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Protein design

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https://www.readbyqxmd.com/read/28644986/designing-novel-inhibitors-against-histone-acetyltransferase-hat-%C3%A2-gcn5-of-plasmodium-falciparum
#1
Amarjeet Kumar, Krishanu Bhowmick, Kunwar Somesh Vikramdeo, Neelima Mondal, Naidu Subbarao, Suman Kumar Dhar
During active proliferation phase of intra-erythrocytic cycle, the genome of P. falciparum is regulated epigenetically and evolutionary conserved parasite-specific histone proteins are extensively acetylated. The reversible process of lysine acetylation, causing transcriptional activation and its deacetylation, causing transcriptional repression is regulated by balanced activities of HATs and HDACs. They are also known to regulate antigenic variations and gametocytic conversion in P. falciparum. These histone modifying enzymes have been identified as potential targets for development of anitmalarials in literature...
June 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28644853/the-novel-phospholipid-mimetic-kpc34-is-highly-active-against-preclinical-models-of-philadelphia-chromosome-positive-acute-lymphoblastic-leukemia
#2
Peter M Alexander, David L Caudell, Gregory L Kucera, Kristin M Pladna, Timothy S Pardee
Philadelphia chromosome positive B cell acute lymphoblastic leukemia (Ph+ ALL) is an aggressive cancer of the bone marrow. The addition of tyrosine kinase inhibitors (TKIs) has improved outcomes but many patients still suffer relapse and novel therapeutic agents are needed. KPC34 is an orally available, novel phospholipid conjugate of gemcitabine, rationally designed to overcome multiple mechanisms of resistance, inhibit the classical and novel isoforms of protein kinase C, is able to cross the blood brain barrier and is orally bioavailable...
2017: PloS One
https://www.readbyqxmd.com/read/28644732/lipophilicity-and-biomimetic-properties-to-support-drug-discovery
#3
Fotios Tsopelas, Constantinos Giaginis, Anna Tsantili-Kakoulidou
Lipophilicity, expressed as the octanol-water partition coefficient, constitutes the most important property in drug action, influencing both pharmacokinetic and pharmacodynamics processes as well as drug toxicity. On the other hand, biomimetic properties defined as the retention outcome on HPLC columns containing a biological relevant agent, provide a considerable advance for rapid experimental -based estimation of ADME properties in early drug discovery stages. Areas covered: This review highlights the paramount importance of lipophilicity in almost all aspects of drug action and safety...
June 23, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28644630/expanding-the-therapeutic-potential-of-the-iron-chelator-deferasirox-in-the-development-of-aqueous-stable-ti-iv-anticancer-complexes
#4
Sergio A Loza-Rosas, Alexandra M Vázquez-Salgado, Kennett I Rivero, Lenny J Negrón, Yamixa Delgado, Josué A Benjamín-Rivera, Angel L Vázquez-Maldonado, Timothy B Parks, Charlene Munet-Colón, Arthur D Tinoco
The recent X-ray structure of titanium(IV)-bound human serum transferrin (STf) exhibiting citrate as a synergistic anion reveals a difference in Ti(IV) coordination versus iron(III), the metal endogenously delivered by the protein to cells. This finding enriches our bioinspired drug design strategy for Ti(IV)-based anticancer therapeutics, which applies a family of Fe(III) chelators termed chemical transferrin mimetic (cTfm) ligands to inhibit Fe bioavailability in cancer cells. Deferasirox, a drug used for iron overload disease, is a cTfm ligand that models STf coordination to Fe(III), favoring Fe(III) binding versus Ti(IV)...
June 23, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28644609/galnac-tyrosine-is-a-ligand-of-plant-lectins-antibodies-and-human-and-murine-macrophage-galactose-type-lectins
#5
Ruslan Gibadullin, David Wayne Farnsworth, Joseph J Barchi, Jeffrey C Gildersleeve
In 2011, a new type of protein O-glycosylation was discovered in which N-acetylgalactosamine is attached to the side chain of tyrosine (GalNAc-Tyr). While present on dozens of proteins, the biological roles of GalNAc-Tyr are unknown. To gain insight into this new type of modification, we synthesized a group of GalNAc-Tyr glycopeptides, constructed microarrays, and evaluated potential recognition of GalNAc-Tyr by a series of glycan-binding proteins. Through a series of >150 microarray experiments, we assessed binding properties of a variety of plant lectins, monoclonal antibodies, and endogenous lectins...
June 23, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28644390/the-electrosome-a-surface-displayed-enzymatic-cascade-in-a-biofuel-cell-s-anode-and-a-high-density-surface-displayed-biocathodic-enzyme
#6
Alon Szczupak, Dror Aizik, Sarah Moraïs, Yael Vazana, Yoav Barak, Edward A Bayer, Lital Alfonta
The limitation of surface-display systems in biofuel cells to a single redox enzyme is a major drawback of hybrid biofuel cells, resulting in a low copy-number of enzymes per yeast cell and a limitation in displaying enzymatic cascades. Here we present the electrosome, a novel surface-display system based on the specific interaction between the cellulosomal scaffoldin protein and a cascade of redox enzymes that allows multiple electron-release by fuel oxidation. The electrosome is composed of two compartments: (i) a hybrid anode, which consists of dockerin-containing enzymes attached specifically to cohesin sites in the scaffoldin to assemble an ethanol oxidation cascade, and (ii) a hybrid cathode, which consists of a dockerin-containing oxygen-reducing enzyme attached in multiple copies to the cohesin-bearing scaffoldin...
June 23, 2017: Nanomaterials
https://www.readbyqxmd.com/read/28644022/hot-spot-residues-to-be-mutated-common-in-g-protein-coupled-receptors-of-class-a-identification-of-thermostabilizing-mutations-followed-by-determination-of-three-dimensional-structures-for-two-example-receptors
#7
Satoshi Yasuda, Yuta Kajiwara, Yosuke Toyoda, Kazushi Morimoto, Ryoji Suno, So Iwata, Takuya Kobayashi, Takeshi Murata, Masahiro Kinoshita
G protein-coupled receptors (GPCRs), which are indispensable to life and also implicated in a number of diseases, construct important drug targets. For the efficient structure-guided drug design, however, their structural stabilities must be enhanced. An amino-acid mutation is known to possibly lead to the enhancement, but currently available experimental and theoretical methods for identifying stabilizing mutations suffer such drawbacks as the incapability of exploring the whole mutational space with minor effort and the unambiguous physical origin of the enhanced or lowered stability...
June 23, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28644007/cyclotides-as-tools-in-chemical-biology
#8
Simon J de Veer, Joachim Weidmann, David J Craik
Among the various molecules that plants produce for defense against pests and pathogens, cyclotides stand out as exceptionally stable and structurally unique. These ribosomally synthesized peptides are around 30 amino acids in size, and are stabilized by a head-to-tail cyclic peptide backbone and three disulfide bonds that form a cystine knot. They occur in certain plants of the Rubiaceae, Violaceae, Cucurbitaceae, Fabaceae, and Solanaceae families, with an individual plant producing up to hundreds of different cyclotides...
June 23, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28643574/stability-and-in-vitro-release-behaviour-of-encapsulated-omega-fatty-acid-rich-oils-in-lentil-protein-isolate-based-microcapsules
#9
C Chang, M T Nickerson
The objective of this study was to investigate the use of a lentil protein isolate-based microcapsule design as a platform for entrapping different types of omega fatty acid-rich oil (e.g. canola, fish and flaxseed oils) and to characterise differences in the physical properties (e.g. moisture content, water activity, colour, wettability, particle size, surface oil and entrapment efficiency), storage stability and in vitro release behaviour of the entrapped oils. All microcapsules displayed similar physical properties regardless of the core material...
June 23, 2017: International Journal of Food Sciences and Nutrition
https://www.readbyqxmd.com/read/28643392/retroviruses-and-microtubule-associated-motor-proteins
#10
REVIEW
Gloria Arriagada
Retroviruses are obligate intracellular parasites of eukaryotic cells. After reverse transcription, the viral DNA contained in the preintegration complex (PIC) is delivered to the nucleus of the host cell, where it integrates. Before reaching the nucleus, the incoming particle and the PIC must travel throughout the cytoplasm. Likewise the newly synthesized viral proteins and viral particles must transit the cytoplasm during exit. The cytoplasm is a crowded environment and simple diffusion is difficult. Therefore, viruses have evolved to utilize the cellular mechanisms of movement through the cytoplasm, where microtubules are the roads, and the ATP dependent motors dynein and kinesin are the vehicles for retrograde and anterograde trafficking...
June 22, 2017: Cellular Microbiology
https://www.readbyqxmd.com/read/28643382/synthesis-and-biological-evaluation-of-arginyl-diosgenin-conjugate-as-a-potential-bone-tissue-engineering-agent
#11
Ai-Mei Liao, Hana Jung, Ji Won Yu, Dong Hee Lee, Sang-Soo Park, Bangrong Cai, ChangJu Chun
Water-soluble arginyl-diosgenin (Arg-DG) conjugate was designed, synthesized, and evaluated for a biological activity. The Arg-DG conjugate was characterized using FT-IR, (1) H NMR, (13) C NMR, and HPLC-MS analyses, followed by a biological activity evaluation. Compared with DG, the Arg-DG conjugate showed a decreased cytotoxicity against L929 cells and an increased anti-proliferative activity against hepatocellular cells. The safety of the Arg-DG conjugate was confirmed using the highly sensitive Alamar Blue assay, which indicated that it increased the cellular metabolic activity at suitable concentrations...
June 23, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28643248/computational-prediction-of-crispr-cas9-target-sites-reveals-potential-off-target-risks-in-human-and-mouse
#12
Qingbo Wang, Kumiko Ui-Tei
The clustered regularly interspaced short palindromic repeat (CRISPR)/CRISPR-associated (Cas) system is a prominent genome engineering technology. In the CRISPR/Cas system, the RNA-guided endonuclease Cas protein introduces a DNA double-stranded break at the genome position recognized by a guide RNA (gRNA) based on complementary base-pairing of about 20-nucleotides in length. The 8- or 12-mer gRNA sequence in the proximal region is especially important for target recognition, and the genes with sequence complementarity to such regions are often disrupted...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28643233/assessing-environmental-exposure-to-%C3%AE-n-methylamino-l-alanine-bmaa-in-complex-sample-matrices-a-comparison-of-the-three-most-popular-lc-ms-ms-methods
#13
Teesha C Baker, Fiona J M Tymm, Susan J Murch
β-N-Methylamino-L-alanine (BMAA) is a naturally occurring non-protein amino acid produced by cyanobacteria, accumulated through natural food webs, found in mammalian brain tissues. Recent evidence indicates an association between BMAA and neurological disease. The accurate detection and quantification of BMAA in food and environmental samples are critical to understanding BMAA metabolism and limiting human exposure. To date, there have been more than 78 reports on BMAA in cyanobacteria and human samples, but different methods give conflicting data and divergent interpretations in the literature...
June 22, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/28643139/cysteamine-revisited-repair-of-arginine-to-cysteine-mutations
#14
REVIEW
L Gallego-Villar, L Hannibal, J Häberle, B Thöny, T Ben-Omran, G K Nasrallah, Al-N Dewik, W D Kruger, H J Blom
Cysteamine is a small aminothiol endogenously derived from coenzyme A degradation. For some decades, synthetic cysteamine has been employed for the treatment of cystinosis, and new uses of the drug continue to emerge. In this review, we discuss the role of cysteamine in cellular and extracellular homeostasis and focus on the potential use of aminothiols to reconstitute the function of proteins harboring arginine (Arg) to cysteine (Cys) mutations, via repair of the Cys residue into a moiety that introduces an amino group, as seen in basic amino acid residues Lys and Arg...
June 22, 2017: Journal of Inherited Metabolic Disease
https://www.readbyqxmd.com/read/28643003/recent-developments-in-solution-nuclear-magnetic-resonance-nmr-based-molecular-biology
#15
REVIEW
Joshua J Ziarek, Diego Baptista, Gerhard Wagner
Visualizing post-translational modifications, conformations, and interaction surfaces of protein structures at atomic resolution underpins the development of novel therapeutics to combat disease. As computational resources expand, in silico calculations coupled with experimentally derived structures and functional assays have led to an explosion in structure-based drug design (SBDD) with several compounds in clinical trials. It is increasingly clear that "hidden" transition-state structures along activation trajectories can be harnessed to develop novel classes of allosteric inhibitors...
June 23, 2017: Journal of Molecular Medicine: Official Organ of the "Gesellschaft Deutscher Naturforscher und Ärzte"
https://www.readbyqxmd.com/read/28642758/time-and-antigen-stimulation-history-influence-memory-cd8-t-cell-bystander-responses
#16
Matthew D Martin, Qiang Shan, Hai-Hui Xue, Vladimir P Badovinac
Memory CD8 T cells can be activated and induced to produce cytokines and increase stores of cytolytic proteins not only in response to cognate antigen (Ag) but also in response to inflammatory cytokines (bystander responses). Importantly, bystander memory CD8 T cell functions have been shown to be dependent upon memory CD8 T cell fitness, since exhausted CD8 T cells have diminished capacity to respond to inflammatory cues. While it is known that memory CD8 T cell functional abilities, including ability to produce cytokines in response to cognate Ag, change with time after initial Ag encounter and upon multiple Ag stimulations (e...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28642475/a-novel-bzip-protein-gsb1-is-required-for-oxidative-stress-response-mating-and-virulence-in-the-human-pathogen-cryptococcus-neoformans
#17
Seon Ah Cheon, Eun Jung Thak, Yong-Sun Bahn, Hyun Ah Kang
The human pathogen Cryptococcus neoformans, which causes life-threatening meningoencephalitis in immunocompromised individuals, normally faces diverse stresses in the human host. Here, we report that a novel, basic, leucine-zipper (bZIP) protein, designated Gsb1 (general stress-related bZIP protein 1), is required for its normal growth and diverse stress responses. C. neoformans gsb1Δ mutants grew slowly even under non-stressed conditions and showed increased sensitivity to high or low temperatures. The hypersensitivity of gsb1Δ to oxidative and nitrosative stresses was reversed by addition of a ROS scavenger...
June 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28642439/assembly-principles-and-structure-of-a-6-5-mda-bacterial-microcompartment-shell
#18
Markus Sutter, Basil Greber, Clement Aussignargues, Cheryl A Kerfeld
Many bacteria contain primitive organelles composed entirely of protein. These bacterial microcompartments share a common architecture of an enzymatic core encapsulated in a selectively permeable protein shell; prominent examples include the carboxysome for CO2 fixation and catabolic microcompartments found in many pathogenic microbes. The shell sequesters enzymatic reactions from the cytosol, analogous to the lipid-based membrane of eukaryotic organelles. Despite available structural information for single building blocks, the principles of shell assembly have remained elusive...
June 23, 2017: Science
https://www.readbyqxmd.com/read/28642082/clinical-trial-of-the-effects-of-vitamin-d-supplementation-on-psychological-symptoms-and-metabolic-profiles-in-maintenance-methadone-treatment-patients
#19
Amir Ghaderi, Hamid Reza Banafshe, Maryam Motmaen, Morad Rasouli-Azad, Fereshteh Bahmani, Zatollah Asemi
BACKGROUND: Vitamin D deficiency may be associated with some complications including nonspecific musculoskeletal pain and periodontal disease in maintenance methadone treatment (MMT) patients. This study was designed to determine the effect of vitamin D supplementation on psychological symptoms and metabolic profiles in MMT patients. METHODS: This randomized, double-blind, placebo-controlled, clinical trial was carried out among 68 MMT patients. Participants were randomly allocated to receive either 50,000IU vitamin D supplements (n=34) or placebo (n=34) every 2weeks for 12weeks...
June 19, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28641563/pentapeptide-prosequence-enhances-expression-and-structure-folding-of-recombinant-thermomyces-lanuginosus-lipase-in-pichia-pastoris
#20
Haiying Cai, Minjie Zhao, Yang Li, Jianwei Mao, Chenggang Cai, Fengqin Feng
Propeptides have been demonstrated to influence many properties of their mature proteins as intramolecular chaperones. In our study, the role of pentapeptide prosequence of Thermomyces lanuginosus lipase (TLL) was determined through its effect on the recombinant expression of TLL in P. pastoris. The result showed that the average lipase activity of recombinant strains GS-pTL reached 434.32 U/mL, higher than that of GS-TL 377.71 U/mL, indicating that the propeptide "SPIRR-" sequence is beneficial for enhancing TLL expression...
June 21, 2017: Protein and Peptide Letters
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