14,990 results match your criteria Bioorganic & medicinal chemistry[Journal]


TSC2 pathogenic variants are predictive of severe clinical manifestations in TSC infants: results of the EPISTOP study.

Genet Med 2020 May 28. Epub 2020 May 28.

Department of Medicine, Brigham and Women's Hospital, Boston, MA, USA.

Purpose: To perform comprehensive genotyping of TSC1 and TSC2 in a cohort of 94 infants with tuberous sclerosis complex (TSC) and correlate with clinical manifestations.

Methods: Infants were enrolled at age <4 months, and subject to intensive clinical monitoring including electroencephalography (EEG), brain magnetic resonance imaging (MRI), and neuropsychological assessment. Targeted massively parallel sequencing (MPS), genome sequencing, and multiplex ligation-dependent probe amplification (MLPA) were used for variant detection in TSC1/TSC2. Read More

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http://dx.doi.org/10.1038/s41436-020-0823-4DOI Listing

Author Correction: Identification of a binding protein for sesamin and characterization of its roles in plant growth.

Sci Rep 2020 May 28;10(1):8987. Epub 2020 May 28.

Bioorganic Research Institute, Suntory Foundation for Life Sciences (SUNBOR), 8-1-1 Seikadai, Seika, Soraku, Kyoto, 619-0284, Japan.

An amendment to this paper has been published and can be accessed via a link at the top of the paper. Read More

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http://dx.doi.org/10.1038/s41598-020-66086-7DOI Listing

TASK-3: New Target for Pain-Relief.

Neurosci Bull 2020 May 26. Epub 2020 May 26.

International Collaborative Centre on Big Science Plan for Purine Signaling, Chengdu University of Traditional Chinese Medicine, Chengdu, 610075, China.

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http://dx.doi.org/10.1007/s12264-020-00516-4DOI Listing

Local Overheating of Biotissue Labeled With Upconversion Nanoparticles Under Yb Resonance Excitation.

Front Chem 2020 8;8:295. Epub 2020 May 8.

Scientific Research Center "Crystallography and Photonics," Russian Academy of Sciences, Moscow, Russia.

Local overheating of biotissue is a critical step for biomedical applications, such as photothermal therapy, enhancement of vascular permeability, remote control of drug release, and so on. Overheating of biological tissue when exposed to light is usually realized by utilizing the materials with a high-absorption cross section (gold, silica, carbon nanoparticles, etc.). Read More

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http://dx.doi.org/10.3389/fchem.2020.00295DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7225365PMC

Measuring Intratumoral Heterogeneity of Immune Repertoires.

Front Oncol 2020 8;10:512. Epub 2020 May 8.

Laboratory of Genomics of Antitumor Adaptive Immunity, Privolzhsky Research Medical University, Nizhny Novgorod, Russia.

There is considerable clinical and fundamental value in measuring the clonal heterogeneity of T and B cell expansions in tumors and tumor-associated lymphoid structures-along with the associated heterogeneity of the tumor neoantigen landscape-but such analyses remain challenging to perform. Here, we propose a straightforward approach to analyze the heterogeneity of immune repertoires between different tissue sections in a quantitative and controlled way, based on a beta-binomial noise model trained on control replicates obtained at the level of single-cell suspensions. This approach allows to identify local clonal expansions with high accuracy. Read More

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http://dx.doi.org/10.3389/fonc.2020.00512DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7227437PMC

New insights into ligand binding by plant lipid transfer proteins: A case study of the lentil Lc-LTP2.

Biochem Biophys Res Commun 2020 May 23. Epub 2020 May 23.

M.M. Shemyakin and Yu.A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya str., 16/10, 117997, Moscow, Russia. Electronic address:

Lipid transfer proteins (LTPs) are an important class of plant proteins containing an internal cavity and binding hydrophobic ligands. Although LTP structures and functions are well studied, mechanisms of ligand binding remain unclear. Earlier, we discovered the lentil lipid transfer protein Lc-LTP2 capable of binding and transfer various ligands. Read More

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http://dx.doi.org/10.1016/j.bbrc.2020.04.139DOI Listing

Nutrient and Sensory Metabolites Profiling of L. (Starfruit) in the Context of Its Origin and Ripening Stage by GC/MS and Chemometric Analysis.

Molecules 2020 May 22;25(10). Epub 2020 May 22.

Pharmacognosy Department, College of Pharmacy, Cairo University, Kasr El Aini St., P.B. 11562 Cairo, Egypt.

L. is a tropical tree with edible fruit that grows at different climatic conditions. Despite its nutritive value and reported health benefits, it is a controversial fruit owing to its rich oxalate content. Read More

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http://dx.doi.org/10.3390/molecules25102423DOI Listing

Computational Tools and Resources Supporting CRISPR-Cas Experiments.

Cells 2020 May 22;9(5). Epub 2020 May 22.

Department of Genome Engineering, Institute of Bioorganic Chemistry, Polish Academy of Sciences, Noskowskiego 12/14, 61-704 Poznan, Poland.

The CRISPR-Cas system has become a cutting-edge technology that revolutionized genome engineering. The use of Cas9 nuclease is currently the method of choice in most tasks requiring a specific DNA modification. The rapid development in the field of CRISPR-Cas is reflected by the constantly expanding ecosystem of computational tools aimed at facilitating experimental design and result analysis. Read More

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http://dx.doi.org/10.3390/cells9051288DOI Listing

Amaryllidaceae Alkaloids of Belladine-Type from cv. Carlton as New Selective Inhibitors of Butyrylcholinesterase.

Biomolecules 2020 May 22;10(5). Epub 2020 May 22.

ADINACO Research Group, Department of Pharmaceutical Botany, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.

Thirteen known (- and ) and three previously undescribed Amaryllidaceae alkaloids of belladine structural type, named carltonine A-C (-), were isolated from bulbs of cv. Carlton (Amaryllidaceae) by standard chromatographic methods. Compounds isolated in sufficient amounts, and not tested previously, were evaluated for their in vitro acetylcholinesterase (AChE; E. Read More

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http://dx.doi.org/10.3390/biom10050800DOI Listing

Isolation, Characterization and Chemical Synthesis of Large Spectrum Antimicrobial Cyclic Dipeptide (l-leu-l-pro) from V16R3Y1 Bacteria Extracts. A Novel H NMR Metabolomic Approach.

Antibiotics (Basel) 2020 May 21;9(5). Epub 2020 May 21.

LR03ES03, Laboratoire de Microorganismes et Biomolécules Actives, Faculté des Sciences de Tunis, Université Tunis Manar, Tunis 2092, Tunisia.

Streptomyces is the most frequently described genus of Actinomycetes, a producer of biologically active secondary metabolites. Indeed, the Streptomyces species produces about 70% of antibiotics and 60% of antifungal molecules used in agriculture. Our study was carried out with the goal of isolating and identifying antimicrobial secondary metabolites from V16R3Y1 isolated from the date palm rhizosphere (southern Tunisia). Read More

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http://dx.doi.org/10.3390/antibiotics9050270DOI Listing

Cysteine Cathepsins Inhibition Affects Their Expression and Human Renal Cancer Cell Phenotype.

Cancers (Basel) 2020 May 21;12(5). Epub 2020 May 21.

Institute of Molecular Medicine, Sechenov First Moscow State Medical University, 119991 Moscow, Russia.

Renal cancer would greatly benefit from new therapeutic strategies since, in advanced stages, it is refractory to classical chemotherapeutic approaches. In this context, lysosomal protease cysteine cathepsins may represent new pharmacological targets. In renal cancer, they are characterized by a higher expression, and they were shown to play a role in its aggressiveness and spreading. Read More

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http://dx.doi.org/10.3390/cancers12051310DOI Listing

Ticagrelor Exerts Immune-Modulatory Effect by Attenuating Neutrophil Extracellular Traps.

Int J Mol Sci 2020 May 21;21(10). Epub 2020 May 21.

Laboratory of Molecular Hematology, Department of Medicine, Democritus University of Thrace, 68100 Alexandroupolis, Greece.

Neutrophils through the release of neutrophil extracellular traps (NETs) containing active tissue factor (TF) are key components of thrombo-inflammation. Platelets-neutrophils interplay in ST elevation myocardial infarction (STEMI) promotes NET formation via inorganic polyphosphates (polyP) released by thrombin-activated platelets. NETs, however, are also induced by biomaterials in a platelet-independent manner. Read More

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http://dx.doi.org/10.3390/ijms21103625DOI Listing

Effects of Glycyrrhetic Acid on Human Chronic Myelogenous Leukemia Cells.

Turk J Pharm Sci 2020 Feb 19;17(1):49-55. Epub 2020 Feb 19.

Kumamoto University, School of Pharmacy, Department of Bioorganic Medicinal Chemistry, Kumamoto, Japan.

Objectives: Chronic myelogenous leukemia (CML) is a type of blood cancer that is initially treated with imatinib (first Abl kinase inhibitor). However, some patients with CML develop imatinib resistance. Several new generation drugs have been developed, but do not overcome this problem. Read More

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http://dx.doi.org/10.4274/tjps.galenos.2018.49389DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7227864PMC
February 2020

Structure and biological evaluation of pyridine-2-carboxamidine copper(II) complex resulting from N'-(4-nitrophenylsulfonyloxy)2-pyridine-carboxamidoxime.

J Inorg Biochem 2020 Apr 22;208:111085. Epub 2020 Apr 22.

Laboratory of Inorganic Chemistry, Faculty of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Greece. Electronic address:

The interaction of Cu(NO)·3HO with the sulfonyl o-pyridine carboxamidoxime N'-(4-nitrophenylsulfonyloxy)picolinimidamide (L) resulted in the mononuclear complex [Cu(L)](L) (1), where L = pyridine-2-carboxamidine ligand and (L) = 4-nitrobenzenesulfonate anion derived from the homolytic cleavage of the NO bond of L. The complex was characterized by diverse techniques including single-crystal X-ray crystallography. From the antimicrobial tests performed, complex 1 seems to be active against gram-negative bacterial strains. Read More

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http://dx.doi.org/10.1016/j.jinorgbio.2020.111085DOI Listing

Polysomes Bypass a 50 Nucleotide Coding Gap less Efficiently than Monosomes Due to Attenuation of a 5' mRNA Stem Loop and Enhanced Drop-off.

J Mol Biol 2020 May 23. Epub 2020 May 23.

School of Biochemistry, University College Cork, Western Gateway Building, Western Road, Cork, T12 YT57, Ireland; School of Microbiology, University College Cork, Western Gateway Building, Western Road, Cork, T12 YT57, Ireland; Department of Human Genetics, University of Utah, Salt Lake City, UT 84112-5330, USA. Electronic address:

Efficient translational bypassing of a 50 nt non-coding gap in a phage T4 topoisomerase subunit gene (gp60) requires several recoding signals. Here we investigate the function of the mRNA stem loop 5' of the take-off codon, as well as the importance of ribosome loading density on the mRNA for efficient bypassing. We show that polysomes are less efficient at mediating bypassing than monosomes, both in vitro and in vivo, due to their preventing formation of a stem loop 5' of the take-off codon and allowing greater peptidyl-tRNA drop off. Read More

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http://dx.doi.org/10.1016/j.jmb.2020.05.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7245268PMC

Laser-induced formation of "craters" and "hills" in azobenzene-containing polymethacrylate films.

Soft Matter 2020 May 26. Epub 2020 May 26.

Institute of Physics, The Czech Academy of Sciences, 182 21 Prague 8, Czech Republic.

Functional organic polymer materials with an ability to change their surface topography in response to external contactless stimuli, like light irradiation, have attracted considerable attention. This work is devoted to the study of contactless control of the surface topography and the formation of the surface features in the amorphousized and liquid crystalline films of two azobenzene-containing polymers. The investigated polymers are side-chain polymethacrylates containing azobenzene chromophores with two lateral methyl substituents in ortho-positions and differing in the length of flexible spacer with six and ten methylene units. Read More

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http://dx.doi.org/10.1039/d0sm00601gDOI Listing

FAK-targeting PROTAC as a chemical tool for the investigation of non-enzymatic FAK function in mice.

Protein Cell 2020 May 25. Epub 2020 May 25.

MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University, Beijing, 100084, China.

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http://dx.doi.org/10.1007/s13238-020-00732-8DOI Listing

FAD-dependent enzyme-catalysed intermolecular [4+2] cycloaddition in natural product biosynthesis.

Nat Chem 2020 May 25. Epub 2020 May 25.

Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Synthetic and Functional Biomolecules Center, and Peking-Tsinghua Center for Life Sciences, Peking University, Beijing, China.

The Diels-Alder reaction is one of the most powerful and widely used methods in synthetic chemistry for the stereospecific construction of carbon-carbon bonds. Despite the importance of Diels-Alder reactions in the biosynthesis of numerous secondary metabolites, no naturally occurring stand-alone Diels-Alderase has been demonstrated to catalyse intermolecular Diels-Alder transformations. Here we report a flavin adenine dinucleotide-dependent enzyme, Morus alba Diels-Alderase (MaDA), from Morus cell cultures, that catalyses an intermolecular [4+2] cycloaddition to produce the natural isoprenylated flavonoid chalcomoracin with a high efficiency and enantioselectivity. Read More

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http://dx.doi.org/10.1038/s41557-020-0467-7DOI Listing

Functionalized aromatic esters of the Amaryllidaceae alkaloid haemanthamine and their in vitro and in silico biological activity connected to Alzheimer's disease.

Bioorg Chem 2020 May 17;100:103928. Epub 2020 May 17.

ADINACO Research Group, Department of Pharmaceutical Botany, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic. Electronic address:

A novel series of aromatic esters (1a-1m) related to the Amaryllidaceae alkaloid (AA) haemanthamine were designed, synthesized and tested in vitro with particular emphasis on the treatment of neurodegenerative diseases. Some of the synthesized compounds revealed promising acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory profile. Significant human AChE (hAChE) inhibition was demonstrated by 11-O-(3-nitrobenzoyl)haemanthamine (1j) with ICvalue of 4. Read More

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http://dx.doi.org/10.1016/j.bioorg.2020.103928DOI Listing

Regulation of the p53 expression profile by hnRNP K under stress conditions.

RNA Biol 2020 May 23. Epub 2020 May 23.

Institute of Bioorganic Chemistry, Polish Academy of Sciences , Noskowskiego 12/14, 61-704 Poznan, Poland.

The p53 protein is one of the transcription factors responsible for cell cycle regulation and prevention of cancer development. Its expression is regulated at the transcriptional, translational and post-translational levels. Recent years of research have shown that the 5' terminus of p53 mRNA plays an important role in this regulation. Read More

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http://dx.doi.org/10.1080/15476286.2020.1771944DOI Listing

2-(3-Hydroxy-5-phosphonooxymethyl-2-methyl-4-pyridyl)-1,3-thiazolidine-4-carboxylic Acid, Novel Metabolite of Pyridoxal 5'-Phosphate and Cysteine Is Present in Human Plasma-Chromatographic Investigations.

Int J Mol Sci 2020 May 18;21(10). Epub 2020 May 18.

Department of Environmental Chemistry, Faculty of Chemistry, University of Lodz, 163 Pomorska Str., 90-236 Łódź, Poland.

It is well-established that aminothiols, to which cysteine (Cys) belongs, are highly reactive towards aldehydes in an aqueous environment, forming substituted thiazolidine carboxylic acids. This report provides evidence that formation of the product containing a thiazolidine ring through non-enzymatic condensation of Cys and an active form of vitamin B6 pyridoxal 5'-phosphate (PLP) occurs in vivo in humans. To prove this point, a new method, based on a gas chromatography coupled with mass spectrometry (GC-MS), has been designed to identify and quantify Cys and PLP adduct, 2-(3-hydroxy-5-phosphonooxymethyl-2-methyl-4-pyridyl)-1,3-thiazolidine-4-carboxylic acid (HPPTCA) in human plasma. Read More

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http://dx.doi.org/10.3390/ijms21103548DOI Listing

Structure and in vitro Bioactivity against Cancer Cells of the Capsular Polysaccharide from the Marine Bacterium Psychrobacter .

Mar Drugs 2020 May 19;18(5). Epub 2020 May 19.

G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch, Russian Academy of Sciences, 159/2, Prospect 100 let Vladivostoku, 690022 Vladivostok, Russia.

Psychrobacter KMM 277 is a psychrophilic Gram-negative bacterium that has been isolated from the internal tissues of an ascidian sp. Here, we report the structure of the capsular polysaccharide from P. KMM 277 and its effect on the viability and colony formation of human acute promyelocytic leukemia HL-60 cells. Read More

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http://dx.doi.org/10.3390/md18050268DOI Listing

Autologous adipose tissue injection versus platelet-rich plasma (PRP) injection in the treatment of knee osteoarthritis: a randomized, controlled study - study protocol.

BMC Musculoskelet Disord 2020 May 20;21(1):314. Epub 2020 May 20.

Department of Orthopedic Surgery, Rehasport Clinic, Poznan, Poland.

Background: Knee osteoarthritis (OA) is a common, chronic, progressive and degenerative disease which affects patients' quality of life and may cause disability and social isolation. OA is a huge economic burden for the patient and a large strain for the whole healthcare system. Articular cartilage has a small potential to repair, with progressively more clinicians emphasizing cellular therapy. Read More

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http://dx.doi.org/10.1186/s12891-020-03345-8DOI Listing

Biological macromolecule binding and anticancer activity of synthetic alkyne-containing L-phenylalanine derivatives.

Amino Acids 2020 May 19;52(5):755-769. Epub 2020 May 19.

Istituto di Biostrutture e Bioimmagini, IBB-CNR, Via Mezzocannone 16, 80134, Naples, Italy.

Herein, we described the synthesis of two L-phenylalanines α-derivatized with a terminal alkyne moiety whose structures differed by phenyl ring halogen substitution (two o-Cl in 1 vs. one p-Br in 2) and investigated their effect on biological macromolecules and living cells. We explored their interaction with quadruplex DNA (G4 DNA), using tel and c-myc as models, and bovine serum albumin (BSA). Read More

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http://dx.doi.org/10.1007/s00726-020-02849-wDOI Listing

New Conjugates of Polyhydroxysteroids with Long-Chain Fatty Acids from the Deep-Water Far Eastern Starfish and Their Anticancer Activity.

Mar Drugs 2020 May 15;18(5). Epub 2020 May 15.

G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Sciences, Pr. 100-let Vladivostoku 159, 690022 Vladivostok, Russia.

Four new conjugates, esters of polyhydroxysteroids with long-chain fatty acids (-), were isolated from the deep-water Far Eastern starfish Ceramaster patagonicus The structures of - were established by NMR and ESIMS techniques as well as chemical transformations. Unusual compounds - contain the same 5α-cholestane-3β,6β,15α,16β,26-pentahydroxysteroidal moiety and differ from each other in the fatty acid units: 5'Z,11'Z-octadecadienoic (), 11'Z-octadecenoic (), 5'Z,11'Z-eicosadienoic (), and 7'Z-eicosenoic () acids. Previously, only one such steroid conjugate with a fatty acid was known from starfish. Read More

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http://dx.doi.org/10.3390/md18050260DOI Listing

Marine Polyhydroxynaphthoquinone, Echinochrome A: Prevention of Atherosclerotic Inflammation and Probable Molecular Targets.

J Clin Med 2020 May 15;9(5). Epub 2020 May 15.

G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science, 159 Prospect 100-letiya Vladivostoka, Vladivostok 690022, Russia.

The effect of low doses of echinochrome A (EchA), a natural polyhydroxy-1,4-naphthoquinone pigment from the sea urchin , has been studied in clinical trials, when it was used as an active substance of the drug Histochrome and biologically active supplement Thymarin. Several parameters of lipid metabolism, antioxidant status, and the state of the immune system were analyzed in patients with cardiovascular diseases (CVD), including contaminating atherosclerosis. It has been shown that EchA effectively normalizes lipid metabolism, recovers antioxidant status and reduces atherosclerotic inflammation, regardless of the method of these preparations' administrations. Read More

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http://dx.doi.org/10.3390/jcm9051494DOI Listing

Screening Snake Venoms for Toxicity to Revealed Anti-Protozoan Activity of Cobra Cytotoxins.

Toxins (Basel) 2020 May 15;12(5). Epub 2020 May 15.

Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, ul. Miklukho-Maklaya 16/10, Moscow 117997, Russia.

Snake venoms possess lethal activities against different organisms, ranging from bacteria to higher vertebrates. Several venoms were shown to be active against protozoa, however, data about the anti-protozoan activity of cobra and viper venoms are very scarce. We tested the effects of venoms from several snake species on the ciliate . Read More

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http://dx.doi.org/10.3390/toxins12050325DOI Listing

Translation at first sight: the influence of leading codons.

Nucleic Acids Res 2020 May 19. Epub 2020 May 19.

Skolkovo Institute of Science and Technology, Skolkovo, Moscow region 143025, Russia.

First triplets of mRNA coding region affect the yield of translation. We have applied the flowseq method to analyze >30 000 variants of the codons 2-11 of the fluorescent protein reporter to identify factors affecting the protein synthesis. While the negative influence of mRNA secondary structure on translation has been confirmed, a positive role of rare codons at the beginning of a coding sequence for gene expression has not been observed. Read More

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http://dx.doi.org/10.1093/nar/gkaa430DOI Listing

A Ferritin-Albumin-Cu Nanoparticle that Efficaciously Delivers Copper(II) Ions to a Tumor and Improves the Therapeutic Efficacy of Disulfiram.

ACS Omega 2020 May 1;5(18):10415-10422. Epub 2020 May 1.

Synthetic and Functional Biomolecules Center, Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Molecular Engineering, Innovation Center for Genomics, Peking University, Beijing 100871, China.

The application of disulfiram can be traced back to the 1920s, from when it was utilized to facilitate alcohol abstinence by producing allergic reactions toward alcohol. In previous research, combination of disulfiram and copper ions has demonstrated significant anti-tumor activity. However, both disulfiram and copper ions lack the ability of specific targeting to tumor tissues and may lead to a high risk of side effects, especially for copper ion, which is a kind of toxic heavy metal. Read More

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http://dx.doi.org/10.1021/acsomega.0c00293DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7226858PMC

Calcium Carbonate Addition Improves L-Methionine Biosynthesis by Metabolically Engineered W3110-BL.

Front Bioeng Biotechnol 2020 24;8:300. Epub 2020 Apr 24.

Key Laboratory of Bioorganic Synthesis of Zhejiang Province, College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou, China.

L-Methionine (L-Met) is a sulfur-containing amino acid, which is one of the eight essential amino acids to human body. In this work, the fermentative production of L-Met with genetically engineered W3110-BL in a 5-L fermentor was enhanced through supplement of Ca into the fermentation medium. With the addition of 30 g/L calcium carbonate (CaCO), the titer of L-Met and yield against glucose reached 1. Read More

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http://dx.doi.org/10.3389/fbioe.2020.00300DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7212366PMC

A adenosine receptor antagonists: From caffeine to selective non-xanthines.

Br J Pharmacol 2020 May 18. Epub 2020 May 18.

Department of Cell and Molecular Biology, Science for Life Laboratory, Uppsala University, SE-75124, Uppsala, Sweden.

A long evolution of knowledge of the psychostimulant caffeine, led in the 1960s to another purine natural product, adenosine and its A adenosine receptor (A AR). Adenosine is a short-lived autocrine/paracrine mediator that acts pharmacologically at four ARs in a manner opposite to pan-antagonist caffeine and serves as an endogenous allostatic regulator. Although detrimental in the developing brain, caffeine appears to be cerebroprotective in aging. Read More

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http://dx.doi.org/10.1111/bph.15103DOI Listing
May 2020
4.842 Impact Factor

Selected arylsulphonyl pyrazole derivatives as potential Chk1 kinase ligands-computational investigations.

J Mol Model 2020 May 18;26(6):144. Epub 2020 May 18.

Chair and Department of Organic Chemistry, Faculty of Pharmacy, Poznan University of Medical Sciences, ul. Grunwaldzka 6, 60-780, Poznan, Poland.

Protein kinases control diversity of biochemical processes in human organism. Checkpoint 1 kinase (Chk1) is an important element of the checkpoint signalling pathways and is responsible for DNA damage repair. Hence, this kinase plays an essential role in cancer cells survival and has become an important target for anticancer agents. Read More

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http://dx.doi.org/10.1007/s00894-020-04407-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7235069PMC

Structural insights into the inhibition mechanism of human sterol O-acyltransferase 1 by a competitive inhibitor.

Nat Commun 2020 May 18;11(1):2478. Epub 2020 May 18.

State Key Laboratory of Membrane Biology, Institute of Molecular Medicine, Peking University, Beijing Key Laboratory of Cardiometabolic Molecular Medicine, 100871, Beijing, China.

Sterol O-acyltransferase 1 (SOAT1) is an endoplasmic reticulum (ER) resident, multi-transmembrane enzyme that belongs to the membrane-bound O-acyltransferase (MBOAT) family. It catalyzes the esterification of cholesterol to generate cholesteryl esters for cholesterol storage. SOAT1 is a target to treat several human diseases. Read More

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http://dx.doi.org/10.1038/s41467-020-16288-4DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7234994PMC

HLA-DR-expressing NK cells: Effective killers suspected for antigen presentation.

J Leukoc Biol 2020 May 18. Epub 2020 May 18.

Laboratory of Cell Interactions, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Moscow, Russia.

HLA-DR-expressing cells comprise an intriguing group of NK cells, which combine phenotypic characteristics of both NK cells and dendritic cells. These cells can be found in humans and mice; they are present in blood and tissues in healthy conditions and can expand in a spectrum of pathologies. HLA-DR NK cells are functionally active: they produce proinflammatory cytokines, degranulate, and easily proliferate in response to stimuli. Read More

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http://dx.doi.org/10.1002/JLB.3RU0420-668RRDOI Listing

[Proteins and immunohistochemical markers of breast diseases].

Biomed Khim 2020 Feb;66(2):167-173

Institute of Molecular Biology and Biophysics, Novosibirsk, Russia.

In this work, we have compared malignant and non-malignant diseases of the mammary gland using 8 proteins: HRG, MUC1, PAI-1, HSP90αA1, CDH1, ERα, PGR and IL-12. Their concentrations in the supernatants of blood cells and breast biopsies were compared in terms of spontaneous production, induced by a polyclonal activator and after exposure to biopsy samples of the HLDF differentiation factor, as well as the indices of the effect of the polyclonal activator and HLDF on the protein production. In addition, the correlation relationships of the above indicators with the expression of markers of the epithelial-mesenchymal transition: collagen type II (CII), β-1 integrin (CD29) and cadherin-E (CDH1) were studied. Read More

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http://dx.doi.org/10.18097/PBMC20206602167DOI Listing
February 2020

Switch Off "Parallel Circuit": Insight of New Strategy of Simultaneously Suppressing Canonical and Noncanonical Inflammation Activation in Endotoxemic Mice.

Adv Biosyst 2020 May 18:e2000037. Epub 2020 May 18.

Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing, 100082, China.

Sepsis is a life-threatening inflammatory disease with a high mortality rate and huge implicative costs. Lipopolysaccharide (LPS) from gram-negative bacteria activates toll-like receptor 4 (TLR4) and may trigger septic shock. However, potent TLR4 inhibitors TAK-242 and Eritoran have been terminated in phase III clinical trials because of inadequate efficacy. Read More

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http://dx.doi.org/10.1002/adbi.202000037DOI Listing

Ligand-centered assessment of SARS-CoV-2 drug target models in the Protein Data Bank.

FEBS J 2020 May 17. Epub 2020 May 17.

Department of Crystallography, Faculty of Chemistry, A. Mickiewicz University, Poznan, Poland.

A bright spot in the SARS-CoV-2 (CoV-2) coronavirus pandemic has been the immediate mobilization of the biomedical community, working to develop treatments and vaccines for COVID-19. Rational drug design against emerging threats depends on well-established methodology, mainly utilizing X-ray crystallography, to provide accurate structure models of the macromolecular drug targets and of their complexes with candidates for drug development. In the current crisis the structural biological community has responded by presenting structure models of CoV-2 proteins and depositing them in the Protein Data Bank (PDB), usually without time embargo and before publication. Read More

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http://dx.doi.org/10.1111/febs.15366DOI Listing

Fluorescence lifetime imaging reveals regulation of presynaptic Ca by glutamate uptake and mGluRs, but not somatic voltage in cortical neurons.

J Neurochem 2020 May 17. Epub 2020 May 17.

Queen Square Institute of Neurology, University College London, Queen Square, London, WC1N 3BG, U.K.

Brain function relies on vesicular release of neurotransmitters at chemical synapses. The release probability depends on action potential-evoked presynaptic Ca entry, but also on the resting Ca level. Whether these basic aspects of presynaptic calcium homeostasis show any consistent trend along the axonal path, and how they are controlled by local network activity, remains poorly understood. Read More

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http://dx.doi.org/10.1111/jnc.15094DOI Listing

Early Cognitive Training Rescues Remote Spatial Memory but Reduces Cognitive Flexibility in Alzheimer's Disease Mice.

J Alzheimers Dis 2020 May 11. Epub 2020 May 11.

Department of Neuro-/Pathology, Translational Neurodegeneration Research and Neuropathology Lab, University of Oslo (UiO) and Oslo University Hospital (OUS), Oslo, Norway.

Background: Spatial memory dysfunction has been demonstrated in mouse models of Alzheimer's disease (AD) which is consistent with the clinical finding that the early signature of AD includes difficulties in the formation and/or storage of a memory. A stored memory-a long term memory-can be modulated via process called as memory retrieval that can either lead toward memory reconsolidation or even memory extinction.

Objective: We aim to shed light on the fate of the spatial memory during memory reactivation and memory extinction using a water maze task. Read More

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http://dx.doi.org/10.3233/JAD-200161DOI Listing

Structural and kinetic properties of serine hydroxymethyltransferase from the halophytic cyanobacterium Aphanothece halophytica provide a rationale for salt tolerance.

Int J Biol Macromol 2020 May 15;159:517-529. Epub 2020 May 15.

Istituto Pasteur Italia-Fondazione Cenci Bolognetti and Dipartimento di Scienze Biochimiche "A. Rossi Fanelli", Sapienza Università di Roma, Roma, Italy. Electronic address:

Serine hydroxymethyltransferase (SHMT) is a pyridoxal 5'-phosphate-dependent enzyme that plays a pivotal role in cellular one‑carbon metabolism. In plants and cyanobacteria, this enzyme is also involved in photorespiration and confers salt tolerance, as in the case of SHMT from the halophilic cyanobacterium Aphanothece halophytica (AhSHMT). We have characterized the catalytic properties of AhSHMT in different salt and pH conditions. Read More

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http://dx.doi.org/10.1016/j.ijbiomac.2020.05.081DOI Listing

Antiproliferative and Carbonic Anhydrase II Inhibitory Potential of Chemical Constituents from and : Evidence from In Silico Target Fishing and In Vitro Testing.

Pharmaceuticals (Basel) 2020 May 13;13(5). Epub 2020 May 13.

Natural & Medical Sciences Research Center, University of Nizwa, P.O Box 33, 616 Birkat Al Mauz, Nizwa, Sultanate of Oman.

Roem. & Schult and resin of (L.) BURM. Read More

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http://dx.doi.org/10.3390/ph13050094DOI Listing

Evaluation of aliphatic/aromatic compounds and fluorophores in dissolved organic matter of contrasting natural waters by SEC-HPLC with multi-wavelength absorbance and fluorescence detections.

Spectrochim Acta A Mol Biomol Spectrosc 2020 May 5;238:118450. Epub 2020 May 5.

Institute of Basic Biological Problems, Russian Academy of Sciences, 142290 Pushchino, Moscow region, Russia. Electronic address:

The analytical high performance size exclusion liquid chromatography (SEC-HPLC) with multi-wavelength absorbance and fluorescence detections and fluorescence 3D-excitation/emission matrix (EEM) were used for the analysis of average molecular size (MS), molecular size distribution of aliphatic/aromatic compounds and fluorophores in dissolved organic matter (DOM) from Suwannee River (SRDOM) and two Karelian lakes (Vodoprovodnoe Lake - L1DOM and Onego Lake - L2DOM). The average MS of DOM samples varied in the order SRDOM > L1DOM > L2DOM. The absorbance ratios A250/A365 and A210/A254 have been used for the DOM samples characterization. Read More

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http://dx.doi.org/10.1016/j.saa.2020.118450DOI Listing

Mutational biosynthesis to generate novel analogs of nosiheptide featuring a fluorinated indolic acid moiety.

Org Biomol Chem 2020 May 15. Epub 2020 May 15.

State Key Laboratory of Bioorganic and Natural Products Chemistry, Center for Excellence on Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China. and Huzhou Center of Bio-Synthetic Innovation, 1366 Hongfeng Road, Huzhou 313000, China.

Nosiheptide (NOS) is a member of bicyclic thiopeptides possessing a biologically important indolic acid (IA) moiety appended onto the family-characteristic core system. The IA formation relies primarily on NosL, a radical S-adenosylmethionine (SAM) protein that catalyzes a complex rearrangement of the carbon side chain of l-tryptophan, leading to the generation of 3-methyl-2-indolic acid (MIA). Here, we establish an efficient mutational biosynthesis strategy for the structural expansion of the side-ring system of NOS. Read More

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http://dx.doi.org/10.1039/d0ob00084aDOI Listing

RNA-Seq-Based TCR Profiling Reveals Persistently Increased Intratumoral Clonality in Responders to Anti-PD-1 Therapy.

Front Oncol 2020 28;10:385. Epub 2020 Apr 28.

Laboratory of Genomics of Antitumor Adaptive Immunity, Privolzhsky Research Medical University, Nizhny Novgorod, Russia.

Substantial effort is being invested in the search for peripheral or intratumoral T cell receptor (TCR) repertoire features that could predict the response to immunotherapy. Here we demonstrate the utility of MiXCR software for TCR and immunoglobulin repertoire extraction from RNA-Seq data obtained from sorted tumor-infiltrating T and B cells. We use this approach to extract TCR repertoires from RNA-Seq data obtained from sorted tumor-infiltrating CD4 and CD8 T cells in an HKP1 (Krasp53) syngeneic mouse model of lung cancer after anti-PD-1 treatment. Read More

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http://dx.doi.org/10.3389/fonc.2020.00385DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7199218PMC

Polysubstituted Pyrimidines as mPGES-1 Inhibitors: Discovery of Potent Inhibitors of PGE2 Production with a Strong Anti-inflammatory Effects in Carrageenan-Induced Rat Paw Edema.

ChemMedChem 2020 May 15. Epub 2020 May 15.

Institute of Organic Chemistry and Biochemistry, CAS, Bioorganic & Medicinal Chemistry, Flemingovo nam. 2, 16610, Prague, CZECH REPUBLIC.

We report an extensive structure-activity relationship optimization of polysubstituted pyrimidines that led to a discovery of 5-butyl-4-(4-benzyloxyphenyl)-6-phenylpyrimidin-2-amine, and its difluorinated analogue. These compounds are submicromolar inhibitors of PGE 2 production (IC 50 as low as 12 nM). In order to identify the molecular target of anti-inflammatory pyrimidines, we performed extensive studies including enzymatic assays, homology modeling and docking. Read More

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http://dx.doi.org/10.1002/cmdc.202000258DOI Listing
May 2020
2.968 Impact Factor

Regulation of aerobic glycolysis to decelerate tumor proliferation by small molecule inhibitors targeting glucose transporters.

Protein Cell 2020 Jun;11(6):446-451

Tsinghua University-Peking University Joint Center for Life Sciences, Tsinghua University, Beijing, 100084, China.

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http://dx.doi.org/10.1007/s13238-020-00725-7DOI Listing
June 2020
2.851 Impact Factor

Allosteric Antagonism of the A Adenosine Receptor by a Series of Bitopic Ligands.

Cells 2020 May 12;9(5). Epub 2020 May 12.

Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.

Allosteric antagonism by bitopic ligands, as reported for many receptors, is a distinct modulatory mechanism. Although several bitopic A adenosine receptor (AAR) ligand classes were reported as pharmacological tools, their receptor binding and functional antagonism patterns, i.e. Read More

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http://dx.doi.org/10.3390/cells9051200DOI Listing

-Alkyl-2-[4-(trifluoromethyl)benzoyl]hydrazine-1-carboxamides and Their Analogues: Synthesis and Multitarget Biological Activity.

Molecules 2020 May 12;25(10). Epub 2020 May 12.

Department of Organic and Bioorganic Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic.

Based on the isosterism concept, we have designed and synthesized homologous -alkyl-2-[4-(trifluoromethyl)benzoyl]hydrazine-1-carboxamides (from C to C) as potential antimicrobial agents and enzyme inhibitors. They were obtained from 4-(trifluoromethyl)benzohydrazide by three synthetic approaches and characterized by spectral methods. The derivatives were screened for their inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) via Ellman's method. Read More

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http://dx.doi.org/10.3390/molecules25102268DOI Listing

One-step utilization of inulin for docosahexaenoic acid (DHA) production by recombinant Aurantiochytrium sp. carrying Kluyveromyces marxianus inulinase.

Bioprocess Biosyst Eng 2020 May 13. Epub 2020 May 13.

Jiangsu Key Laboratory for Biomass-Based Energy and Enzyme Technology, Huaiyin Normal University, Huaian, 223300, People's Republic of China.

This study aimed to express an inulinase gene from the yeast Kluyveromyces marxianus (KmINU) in Aurantiochytrium sp. and realized one-step utilization of inulin resource for DHA production without any chemical pretreatment. An expression cassette with a length of 6052 bp for expressing the inulinase gene was constructed by a fast two-step PCR method and then was transferred into the Aurantiochytrium sp. Read More

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http://dx.doi.org/10.1007/s00449-020-02371-zDOI Listing

Inspired by Sea Urchins: Warburg Effect Mediated Selectivity of Novel Synthetic Non-Glycoside 1,4-Naphthoquinone-6S-Glucose Conjugates in Prostate Cancer.

Mar Drugs 2020 May 11;18(5). Epub 2020 May 11.

Department of Oncology, Hematology and Bone Marrow Transplantation with Section Pneumology, Hubertus Wald-Tumorzentrum, University Medical Center Hamburg-Eppendorf, 20251 Hamburg, Germany.

The phenomenon of high sugar consumption by tumor cells is known as Warburg effect. It results from a high glycolysis rate, used by tumors as preferred metabolic pathway even in aerobic conditions. Targeting the Warburg effect to specifically deliver sugar conjugated cytotoxic compounds into tumor cells is a promising approach to create new selective drugs. Read More

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http://dx.doi.org/10.3390/md18050251DOI Listing