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https://www.readbyqxmd.com/read/29352320/high-level-production-and-purification-in-a-functional-state-of-an-extrasynaptic-gamma-aminobutyric-acid-type-a-receptor-containing-%C3%AE-4%C3%AE-3%C3%AE-subunits
#1
Xiaojuan Zhou, Rooma Desai, Yinghui Zhang, Wojciech J Stec, Keith W Miller, Youssef Jounaidi
The inhibitory γ-aminobutyric acid type A receptors are implicated in numerous physiological processes, including cognition and inhibition of neurotransmission, rendering them important molecular targets for many classes of drugs. Functionally, the entire GABAAR family of receptors can be subdivided into phasic, fast acting synaptic receptors, composed of α-, β- and γ-subunits, and tonic extrasynaptic receptors, many of which contain the δ-subunit in addition to α- and β-subunits. Whereas the subunit arrangement of the former group is agreed upon, that of the αβδ GABAARs remains unresolved by electrophysiological and pharmacological research...
2018: PloS One
https://www.readbyqxmd.com/read/29350522/chemical-design-of-both-a-glutathione-sensitive-dimeric-drug-guest-and-a-glucose-derived-nanocarrier-host-to-achieve-enhanced-osteosarcoma-lung-metastatic-anticancer-selectivity
#2
Lu Su, Richen Li, Sarosh Khan, Ryan Clanton, Fuwu Zhang, Yen-Nan Lin, Yue Song, Hai Wang, Jingwei Fan, Soleil Hernandez, Andrew S Butters, Gamal Akabani, Ronan MacLoughlin, Justin Smolen, Karen L Wooley
Although nanomedicines have been pursued for nearly 20 years, fundamental chemical strategies that seek to optimize both the drug and drug carrier together in a concerted effort remain uncommon yet may be powerful. In this work, two block polymers and one dimeric prodrug molecule were designed to be coassembled into degradable, functional nanocarriers, where the chemistry of each component was defined to accomplish important tasks. The result is a poly(ethylene glycol) (PEG)-protected redox-responsive dimeric paclitaxel (diPTX)-loaded cationic poly(d-glucose carbonate) micelle (diPTX@CPGC)...
January 19, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29350484/paraptosis-inducing-nanomedicine-overcomes-cancer-drug-resistance-for-a-potent-cancer-therapy
#3
Yongcun Zhou, Feiteng Huang, Ying Yang, Pingli Wang, Zhen Zhang, Yining Tang, Youqing Shen, Kai Wang
Most chemotherapeutic drugs and their nanomedicine formulations exert anticancer activity by inducing cancer cell apoptosis. However, cancer cells inherently have and acquire many antiapoptosis mechanisms, causing cancer drug resistance and poor prognoses in patients. Herein, a potent paraptosis-inducing nanomedicine is reported that causes quick nonapoptotic death of cancer cells, overcoming apoptosis-based resistance and effectively inhibiting drug-resistant tumor growth. The nanomedicine is composed of micelles made from an amphiphilic 8-hydroxyquinoline (HQ)-conjugate block copolymer with polyethylene glycol...
January 19, 2018: Small
https://www.readbyqxmd.com/read/29350229/aggregate-evolution-in-aqueous-solutions-of-a-gemini-surfactant-derived-from-dehydroabietic-acid
#4
Lin Feng, Danhua Xie, Binglei Song, Jiayu Zhang, Xiaomei Pei, Zhenggang Cui
Innovations in surfactant structure are a feasible way to probe molecular self-assembly principles. Herein, the solution behaviour of a newly synthesized Gemini surfactant derived from dehydroabietic acid, abbreviated R-(EO)-E-R, was investigated using surface tension, fluorescence, isothermal titration calorimetry (ITC), rheology, freeze-fracture transmission electron microscopy (FF-TEM) and cryogenic transmission electron microscopy (cryo-TEM) methods. R-(EO)-E-R has two large, rigid hydrophobic groups. At low concentrations, R-(EO)-E-R forms micelles with an aggregation number of approximately 10, which is smaller than those of Gemini surfactants containing flexible alkyl tails...
January 19, 2018: Soft Matter
https://www.readbyqxmd.com/read/29350064/comparison-of-hyaluronic-acid-based-micelles-and-polyethylene-glycol-based-micelles-on-reversal-of-multidrug-resistance-and-enhanced-anticancer-efficacy-in-vitro-and-in-vivo
#5
Jinling Wang, Ying Li, Lifang Wang, Xiaohui Wang, Pengfei Tu
Polyethylene glycol (PEG)-based block copolymer micelles and hyaluronic acid (HA)-based grafted copolymer micelles have been widely investigated in chemotherapy. In this study, to evaluate the differences among HA-based grafted polymer micelles, PEG-based block polymer micelles and the mixed of these two micelles in enhancing antitumor effects and overcoming MDR, two amphiphilic vitamin E succinate (VES) derivatives, HA VES (HA-g-VES) and PEG 2000 VES (TPGS2k), were applied as nanocarriers to prepare HA-VES micelles (HA-PMs), TPGS2k micelles (TPGS2k-PMs) and the mixed micelles (HA/TPGS2k-PMs) for the co-delivery of doxorubicin (DOX) and curcumin (Cur)...
November 2018: Drug Delivery
https://www.readbyqxmd.com/read/29349619/1h-15n-and-13c-chemical-shift-assignments-of-the-micelle-immersed-fat-c-terminal-fatc-domains-of-the-human-protein-kinases-ataxia-telangiectasia-mutated-atm-and-dna-dependent-protein-kinase-catalytic-subunit-dna-pkcs-fused-to-the-b1-domain-of-streptococcal
#6
Munirah S Abd Rahim, Lisa A M Sommer, Anja Wacker, Martin Schaad, Sonja A Dames
FAT C-terminal (FATC) is a circa 33 residue-long domain. It controls the kinase functionality in phosphatidylinositol-3 kinase-related kinases (PIKKs). Recent NMR- and CD-monitored interaction studies indicated that the FATC domains of all PIKKs can interact with membrane mimetics albeit with different preferences for membrane properties such as surface charge and curvature. Thus they may generally act as membrane anchoring unit. Here, we present the 1H, 15N, and 13C chemical shift assignments of the DPC micelle immersed FATC domains of the human PIKKs ataxia-telangiectasia mutated (ATM, residues 3024-3056) and DNA protein kinase catalytic subunit (DNA-PKcs, residues 4096-4128), both fused to the 56 residue long B1 domain of Streptococcal protein G (GB1)...
January 18, 2018: Biomolecular NMR Assignments
https://www.readbyqxmd.com/read/29349595/the-development-of-a-nano-based-approach-to-alleviate-cisplatin-induced-ototoxicity
#7
Mohammad N Kayyali, Andrew J Ramsey, Elizabeth M Higbee-Dempsey, Lesan Yan, Bert W O'Malley, Andrew Tsourkas, Daqing Li
Cisplatin-induced hearing loss is experienced by a high percentage of patients with squamous cell carcinoma undergoing cisplatin chemotherapy. A novel nano-construct capable of sequestering extracellular cisplatin was developed to combat this problem. The nano-construct consisted of superparamagnetic iron oxide nanoparticles (SPIONs) entrapped within polymeric micelles, which were formed from a glutathione diethyl ester-conjugated amphiphilic diblock copolymer. The glutathione-micelles were analyzed at the cellular level and in an organotypic study for safety evaluation...
January 18, 2018: Journal of the Association for Research in Otolaryngology: JARO
https://www.readbyqxmd.com/read/29348199/origins-of-low-symmetry-phases-in-asymmetric-diblock-copolymer-melts
#8
Kyungtae Kim, Akash Arora, Ronald M Lewis, Meijiao Liu, Weihua Li, An-Chang Shi, Kevin D Dorfman, Frank S Bates
Cooling disordered compositionally asymmetric diblock copolymers leads to the formation of nearly spherical particles, each containing hundreds of molecules, which crystallize upon cooling below the order-disorder transition temperature (TODT). Self-consistent field theory (SCFT) reveals that dispersity in the block degrees of polymerization stabilizes various Frank-Kasper phases, including the C14 and C15 Laves phases, which have been accessed experimentally in low-molar-mass poly(isoprene)-b-poly(lactide) (PI-PLA) diblock copolymers using thermal processing strategies...
January 18, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29347646/marangoni-effect-on-small-amplitude-capillary-waves-in-viscous-fluids
#9
Li Shen, Fabian Denner, Neal Morgan, Berend van Wachem, Daniele Dini
We derive a general integro-differential equation for the transient behavior of small-amplitude capillary waves on the planar surface of a viscous fluid in the presence of the Marangoni effect. The equation is solved for an insoluble surfactant solution in concentration below the critical micelle concentration undergoing convective-diffusive surface transport. The special case of a diffusion-driven surfactant is considered near the the critical damping wavelength. The Marangoni effect is shown to contribute to the overall damping mechanism, and a first-order term correction to the critical wavelength with respect to the surfactant concentration difference and the Schmidt number is proposed...
November 2017: Physical Review. E
https://www.readbyqxmd.com/read/29347293/shear-banding-and-superdiffusivity-in-entangled-polymer-solutions
#10
Seunghwan Shin, Kevin D Dorfman, Xiang Cheng
Using high-resolution confocal rheometry, we study the shear profiles of well-entangled DNA solutions under large-amplitude oscillatory shear in a rectilinear planar shear cell. With increasing Weissenberg number (Wi), we observe successive transitions from normal Newtonian linear shear profiles to wall-slip dominant shear profiles and, finally, to shear-banding profiles at high Wi. To investigate the microscopic origin of the observed shear banding, we study the dynamics of micron-sized tracers embedded in DNA solutions...
December 2017: Physical Review. E
https://www.readbyqxmd.com/read/29347218/effect-of-particle-size-dynamics-on-properties-of-dense-spongy-particle-systems-approach-towards-equilibrium
#11
Monica E A Zakhari, Patrick D Anderson, Markus Hütter
Open-porous deformable particles, often envisaged as sponges, are ubiquitous in biological and industrial systems (e.g., casein micelles in dairy products and microgels in cosmetics). The rich behavior of these suspensions is owing to the elasticity of the supporting network of the particle, and the viscosity of permeating solvent. Therefore, the rate-dependent size change of these particles depends on their structure, i.e., the permeability. This work aims at investigating the effect of the particle-size dynamics and the underlying particle structure, i...
July 2017: Physical Review. E
https://www.readbyqxmd.com/read/29347138/anomalous-diffusion-and-stress-relaxation-in-surfactant-micelles
#12
Subas Dhakal, Radhakrishna Sureshkumar
We investigate the mechanisms of anomalous diffusion in cationic surfactant micelles using molecular dynamics simulations in the presence of explicit salt and solvent-mediated interactions. Simulations show that when the counterion density increases, saddle-shaped branched interfaces manifest. In experiments, branched structures exhibit lower viscosity as compared to linear and wormlike micelles. This has long been attributed to stress relaxation arising from the sliding motion of branches along the main chain...
July 2017: Physical Review. E
https://www.readbyqxmd.com/read/29346965/solute-mediated-interactions-between-active-droplets
#13
Pepijn G Moerman, Henrique W Moyses, Ernest B van der Wee, David G Grier, Alfons van Blaaderen, Willem K Kegel, Jan Groenewold, Jasna Brujic
Concentration gradients play a critical role in embryogenesis, bacterial locomotion, as well as the motility of active particles. Particles develop concentration profiles around them by dissolution, adsorption, or the reactivity of surface species. These gradients change the surface energy of the particles, driving both their self-propulsion and governing their interactions. Here, we uncover a regime in which solute gradients mediate interactions between slowly dissolving droplets without causing autophoresis...
September 2017: Physical Review. E
https://www.readbyqxmd.com/read/29346731/direct-polymerization-of-the-arsenic-drug-penao-to-obtain-nanoparticles-with-high-thiol-reactivity-and-anti-cancer-efficiency
#14
Janina-Miriam Noy, Hongxu Lu, Philip Hogg, Jia-Lin Yang, Martina H Stenzel
PENAO (4-(N-(S-penicillaminylacetyl)amino) phenylarsonous acid), which is a mitochondria inhibitor that reacts with adenine nucleotide translocator (ANT), is currently being trialed in patients with solid tumors. To increase the stability of the drug, the formation of nanoparticles has been proposed. Herein, the direct synthesis of polymeric micelles based on the anti-cancer drug PENAO is presented. PENAO is readily available for amidation reaction to form PENAO MA (4-(N-(S-penicillaminylacetyl) amino) phenylarsonous acid methacrylamide) which undergoes RAFT (reversible addition fragmentation chin transfer) polymerization with poly(polyethylene glycol methyl ether methacrylate) (PEGMA) as comonomer and poly(methylmethacrylate) (pMMA) as chain transfer agent, resulting in p(MMA)-b-p(PEG-co-PENAO) block copolymers with 3-15 wt...
January 18, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29346330/formulation-of-poloxamers-for-drug-delivery
#15
REVIEW
Andrew M Bodratti, Paschalis Alexandridis
Poloxamers, also known as Pluronics®, are block copolymers of poly(ethylene oxide) (PEO) and poly(propylene oxide) (PPO), which have an amphiphilic character and useful association and adsorption properties emanating from this. Poloxamers find use in many applications that require solubilization or stabilization of compounds and also have notable physiological properties, including low toxicity. Accordingly, poloxamers serve well as excipients for pharmaceuticals. Current challenges facing nanomedicine revolve around the transport of typically water-insoluble drugs throughout the body, followed by targeted delivery...
January 18, 2018: Journal of Functional Biomaterials
https://www.readbyqxmd.com/read/29345955/investigation-of-polymer-surfactant-interactions-and-their-impact-on-itraconazole-solubility-and-precipitation-kinetics-for-developing-spray-dried-amorphous-solid-dispersions
#16
Tanvi Mahesh Deshpande, Helen Shi, John Pietryka, Stephen W Hoag, Ales Medek
Methods were developed to systematically screen different polymer-surfactant combinations for the purpose of enhancing amorphous active pharmaceutical ingredient (API) solubility while maintaining its physical stability. Itraconazole (ITZ) was chosen as the model API mostly due to its low aqueous solubility. Special attention was paid to determine the effect of a reduction in the critical micelle concentration (CMC) by specific polymer/surfactant combinations on the ITZ solubility and physical stability. However, only a slight correlation was actually found...
January 18, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29345701/effects-of-particle-size-and-annealing-on-plasmon-induced-charge-separation-at-self-assembled-gold-nanoparticle-arrays
#17
Kun-Che Kao, Hiroyasu Nishi, Tetsu Tatsuma
Two-dimensional periodic Au nanoparticle arrays were constructed on TiO2 thin films by a micelle lithography method and seed-mediated photoelectrochemical growth. Their adjustable interparticle distance allows investigation of a particle size effect on plasmon-induced charge separation (PICS) efficiencies without interference from particle aggregation or plasmon coupling. External or internal PICS efficiencies were found to increase and decrease, respectively, with an increase in particle diameter from 25 to 38 nm...
January 18, 2018: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29342326/mixed-fluorotryptophan-substitutions-at-the-same-residue-expand-the-versatility-of-%C3%A2-%C3%A2-f-protein-nmr-spectroscopy
#18
Calem Kenward, Kyungsoo Shin, Jan Rainey
The strategy of applying fluorine NMR to characterize ligand binding to a membrane protein prepared with mixtures of tryptophans substituted with F at different positions on the indole ring was tested. The ¹⁹F NMR behavior of 4-, 5-, 6-, and 7-fluorotryptophan were directly compared as a function of both micellar environment and fragment size for two overlapping apelin receptor (AR/APJ) segments - one with a single transmembrane (TM) helix and two tryptophan residues, the other with three TM helices and two additional tryptophan residues...
January 17, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29341946/microemulgel-of-voriconazole-an-unfathomable-protection-to-counter-fungal-contagiousness
#19
Kalpesh C Ashara, Jalpa S Paun, Moinuddin M Soniwala, Jayant R Chavda
BACKGROUND: Fluconazole and ketoconazole both have poor minimum inhibitory concentration than voriconazole. Voriconazole had serious side effects in oral and intravenous doses. It has poor water solubility. The objective of the study was to prepare and optimize microemulgel of voriconazole for topical delivery. AIM: Formulation, development, and evaluation of voriconazole microemulgel for topical delivery. METHODS: Oil and emulsifi ers selected were on the basis of equilibrium solubility study and emulsification property respectively...
December 20, 2017: Folia Medica
https://www.readbyqxmd.com/read/29340361/a-curcumin-loaded-polymeric-micelle-as-a-carrier-of-a-microrna-21-antisense-oligonucleotide-for-enhanced-anti-tumor-effects-in-a-glioblastoma-animal-model
#20
Xiaonan Tan, Gyeungyun Kim, Dahee Lee, Jungju Oh, Minkyung Kim, Chunxian Piao, Jaewon Lee, Min Sang Lee, Ji Hoon Jeong, Minhyung Lee
A glioblastoma is a common primary brain tumor that expresses microRNA-21 (miR-21), which inhibits the expression of pro-apoptotic genes such as phosphatase and tensin homologue (PTEN) and programmed cell death 4 (PDCD4). Therefore, an antisense-oligonucleotide against miR-21 (miR21ASO) could have therapeutic effects for glioblastomas. In this study, curcumin was loaded into deoxycholic acid-conjugated polyethylenimine (DP) micelles. The curcumin-loaded DP micelle (DP-Cur) was evaluated as a carrier for the combined delivery of curcumin and miR21ASO...
January 17, 2018: Biomaterials Science
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