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Biological Chemistry

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https://www.readbyqxmd.com/read/28817664/gold-nanoparticles-partition-to-and-increase-the-activity-of-glucose-6-phosphatase-in-a-synthetic-phospholipid-membrane-system
#1
Tyson J MacCormack, Amanda M Rundle, Michael Malek, Abhilash Raveendran, Maria-Victoria Meli
Engineered nanomaterials can alter the structure and/or function of biological membranes and membrane proteins but the underlying mechanisms remain unclear. We addressed this using a Langmuir phospholipid monolayer containing an active transmembrane protein, glucose-6-phosphatase (G6Pase). Gold nanoparticles (nAu) with varying ligand shell composition and hydrophobicity were synthesized, and their partitioning in the membrane and effects on protein activity characterized. nAu incorporation did not alter the macroscopic properties of the membrane...
2017: PloS One
https://www.readbyqxmd.com/read/28816379/from-enzymes-to-functional-materials-towards-activation-of-small-molecules
#2
Frauke Möller, Stefan Piontek, Reece G Miller, Ulf-Peter Apfel
The design of non-noble metal containing heterogenous catalysts for the activation of small molecules is of utmost importance for our society. While nature possesses very sophisticated machineries to perform such conversions, rationally designed catalytic materials are rare. Herein, we aim to raise the awareness of the overall common design and working principles of catalysts and "break down the boundaries" between biology, chemistry and material sciences.
August 17, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28814834/intracellular-trafficking-of-new-anticancer-therapeutics-antibody-drug-conjugates
#3
REVIEW
Muhammad Kalim, Jie Chen, Shenghao Wang, Caiyao Lin, Saif Ullah, Keying Liang, Qian Ding, Shuqing Chen, Jinbiao Zhan
Antibody-drug conjugate (ADC) is a milestone in targeted cancer therapy that comprises of monoclonal antibodies chemically linked to cytotoxic drugs. Internalization of ADC takes place via clathrin-mediated endocytosis, caveolae-mediated endocytosis, and pinocytosis. Conjugation strategies, endocytosis and intracellular trafficking optimization, linkers, and drugs chemistry present a great challenge for researchers to eradicate tumor cells successfully. This inventiveness of endocytosis and intracellular trafficking has given considerable momentum recently to develop specific antibodies and ADCs to treat cancer cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28813151/the-medicinal-and-biological-chemistry-mbc-library-an-efficient-source-on-new-hits
#4
Víctor Sebastián Pérez, Carlos Roca, Mahendra Awale, Jean-Louis Reymond, Ana Martínez, Carmen Gil, Nuria E Campillo
Identification of new hits is one of the biggest challenges in drug discovery. Creating a library of well-characterized drug-like compounds is a key step in this process. Our group has developed an in-house chemical library called Medicinal and Biological Chemistry (MBC) library. This collection has been successfully used to start several medicinal chemistry programs and developed in an accumulation of more than thirty years of experience in drug design and discovery of new drugs for unmet diseases. It contains over 1,000 compounds, mainly heterocyclic scaffolds...
August 16, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28811262/probe-microscopy-methods-and-applications-in-imaging-of-biological-materials
#5
REVIEW
Alper D Ozkan, Ahmet E Topal, Fatma B Dikecoglu, Mustafa O Guler, Aykutlu Dana, Ayse B Tekinay
Atomic force microscopy is an emerging tool for investigating the biomolecular aspects of cellular interactions; however, cell and tissue analyses must frequently be performed in aqueous environment, over rough surfaces, and on complex adhesive samples that complicate the imaging process and readily facilitate the blunting or fouling of the AFM probe. In addition, the shape and surface chemistry of the probe determine the quality and types of data that can be acquired from biological materials, with certain information becoming available only within a specific range of tip lengths or diameters, or through the assistance of specific chemical or biological functionalization procedures...
August 12, 2017: Seminars in Cell & Developmental Biology
https://www.readbyqxmd.com/read/28810197/photochemical-formation-of-chitosan-stabilized-near-infrared-absorbing-silver-nanoworms-a-green-synthetic-strategy-and-activity-on-gram-negative-pathogenic-bacteria
#6
Sreekar Marpu, Samar S Kolailat, Daniel Korir, Brian L Kamras, Ratnesh Chaturvedi, Abel Joseph, Christopher M Smith, Misael C Palma, Jyoti Shah, Mohammad A Omary
A facile, single-step, non-seeded photochemical protocol for producing a new type of anisotropic silver nanostructure, "nanoworms", with curved longer dimensions and smooth, rounded edges. The nanoworms exhibit surface plasmon resonance (SPR) absorption in the near-infrared window (NIRW) region and are stabilized using biocompatible polymer chitosan, rendering biocompatibility and amplified safety for biological utility of the composition. Both NIRW-absorbing nanoworms and visible-absorbing nanospheres herein are attained exclusively by employing green chemistry principles...
August 4, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28810078/discovery-of-key-physicochemical-structural-and-spatial-properties-of-rna-targeted-bioactive-ligands
#7
Brittany S Morgan, Jordan E Forte, Rebecca N Culver, Yuqi Zhang, Amanda E Hargrove
While myriad non-coding RNAs are known to be essential in cellular processes and misregulated in diseases, the development of RNA-targeted small molecule probes has met with limited success. To elucidate guiding principles for selective small molecule:RNA recognition, we analyzed cheminformatic and shape-based descriptors for 104 RNA-targeted ligands with demonstrated biological activity (RNA-targeted BIoactive ligaNd Database, RBIND). We then compared R-BIND to both FDA-approved small molecule drugs and RNA ligands without reported bioactivity...
August 15, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28809975/discovery-of-synthetic-small-molecules-that-enhance-the-number-of-stomata-c-h-functionalization-chemistry-for-plant-biology
#8
Asraa Ziadi, Naoyuki Uchida, Hiroe Kato, Rina Hisamatsu, Ayato Sato, Shinya Hagihara, Kenichiro Itami, Keiko U Torii
The increasing climate changes and global warming are leading to colossal agricultural problems such as abatement of food production and quality. As stomatal development is considered to play a key role in crop plant productivity and water-use efficiency, studying stomatal development is useful for understanding the productivity of plant systems for both natural and agricultural systems. Herein, we report the first-in-class synthetic small molecules enhancing the number of stomata in Arabidopsis thaliana that have been discovered by screening of the chemical library and further optimized by the Pd-catalyzed C-H arylation reaction...
August 15, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28808678/interest-in-stem-is-contagious-for-students-in-biology-chemistry-and-physics-classes
#9
Zahra Hazari, Geoff Potvin, Jennifer D Cribbs, Allison Godwin, Tyler D Scott, Leidy Klotz
We report on a study of the effect of peers' interest in high school biology, chemistry, and physics classes on students' STEM (science, technology, engineering, and mathematics)-related career intentions and course achievement. We define an interest quorum as a science class where students perceive a high level of interest for the subject matter from their classmates. We hypothesized that students who experience such an interest quorum are more likely to choose STEM careers. Using data from a national survey study of students' experiences in high school science, we compared the effect of five levels of peer interest reported in biology, chemistry, and physics courses on students' STEM career intentions...
August 2017: Science Advances
https://www.readbyqxmd.com/read/28808262/generation-of-broadband-ultraviolet-frequency-entangled-photons-using-cavity-quantum-plasmonics
#10
Hisaki Oka
Application of quantum entangled photons is now extending to various fields in physics, chemistry and biology. In particular, in terms of application to molecular science, broadband ultraviolet frequency-entangled photons are desired because molecules inducing photochemical reactions of interest often have electronic transition energies in the ultraviolet region. Recent standard method for generating such entangled photons is a chirped quasi-phase-matching method, however this method is not suitable for the generation of ultraviolet frequency-entangled photons because it requires down-conversion of a photon with a wavelength shorter than ultraviolet into an entangled photon pair...
August 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28807652/severity-indices-in-rheumatoid-arthritis-a-systematic-review
#11
Esther Toledano, M Jesús García de Yébenes, Isidoro González-Álvaro, Loreto Carmona
OBJECTIVE: To identify tools designed to evaluate the severity of patients with rheumatoid arthritis (RA) in order to use them in the investigation of prognostic markers in early arthritis. METHODS: We conducted a systematic review of studies that developed/validated an index for RA disease severity. They were analyzed using the COSMIN checklist to assess their methodological quality. In addition, all the variables included were evaluated for their clarity of definition, feasibility and probability of being present in each outcome during the first 2 years of the disease course...
August 11, 2017: Reumatología Clinica
https://www.readbyqxmd.com/read/28804798/probing-biological-redox-chemistry-with-large-amplitude-fourier-transformed-ac-voltammetry
#12
Hope Adamson, Alan M Bond, Alison Parkin
Biological electron-exchange reactions are fundamental to life on earth. Redox reactions underpin respiration, photosynthesis, molecular biosynthesis, cell signalling and protein folding. Chemical, biomedical and future energy technology developments are also inspired by these natural electron transfer processes. Further developments in techniques and data analysis are required to gain a deeper understanding of the redox biochemistry processes that power Nature. This review outlines the new insights gained from developing Fourier transformed ac voltammetry as a tool for protein film electrochemistry...
August 14, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28804757/one-aptamer-two-functions-the-full-length-aptamer-inhibits-ampa-receptors-while-the-short-one-inhibits-both-ampa-and-kainate-receptors
#13
William J Jaremko, Zhen Huang, Wei Wen, Andrew Wu, Nicholas Karl, Li Niu
AMPA and kainate receptors, along with NMDA receptors, are distinct subtypes of glutamate ion channels. Excessive activity of AMPA and kainate receptors has been implicated in neurological diseases, such as epilepsy and neuropathic pain. Antagonists that block their activities are therefore potential drug candidates. In a recent article in the Journal of Biological Chemistry by Jaremko et al. 2017, we have reported on the discovery and molecular characterization of an RNA aptamer of a dual functionality: the full-length RNA (101 nucleotide) inhibits AMPA receptors while the truncated or the short (55 nucleotide) RNA inhibits both the AMPA and kainate receptors...
2017: RNA & Disease
https://www.readbyqxmd.com/read/28803677/indole-fused-azepines-and-analogues-as-anticancer-lead-molecules-privileged-findings-and-future-directions
#14
REVIEW
Ashok K Singh, Vinit Raj, Sudipta Saha
The search for new lead compounds of simple structure, displaying highest quality anti-tumor potency with new mechanisms of action and least adverse effects is the major intention of cancer drug discovery now a days. For the time being, indole-fused azepines emerged as a simple class of compounds prolifically designed with strong pharmacological significances in particular of cancer protecting ability. In the recent years from the efforts of our research group, indole-fused heteroazepines, a simple structural class achieved by fusion of indole with oxygen, sulphur and nitrogen containing heteroazepine rings, have known for its superior outcomes in cancer treatment...
August 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28803046/design-synthesis-and-biological-evaluation-of-novel-pyrazolochalcones-as-potential-modulators-of-pi3k-akt-mtor-pathway-and-inducers-of-apoptosis-in-breast-cancer-cells
#15
Anver Basha Shaik, Garikapati Koteswara Rao, G Bharath Kumar, Nibeditha Patel, Vangala Santhosh Reddy, Irfan Khan, Sunitha Rani Routhu, C Ganesh Kumar, Immadi Veena, Kunta Chandra Shekar, Madan Barkume, Shailesh Jadhav, Aarti Juvekar, Jyoti Kode, Manika Pal-Bhadra, Ahmed Kamal
Cancer has been established as the "Emperor of all maladies". In recent years, medicinal chemistry has focused on identifying novel anti-cancer compounds; though discovery of these compounds appears to be a herculean task. In present study, we synthesized forty pyrazolochalcone conjugates and explored their cytotoxic activity against a panel of sixty cancer cell lines. Fifteen conjugates of the series showed excellent growth inhibition (13b-e, 13h-j, 14c-d, 15 a, 15 c-d, 16b, 16d and 18f; GI50 for MCF-7: 0...
July 25, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28802072/fifty-years-of-benz-oxaphospholene-chemistry
#16
Jan Berton, Thomas Heugebaert, David Virieux, Chris Victor Stevens
The first synthesis of benzoxaphospholenes dates back to the 60s. Since then, the structural variety of reported (benz)oxaphospholenes has steadily increased. Organophosphorus compounds have caught the interest of synthetic chemists for a couple of decades now because of their interesting biological properties. Oxaphospholenes, in particular, could serve as carbohydrate mimetics, while benzoxaphospholenes have been reported to possess bactericidal, insecticidal, herbicidal and fungistatical properties. Transesterification reactions and addition of phosphorus nucleophiles to carbonyl compounds were reaction types that led to the production of the first (benz)oxaphospholenes...
August 12, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28799716/rational-design-of-membrane-pore-forming-peptides
#17
Max Pillong, Jan A Hiss, Petra Schneider, Yen-Chu Lin, Gernot Posselt, Bernhard Pfeiffer, Markus Blatter, Alex T Müller, Simon Bachler, Claudia S Neuhaus, Petra S Dittrich, Karl-Heinz Altmann, Silja Wessler, Gisbert Schneider
Specific interactions of peptides with lipid membranes are essential for cellular communication and constitute a central aspect of the innate host defense against pathogens. A computational method for generating innovative membrane-pore-forming peptides inspired by natural templates is presented. Peptide representation in terms of sequence- and topology-dependent hydrophobic moments is introduced. This design concept proves to be appropriate for the de novo generation of first-in-class membrane-active peptides with the anticipated mode of action...
August 11, 2017: Small
https://www.readbyqxmd.com/read/28799656/review-of-the-effects-of-manufactured-nanoparticles-on-mammalian-target-organs
#18
REVIEW
Tianshu Wu, Meng Tang
Nanotechnology had matured significantly during the last two decades as it has transitioned from bench top science to applied technology. Even though the issue of safety of nanotechnology has been raised nearly one decade ago, the rapid progress in development and use of nanomaterials has not yet been matched by toxicological investigations. Many recent studies have simply outlined the toxic effects of nanoparticles (NPs), but few have systematically addressed their potentially adverse biological effects on target organs...
August 11, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/28799500/editorial-impact-of-biological-science-to-medicinal-chemistry
#19
EDITORIAL
Guo-Ping Zhou
No abstract text is available yet for this article.
2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28798211/do-biology-students-really-hate-math-empirical-insights-into-undergraduate-life-science-majors-emotions-about-mathematics
#20
Lucas P Wachsmuth, Christopher R Runyon, John M Drake, Erin L Dolan
Undergraduate life science majors are reputed to have negative emotions toward mathematics, yet little empirical evidence supports this. We sought to compare emotions of majors in the life sciences versus other natural sciences and math. We adapted the Attitudes toward the Subject of Chemistry Inventory to create an Attitudes toward the Subject of Mathematics Inventory (ASMI). We collected data from 359 science and math majors at two research universities and conducted a series of statistical tests that indicated that four AMSI items comprised a reasonable measure of students' emotional satisfaction with math...
2017: CBE Life Sciences Education
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