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Biologic Scaffold

Johannes Diesel, Anastasiia M Finogenova, Nicolai Cramer
Annulated pyridones are an important scaffold found in many biologically active compounds. A Ni(0)-catalyzed C-H functionalization of 2- and 4-pyridone is disclosed, providing access to annulated pyridones via enantioselective intramolecular olefin hydroarylation. Key to the success of the transformation was the development of a sterically hindered and tunable N-heterocyclic carbene ligand resembling a chiral version of IPr. This ligand allows for mild reaction temperatures, and leads to the annulated pyridones in excellent yields and enantioselectivities...
March 15, 2018: Journal of the American Chemical Society
Aleta Pupovac, Berna Senturk, Chiara Griffoni, Katharina Maniura-Weber, Markus Rottmar, Sally L McArthur
3D human skin models provide a platform for toxicity testing, biomaterials evaluation, and investigation of fundamental biological processes. However, the majority of current in vitro models lack an inflammatory system, vasculature, and other characteristics of native skin, indicating scope for more physiologically complex models. Looking at the immune system, there are a variety of cells that could be integrated to create novel skin models, but to do this effectively it is also necessary to understand the interface between skin biology and tissue engineering as well as the different roles the immune system plays in specific health and disease states...
March 15, 2018: Advanced Healthcare Materials
Colin R O'Dowd, Matthew D Helm, J S Shane Rountree, Jakub T Flasz, Elias Arkoudis, Hugues Miel, Peter R Hewitt, Linda Jordan, Oliver Barker, Caroline Hughes, Ewelina Rozycka, Eamon Cassidy, Keeva McClelland, Ewa Odrzywol, Natalie Page, Stephanie Feutren-Burton, Scarlett Dvorkin, Gerald Gavory, Timothy Harrison
Ubiquitin specific protease 7 (USP7, HAUSP) has become an attractive target in drug discovery due to the role it plays in modulating Mdm2 levels and consequently p53. Increasing interest in USP7 is emerging due to its potential involvement in oncogenic pathways as well as possible roles in both metabolic and immune disorders in addition to viral infections. Potent, novel, and selective inhibitors of USP7 have been developed using both rational and structure-guided design enabled by high-resolution cocrystallography...
March 8, 2018: ACS Medicinal Chemistry Letters
Monica Sanna, Giovanna Sicilia, Ali Alazzo, Nishant Singh, Francesca Musumeci, Silvia Schenone, Keith A Spriggs, Jonathan C Burley, Martin C Garnett, Vincenzo Taresco, Cameron Alexander
A miniaturized assay was optimized to evaluate the enhanced apparent water solubility of pyrazolo[3,4- d ]pyrimidine derivatives used extensively as anticancer drug scaffolds. The applied amount of drugs used in the reported strategy ranged from 5 to 10 μg per formulation which were dispensed by an inkjet 2D printer directly into a 96-well plate. The selected polymer/drug formulations with high water solubility demonstrated improved cytotoxicity against a human lung adenocarcinoma cancer cell line (A549) compared to the free drugs...
March 8, 2018: ACS Medicinal Chemistry Letters
Lorenzo Vannozzi, Immihan Ceren Yasa, Hakan Ceylan, Arianna Menciassi, Leonardo Ricotti, Metin Sitti
Programming materials with tunable physical and chemical interactions among its components pave the way of generating 3D functional active microsystems with various potential applications in tissue engineering, drug delivery, and soft robotics. Here, the development of a recapitulated fascicle-like implantable muscle construct by programmed self-folding of poly(ethylene glycol) diacrylate hydrogels is reported. The system comprises two stacked layers, each with differential swelling degrees, stiffnesses, and thicknesses in 2D, which folds into a 3D tube together...
March 14, 2018: Macromolecular Bioscience
E M Kithsiri Wijeratne, Maria C F Oliveira, Jair Mafezoli, Ya-Ming Xu, Sandro Minguzzi, Pedro H J Batista, Otília D L Pessoa, Luke Whitesell, A A Leslie Gunatilaka
Withanolides constitute a valuable class of bioactive natural products because some members of the class are known to exhibit cytotoxic activity and also induce a cytoprotective heat-shock response. In order to understand the relationship between their structures and these dual bioactivities of the withanolide scaffold, we obtained 25 analogues of withaferin A (WA) and withanolide D (WD) including 17 new compounds by semisynthesis involving chemical and microbial transformations. Hitherto unknown 16β-hydroxy analogues of WA and WD were prepared by their reaction with triphenylphosphine/iodine, providing unexpected 5β-hydroxy-6α-iodo analogues (iodohydrins) followed by microbial biotransformation with Cunninghamella echinulata and base-catalyzed cyclization of the resulting 16β-hydroxy iodohydrins...
March 14, 2018: Journal of Natural Products
Chih-Chien Wang, Chih-Hsin Wang, Hsiang-Cheng Chen, Juin-Hong Cherng, Shu-Jen Chang, Yi-Wen Wang, Adrienne Chang, Jue-Zong Yeh, Yi-Huei Huang, Cheng-Che Liu
Repair and regeneration of craniofacial tissues is particularly challenging because they comprise a complex structure of hard and soft tissues involved in intricate functions. This study combined collagen scaffolds and human adipose stem cells (hASCs) for oral mucosal and calvarial bone regeneration by using resveratrol (RSV), which affects the differentiation of mesenchymal stem cells. We have evaluated the effect of collagen scaffold-containing RSV (collagen/RSV) scaffolds both in vitro and in vivo for their wound healing and bone regeneration potential...
March 13, 2018: International Wound Journal
Akande Akinsola Adegboye, Khalid Mohammed Khan, Uzma Salar, Sherifat Adeyinka Aboaba, Kanwal, Sridevi Chigurupati, Itrat Fatima, Mohammad Taha, Abdul Wadood, Jahidul Isalm Mohammad, Huma Khan, Shahnaz Perveen
Despite of many diverse biological activities exhibited by benzimidazole scaffold, it is rarely explored for the α-amylase inhibitory activity. For that purpose, 2-aryl benzimidazole derivatives 1-45 were synthesized and screened for in vitro α-amylase inhibitory activity. Structures of all synthetic compounds were deduced by various spectroscopic techniques. All compounds revealed inhibition potential with IC50 values of 1.48 ± 0.38-2.99 ± 0.14 μM, when compared to the standard acarbose (IC50  = 1...
March 6, 2018: European Journal of Medicinal Chemistry
Sonoko Kinjo, Masato Kiyomoto, Takashi Yamamoto, Kazuho Ikeo, Shunsuke Yaguchi
To understand the mystery of life, it is important to accumulate genomic information for various organisms because the whole genome encodes the commands for all the genes. Since the genome of Strongylocentrotus purpratus was sequenced in 2006 as the first sequenced genome in echinoderms, the genomic resources of other North American sea urchins have gradually been accumulated, but no sea urchin genomes are available in other areas, where many scientists have used the local species and reported important results...
March 13, 2018: Development, Growth & Differentiation
Lindon W K Moodie, Gunnar Cervin, Rozenn Trepos, Christophe Labriere, Claire Hellio, Henrik Pavia, Johan Svenson
By combining the recently reported repelling natural dihydrostilbene scaffold with an oxime moiety found in many marine antifoulants, a library of nine antifouling hybrid compounds was developed and biologically evaluated. The prepared compounds were shown to display a low antifouling effect against marine bacteria but a high potency against the attachment and growth of microalgae down to MIC values of 0.01 μg/mL for the most potent hybrid. The mode of action can be characterized as repelling via a reversible non-toxic biostatic mechanism...
March 13, 2018: Marine Biotechnology
Penghui Wang, Lulu Jiang, Yang Cao, Xiaodan Zhang, Bangjing Chen, Shiyu Zhang, Ke Huang, Deyong Ye, Lu Zhou
Phosphoglycerate mutase 1 (PGAM1) is a glycolytic enzyme that dynamically converts 3-phosphoglycerate (3PG) to 2-phosphoglycerate (2PG), which was upregulated to coordinate glycolysis, pentose phosphate pathway (PPP) and serine biosynthesis to promote cancer cell proliferation and tumor growth in a variety of cancers. However, only a few inhibitors of PGAM1 have been reported with poor molecular or cellular efficacy. In this paper, a series of xanthone derivatives were discovered as novel PGAM1 inhibitors through scaffold hopping and sulfonamide reversal strategy based on the lead compound PGMI-004A...
February 24, 2018: Bioorganic & Medicinal Chemistry
Orestis G Andriotis, Sylvia Desissaire, Philipp J Thurner
Tissue hydration is well known to influence tissue mechanics and can be tuned via osmotic pressure. Collagen fibrils are nature's nanoscale building blocks to achieve biomechanical function in a broad range of biological tissues and across many species. Intrafibrillar covalent cross-links have long been thought to play pivotal role for collagen fibril elasticity, but predominantly at large, far from physiological, strains. Performing nanotensile experiments of collagen fibrils at varying hydration levels by adjusting osmotic pressure in situ during atomic force microscopy experiments, we show the power the intrafibrillar non-covalent interactions have for defining collagen fibril tensile elasticity at low fibril strains...
March 12, 2018: ACS Nano
Zhen He, Harry Shrives, José A Fernández-Salas, Alberto Abengózar, Jessica Neufeld, Kevin Yang, Alex P Pulis, David John Procter
Functionalized benzothiophenes are important scaffolds found in molecules with wide ranging biological activity and in organic materials. We describe an efficient, metal-free synthesis of C2 arylated, allylated and propargylated benzothiophenes. The reaction utilizes synthetically unexplored yet readily accessible benzothiophene S-oxides and phenols, allyl- or propargyl silanes in a unique cascade sequence. An interrupted Pummerer reaction between benzothiophene S-oxides and the coupling partners yields sulfonium salts that lack aromaticity and therefore allow facile [3,3]-sigmatropic rearrangement...
March 12, 2018: Angewandte Chemie
Ivan V Surovtsev, Christine Jacobs-Wagner
Spatial organization is a hallmark of all living systems. Even bacteria, the smallest forms of cellular life, display defined shapes and complex internal organization, showcasing a highly structured genome, cytoskeletal filaments, localized scaffolding structures, dynamic spatial patterns, active transport, and occasionally, intracellular organelles. Spatial order is required for faithful and efficient cellular replication and offers a powerful means for the development of unique biological properties. Here, we discuss organizational features of bacterial cells and highlight how bacteria have evolved diverse spatial mechanisms to overcome challenges cells face as self-replicating entities...
March 8, 2018: Cell
Biraja C Dash, Zhenzhen Xu, Lawrence Lin, Andrew Koo, Sifon Ndon, Francois Berthiaume, Alan Dardik, Henry Hsia
The normal wound healing process involves a well-organized cascade of biological pathways and any failure in this process leads to wounds becoming chronic. Non-healing wounds are a burden on healthcare systems and set to increase with aging population and growing incidences of obesity and diabetes. Stem cell-based therapies have the potential to heal chronic wounds but have so far seen little success in the clinic. Current research has been focused on using polymeric biomaterial systems that can act as a niche for these stem cells to improve their survival and paracrine activity that would eventually promote wound healing...
March 9, 2018: Bioengineering
Mohammed Benadallah, Oualid Talhi, Fatiha Nouali, Nourredine Choukchou-Braham, Khaldoun Bachari, Artur M S Silva
The present review deals with the progress in medicinal chemistry of spirocyclic compounds, a wider class of natural and synthetic organic molecules, defined as a hybrid of two molecular entities covalently linked via a unique tetrahedral carbon. This spiro central carbon confers to the molecules a tridimensional structurally oriented framework, which is found in many medicinally relevant compounds, a well-known example is the anti-hypertensive spironolactone. Various bioactive natural products possess the privileged spiro linkage and different chemo-types thereof become synthetically accessible since the 20th century...
March 9, 2018: Current Medicinal Chemistry
Carson Holt, Michael Campbell, David A Keays, Nathaniel Edelman, Aurélie Kapusta, Emily Maclary, Eric Domyan, Alexander Suh, Wesley C Warren, Mark Yandell, M Thomas P Gilbert, Michael D Shapiro
The domestic rock pigeon ( Columba livia ) is among the most widely distributed and phenotypically diverse avian species. C. livia is broadly studied in ecology, genetics, physiology, behavior, and evolutionary biology, and has recently emerged as a model for understanding the molecular basis of anatomical diversity, the magnetic sense, and other key aspects of avian biology. Here we report an update to the C. livia genome reference assembly and gene annotation dataset. Greatly increased scaffold lengths in the updated reference assembly, along with an updated annotation set, provide improved tools for evolutionary and functional genetic studies of the pigeon, and for comparative avian genomics in general...
March 8, 2018: G3: Genes—Genomes—Genetics
Maria Touri, Fathollah Moztarzadeh, Noor Azuan Abu Osman, Mohammad Mehdi Dehghan, Masoud Mozafari
Tissue engineering scaffolds with oxygen generating elements have shown to be able to increase the level of oxygen and cell survivability in specific conditions. In this study, biphasic calcium phosphate (BCP) scaffolds with the composition of 60% hydroxyapatite (HA) and 40% beta-tricalcium phosphate (β-TCP), which have shown a great potential for bone tissue engineering applications, were fabricated by a direct-write assembly (robocasting) technique. Then, the three-dimensional (3D)-printed scaffolds were coated with different ratios of an oxygen releasing agent, calcium peroxide (CPO), which encapsulated within a polycaprolactone (PCL) matrix through dip-coating, and used for in situ production of oxygen in the implanted sites...
March 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Yanfei Gao, Weili Shao, Wang Qian, Jianxin He, Yuman Zhou, Kun Qi, Lidan Wang, Shizhong Cui, Rui Wang
In bone tissue engineering, the fabrication of a scaffold with a hierarchical architecture, excellent mechanical properties, and good biocompatibility remains a challenge. Here, a solution of polylactic acid (PLA) and Tussah silk fibroin (TSF) was electrospun into nanofiber yarns and woven into multilayer fabrics. Then, composite scaffolds were obtained by mineralization in simulated body fluid (SBF) using the multilayer fabrics as a template. The structure and related properties of the composite scaffolds were characterized using different techniques...
March 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Bidisha Sarkar, Santanu Maiti, Gajanan Raosaheb Jadhav, Priyankar Paira
Adenosine is known as an endogenous purine nucleoside and it modulates a wide variety of physiological responses by interacting with adenosine receptors. Among the four adenosine receptor subtypes, the A3 receptor is of major interest in this study as it is overexpressed in some cancer cell lines. Herein, we have highlighted the strategy of designing the h A3 receptor targeted novel benzothiazolylquinoline scaffolds. The radioligand binding data of the reported compounds are rationalized with the molecular docking results...
February 2018: Royal Society Open Science
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