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Neha Arora, M Ibrahim Dar, Mojtaba Abdi-Jalebi, Fabrizio Giordano, Norman Pellet, Gwenole Jacopin, Richard H Friend, Shaik Mohammed Zakeeruddin, Michael Grätzel
We report on both intrinsic and extrinsic stability of formamidinium lead bromide [CH(NH2)2PbBr3=FAPbBr3] perovskite solar cell that yield a high photovoltage. The fabrication of FAPbBr3 devices displaying an outstanding photovoltage of 1.53 V and a power conversion efficiency of over 8% was realized by modifying the mesoporous TiO2/FAPbBr3 interface using lithium treatment. Reasons for improved photovoltaic performance were revealed by a combination of techniques, including photothermal deflection absorption spectroscopy (PDS), transient photovoltage and charge extraction analysis, and time-integrated and time-resolved photoluminescence...
October 24, 2016: Nano Letters
Jamal Chauhan, Steven Cardinale, Lei Fang, Jing Huang, Steven M Kwasny, M Ross Pennington, Kelly Basi, Robert diTargiani, Benedict R Capacio, Alexander D MacKerell, Timothy J Opperman, Steven Fletcher, Erik P H de Leeuw
Recently we described a novel di-benzene-pyrylium-indolene (BAS00127538) inhibitor of Lipid II. BAS00127538 (1-Methyl-2,4-diphenyl-6-((1E,3E)-3-(1,3,3-trimethylindolin-2-ylidene)prop-1-en-1-yl)pyryl-1-ium) tetrafluoroborate is the first small molecule Lipid II inhibitor and is structurally distinct from natural agents that bind Lipid II, such as vancomycin. Here, we describe the synthesis and biological evaluation of 50 new analogs of BAS00127538 designed to explore the structure-activity relationships of the scaffold...
2016: PloS One
Seung Hyuk Im, Youngmee Jung, Yangsoo Jang, Soo Hyun Kim
Most biomaterials composed of biodegradable polymers will contact either accidentally or consistently with blood and this commonly requires both good  mechanical strength and blood compatibility. Despite this demand, current processing methods still make it difficult and complex to simultaneously improve the two properties. To overcome present limitations, the aim of this work is to develop a solid-state drawing which is a novel method for blood-contact biomaterials that can simultaneously improve the two essential factors of mechanical strength and blood compatibility, as well as induce a micro-patterned surface...
October 24, 2016: Biofabrication
Isabel Ortuño-Lizarán, Guillermo Vilariño-Feltrer, Cristina Martínez-Ramos, Manuel Monleón Pradas, Ana Vallés-Lluch
Hydrogels have widely been proposed lately as strategies for neural tissue regeneration, but there are still some issues to be solved before their efficient use in tissue engineering of trauma, stroke or the idiopathic degeneration of the nervous system. In a previous work of the authors a novel Schwann-cell structure with the shape of a hollow cylinder was obtained using a three-dimensional conduit based in crosslinked hyaluronic acid as template. This original engineered tissue of tightly joined Schwann cells obtained in a conduit lumen having 400 μm in diameter is a consequence of specific cell-material interactions...
October 24, 2016: Biofabrication
Zhe Wang, Fuwu Zhang, Zhantong Wang, Xiao Fu, Albert Jin, Bryant C Yung, Jing Fan, Xiangyu Yang, Gang Niu, Xiaoyuan Chen
Molecular design of biomaterials with unique features reca-pitulating nature's niche to influence biological activities has been a prolific area of investigation in chemistry and material science. The extracellular matrix (ECM) provides a wealth of bioactive molecules in supporting cell proliferation, migra-tion and differentiation. The well-patterned fibril and inter-twining architecture of the ECM profoundly influences cell behavior and development. Inspired by those features from the ECM, we attempted to integrate essential biological fac-tors from the ECM to design bioactive molecules to construct artificial self-supportive ECM mimics to advance stem cell culture...
October 24, 2016: Journal of the American Chemical Society
Andreas Gollner, Dorothea Rudolph, Heribert Arnhof, Markus Bauer, Sophia Maria Blake, Guido Boehmelt, Xiao-Ling Cockcroft, Georg Dahmann, Peter Ettmayer, Thomas Gerstberger, Jale Karolyi-Oezguer, Dirk Kessler, Christiane Kofink, Juergen Ramharter, Jörg Rinnenthal, Alexander Savchenko, Renate Schnitzer, Harald Weinstabl, Ulrike Weyer-Czernilofsky, Tobias Wunberg, Darryl B McConnell
Scaffold modification based on Wang´s pioneering MDM2-p53 inhibitors led to novel, chemically stable spiro-oxindole compounds bearing a spiro[3H-indole-3,2´-pyrrolidin]-2(1H)-one scaffold that are not prone to epimerization as observed for the initial spiro[3H-indole-3,3´-pyrrolidin]-2(1H)-one scaffold. Further structure based optimization inspired by natural product architectures led to a complex fused ring system ideally suited to bind to the MDM2 protein and to interrupt its protein-protein interaction (PPI) with TP53...
October 24, 2016: Journal of Medicinal Chemistry
Yu Zhang, Yifei Lu, Feng Wang, Sai An, Yujie Zhang, Tao Sun, Jianhua Zhu, Chen Jiang
Inflammation has been reported as one significant hallmark of breast cancer in relation to tumor development, metastasis, and invasion. The bradykinin receptor 1 (B1R) is highly expressed on inflammatory breast tumor cells thus providing a promising targeting site for tumor recognition and sufficient receptor mediated endocytosis. In this study, the authors evaluate the targeting efficiency of l-form and d-form [des-Arg(10) ]kallidin both in vitro and in vivo. To further improve the drug delivery efficiency, the authors establish a dandelion like nanoparticle by combining the polymeric drug conjugates and aptamer complex together...
October 24, 2016: Small
Ya Gao, Yingbo Wang, Yimin Wang, Wenguo Cui
A major goal of biomimetics is the development of chemical compositions and structures that simulate the extracellular matrix. In this study, gelatin-based electrospun composite fibrous membranes were prepared by electrospinning to generate bone scaffold materials. The gelatin-based multicomponent composite fibers were fabricated using co-electrospinning, and the composite fibers of chitosan (CS), gelatin (Gel), hydroxyapatite (HA), and graphene oxide (GO) were successfully fabricated for multi-function characteristics of biomimetic scaffolds...
October 21, 2016: Marine Drugs
Christine Radtke
Spider silk and its synthetic derivatives have a light weight in combination with good strength and elasticity. Their high cytocompatibility and low immunogenicity make them well suited for biomaterial products such as nerve conduits. Silk proteins slowly degrade enzymatically in vivo, thus allowing for an initial therapeutic effect such as in nerve scaffolding to facilitate endogenous repair processes, and then are removed. Silks are biopolymers naturally produced by many species of arthropods including spiders, caterpillars and mites...
October 20, 2016: International Journal of Molecular Sciences
Claudia Melis, Rita Meleddu, Andrea Angeli, Simona Distinto, Giulia Bianco, Clemente Capasso, Filippo Cottiglia, Rossella Angius, Claudiu T Supuran, Elias Maccioni
The isatin scaffold is the constitutive fragment of several natural and synthetic bioactive molecules. Albeit several benzene sulphonamide-based carbonic anhydrase inhibitors (CAIs) have been reported, only recently isatin benzene sulphonamides have been studied and proposed as CAIs. In this study we have designed, synthesised, and evaluated the biological activity of a series of differently substituted isatin-based benzene sulphonamides which have been designed for the inhibition of carbonic anhydrase isoforms...
October 24, 2016: Journal of Enzyme Inhibition and Medicinal Chemistry
Niloofar Eslahi, Marjan Abdorahim, Abdolreza Arash Simchi
Stimuli responsive hydrogels (SRHs) are attractive bio-scaffolds for tissue engineering. The structural similarity of SRHs to the extracellular matrix (ECM) of many tissues offers great advantages for a minimally invasive tissue repair. Among various potential applications of SRHs, cartilage regeneration has attracted significant attention. The repair of cartilage damage is challenging in orthopedics owing to its low repair capacity. Recent advances include development of injectable hydrogels to minimize invasive surgery with nanostructured features and rapid stimuli-responsive characteristics...
October 24, 2016: Biomacromolecules
Keiichi Mochida, Tetsuya Sakurai, Hikaru Seki, Takuhiro Yoshida, Kotaro Takahagi, Satoru Sawai, Hiroshi Uchiyama, Toshiya Muranaka, Kazuki Saito
Chinese liquorice/licorice (Glycyrrhiza uralensis) is a leguminous plant species whose roots and rhizomes have been widely used as a herbal medicine and natural sweetener. Whole-genome sequencing is essential for gene discovery studies and molecular breeding in liquorice. Here, we report a draft assembly of the approximately 379-Mb whole-genome sequence of strain 308-19 of G. uralensis; this assembly contains 34 445 predicted protein-coding genes. Comparative analyses suggested well-conserved genomic components and collinearity of gene loci (synteny) between the genome of liquorice and those of other legumes such as Medicago and chickpea...
October 24, 2016: Plant Journal: for Cell and Molecular Biology
Matthew Osmond, Sarah M Bernier, Mina B Pantcheva, Melissa D Krebs
Glaucoma is a disease in which damage to the optic nerve leads to progressive, irreversible vision loss. The intraocular pressure (IOP) is the only modifiable risk factor for glaucoma and its lowering is considered a useful strategy for preventing or slowing down the progression of glaucomatous neuropathy. Elevated intraocular pressure associated with glaucoma is due to increased aqueous humor outflow resistance, primarily through the trabecular meshwork (TM) of the eye. Current in vitro models of the trabecular meshwork are oversimplified and do not capture the organized and complex three-dimensional nature of this tissue that consists primarily of collagen and glycoasaminoglycans...
October 24, 2016: Biotechnology and Bioengineering
Abdul Hameed, Mariya Al-Rashida, Maliha Uroos, Syed Ali, Khalid M Khan
Schiff bases are synthetically accessible and structurally diverse compounds, typically obtained by facile condensation between an aldehyde, or a ketone with primary amines. Schiff bases contain an azomethine (-C=N-) linkage that stitches together two or more biologically active aromatic/heterocyclic scaffolds to form various molecular hybrids with interesting biological properties. Schiff bases are versatile metal complexing agents and have been known to coordinate all metals to form stable metal complexes with vast therapeutic applications...
October 24, 2016: Expert Opinion on Therapeutic Patents
Atul Kumar Chaturvedi, Ruchir Kant, Namrata Rastogi
A novel strategy is reported here for the synthesis of an indenopyrazole scaffold bearing a phosphonate group. The entire sequence includes nucleophilic addition-elimination, Seyferth-Gilbert homologation, transphosphorylation, and a 1,3-dipolar cycloaddition reaction of diazoalkylphosphonates in a perfect "domino" manner.
October 24, 2016: Journal of Organic Chemistry
Ibrahim J Domian, Hanry Yu, Nikhil Mittal
In this essay the authors argue that chamber pressure dominates the biomechanics of the contraction cycle of the heart, while tissue stiffness dominates the relaxation cycle. This appears to be an under-recognized challenge in cardiac tissue engineering. Optimal approaches will involve constructing chambers or modulating the stiffness of the scaffold/substrate in synchrony with the beating cycle.
October 24, 2016: Advanced Healthcare Materials
Alfonso Ielasi, Attilio Varricchio, Gianluca Campo, Massimo Leoncini, Bernardo Cortese, Paolo Vicinelli, Salvatore Brugaletta, Fortunato Scotto di Uccio, Azeem Latib, Maurizio Tespili
OBJECTIVES: To assess the feasibility and the clinical results following a prespecified bioresorbable vascular scaffold (Absorb BVS) implantation strategy in ST-elevation myocardial infarction (STEMI) patients. BACKGROUNDS: Concerns raised about the BVS safety in STEMI setting because a not negligible thrombosis rate was reported within 30 days and 12 months after implantation. Technical procedural issues related to the structural BVS features were advocated as probable causes for the thrombotic events...
October 24, 2016: Catheterization and Cardiovascular Interventions
Yu Zhao, Michael D Pluth
Hydrogen sulfide (H2 S) exhibits promising protective effects in many (patho)physiological processes, as evidenced by recent reports using synthetic H2 S donors in different biological models. Herein, we report the design and evaluation of compounds denoted PeroxyTCM, which are the first class of reactive oxygen species (ROS)-triggered H2 S donors. These donors are engineered to release carbonyl sulfide (COS) upon activation, which is quickly hydrolyzed to H2 S by the ubiquitous enzyme carbonic anhydrase (CA)...
October 24, 2016: Angewandte Chemie
Kathleen M Clark, Jermaine L Jenkins, Nadia Fedoriw, Mark E Dumont
The function and localization of proteins and peptides containing C-terminal "CaaX" (Cys-aliphatic-aliphatic-anything) sequence motifs are modulated by post-translational attachment of isoprenyl groups to the cysteine sulfhydryl, followed by proteolytic cleavage of the aaX amino acids. The zinc metalloprotease ZMPSTE24 is one of two enzymes known to catalyze this cleavage. The only identified target of mammalian ZMPSTE24 is prelamin A, the precursor to the nuclear scaffold protein lamin A. ZMPSTE24 also cleaves prelamin A at a second site 15 residues upstream from the CaaX site...
October 24, 2016: Protein Science: a Publication of the Protein Society
Jason M Law, Sebastian C Stark, Ke Liu, Norah E Liang, Mahmud M Hussain, Matthias Leiendecker, Daisuke Ito, Oscar Verho, Andrew M Stern, Stephen E Johnston, Yan-Ling Zhang, Gavin P Dunn, Alykhan F Shamji, Stuart L Schreiber
Evidence suggests that specific mutations of isocitrate dehydrogenases 1 and 2 (IDH1/2) are critical for the initiation and maintenance of certain tumor types and that inhibiting these mutant enzymes with small molecules may be therapeutically beneficial. In order to discover mutant allele-selective IDH1 inhibitors with chemical features distinct from existing probes, we screened a collection of small molecules derived from diversity-oriented synthesis. The assay identified compounds that inhibit the IDH1-R132H mutant allele commonly found in glioma...
October 13, 2016: ACS Medicinal Chemistry Letters
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