12,924 results match your criteria Bioorganic & Medicinal Chemistry[Journal]
Adv Mater 2018 Dec 14:e1806747. Epub 2018 Dec 14.
Beijing National Laboratory for Molecular Sciences (BNLMS), Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Key Laboratory of Polymer Chemistry and Physics of Ministry of Education, Center of Soft Matter Science and Engineering, College of Chemistry and Molecular Engineering, Peking University, Beijing, 100871, China.
Wafer-scale fabrication of high-performance uniform organic electronic materials is of great challenge and has rarely been realized before. Previous large-scale fabrication methods always lead to different layer thickness and thereby poor film and device uniformity. Herein, the first demonstration of 4 in. Read More
Microb Biotechnol 2018 Dec 13. Epub 2018 Dec 13.
Department of Applied and Ecological Microbiology, Institute of Microbiology, Friedrich Schiller University, Philosophenweg 12, D-07743, Jena, Germany.
Cobamides (Cbas) are essential cofactors of reductive dehalogenases (RDases) in organohalide-respiring bacteria (OHRB). Changes in the Cba structure can influence RDase function. Here, we report on the cofactor versatility or selectivity of Desulfitobacterium RDases produced either in the native organism or heterologously. Read More
Chemistry 2018 Dec 13. Epub 2018 Dec 13.
Polish Academy of Sciences, Institute of Organic Chemistry, Kasprzaka 44/52, 01-224, Warsaw, POLAND.
Directional self-assembly of uncharged molecules in water is a major challenge in supramolecular chemistry. In this paper we demonstrate that peptide-based cavitands wrap around a hydrophobic core (fullerene C60) forming highly ordered three-component complexes in water by a combination of hydrophobic effect and hydrogen bonding interactions (thus resembling the molten globule stage of protein folding). The complexes are characterized by NMR (diffusion-ordered spectroscopy, DOSY), SAXS, and circular dichroism, and their structure was ultimately confirmed by X-ray crystallography. Read More
Mar Drugs 2018 Dec 12;16(12). Epub 2018 Dec 12.
Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, ul. Miklukho-Maklaya 16/10, 117997 Moscow, Russia.
Acid-sensing ion channel 3 (ASIC3) makes an important contribution to the development and maintenance of inflammatory and acid-induced pain. We compared different ASIC3 inhibitors (peptides from sea anemones (APETx2 and Ugr9-1) and nonpeptide molecules (sevanol and diclofenac)) in anti-inflammatory action and analgesic effects. All tested compounds had distinct effects on pH-induced ASIC3 current. Read More
Int J Mol Sci 2018 Dec 11;19(12). Epub 2018 Dec 11.
Institute of Basic Biological Problems RAS, Pushchino 142290, Russia.
Jasmonates are plant hormones that are involved in the regulation of different aspects of plant life, wherein their functions and molecular mechanisms of action in wheat are still poorly studied. With the aim of gaining more insights into the role of jasmonic acid (JA) in wheat growth, development, and responses to environmental stresses, we have generated transgenic bread wheat plants overexpressing (), one of the key genes of the JA biosynthesis pathway. Analysis of transgenic plants showed that overexpression affects wheat development, including germination, growth, flowering time, senescence, and alters tolerance to environmental stresses. Read More
Molecules 2018 Dec 7;23(12). Epub 2018 Dec 7.
Department of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Silesian University of Technology, B. Krzywoustego 4, 44-100 Gliwice, Poland.
Raw vegetable oil from was subjected to oxidative treatment to enhance its viscosity. The oxidation processes were carried out in the presence of -hydroxyphthalimide with or without supercritical CO₂ as a solvent. Four spectroscopic techniques (Raman, UV-VIS, FT-IR, NMR) were applied to assess the chemical changes taking place during the oxidation. Read More
Bioresour Technol 2018 Dec 3;274:371-378. Epub 2018 Dec 3.
Key Laboratory of Bioorganic Synthesis of Zhejiang Province, College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China; Engineering Research Center of Bioconversion and Biopurification of Ministry of Education, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China.
To develop a highly efficient method for aprepitant chiral intermediate (S)-4-fluorophenylglycine, a continuous reaction system was established in packed bed bioreactor using amidase covalently immobilized on epoxy resin as biocatalyst. The epoxy resin was firstly modified by metal-chelate method and functional groups (Cu-IDA) generated were able to rapidly adsorb amidases, which were further covalently bound onto the modified resin with 90.1% immobilization yield and 80. Read More
Eur J Med Chem 2018 Dec 1;163:481-499. Epub 2018 Dec 1.
Center for Natural Products Research, Faculty of Chemistry, University of Havana, Zapata y G, 10400, La Habana, Cuba; Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Weinberg 3, 06120, Halle/Saale, Germany. Electronic address:
The Escherichia coli neutral M1-aminopeptidase (ePepN) is a novel target identified for the development of antimicrobials. Here we describe a solid-phase multicomponent approach which enabled the discovery of potent ePepN inhibitors. The on-resin protocol, developed in the frame of the Distributed Drug Discovery (D3) program, comprises the implementation of parallel Ugi-azide four-component reactions with resin-bound amino acids, thus leading to the rapid preparation of a focused library of tetrazole-peptidomimetics (TPMs) suitable for biological screening. Read More
Bioorg Med Chem 2018 Nov 28. Epub 2018 Nov 28.
Institute of Bioorganic and Medicinal Chemistry, Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China. Electronic address:
Based on the advantages of azole molecules and fluoroquinolone drugs, we designed and synthesized 34 clinafloxacin-azole conjugates using fragment-based drug design and drug combination principles. The in vitro activities of the synthesized conjugates against Mycobacterium tuberculosis (H37Rv), Hela cell as well as Gram-positive and Gram-negative bacteria were assayed. The bioassay results revealed that most of the target molecules had anti-tuberculosis (anti-TB) activity, of which 14 compounds had very strong anti-TB activity [minimum inhibitory concentration (MIC) < 2 μM]. Read More
Chem Commun (Camb) 2018 Dec 12. Epub 2018 Dec 12.
MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University, Beijing 100084, P. R. China.
Poly (ADP-ribose) polymerase-1 (PARP1) is a major member of the PARP superfamily that is involved in DNA damage signalling and other important cellular processes. Here we report the development of a small molecule targeting PARP1 based on the PROTAC strategy. In the MDA-MB-231 cell line, the representative compound 3 can induce significant PARP1 cleavage and programmed cell death. Read More
Prog Nucl Magn Reson Spectrosc 2018 Oct 13;108:17-73. Epub 2018 Oct 13.
A.E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, Favorsky St. 1, 664033 Irkutsk, Russia. Electronic address:
Structural applications of theoretical calculations of carbon-hydrogen spin-spin coupling constants are reviewed covering papers published mainly during the last 10-15 years with a special emphasis on the most notable studies of hybridization, substitution and stereoelectronic effects together with the investigation of hydrogen bonding and intermolecular interactions. The wide scope of different applications of calculated carbon-hydrogen couplings in the structural elucidation of particular classes of organic and bioorganic molecules is reviewed, concentrating mainly on saturated, unsaturated, aromatic and heteroaromatic compounds and their functional derivatives, as well as on natural compounds and carbohydrates. The review is dedicated to Professor Emeritus Michael Barfield in view of his invaluable pioneering contribution to this field. Read More
J Biol Inorg Chem 2018 Dec 7. Epub 2018 Dec 7.
Department of Chemistry, University of Minnesota, 207 Pleasant Street SE, Minneapolis, MN, 55455-0431, USA.
"In the original online publication, the Foreword was incorrectly attributed. The correct author is Lawrence Que, Jr." Read More
Microbiol Resour Announc 2018 Sep 20;7(11). Epub 2018 Sep 20.
All-Russian Collection of Microorganisms (VKM), G. K. Skryabin Institute of Biochemistry and Physiology of Microorganisms, Pushchino, Russia.
Draft genome sequences of 11 bacteria belonging to the family Microbacteriaceae were obtained using Illumina technology. The genomes of these strains have sizes from 3.14 to 4. Read More
ACS Omega 2018 Nov 2;3(11):14726-14731. Epub 2018 Nov 2.
Department of Chemistry, Organic and Bioorganic Chemistry, Bielefeld University, Universitätsstraße 25, D-33615 Bielefeld, Germany.
Traditional chemotherapeutics used in cancer therapy do not preferentially accumulate in tumor tissues. The conjugation to delivery vehicles like antibodies or small molecules has been proposed as a strategy to increase the tumor uptake and improve the therapeutic window of these drugs. Here, we report the synthesis and the biological evaluation of a novel small molecule-drug conjugate (SMDC) comprising a high-affinity bidentate acetazolamide derivative, targeting carbonic anhydrase IX (CAIX), and cryptophycin, a potent microtubule destabilizer. Read More
Bioorg Chem 2018 Nov 24;84:326-338. Epub 2018 Nov 24.
Institute of Chemistry, University of Silesia, Szkolna 9, 40-006 Katowice, Poland.
8-Hydroxyquinoline scaffold is a privileged structure used in designing a new active agents with therapeutic potential. Its connections with the sugar unit is formed to improve the pharmacokinetic properties. The broad spectrum of activity of quinoline derivatives, especially glycoconjugates, is often associated with the ability to chelate metal ions or with the ability to intercalate into DNA. Read More
J Inorg Biochem 2018 Nov 15;191:154-163. Epub 2018 Nov 15.
Institut Pasteur, Department of Structural Biology and Chemistry, Laboratory for Bioorganic Chemistry of Nucleic Acids, CNRS UMR3523, 28, rue du Docteur Roux, 75724 Paris Cedex 15, France. Electronic address:
The identification of synthetic nucleotides that sustain the formation of orthogonal, unnatural base pairs is an important goal in synthetic biology. Such artificial synthons have been used for the generation of semi-synthetic organisms as well as functional nucleic acids with enhanced binding properties. The enzymatic formation of artificial metal-base pairs is a vastly underexplored and alluring alternative to existing systems. Read More
Future Med Chem 2018 Dec 10. Epub 2018 Dec 10.
Department of Neurosurgery, Harvey Cushing Neuro-Oncology Laboratories, Brigham & Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.
J Nat Prod 2018 Dec 7. Epub 2018 Dec 7.
G. B. Elyakov Pacific Institute of Bioorganic Chemistry , Far Eastern Branch of the Russian Academy of Sciences , Prospect 100-let Vladivostoku 159 , Vladivostok 690022 , Russian Federation.
Melonoside B (1) and melonosins B (2) and A (3), new lipids based on polyoxygenated fatty acid amides, and known melonoside A (4) were isolated from two different collections of the marine sponge Melonanchora kobjakovae. The structures of these compounds, including their absolute configurations, were established using detailed analysis of 1D and 2D NMR, ECD, and mass spectra as well as chemical transformations. Melonosins 2 and 3 inhibit AP-1- and NF-kB-dependent transcriptional activities in JB6 Cl41 cells at noncytotoxic concentrations, demonstrating potential cancer preventive activity. Read More
Eur J Med Chem 2018 Nov 28;163:207-214. Epub 2018 Nov 28.
Department of Neurosurgery, Kurume University, School of Medicine, Fukuoka, Japan. Electronic address:
Ischemia-reperfusion injuries produce reactive oxygen species that promote the peroxide lipid oxidation process resulting in the production of an endogenic lipid peroxide, 4-hydroxy-trans-2-nonenal (4-HNE), a highly cytotoxic aldehyde that induces cell death. We synthesized a novel 4-HNE scavenger - a carnosine-hydrazide derivative, l-carnosine hydrazide (CNN) - and examined its neuroprotective effect in a model of transient ischemia. PC-12 cells were pre-incubated with various doses (0-50 mmol/L) of CNN for 30 min, followed by incubation with 4-HNE (250 μM). Read More
Antonie Van Leeuwenhoek 2018 Dec 5. Epub 2018 Dec 5.
G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch, Russian Academy of Sciences, Prospect 100 Let Vladivostoku, 159, Vladivostok, Russia, 690022.
An aerobic, Gram-negative, yellow-pigmented non-motile rod-shaped bacterium Kr9-9 was isolated from a brown alga specimen collected near the Kuril Islands. Based on the 16S rRNA gene sequence analysis strain Kr9-9 was assigned to the genus Winogradskyella, and its close phylogenetic neighbors were found to be Winogradskyella damuponensis KCTC 23552, Winogradskyella sediminis LMG 28075, and Winogradskyella rapida CCUG 59098 showing high similarities of 98.1%, 97. Read More
Front Microbiol 2018 21;9:2827. Epub 2018 Nov 21.
Federal Research and Clinical Centre of Physical-Chemical Medicine, Moscow, Russia.
Prokaryotes are actively studied objects in the scope of genomic regulation. Microbiologists need special tools for complex analysis of data to study and identification of regulatory mechanism in bacteria and archaea. We developed a tool BAC-BROWSER, specifically for visualization and analysis of small prokaryotic genomes. Read More
JCI Insight 2018 Dec 6;3(23). Epub 2018 Dec 6.
Department of Animal Radiology, Graduate School of Agriculture and Life Sciences, The University of Tokyo, Tokyo, Japan.
In diabetic retinopathy (DR), pericyte dropout from capillary walls is believed to cause the breakdown of the blood-retina barrier (BRB), which subsequently leads to vision-threatening retinal edema. While various proinflammatory cytokines and chemokines are upregulated in eyes with DR, their distinct contributions to disease progression remain elusive. Here, we evaluated roles of stromal cell-derived factor-1α (SDF-1α) and its receptor CXCR4 in the BRB breakdown initiated by pericyte deficiency. Read More
RNA Biol 2018 Dec 6. Epub 2018 Dec 6.
a Institute of Bioorganic Chemistry, Polish Academy of Sciences , Poznan , Poland.
Transcription initiation sites of Trp53 gene in mice were determined using the 5'RACE method. Based on sequence alignment of the 5'-terminal regions of p53 mRNA in mammals, the site for the most abundant transcript turned out to be essentially identical with that determined for human TP53 gene and slightly differed for the longest transcripts, in mice and humans. Secondary structures of the 5' -terminal regions of the shorter, most abundant and the longest mouse transcripts were determined in vitro and the shorter transcript was also mapped in transfected mouse cells. Read More
Mar Drugs 2018 Dec 4;16(12). Epub 2018 Dec 4.
Institute for Inorganic and Analytical Chemistry, Bioorganic Analytics, Friedrich Schiller University Jena, Lessingstr. 8, D-07743 Jena, Germany.
Algicidal bacteria can lyse microalgal blooms and trigger shifts within plankton communities. Resistant algal species can escape lysis, and have the opportunity to dominate the phytoplankton after a bacterial infection. Despite their important function in ecosystem regulation, little is known about mechanisms of resistance. Read More
Bioorg Chem 2018 Nov 27;84:254-259. Epub 2018 Nov 27.
Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing 100084, China; Beijing Institute for Brain Disorders, Beijing 100069, China; Center for Synthetic and Systems Biology, Tsinghua University, Beijing 100084, China. Electronic address:
TAR DNA binding protein 43 (TDP-43) is a key target in amyotrophic lateral sclerosis (ALS) treatment. Here, based on hydrophobic tagging strategy, we designed and synthesized a series of single or double hydrophobic tags conjugated peptides D1-D8. Among them, it was found that D4 displayed strongest ability to induce TDP-43 degradation in cells. Read More
Chem Commun (Camb) 2018 Dec 3. Epub 2018 Dec 3.
Beijing National Laboratory of Molecular Sciences (BNLMS), Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry, Peking University, Beijing 100871, China. and The State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China.
A palladium-catalyzed oxidative borylation reaction of conjugated enynones is developed. This reaction represents a new method for the synthesis of furyl-substituted alkenylboronates. The reaction works well with a series of conjugated enynones. Read More
Data Brief 2018 Dec 3;21:1659-1663. Epub 2018 Nov 3.
Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 16/10 Miklukho-Maklaya Street, Moscow 117997, Russia.
Mms6 is a protein that plays crucial role in the biomineralization and formation of magnetosomes in magnetotactic bacteria Magnetospirillum magneticum (strain AMB-1). We developed a fusion protein of C-term part of Mms6 and Barstar (natural inhibitor of ribonuclease Barnase), namely, Bs-C-Mms6. This protein successfully stabilized uncoated monocrystalline FeO magnetite nanoparticles in buffered solutions. Read More
Colloids Surf B Biointerfaces 2018 Nov 26;174:587-597. Epub 2018 Nov 26.
Department of Biomedical Engineering, Faculty of Fundamental Problems of Technology, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland. Electronic address:
We report a multistep strategy of biochemical surface modifications that resulted in the synthesis of new, effective and biocompatible intravascular implants coating with immobilized anti-CD133 antibodies, that proved to be the most effective in endothelial progenitor cells capture and reduced smooth muscle cells growth. Biomolecules were immobilized on differently functionalized surfaces. The distribution, nanostructural characteristics and intramolecular interactions of anti-CD133 molecules as well as their ability to bind EPCs was evaluated. Read More
PLoS One 2018 5;13(12):e0208469. Epub 2018 Dec 5.
Laboratory of Cell Interactions, Department of Immunology, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Science, Moscow, Russian Federation.
In this work, we analyzed the phenotype and growth of human NK cell clones obtained by the stimulation of individual NK cells with IL-2 and gene-modified K562 feeder cells expressing membrane-bound IL-21 (K562-mbIL21). We generated clones from NK cells at distinct differentiation and activation stages, determined by CD56, CD57 and HLA-DR expression levels. Less differentiated CD56bright NK cell subsets showed higher cloning efficiency compared with more differentiated CD56dim subsets, especially with the CD57bright subset. Read More
Org Biomol Chem 2018 Dec;16(48):9373-9376
State Key Laboratory of Bioorganic and Natural Products Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China.
Using a highly effective heterologous expression system, the YM-216391 (1) biosynthetic gene cluster was engineered to yield aurantizolicin (2) and the hybrid compound 3. Both of these compounds were isolated and fully structurally characterised and the bioactivity was evaluated. The results indicate that compound 3 exhibits significantly improved antitumor activity. Read More
Biomed Res Int 2018 1;2018:6192059. Epub 2018 Nov 1.
Key Laboratory of Bioorganic Synthesis of Zhejiang Province, College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou 310014, China.
A mutant L206F/P207F/L259F of lipase (TTL) exhibited high hydrolytic activity towards 2-carboxyethyl-3-cyano-5-methylhexanoic acid ethyl ester (CNDE) for synthesis of ()-2-carboxyethyl-3-cyano-5-methylhexanoic acid (-CCMA), a key chiral intermediate of pregabalin. However, low conversion at high CNDE concentration and unreusability of the free TTL mutant restricted its industrial applications. In this study, the TTL mutant was immobilized onto epoxy resin and its catalytic properties for kinetic resolution of CNDE were investigated. Read More
Chimia (Aarau) 2018 Nov;72(11):782-790
Department of Chemical Biology College of Chemistry and Molecular Engineering Beijing National Laboratory for Molecular Sciences Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education Synthetic and Functional Biomolecules Center and Peking-Tsinghua Center for Life Sciences Peking University, Beijing 100871, China;, Email:
Understanding of biological systems has always been the general interest in chemical biology, and chemical modifications of biomolecules are often required to elucidate their functions and properties. There has thus been a rapid development of covalent chemistries for the modification of macromolecules. Among these strategies, photochemistry provides the advantage of using biocompatible light as an energy source to trigger bioconjugation reactions; this circumvents the use of toxic reagents (e. Read More
Mar Drugs 2018 Dec 1;16(12). Epub 2018 Dec 1.
Institute of Experimental Medicine, Acad. Pavlov Str. 12, Saint Petersburg 197376, Russia.
Antimicrobial peptides from marine invertebrates are known not only to act like cytotoxic agents, but they also can display some additional activities in mammalian organisms. In particular, these peptides can modulate the complement system as was described for tachyplesin, a peptide from the horseshoe crab. In this work, we investigated the influence on complement activation of the antimicrobial peptide arenicin-1 from the marine polychaete . Read More
Molecules 2018 Nov 30;23(12). Epub 2018 Nov 30.
Department of Chemical Engineering, Biotechnology and Materials, Ariel University, Ariel 4070000, Israel.
The well-known and rapidly growing phenomenon of bacterial resistance to antibiotics is caused by uncontrolled, excessive and inappropriate use of antibiotics. One of alternatives to antibiotics is Photodynamic Antibacterial Chemotherapy (PACT). In the present study, the effect of PACT using a photosensitizer Rose Bengal alone and in combination with antibiotics including methicillin and derivatives of sulfanilamide synthesized by us was tested against antibiotic-sensitive and antibiotic-resistant clinical isolates of Gram-positive and Gram-negative . Read More
ACS Infect Dis 2018 Dec 4. Epub 2018 Dec 4.
Biology Department , 1001 E. Third Street , Indiana University , Bloomington , Indiana 47401 , United States.
Not all career paths are clearly defined from the beginning. In my case, biochemistry training in enzymology provided the tools to move from a basic research beginning in biophysical/bioorganic chemistry to an applied microbiology career in antibiotic drug discovery and development. This pathway required essential contributions from family, professional colleagues, co-workers, and mentors who all provided input at critical times during changes in career directions. Read More
Front Cell Infect Microbiol 2018 19;8:393. Epub 2018 Nov 19.
Molecular Biology Department, Instituto de Parasitología y Biomedicina "López Neyra", Consejo Superior de Investigaciones Científicas, Granada, Spain.
The host immunological response is a key factor determining the pathogenesis of cutaneous leishmaniasis. It is known that a Th1 cellular response is associated with infection control and that antigen-specific memory T cells are necessary for the development of a rapid and strong protective cellular response. The present manuscript reports the analysis of the functional and phenotypic profiles of antigen-specific CD4 and CD8 T cells from patients cured of cutaneous leishmaniasis (CL), patients with an active process of cutaneous leishmaniasis, asymptomatic individuals with a positive Montenegro test and healthy donors (HD). Read More
Nat Cell Biol 2018 Dec 3. Epub 2018 Dec 3.
State Key Laboratory of Membrane Biology, Institute of Molecular Medicine, Beijing Key Laboratory of Cardiometabolic Molecular Medicine and Peking-Tsinghua Center for Life Sciences, Peking University, Beijing, China.
N6-methyldeoxyadenine (6mA), a major type of DNA methylation in bacteria, represents a part of restriction-modification systems to discriminate host genome from invader DNA. With the recent advent of more sensitive detection techniques, 6mA has also been detected in some eukaryotes. However, the physiological function of this epigenetic mark in eukaryotes remains elusive. Read More
Int J Biol Macromol 2018 Nov 28;124:810-818. Epub 2018 Nov 28.
Department of Molecular Medicine and USF Health Byrd Alzheimer's Research Institute, Morsani College of Medicine, University of South Florida, Tampa, FL, USA; Institute for Biological Instrumentation, Russian Academy of Sciences, Pushchino, Moscow Region 142290, Russia. Electronic address:
In this work, we studied the effect of the C-terminally attached poly-histidine tag (His-tag), as well as the peculiarities of the protein purification procedure by the immobilized metal affinity chromatography (IMAC) on the activity and structure of the metalloenzyme, l-alanyl-d-glutamate peptidase of bacteriophage T5 (EndoT5), whose zinc binding site and catalytic aspartate are located near the C-terminus. By itself, His-tag did not have a significant effect on either activity or folding of the polypeptide chain, nor on the binding of zinc and calcium ions to the protein. However, the His-tagged EndoT5 samples had low shelf-life, with storage of these samples resulting in an increased propensity for protein self-association and decreased enzymatic activity of EndoT5. Read More
Biochim Biophys Acta Bioenerg 2019 Jan 18;1860(1):1-11. Epub 2018 Sep 18.
Shemyakin & Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997 Moscow, Ul. Miklukho-Maklaya, 16/10, Russian Federation. Electronic address:
ESR from Exiguobacterium sibiricum is a retinal protein which functions as a proton pump. Unusual feature of ESR is that a lysine residue is present at a site for the internal proton donor, which in other proton pumps is a carboxylic residue. Replacement of Lys96 with alanine slows reprotonation of the Schiff base by two orders of magnitude, indicating that Lys96 and interacting water molecules function as internal proton donor to the Schiff base. Read More
iScience 2018 Nov 14;10:11-22. Epub 2018 Nov 14.
School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing, China; Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing, China. Electronic address:
In transition metal-catalyzed asymmetric synthesis, enantioselectivity strongly depends on the structures of chiral ligands, so the development of new chiral ligands is crucial. Here, an efficient and highly enantioselective palladium-catalyzed intramolecular hydroarylation has been developed, and a new kind of N-heterocycles, 1H-pyrazolo[5,1-a]isoindol-2(8H)-ones containing a quaternary stereocenter, was prepared in high yields and excellent enantiomeric excess values. The reaction was effectively catalyzed by palladium-diphosphine complexes with numerous functional group tolerance, in which the newly developed axially chiral cyclic diphosphine ligands played key roles in the reactivity and enantioselectivity of the substrates. Read More
Int J Biol Macromol 2018 Nov 26;124:220-228. Epub 2018 Nov 26.
G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Sciences, 159, prosp. 100 Let Vladivostoku, 690022 Vladivostok, Russian Federation.
Fucoidans are valuable biologically active polysaccharides of brown algae. The aim of this study was to investigate the structure of fucoidan from Sargassum feldmannii and the anticancer effects of native and modified polysaccharides from S. feldmannii and S. Read More
Biofactors 2018 Nov 29. Epub 2018 Nov 29.
Siberian Division of Russian Academy of Sciences, Institute of Chemical Biology and Fundamental Medicine, Novosibirsk, Russia.
Histones act as damage-associated molecules, while anti-DNA antibodies are directed against histone-DNA nucleosomal complexes. Myelin basic protein (MBP) plays an important role in the pathogenesis of multiple sclerosis. Autoantibodies (Abs) with enzymatic activities are the distinctive feature of some autoimmune and viral diseases. Read More
Org Lett 2018 Nov 29. Epub 2018 Nov 29.
School of Pharmaceutical Sciences, Key Laboratory of Bioorganic Phosphorous Chemistry & Chemical Biology (Ministry of Education) , Tsinghua University , Beijing , 100084 , China.
An unprecedented example of NHC-catalyzed chemoselective S-O bond cleavage of dinitrobenzenesulfonic carbamates is described. This protocol features several advantages, including mild reaction conditions, broad substrate scope, and operational simplicity, which allows it to be an attractive synthetic method for hydroxylamine synthesis. Notably, dinitrobenzenesulfonic carbamates not only work as "O" synthons but also serve as an efficient oxidant in this reaction. Read More
Bioprocess Biosyst Eng 2018 Nov 28. Epub 2018 Nov 28.
Key Laboratory of Bioorganic Synthesis of Zhejiang Province, College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou, 310014, China.
Nitrilase is the member of carbon-nitrogen hydrogen hydrolase superfamily, which has been widely used for the hydrolysis of nitriles into corresponding carboxylic acids. But most nitrilases are plagued by product inhibition in the industrial application. In this study, a "super nitrilase mutant" of nitrilase with high activity, thermostability and improved product tolerance from Acidovorax facilis ZJB09122 was characterized. Read More
Nat Commun 2018 11 28;9(1):5032. Epub 2018 Nov 28.
CAS Center for Excellence in Nanoscience, CAS Key Laboratory of Biomedical Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Beijing, 100190, China.
Adverse drug reactions (ADRs) restrict the maximum doses applicable in chemotherapy, which leads to failure in cancer treatment. Various approaches, including nano-drug and prodrug strategies aimed at reducing ADRs, have been developed, but these strategies have their own pitfalls. A renovated strategy for ADR reduction is urgently needed. Read More
Molecules 2018 Nov 28;23(12). Epub 2018 Nov 28.
Grain and Oil Products Quality Inspection Center of Zhejiang Province, Hangzhou 310012, China.
The recombinant carbonyl reductase from WZ010 (ReCR) demonstrated strict ()-stereoselectivity and catalyzed the irreversible reduction of -Boc-3-piperidone (NBPO) to ()--Boc-3-hydroxypiperidine [()-NBHP], a key chiral intermediate in the synthesis of ibrutinib. The NAD(H)-specific enzyme was active within broad ranges of pH and temperature and had remarkable activity in the presence of higher concentration of organic solvents. The amino acid residue at position 54 was critical for the activity and the substitution of Tyr54 to Phe significantly enhanced the catalytic efficiency of ReCR. Read More
Int J Mol Sci 2018 Nov 28;19(12). Epub 2018 Nov 28.
Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya 16/10, 117997 Moscow, Russia.
Fluorogens are an attractive type of dye for imaging applications, eliminating time-consuming washout steps from staining protocols. With just a handful of reported fluorogen-protein pairs, mostly in the green region of spectra, there is a need for the expansion of their spectral range. Still, the origins of solvatochromic and fluorogenic properties of the chromophores suitable for live-cell imaging are poorly understood. Read More
Mar Drugs 2018 Nov 27;16(12). Epub 2018 Nov 27.
Laboratory of Marine Biochemistry, G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch, Russian Academy of Science, 159, Stoletya Vladivostoku str., Vladivostok 690022, Russia.
The GalNAc/Gal-specific lectin from the sea mussel (CGL) with anticancer activity represents а novel lectin family with β-trefoil fold. Earlier, the crystal structures of CGL complexes with globotriose, galactose and galactosamine, and mutagenesis studies have revealed that the lectin contained three carbohydrate-binding sites. The ability of CGL to recognize globotriose (Gb3) on the surface of breast cancer cells and bind mucin-type glycoproteins, which are often associated with oncogenic transformation, makes this compound to be perspective as a biosensor for cancer diagnostics. Read More
Mar Drugs 2018 Nov 26;16(12). Epub 2018 Nov 26.
M.M. Shemyakin & Yu.A. Ovchinnikov Institute of Bioorganic Chemistry, the Russian Academy of Sciences, Mikhluho-Maklaya str. 16/10, Moscow 117997, Russia.
Biological activity of the new antimicrobial peptide polyphemusin III from the horseshoe crab was examined against bacterial strains and human cancer, transformed, and normal cell cultures. Polyphemusin III has the amino acid sequence RRGCFRVCYRGFCFQRCR and is homologous to other β-hairpin peptides from the horseshoe crab. Antimicrobial activity of the peptide was evaluated and MIC (minimal inhibitory concentration) values were determined. Read More
Chem Biol Drug Des 2018 Nov 28. Epub 2018 Nov 28.
Department of Bioorganic Chemistry, Faculty of Chemistry, Wrocław University of Science and Technology, Wrocław, Poland.
Bisphosphonic acids, which are structural analogs of pyrophosphate, constitute a class of compounds with very high potential for the construction of effective inhibitors of enzymes operating on oligo- and polyphosphates. The bisphosphonate-based methodology was applied for the discovery of inhibitors of two families of polyphosphate kinases (PPK1 and PPK2). Screening of thirty-two structurally diverse bisphosphonic acids and related compounds revealed several micromolar inhibitors of both enzymes. Read More