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E Farcaş et al.
Analytica chimica acta, 984, 211-222 (2017-08-28)
With the emergence of more challenging targets, a relatively new approach, fragment-based drug discovery (FBDD), proved its efficacy and gained increasing importance in the pharmaceutical industry. FBDD identifies low molecular-weight (MW) ligands (fragments) that bind to biologically important macromolecules, then
Seweryn Mroczek et al.
Nature communications, 8(1), 619-619 (2017-09-22)
FAM46C is one of the most frequently mutated genes in multiple myeloma. Here, using a combination of in vitro and in vivo approaches, we demonstrate that FAM46C encodes an active non-canonical poly(A) polymerase which enhances mRNA stability and gene expression.
Martina Sandberg Abelius et al.
Journal of reproductive immunology, 106, 100-109 (2014-07-23)
The immunological milieu in the placenta may be crucial for priming the developing foetal immune system. Early imbalances may promote the establishment of immune-mediated diseases in later life, including allergies. The initial exposure to allergens seems to occur in utero
N M Doll et al.
Science (New York, N.Y.), 367(6476), 431-435 (2020-01-25)
The plant embryonic cuticle is a hydrophobic barrier deposited de novo by the embryo during seed development. At germination, it protects the seedling from water loss and is, thus, critical for survival. Embryonic cuticle formation is controlled by a signaling
Joseph Vamecq et al.
European journal of medicinal chemistry, 45(7), 3101-3110 (2010-04-30)
Five bis-benzamidines were screened towards murine magnesium deficiency-dependent audiogenic seizures, unravelling two compounds with efficacious doses 50 (ED(50)) less than 10mg/kg. They were also screened against maximal electroshock and subcutaneous pentylenetetrazole-induced seizures, and explored for superoxide -scavenging activity. 1,2-Ethane bis-1-amino-4-benzamidine
Yu Cheng Zhu et al.
Pest management science, 68(5), 692-701 (2012-01-10)
The potential development of resistance to Bacillus thuringiensis (Bt) cotton and surging of non-targeted insects is a major risk in the durability of Bt plant technology. Midgut proteinases are involved in Bt activation and degradation. Proteinase inhibitors may be used
Leilani M Chirino et al.
European journal of immunology, 50(1), 48-55 (2019-09-19)
TAM receptors (Tyro3, Axl, and Mer) are receptor tyrosine kinases (RTKs) that are expressed by multiple immune cells including NK cells. Although RTKs typically enhance cellular functions, TAM receptor ligation blocks NK-cell activation. The mechanisms by which RTKs block NK-cell
L Ciesla et al.
Journal of chromatography. A, 1431, 138-144 (2016-01-18)
The α3β4α5 nAChR has been recently shown to be a useful target for smoking cessation pharmacotherapies. Herein, we report on the development and characterization of the α3β4α5 nicotinic receptor column by frontal displacement chromatography. The binding affinity of the nicotine
Kerstin K Viet et al.
Structure (London, England : 1993), 27(8), 1246-1257 (2019-06-11)
TRPML2 is the least structurally characterized mammalian transient receptor potential mucolipin ion channel. The TRPML family hallmark is a large extracytosolic/lumenal domain (ELD) between transmembrane helices S1 and S2. We present crystal structures of the tetrameric human TRPML2 ELD at
Janet Newman et al.
Journal of computer-aided molecular design, 26(5), 497-503 (2011-12-22)
Part of the latest SAMPL challenge was to predict how a small fragment library of 500 commercially available compounds would bind to a protein target. In order to assess the modellers' work, a reasonably comprehensive set of data was collected
Anaid Benitez et al.
Molecular cell, 71(4), 621-628 (2018-07-31)
FANCA is a component of the Fanconi anemia (FA) core complex that activates DNA interstrand crosslink repair by monoubiquitination of FANCD2. Here, we report that purified FANCA protein catalyzes bidirectional single-strand annealing (SA) and strand exchange (SE) at a level
Sheeba Jem Irudayam et al.
The journal of physical chemistry. B, 113(17), 5871-5884 (2009-04-09)
Two theoretical formulations are proposed and compared for the loss of translational and rotational entropy upon protein-ligand binding in water. The two theories share the same approach to evaluate the translational and rotational entropy of the ligand when bound. The
B G Cooper et al.
Osteoarthritis and cartilage, 25(7), 1143-1149 (2017-03-13)
Osteoarthritis (OA) is associated with increased articular cartilage hydraulic permeability and decreased maintenance of high interstitial fluid load support (IFLS) during articulation, resulting in increased friction on the cartilage solid matrix. This study assesses frictional response following in situ synthesis
Gaurav Dwivedi et al.
PLoS computational biology, 11(11), e1004582-e1004582 (2015-11-13)
Quantifying the magnitude and dynamics of protein oxidation during cell signaling is technically challenging. Computational modeling provides tractable, quantitative methods to test hypotheses of redox mechanisms that may be simultaneously operative during signal transduction. The interleukin-4 (IL-4) pathway, which has
Nikola Loncar et al.
Archives of insect biochemistry and physiology, 74(4), 232-246 (2010-06-16)
Trypsin-like enzyme (TLE) from the anterior midgut of Morimus funereus larvae was purified by anion exchange chromatography and gel filtration chromatography and characterized. Specific TLE activity was increased 322-fold by purification of the crude midgut extract. The purified enzyme had
Eshan Ghosh et al.
Cell reports, 28(13), 3287-3299 (2019-09-26)
Desensitization, signaling, and trafficking of G-protein-coupled receptors (GPCRs) are critically regulated by multifunctional adaptor proteins, β-arrestins (βarrs). The two isoforms of βarrs (βarr1 and 2) share a high degree of sequence and structural similarity; still, however, they often mediate distinct
Megan H Touchette et al.
ACS infectious diseases, 3(5), 336-348 (2017-03-10)
Outer membrane lipids in pathogenic mycobacteria are important for virulence and survival. Although the biosynthesis of these lipids has been extensively studied, mechanisms responsible for their assembly in the outer membrane are not understood. In the study of Gram-negative outer
Dhanashri Bagal et al.
Analytical chemistry, 81(18), 7801-7806 (2009-09-15)
The use of gas phase additives to stabilize noncovalent protein complexes in electrospray ionization mass spectrometry (ES-MS) is demonstrated for two protein-ligand interactions, an enzyme-small molecule inhibitor complex, and a protein-disaccharide complex. It is shown that the introduction of gas
Adam Kecskemeti et al.
Talanta, 166, 275-283 (2017-02-19)
This paper demonstrates the design, efficiency and applicability of a simple, inexpensive and high sample throughput microchip immobilized enzymatic reactor (IMER) for rapid protein digestion. The IMER contains conventional silica particles with covalently immobilized trypsin packed inside of a poly(dimethylsiloxane)
Anita de Ruiter et al.
Journal of computational chemistry, 34(12), 1024-1034 (2013-01-22)
The performances of Bennett's acceptance ratio method and thermodynamic integration (TI) for the calculation of free energy differences in protein simulations are compared. For the latter, the standard trapezoidal rule, Simpson's rule, and Clenshaw-Curtis integration are used as numerical integration
Amy Capes et al.
Bioorganic & medicinal chemistry, 20(4), 1607-1615 (2012-01-24)
Quinols have been developed as a class of potential anti-cancer compounds. They are thought to act as double Michael acceptors, forming two covalent bonds to their target protein(s). Quinols have also been shown to have activity against the parasite Trypanosoma
María Ángeles Corral-Rodríguez et al.
Blood, 117(26), 7164-7173 (2011-05-11)
Thrombin-catalyzed activation of coagulation factor V (FV) is an essential positive feedback reaction within the blood clotting system. Efficient processing at the N- (Arg(709)-Ser(710)) and C-terminal activation cleavage sites (Arg(1545)-Ser(1546)) requires initial substrate interactions with 2 clusters of positively charged
David J Busch et al.
Nature communications, 6, 7875-7875 (2015-07-25)
Assembly of highly curved membrane structures is essential to cellular physiology. The prevailing view has been that proteins with curvature-promoting structural motifs, such as wedge-like amphipathic helices and crescent-shaped BAR domains, are required for bending membranes. Here we report that
Xiuping Jiang et al.
International journal of biological macromolecules, 48(1), 129-133 (2010-10-26)
Snake venom thrombin-like enzymes (SVTLEs) are widely applied in the treatment of thrombotic diseases, however, the molecular mechanism of its inhibition by synthetic and natural proteinaceous inhibitors is not yet understood. Here we investigated effects of protease inhibitors including phenylmethylsulfonil
Arnaud Cutivet et al.
Journal of the American Chemical Society, 131(41), 14699-14702 (2009-09-25)
We demonstrate, on the example of trypsin, the use of water-soluble molecularly imprinted polymer microgels as specific enzyme inhibitors. Using a strong anchoring monomer, methacryloylaminobenzamidine, the growing polymer chains are confined to close proximity of the substrate recognition site of
Jude T Chenge et al.
The Journal of biological chemistry, 292(4), 1310-1329 (2016-12-10)
The Mycobacterium tuberculosis H37Rv genome encodes 20 cytochromes P450, including P450s crucial to infection and bacterial viability. Many M. tuberculosis P450s remain uncharacterized, suggesting that their further analysis may provide new insights into M. tuberculosis metabolic processes and new targets
Ashwini K Devkota et al.
Chembiochem : a European journal of chemical biology, 15(16), 2435-2442 (2014-09-17)
eEF-2K is a potential target for treating cancer. However, potent specific inhibitors for this enzyme are lacking. Previously, we identified 2,6-diamino-4-(2-fluorophenyl)-4H-thiopyran-3,5-dicarbonitrile (DFTD) as an inhibitor of eEF-2K. Here we describe its mechanism of action against eEF-2K, on the basis of
Kinya Terao et al.
Pancreas, 47(9), 1156-1164 (2018-09-08)
Severe acute pancreatitis is a highly lethal disease caused by systemic inflammatory response syndrome, leading to multiple organ failure. We recently showed that histidine-rich glycoprotein (HRG) supplemental therapy ameliorated septic acute respiratory distress syndrome due to unnecessary neutrophil activation and
Luca Mannocci et al.
Bioconjugate chemistry, 21(10), 1836-1841 (2010-09-03)
Collections of chemical compounds, individually attached to unique DNA fragments serving as amplifiable identification bar codes, are generally referred to as "DNA-encoded chemical libraries". Such libraries can be used for the de novo isolation of binding molecules against target proteins
Single-molecule approach to DNA minor-groove association dynamics.
Jorge Bordello et al.
Angewandte Chemie (International ed. in English), 51(30), 7541-7544 (2012-06-16)
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