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Search for "proteins" in Full Text gives 508 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

Heterogeneous photocatalysis in flow chemical reactors

  • Christopher G. Thomson,
  • Ai-Lan Lee and
  • Filipe Vilela

Beilstein J. Org. Chem. 2020, 16, 1495–1549, doi:10.3762/bjoc.16.125

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Published 26 Jun 2020

Synthesis of new fluorescent molecules having an aggregation-induced emission property derived from 4-fluoroisoxazoles

  • Kazuyuki Sato,
  • Akira Kawasaki,
  • Yukiko Karuo,
  • Atsushi Tarui,
  • Kentaro Kawai and
  • Masaaki Omote

Beilstein J. Org. Chem. 2020, 16, 1411–1417, doi:10.3762/bjoc.16.117

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  • be visualized using fluorescent probes, the use of AIE fluorescent probes is being investigated as a tool for analyzing the causal relationship between prion diseases and prion proteins. The importance of fluorinated heterocyclic derivatives in the pharmaceutical and agrochemical industries continues
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Published 22 Jun 2020

Photocatalytic trifluoromethoxylation of arenes and heteroarenes in continuous-flow

  • Alexander V. Nyuchev,
  • Ting Wan,
  • Borja Cendón,
  • Carlo Sambiagio,
  • Job J. C. Struijs,
  • Michelle Ho,
  • Moisés Gulías,
  • Ying Wang and
  • Timothy Noël

Beilstein J. Org. Chem. 2020, 16, 1305–1312, doi:10.3762/bjoc.16.111

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  • (Scheme 1A). This property might be responsible for stronger binding affinities of trifluoromethoxylated compounds with the active sites in enzymes, proteins, or other biomolecules [8][9]. Several procedures for the synthesis of trifluoromethyl aryl ethers were reported from the mid-1900s, mostly based on
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Published 15 Jun 2020

Anthelmintic drug discovery: target identification, screening methods and the role of open science

  • Frederick A. Partridge,
  • Ruth Forman,
  • Carole J. R. Bataille,
  • Graham M. Wynne,
  • Marina Nick,
  • Angela J. Russell,
  • Kathryn J. Else and
  • David B. Sattelle

Beilstein J. Org. Chem. 2020, 16, 1203–1224, doi:10.3762/bjoc.16.105

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  • basis for finding compounds that are anthelmintic in vivo but do not cause paralysis, perhaps involving aspects of the interaction with the host, interfering with the secretion of proteins, or other ways of damaging the worm [146]. They are also useful for understanding in more detail the mechanism of
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Published 02 Jun 2020

A smart deoxyribozyme-based fluorescent sensor for in vitro detection of androgen receptor mRNA

  • Ekaterina A. Bryushkova,
  • Erik R. Gandalipov and
  • Julia V. Nuzhina

Beilstein J. Org. Chem. 2020, 16, 1135–1141, doi:10.3762/bjoc.16.100

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  • . Petersburg, 197101, Russian Federation 10.3762/bjoc.16.100 Abstract Nowadays a variety of biosensors are widely used in different fields, including biomedical diagnostics and self-testing. Nucleic acid-based biosensors are typically applied to detect another nucleic acid, proteins, ions, and several other
  • different levels, including DNA, RNA, proteins, and small molecule metabolites. Today, along with other methods in clinical diagnosis biosensors are ubiquitously used in the biomedical field. The first prototype of a biosensor was invented by Leland Clark and Champ Lyons in 1962 as an amperometric Clark
  • . Reproducibility and linearity are also very important as well as costs and ease of manufacturing each component of the biosensor. Unlike proteins or antibodies the nucleic acid-based biosensors (NAs) can be easily commercially synthesized, they are smaller, more stable, and can be repeatedly used without losing
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Published 27 May 2020

Synthesis of esters of diaminotruxillic bis-amino acids by Pd-mediated photocycloaddition of analogs of the Kaede protein chromophore

  • Esteban P. Urriolabeitia,
  • Pablo Sánchez,
  • Alexandra Pop,
  • Cristian Silvestru,
  • Eduardo Laga,
  • Ana I. Jiménez and
  • Carlos Cativiela

Beilstein J. Org. Chem. 2020, 16, 1111–1123, doi:10.3762/bjoc.16.98

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  • in the last few years due to the discovery that truxillic acid derivatives are inhibitors of FABP (fatty acid binding proteins), which are responsible for the cellular reuptake of anandamide, an endocannabinoid neurotransmitter, and that they can be involved in a very efficient treatment for chronic
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Published 25 May 2020

Fluorinated phenylalanines: synthesis and pharmaceutical applications

  • Laila F. Awad and
  • Mohammed Salah Ayoup

Beilstein J. Org. Chem. 2020, 16, 1022–1050, doi:10.3762/bjoc.16.91

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  • . Incorporation of fluorinated aromatic amino acids into proteins increases their catabolic stability especially in therapeutic proteins and peptide-based vaccines. This review seeks to summarize the different synthetic approaches in the literature to prepare ᴅ- or ʟ-fluorinated phenylalanines and their
  • the properties of peptides and proteins [5][6][7], influencing aspects such as protein folding, protein–protein interactions, ribosomal translation, lipophilicity, acidity/basicity, optimal pH, stability, thermal stability, and therapeutic properties [8][9][10]. This extends to metabolic properties of
  • membrane permeability and reactivity [11][12][13][14]. The effect of peptide structure and stability has been found to depend on the position and number of fluorine atoms within the amino acid chains [15][16][17]. Incorporation of fluorinated aromatic amino acids into proteins can increase their shelf life
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Published 15 May 2020

Synthesis of new asparagine-based glycopeptides for future scanning tunneling microscopy investigations

  • Laura Sršan and
  • Thomas Ziegler

Beilstein J. Org. Chem. 2020, 16, 888–894, doi:10.3762/bjoc.16.80

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  • Glycopeptides are generally found on virtually every eukaryotic and prokaryotic cell surface. So far, the study of glycopeptide interactions with other proteins gave some insight into important biological functions, for instance, intracellular communication, cell–cell recognition, immune response, and
  • pathogenesis [1][2][3][4]. Glycosylation is also considered to be one of the most important post-translational modification (PTM) since more than half of all human proteins are glycopeptides or glycoproteins [5]. Therefore, understanding how glycopeptides interact on an intra- and intermolecular level is
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Published 30 Apr 2020

Design and synthesis of diazine-based panobinostat analogues for HDAC8 inhibition

  • Sivaraman Balasubramaniam,
  • Sajith Vijayan,
  • Liam V. Goldman,
  • Xavier A. May,
  • Kyra Dodson,
  • Sweta Adhikari,
  • Fatima Rivas,
  • Davita L. Watkins and
  • Shana V. Stoddard

Beilstein J. Org. Chem. 2020, 16, 628–637, doi:10.3762/bjoc.16.59

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  • involve acetylation/deacetylation of histone proteins by histone deacetylases (HDACs) [1]. HDACs belong to an important family of enzymes consisting of 18 isozymes. They control protein acetylation, which is a change that occurs after translation. In addition, they regulate gene transcription, cell
  • differentiation, cell cycle progression and apoptosis by targeting both histone and non-histone proteins. The balance between acetylation and deacetylation is pivotal for typical cell function. Abnormal or increased HDAC expression has been reported in several human tumors and cancer cell lines [2]. As such, the
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Published 07 Apr 2020

Opening up connectivity between documents, structures and bioactivity

  • Christopher Southan

Beilstein J. Org. Chem. 2020, 16, 596–606, doi:10.3762/bjoc.16.54

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  • . Although their expert-curated numbers are lower (i.e., ≈2 million compounds against ≈3700 human proteins), these open sources have the great advantage of being merged within PubChem. Parallel efforts have focused on the extraction of document-to-compound (D-C-only) connectivity. In the absence of molecular
  • -R indicates C to be a potent inhibitor of P). Compounds: a full range of cheminformatic analysis including 2D or 3D clustering, property prediction and chemical ontology assignments. Proteins: a full range of bioinformatic analysis including gene ontology (GO) assignments, pathway annotation
  •  4 are noteworthy and persist despite the ChEMBL/BindingDB selective mirroring. As for PMID coverage it would be useful to know which types of selectivity were responsible for this divergence in connectivity. For BindingDB some unique proteins are likely to be patent-only but exploring further causes
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Published 02 Apr 2020

Convenient synthesis of the pentasaccharide repeating unit corresponding to the cell wall O-antigen of Escherichia albertii O4

  • Tapasi Manna,
  • Arin Gucchait and
  • Anup Kumar Misra

Beilstein J. Org. Chem. 2020, 16, 106–110, doi:10.3762/bjoc.16.12

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  • cell wall polysaccharides with suitable proteins, which include vaccines against Haemophilia influenza type b (Hib) [12][13], meningitis [14], pneumococcal infections [15][16] and enteric diseases such as cholera [17], diarrhea [18] and urinary tract infections [19]. Despite the possibility of
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Published 22 Jan 2020

Light-controllable dithienylethene-modified cyclic peptides: photoswitching the in vivo toxicity in zebrafish embryos

  • Sergii Afonin,
  • Oleg Babii,
  • Aline Reuter,
  • Volker Middel,
  • Masanari Takamiya,
  • Uwe Strähle,
  • Igor V. Komarov and
  • Anne S. Ulrich

Beilstein J. Org. Chem. 2020, 16, 39–49, doi:10.3762/bjoc.16.6

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  • differences of erythrocytes compared to other somatic cells. Although easily measured, hemolytic activity gives only a rough estimate of toxicity for peptide therapeutics. Erythrocytes are terminally differentiated non-adherent organelle-free cells, densely packed with oxygen-carrying proteins; their
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Published 07 Jan 2020

Synthesis and characterization of bis(4-amino-2-bromo-6-methoxy)azobenzene derivatives

  • David Martínez-López,
  • Amirhossein Babalhavaeji,
  • Diego Sampedro and
  • G. Andrew Woolley

Beilstein J. Org. Chem. 2019, 15, 3000–3008, doi:10.3762/bjoc.15.296

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  • . While many classes of photoswitches are known [1][2], few of these are easily adaptable to controlling targets, such as proteins [3], while simultaneously exhibiting robust photochemistry in the red or near-infrared (NIR) regions of the spectrum [4][5][6][7]. Azonium ions – protonated forms of
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Published 30 Dec 2019

Pigmentosins from Gibellula sp. as antibiofilm agents and a new glycosylated asperfuran from Cordyceps javanica

  • Soleiman E. Helaly,
  • Wilawan Kuephadungphan,
  • Patima Phainuphong,
  • Mahmoud A. A. Ibrahim,
  • Kanoksri Tasanathai,
  • Suchada Mongkolsamrit,
  • Janet Jennifer Luangsa-ard,
  • Souwalak Phongpaichit,
  • Vatcharin Rukachaisirikul and
  • Marc Stadler

Beilstein J. Org. Chem. 2019, 15, 2968–2981, doi:10.3762/bjoc.15.293

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  • , in particular orthopedic implant-related infections, since implants coated with proteins facilitate bacterial attachment and biofilm development [1]. In general, bacteria are known to employ different strategies to cope with the presence of antibiotics, of which a biofilm, an aggregate of
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Published 16 Dec 2019

Chemical synthesis of tripeptide thioesters for the biotechnological incorporation into the myxobacterial secondary metabolite argyrin via mutasynthesis

  • David C. B. Siebert,
  • Roman Sommer,
  • Domen Pogorevc,
  • Michael Hoffmann,
  • Silke C. Wenzel,
  • Rolf Müller and
  • Alexander Titz

Beilstein J. Org. Chem. 2019, 15, 2922–2929, doi:10.3762/bjoc.15.286

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  • peptide biosynthesis has previously been successfully performed using cell lysate, e.g., in case of gramicidin [24], or with purified proteins, e.g., in case of myxochelin [25] and tilivalline [26]. To evaluate if in vitro formation of argyrin is indeed possible, the reaction buffer was incubated with the
  • cell lysate mixture of M. xanthus DK1622 mutants expressing the Arg2-Arg5 argyrin biosynthetic proteins. To ensure that no argyrin is present in the lysate prior to the incubation, a lysate mixture of two different mutants harboring arg2 and arg3-5 genes was used, respectively. Both of the mutants are
  • incapable of argyrin production on their own, however, together they express all the necessary proteins. Despite significant efforts and evaluation of various incubation conditions, in vitro reconstitution of argyrins could never be achieved. The exact reason for this is unknown, however, it is very likely
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Published 05 Dec 2019

Bacterial terpene biosynthesis: challenges and opportunities for pathway engineering

  • Eric J. N. Helfrich,
  • Geng-Min Lin,
  • Christopher A. Voigt and
  • Jon Clardy

Beilstein J. Org. Chem. 2019, 15, 2889–2906, doi:10.3762/bjoc.15.283

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  • can be further modified by tailoring enzymes, but the core structure can be inferred from the organization of the biosynthetic genes and the modular architecture of the associated proteins [7][8]. Terpene biosynthesis has a very different logic. Five-carbon units called isoprenes are joined to create
  • Information File 1, Table S2). CYPs are heme-dependent iron proteins that catalyze a wide range of reactions [83][84]. The reactions typically involve substrate radical generation by the activated iron species and subsequent hydroxylation. Terpenes are mainly composed of nonactivated hydrocarbons that are
  • ent-kaurenoic acid (27 and 28, respectively, Figure 7b) [41]. Characterization of CYPs is typically achieved by in vitro or in vivo studies. E. coli is the most popular host for obtaining proteins for in vitro studies, and proper selection of a redox system is usually the obstacle to reconstitute CYP
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Published 29 Nov 2019

Emission and biosynthesis of volatile terpenoids from the plasmodial slime mold Physarum polycephalum

  • Xinlu Chen,
  • Tobias G. Köllner,
  • Wangdan Xiong,
  • Guo Wei and
  • Feng Chen

Beilstein J. Org. Chem. 2019, 15, 2872–2880, doi:10.3762/bjoc.15.281

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  • 28–73% of sequence identities. Full-length cDNAs for the four TPS genes were cloned and expressed in Escherichia coli to produce recombinant proteins, which were tested for sesquiterpene synthase and monoterpene synthase activities. While neither PpolyTPS2 nor PpolyTPS3 was active, PpolyTPS1 and
  • genes were identified from the transcriptomes. They were designated as PpolyTPS1, PpolyTPS2, PpolyTPS3, and PpolyTPS4. The length of the proteins encoded by PpolyTPS1, PpolyTPS2, PpolyTPS3, and PpolyTPS4s is 334, 347, 353, and 337 amino acids, respectively. Among the four proteins, the highest sequence
  • terpene profiles (Figure 1). Four TPS genes, designated PpolyTPS1–PpolyTPS4, were identified from P. polycephalum. When E. coli-expressed PpolyTPS proteins were tested for terpene synthase activities, PpolyTPS1 was demonstrated to be a sesquiterpene synthase and PpolyTPS4 a monoterpene synthase (Figure 3
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Published 28 Nov 2019

Preparation of anthracene-based tetraperimidine hexafluorophosphate and selective recognition of chromium(III) ions

  • Qing-Xiang Liu,
  • Feng Yang,
  • Zhi-Xiang Zhao,
  • Shao-Cong Yu and
  • Yue Ding

Beilstein J. Org. Chem. 2019, 15, 2847–2855, doi:10.3762/bjoc.15.278

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  • autoimmune and cardiovascular diseases [11]. On the other hand, the excessive incorporation of chromium(III) is toxic to humans, and can cause cancer through the oxidation of DNA and some proteins [12][13][14]. Therefore, the detection of chromium(III) has a vital practical significance for human health
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Published 25 Nov 2019

Palladium-catalyzed synthesis and nucleotide pyrophosphatase inhibition of benzo[4,5]furo[3,2-b]indoles

  • Hoang Huy Do,
  • Saif Ullah,
  • Alexander Villinger,
  • Joanna Lecka,
  • Jean Sévigny,
  • Peter Ehlers,
  • Jamshed Iqbal and
  • Peter Langer

Beilstein J. Org. Chem. 2019, 15, 2830–2839, doi:10.3762/bjoc.15.276

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  • selected inhibitors on isozymes ENPP1 and ENPP3 modelled proteins were in accordance with in vitro experimental studies. Conclusion In conclusion, we have reported a convenient strategy for the preparation of benzo[4,5]furo[3,2-b]indoles based on Suzuki–Miyaura coupling reactions followed by Pd-catalyzed
  • were engaged in core and selected region of homology models [44]. Preparation of ligands and proteins The structures of the most active compounds were drawn by utilizing the MOE builder tool [45]. After introducing hydrogen atoms and charges to the prepared structures, the MMFF94x force field was
  • interactions and binding energies of the selected compounds within the binding pocket of modeled proteins were found out by using MOE (2014.0901). MOE site finder was used to locate the binding site while default setting of the triangular matcher placement method in combination with GBVI/WSA ∆G, were used to
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Published 22 Nov 2019

Chemical tuning of photoswitchable azobenzenes: a photopharmacological case study using nicotinic transmission

  • Lorenzo Sansalone,
  • Jun Zhao,
  • Matthew T. Richers and
  • Graham C. R. Ellis-Davies

Beilstein J. Org. Chem. 2019, 15, 2812–2821, doi:10.3762/bjoc.15.274

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  • ][20] compared to 2, so a simple one-step route can be used to install the maleimides. It is this functionality that allows coupling (often called "tethering", symbolized as "t" for tetherable in Scheme 1) of the probe with mutant proteins. In our case, we developed a three-step route to install the
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Published 21 Nov 2019

An improved, scalable synthesis of Notum inhibitor LP-922056 using 1-chloro-1,2-benziodoxol-3-one as a superior electrophilic chlorinating agent

  • Nicky J. Willis,
  • Elliott D. Bayle,
  • George Papageorgiou,
  • David Steadman,
  • Benjamin N. Atkinson,
  • William Mahy and
  • Paul V. Fish

Beilstein J. Org. Chem. 2019, 15, 2790–2797, doi:10.3762/bjoc.15.271

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  • , Kings Cross, London NW1 1AT, UK 10.3762/bjoc.15.271 Abstract Background: The carboxylesterase Notum has been shown to act as a key negative regulator of the Wnt signalling pathway by mediating the depalmitoleoylation of Wnt proteins. LP-922056 (1) is an orally active inhibitor of Notum. We are
  • Wnt proteins is required for efficient binding to Frizzled receptors and the subsequent signal transduction. The carboxylesterase Notum has been shown to act as a key negative regulator of the Wnt signalling pathway by specifically mediating the depalmitoleoylation of Wnt proteins [3][4]. LP-922056 (1
  • to just 7 steps from 16 and improves the overall yield to 40–50 %. Mouse pharmacokinetics for 1 Assessment of 1 in mouse liver microsomes (MLM) showed excellent metabolic stability (Cli 1.0 μL/min/mg protein) which predicts for low clearance in vivo. Binding to mouse plasma proteins (mPPB) was very
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Published 19 Nov 2019

A review of asymmetric synthetic organic electrochemistry and electrocatalysis: concepts, applications, recent developments and future directions

  • Munmun Ghosh,
  • Valmik S. Shinde and
  • Magnus Rueping

Beilstein J. Org. Chem. 2019, 15, 2710–2746, doi:10.3762/bjoc.15.264

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  • cathodes in the presence of chiral inductors, including tertiary amines, optically active proteins, and alkaloids [19][20], in 1975, Miller’s group reported the first example of the modification of electrodes via covalent binding [21]. They chemically modified air-oxidized graphite electrodes via treatment
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Published 13 Nov 2019

Fluorinated maleimide-substituted porphyrins and chlorins: synthesis and characterization

  • Valentina A. Ol’shevskaya,
  • Elena G. Kononova and
  • Andrei V. Zaitsev

Beilstein J. Org. Chem. 2019, 15, 2704–2709, doi:10.3762/bjoc.15.263

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  • covalently conjugates thiol groups of cysteine residues in proteins or peptides by the thio-Michael addition to the double bond of the maleimide to form a corresponding succinimidyl thioether. Conjugation of the cysteine sulfhydryl group with maleimide moieties allows us to prepare the bioconjugates
  • spectroscopy and mass spectrometry. These novel porphyrins and chlorins are expected to be efficient photosensitizers for cancer treatment. The presence of four maleimide groups in these compounds may provide improved binding with proteins in living systems. Synthesis of fluorinated maleimide-substituted
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Published 13 Nov 2019

Emission solvatochromic, solid-state and aggregation-induced emissive α-pyrones and emission-tuneable 1H-pyridines by Michael addition–cyclocondensation sequences

  • Natascha Breuer,
  • Irina Gruber,
  • Christoph Janiak and
  • Thomas J. J. Müller

Beilstein J. Org. Chem. 2019, 15, 2684–2703, doi:10.3762/bjoc.15.262

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  • prerequisites for the application of fluorescent substances in chemistry, medicine and materials science [1]. With this respect emissive small molecules [2], fluorescent proteins [3], and quantum dots have received considerable attention and remarkable progress in their synthesis and photophysics has been
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Published 12 Nov 2019

Plasma membrane imaging with a fluorescent benzothiadiazole derivative

  • Pedro H. P. R. Carvalho,
  • Jose R. Correa,
  • Karen L. R. Paiva,
  • Daniel F. S. Machado,
  • Jackson D. Scholten and
  • Brenno A. D. Neto

Beilstein J. Org. Chem. 2019, 15, 2644–2654, doi:10.3762/bjoc.15.257

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  • and by poor performances related to most of them. Therefore, many studies are still based on the use of WGA [16] (wheat germ agglutinin) or membrane proteins bearing fluorescent protein tags [11]. Water solubility is another issue that has to be considered. For the development of new fluorogenic dyes
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Published 06 Nov 2019
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