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https://www.readbyqxmd.com/read/28636761/molecular-tools-for-facilitative-carbohydrate-transporters
#1
Marina Tanasova, Joseph R Fedie
Facilitative carbohydrate transporters - Gluts - have received a wide attention over decades due to their essential role in the nutrient uptake and links with various metabolic disorders, including diabetes, obesity, and cancer. Endeavors into understanding mechanisms of Glut-mediated nutrient uptake have resulted in the multidisciplinary research field, branching protein chemistry, chemical biology, organic synthesis, crystallography, and biomolecular modeling. Gluts became attractive targets for cancer research and medicinal chemistry, leading to the development of new approaches to cancer diagnostics and providing avenues for cancer-targeting therapeutics...
June 21, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28636311/insights-into-integrated-lead-generation-and-target-identification-in-malaria-and-tuberculosis-drug-discovery
#2
John Okombo, Kelly Chibale
New, safe and effective drugs are urgently needed to treat and control malaria and tuberculosis, which affect millions of people annually. However, financial return on investment in the poor settings where these diseases are mostly prevalent is very minimal to support market-driven drug discovery and development. Moreover, the imminent loss of therapeutic lifespan of existing therapies due to evolution and spread of drug resistance further compounds the urgency to identify novel effective drugs. However, the advent of new public-private partnerships focused on tropical diseases and the recent release of large data sets by pharmaceutical companies on antimalarial and antituberculosis compounds derived from phenotypic whole cell high throughput screening have spurred renewed interest and opened new frontiers in malaria and tuberculosis drug discovery...
June 21, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28636129/the-52-nd-international-conference-on-medicinal-chemistry-rict-2016-of-the-french-medicinal-chemistry-society-sct-held-in-caen-normandy
#3
EDITORIAL
Janos Sapi, Luc Van Hijfte, Patrick Dallemagne
Outstanding Medchem in France: Guest editors Janos Sapi, Luc Van Hjfte, and Patrick Dallemagne look back at the 52(nd) International Conference on Medicinal Chemistry (RICT 2016) held in Caen, France. They discuss the history of the French Medicinal Chemistry Society (Société de Chimie Thérapeutique, SCT) and provide highlights of last year's events, including some key presentations now collected in this Special Issue.
June 21, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28634827/highly-functionalized-cyclic-%C3%AE-amino-acid-moieties-as-promising-scaffolds-in-peptide-research-and-drug-design
#4
REVIEW
Loránd Kiss, István M Mándity, Ferenc Fülöp
Peptide-based drug research has received high attention in the field of medicinal chemistry over the past decade. For drug design, to improve proteolytic stability, it is desirable to include unnatural building blocks, such as conformationally restricted β-amino acid moieties, into the peptide sequence. Accordingly, the synthesis and incorporation of such conformationally rigid systems into novel type of peptides has gained large interest. Our research group has designed highly efficient methods for the construction of potential antimicrobial peptides...
May 30, 2017: Amino Acids
https://www.readbyqxmd.com/read/28633438/sandpuma-ensemble-predictions-of-nonribosomal-peptide-chemistry-reveals-biosynthetic-diversity-across-actinobacteria
#5
Marc G Chevrette, Fabian Aicheler, Oliver Kohlbacher, Cameron R Currie, Marnix H Medema
Summary: Nonribosomally synthesized peptides (NRPs) are natural products with widespread applications in medicine and biotechnology. Many algorithms have been developed to predict the substrate specificities of nonribosomal peptide synthetase adenylation (A) domains from DNA sequences, which enables prioritization and dereplication, and integration with other data types in discovery efforts. However, insufficient training data and a lack of clarity regarding prediction quality have impeded optimal use...
June 19, 2017: Bioinformatics
https://www.readbyqxmd.com/read/28632928/n-acylsulfonamides-synthetic-routes-and-biological-potential-in-medicinal-chemistry
#6
REVIEW
Alessandra Ammazzalorso, Barbara De Filippis, Letizia Giampietro, Rosa Amoroso
Sulfonamide is a common structural motif in naturally occurring and synthetic medicinal compounds. The rising interest in sulfonamides and N-acyl derivatives is attested by the large number of drugs and lead compounds identified in last years, explored in different fields of medicinal chemistry and showing biological activity. Many acylsulfonamide derivatives were designed and synthesized as isosteres of carboxylic acids, being the characteristics of these functional groups very close. Starting from chemical routes to N-acylsulfonamides, this review explores compounds of pharmaceutical interest, developed as enzymatic inhibitors or targeting receptors...
June 20, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28632420/medicinal-chemistry-advances-in-neurodegenerative-disease-therapy-part-2
#7
Rachel Coleby
No abstract text is available yet for this article.
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632338/difluoromethylation-reactions-of-organic-compounds
#8
Damian E Yerien, Sebastian Barata-Vallejo, Al Postigo
The relevance of the -CF2H moiety has attracted considerable attention from organic synthetic and medicinal chemistry communities, because this group can act as a more lipophilic isostere of the carbinol, thiol, hydroxamic acid or amide groups. Being weakly acidic, the CF2H moiety can establish hydrogen bonding interactions to improve the binding selectivity of biologically active compounds. Therefore, the hydroxyl, amino, and thio substituents of lead structures are routinely replaced by a CF2H motif in drug discovery, with great benefits in the pharmacological activity of drugs and drug candidates and agrochemicals...
June 20, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28632260/visualization-of-the-protein-corona-towards-a-biomolecular-understanding-of-nanoparticle-cell-interactions
#9
Maria Kokkinopoulou, Johanna Simon, Katharina Landfester, Volker Mailänder, Ingo Lieberwirth
The use of nanocarriers in biology and medicine is complicated by the current need to understand how nanoparticles interact in complex biological surroundings. When nanocarriers come into contact with serum, proteins immediately adsorb onto their surface, forming a protein corona which defines their biological identity. Although the composition of the protein corona has been widely determined by proteomics, its morphology still remains unclear. In this study we show for the first time the morphology of the protein corona using transmission electron microscopy...
June 20, 2017: Nanoscale
https://www.readbyqxmd.com/read/28627581/controlled-self-assembly-of-alginate-microgels-by-rapidly-binding-molecule-pairs
#10
Yuebi Hu, Angelo S Mao, Rajiv M Desai, Huanan Wang, David A Weitz, David J Mooney
Controlled self-assembly of cell-encapsulating microscale polymeric hydrogels (microgels) could be advantageous in a variety of tissue engineering and regenerative medicine applications. Here, a method of assembly by chemical modification of alginate polymer with binding pair molecules (BPM) was explored. Alginate was modified with several types of BPM, specifically biotin and streptavidin and click chemistry compounds, and fabricated into 25-30 μm microgels using a microfluidic platform. These microgels were demonstrated to self-assemble under physiological conditions...
June 19, 2017: Lab on a Chip
https://www.readbyqxmd.com/read/28626570/riboflavin-as-a-bioorthogonal-photocatalyst-for-the-activation-of-a-pt-iv-prodrug
#11
Silvia Alonso-de Castro, Emmanuel Ruggiero, Ane Ruiz-de-Angulo, Elixabete Rezabal, Juan C Mareque-Rivas, Xabier Lopez, Fernando López-Gallego, Luca Salassa
Encouraging developments demonstrate that few transition metal and organometallic catalysts can operate in a bioorthogonal fashion and promote non-natural chemistry in living systems by minimizing undesired side reactions with cellular components. These catalytic processes have potential for applications in medicinal chemistry and chemical biology. However, the stringent conditions of the cell environment severely limit the number of accessible metal catalysts and exogenous reactions. Herein, we report an unorthodox approach and a new type of bioorthogonal catalytic reaction, in which a metal complex is an unconventional substrate and an exogenous biological molecule acts as a catalyst...
June 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28625144/detection-of-poor-quality-artemisinin-based-combination-therapy-act-medicines-marketed-in-benin-using-simple-and-advanced-analytical-techniques
#12
Achille Yemoa, Védaste Habyalimana, Jérémie K Mbinze, Victoria Crickboom, Benjamin Muhigirwa, Agnès Ngoya, Pierre-Yves Sacré, Fernand Gbaguidi, Joëlle Quetin-Leclercq, Philippe Hubert, Roland D Marini
BACKGROUND: Poor quality antimalarial medicines still represent a threat to the public health, especially in Sub-Saharan Africa who bears a disproportionate share of the global burden of malaria. It is essential and urgent to strengthen mechanisms against counterfeit medicines. One of the approaches is regular market surveillance through quality controls. METHODS: 12 samples of artemether/lumefantrine were collected from formal and informal drug sellers in Cotonou (Benin) as well as additional other similar samples from Rwanda (13 samples) and from D...
June 15, 2017: Current Drug Safety
https://www.readbyqxmd.com/read/28621537/electrochemical-deposition-of-conformal-and-functional-layers-on-high-aspect-ratio-silicon-micro-nanowires
#13
Tuncay Ozel, Benjamin Zhang, Ruixuan Gao, Robert W Day, Charles M Lieber, Daniel G Nocera
Development of new synthetic methods for the modification of nanostructures has accelerated materials design advances to furnish complex architectures. Structures based on one-dimensional (1D) silicon (Si) structures using top-down and bottom-up methods are especially prominent for diverse applications in chemistry, physics, and medicine. Yet further elaboration of these structures with distinct metal-based and polymeric materials, which could open up new opportunities, has been difficult. We present a general electrochemical method for the deposition of conformal layers of various materials onto high aspect ratio Si micro- and nanowire arrays...
June 16, 2017: Nano Letters
https://www.readbyqxmd.com/read/28620761/medicinal-chemistry-of-%C3%AF-1-receptor-ligands-pharmacophore-models-synthesis-structure-affinity-relationships-and-pharmacological-applications
#14
Frauke Weber, Bernhard Wünsch
In the first part of this chapter, we summarize the various pharmacophore models for σ1 receptor ligands. Common to all of them is a basic amine flanked by two hydrophobic regions, representing the pharmacophoric elements. The development of computer-based models like the 3D homology model is described as well as the first crystal structure of the σ1 receptor. The second part focuses on the synthesis and biological properties of different σ1 receptor ligands, identified as 1-9. Monocyclic piperazines 1 and bicyclic piperazines 2 and 3 were developed as cytotoxic compounds, thus the IC50 values of cell growth and survival inhibition studies are given for all derivatives...
June 16, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28619593/on-the-halt-of-spontaneous-capillary-flows-in-diverging-open-channels
#15
J Berthier, K A Brakke, D Gosselin, F Navarro, N Belgacem, D Chaussy, E Berthier
Due to their compactness and independence of exterior energy sources, capillary microsystems are increasingly used in many different scientific domains, from biotechnology to medicine and biology, chemistry, energy and space. Obtaining a capillary flow depends on channel geometry and contact angle. A general condition for the establishment of a spontaneous capillary flow in a uniform cross section channel has already been derived from Gibbs free energy. In this work, we consider spontaneous capillary flows (SCF) in diverging open rectangular channels and suspended channels, and we show that they do not flow indefinitely but stop at some location in the channel...
June 12, 2017: Medical Engineering & Physics
https://www.readbyqxmd.com/read/28618993/new-perspectives-on-biomedical-applications-of-iron-oxide-nanoparticles
#16
Massimiliano Magro, Davide Baratella, Emanuela Bonaiuto, Jessica de Almeida Roger, Fabio Vianello
Iron oxide nanomaterials are considered promising tools for improved therapeutic efficacy and diagnostic applications in biomedicine. Accordingly, engineered iron oxide nanomaterials are increasingly proposed in biomedicine, and the interdisciplinary researches involving physics, chemistry, biology (nanotechnology) and medicine have led to exciting developments in the last decades. The progresses of the development of magnetic nanoparticles with tailored physico-chemical and surface properties produced a variety of clinically relevant applications, spanning from magnetic resonance imaging (MRI), drug delivery, magnetic hyperthermia, to in vitro diagnostics...
June 16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28609444/identification-of-compounds-that-suppress-toxoplasma-gondii-tachyzoites-and-bradyzoites
#17
Yuho Murata, Tatsuki Sugi, Louis M Weiss, Kentaro Kato
Drug treatment for toxoplasmosis is problematic, because current drugs cannot eradicate latent infection with Toxoplasma gondii and can cause bone marrow toxicity. Because latent infection remains after treatment, relapse of infection is a problem in both infections in immunocompromised patients and in congenitally infected patients. To identify lead compounds for novel drugs against Toxoplasma gondii, we screened a chemical compound library for anti-Toxoplasma activity, host cell cytotoxicity, and effect on bradyzoites...
2017: PloS One
https://www.readbyqxmd.com/read/28608445/tailoring-the-volatility-and-stability-of-oligopeptides
#18
J Schätti, U Sezer, S Pedalino, J P Cotter, M Arndt, M Mayor, V Köhler
Amino acids are essential building blocks of life and fluorinated derivatives have gained interest in chemistry and medicine. Modern mass spectrometry has enabled the study of oligo- and polypeptides as isolated entities in the gas phase, but predominantly as singly or even multiply charged species. While laser desorption of neutral peptides into adiabatically expanding supersonic noble gas jets is possible, UV-VIS spectroscopy, electric or magnetic deflectometry as well as quantum interferometry would profit from the possibility to prepare thermally slow molecular beams...
June 12, 2017: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/28604846/identification-of-active-components-in-yixinshu-capsule-with-protective-effects-against-myocardial-dysfunction-on-human-induced-pluripotent-stem-cell-derived-cardiomyocytes-by-an-integrative-approach
#19
Minyu Zhang, Hongwei Wu, Feifei Guo, Yangyang Yu, Junying Wei, Ya Geng, Shifeng Wang, Shiyou Li, Hongjun Yang
Traditional Chinese medicine (TCM) preparations have significant effects on some refractory diseases; however, these compositions are complex and their mechanisms are unknown. Identification of the active components in these preparations is essential. The mortality rate for heart failure (HF) has been increasing in recent years, and myocardial dysfunction (MD) has been proved to be the pathological basis of HF. Yixinshu Capsule (YXSC) is a multi-component oral drug with therapeutic effects on HF. However, the key active components are still unclear...
June 12, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28603990/hypervalent-iodine-iii-mediated-decarboxylative-ritter-type-amination-leading-to-the-production-of-%C3%AE-tertiary-amine-derivatives
#20
Kensuke Kiyokawa, Tomoki Watanabe, Laura Fra, Takumi Kojima, Satoshi Minakata
α-Tertiary amines (ATAs) are attractive structural motifs that are frequently found in biologically active molecules. Therefore, the development of an efficient method for the synthesis of ATAs represents an important research topic in the field of medicinal chemistry as well as organic chemistry. Although the Ritter reaction is a reliable approach for preparing α-tertiary amine derivatives via intermolecular amination reactions, the typical methods suffer from disadvantages such as harsh reaction conditions and the use of strong acids...
June 12, 2017: Journal of Organic Chemistry
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