisa Liberatore, Pablo Lopez-Tarifa, Matteo Lucchini, Markus Meuwly, Chris Milne, Jacques-E Moser, Ursula Rothlisberger, Grigory Smolentsev, Joël Teuscher, Jeroen A van Bokhoven, Oliver Wenger
The transfer of charge at the molecular level plays a fundamental role in many areas of chemistry, physics, biology and materials science. Today, more than 60 years after the seminal work of R. A. Marcus, charge transfer is still a very active field of research. An important recent impetus comes from the ability to resolve ever faster temporal events, down to the attosecond time scale. Such a high temporal resolution now offers the possibility to unravel the most elementary quantum dynamics of both electrons and nuclei that participate in the complex process of charge transfer...
November 2017: Structural Dynamics (Melville, N.Y.)
https://www.readbyqxmd.com/read/29333400/brentuximab-vedotin-clinical-updates-and-practical-guidance
#19
REVIEW
Jun Ho Yi, Seok Jin Kim, Won Seog Kim
Brentuximab vedotin (BV), a potent antibody-drug conjugate, targets the CD30 antigen. Owing to the remarkable efficacy shown in CD30-positive lymphomas, such as Hodgkin's lymphoma and systemic anaplastic large-cell lymphoma, BV was granted accelerated approval in 2011 by the US Food and Drug Administration. Thereafter, many large-scale trials in various situations have been performed, which led to extensions of the original indication. The aim of this review was to describe the latest updates on clinical trials of BV and the in-practice guidance for the use of BV...
December 2017: Blood Research
https://www.readbyqxmd.com/read/29333088/bone-regeneration-using-silk-hydroxyapatite-hybrid-composite-in-a-rat-alveolar-defect-model
#20
Kyung S Koh, Jong Woo Choi, Eun Jeong Park, Tae Suk Oh
Background: To overcome the limited source of autogenous bone in bone grafting, many efforts have been made to find bone substitutes. The use of hybrid composites of silk and hydroxyapatite to simulate natural bone tissue can overcome the softness and brittleness of the individual components. Methods: Critical-sized, 7 x 4 x 1.5 mm alveolar defects were created surgically in 36 Sprague-Dawley rats. Three treatment groups were tested: an empty defect group (group I), a silk fibrin scaffold group (group II), and a hydroxyapatite-conjugated silk fibrin scaffold group (group III)...
2018: International Journal of Medical Sciences
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