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1. Correction to: An estrogen antagonist, cyclofenil, has anti-dengue-virus activity

Author:
Tohma, Daiki; Tajima, Shigeru; Kato, Fumihiro; Sato, Hirotaka; Kakisaka, Michinori; Hishiki, Takayuki; Kataoka, Michiyo; Takeyama, Haruko; Lim, Chang-Kweng; Aida, Yoko; Saijo, Masayuki
Source:
Archives of virology 2019 v.164 no.1 pp. 235
ISSN:
0304-8608
Subject:
antagonists,   etc   ; actin; antibodies; estrogens;     Show all 4 Subjects
Abstract:
... We would like to correct the information on the antibody used in this study. In Fig. 5 of the article, cellular β-actin was detected as an internal control using anti-β-actin antibody (Fujifilm Wako Pure Chemicals, #017-24573). ...
DOI:
10.1007/s00705-018-4107-0

2. Expanding the synthesizable multisubstituted benzo[b]thiophenes via 6,7-thienobenzynes generated from o-silylaryl triflate-type precursors

Author:
Yoshida, Suguru; Kuribara, Tomoko; Morita, Takamoto; Matsuzawa, Tsubasa; Morimoto, Kazushi; Kobayashi, Takuya; Hosoya, Takamitsu
Source:
RSC advances 2018 v.8 no.39 pp. 21754-21758
ISSN:
2046-2069
Subject:
antagonists,   etc   ; fluorides; ions; thiophenes;     Show all 4 Subjects
Abstract:
... Various 2,3-disubstituted 6,7-thienobenzynes have been efficiently generated from the corresponding o-silylaryl triflate-type precursors by activation with fluoride ions. The method has expanded the scope of synthesizable multisubstituted benzothiophenes, including those with various heteroatom substituents, and can be applied to the synthesis of EP4 antagonist analogs. ...
DOI:
10.1039/c8ra04035d

3. Histamine H1 receptor antagonists enhance the efficacy of antibacterials against Escherichia coli

Author:
Bruer, G. G.; Hagedorn, P.; Kietzmann, M.; Tohamy, A. F.; Filor, V.; Schultz, E.; Mielke-Kuschow, S.; Meissner, J.
Source:
BMC veterinary research 2019 v.15 no.1 pp. 55
ISSN:
1746-6148
Subject:
antagonists,   etc   ; Escherichia coli; antihistamines; histamine; microorganisms; minimum inhibitory concentration;     Show all 6 Subjects
Abstract:
... BACKGROUND: H₁ receptor antagonists are commonly used for the treatment of allergic diseases. The aim of this study was to find out, if antihistaminic compounds like mepyramine have the ability to influence the activity of antibacterials. Therefore, the checkerboard method was chosen to detect these possible effects in vitro. Studies were performed with two different Escherichia coli (E. coli) str ...
DOI:
10.1186/s12917-019-1797-9

4. β-Cyclodextrin-copper (II) complex as chiral selector in capillary electrophoresis for the enantioseparation of β-blockers

Author:
Hu, Shaoqiang; Zhang, Min; Li, Feng; Breadmore, Michael C.
Source:
Journal of chromatography 2019 v.1596 pp. 233-240
ISSN:
0021-9673
Subject:
beta-adrenergic antagonists,   etc   ; beta-cyclodextrin; capillary electrophoresis; chromatography; copper; enantiomers;     Show all 6 Subjects
Abstract:
... The Copper (II) complex of β-cyclodextrin (β-CD), β-CDCu2, was prepared and used as a chiral selector for the enantioseparation of 11 β-blockers by capillary electrophoresis. Resolution for 10 pairs of enantiomers was greater than 1.9 and for the four stereoisomers of labetalol (with two chiral centers), the closest two peaks had a resolution of 1.2. The resolution was superior to that obtained by ...
DOI:
10.1016/j.chroma.2019.03.019

5. Yokukansan-induced reduction of ethanol preference is associated with antagonism of 5-HT3 receptors

Author:
Nakamura, Yukiko; Kondo, Makoto; Koyama, Yoshihisa; Shimada, Shoichi
Source:
Phytomedicine 2019 v.59 pp. 152897
ISSN:
0944-7113
Subject:
antagonists,   etc   ; Uncaria; alkaloids; antagonism; diet; ethanol; mice; receptors;     Show all 8 Subjects
Abstract:
... We recently reported that alkaloids in Uncaria hook (a constituent of yokukansan) contribute to antagonism of 5-HT3 receptors. Many studies have reported that 5-HT3 receptor antagonists reduce alcohol preference. However, the effect of yokukansan on alcohol preference is not clear.This study was performed to investigate the direct effect of yokukansan on alcohol preference and the effect of 5-HT3 ...
DOI:
10.1016/j.phymed.2019.152897

6. Quiescence Modulates Stem Cell Maintenance and Regenerative Capacity in the Aging Brain

Author:
Kalamakis, Georgios; Brüne, Daniel; Ravichandran, Srikanth; Bolz, Jan; Fan, Wenqiang; Ziebell, Frederik; Stiehl, Thomas; Catalá-Martinez, Francisco; Kupke, Janina; Zhao, Sheng; Llorens-Bobadilla, Enric; Bauer, Katharina; Limpert, Stefanie; Berger, Birgit; Christen, Urs; Schmezer, Peter; Mallm, Jan Philipp; Berninger, Benedikt; Anders, Simon; del Sol, Antonio; Marciniak-Czochra, Anna; Martin-Villalba, Ana
Source:
Cell 2019 v.176 no.6 pp. 1407-1419.e14
ISSN:
0092-8674
Subject:
antagonists,   etc   ; brain; homeostasis; mice; neural stem cells; neutralization; transcriptomics;     Show all 7 Subjects
Abstract:
... The function of somatic stem cells declines with age. Understanding the molecular underpinnings of this decline is key to counteract age-related disease. Here, we report a dramatic drop in the neural stem cells (NSCs) number in the aging murine brain. We find that this smaller stem cell reservoir is protected from full depletion by an increase in quiescence that makes old NSCs more resistant to re ...
DOI:
10.1016/j.cell.2019.01.040

7. Determinants of Orexin Receptor Binding and Activation—A Molecular Dynamics Study

Author:
Karhu, Lasse; Magarkar, Aniket; Bunker, Alex; Xhaard, Henri
Source:
TheJournal of physical chemistry 2019 v.123 no.12 pp. 2609-2622
ISSN:
1520-5207
Subject:
antagonists,   etc   ; agonists; ligands; molecular dynamics; neuropeptides; simulation models;     Show all 6 Subjects
Abstract:
... We assess the stability of two previously suggested binding modes for the neuropeptide orexin-A in the OX₂ receptor through extensive molecular dynamics simulations. As the activation determinants of the receptor remain unknown, we simulated an unliganded receptor and two small-molecular ligands, the antagonist suvorexant and the agonist Nag26 for comparison. Each system was simulated in pure POPC ...
DOI:
10.1021/acs.jpcb.8b10220

8. Synthesis of 4-Iodoisoquinolin-1(2H)-ones by a Dirhodium(II)-Catalyzed 1,4-Bisfunctionalization of Isoquinolinium Iodide Salts

Author:
Fang, Zaixiang; Wang, Yi; Wang, Yuanhua
Source:
Organic letters 2019 v.21 no.2 pp. 434-438
ISSN:
1523-7052
Subject:
antagonists,   etc   ; aerobic conditions; chemical structure; iodination; organic compounds; oxidation; salts;     Show all 7 Subjects
Abstract:
... An efficient Rh₂(II,II)-catalyzed reaction has been developed under mild conditions. This synthetic method proceeds through iodination/oxidation of readily available isoquinolinium iodide salts under aerobic conditions with good to excellent yields. 4-Iodoisoquinolin-1(2H)-ones are important building blocks for biologically and medicinally important compounds. The developed methodology was applied ...
DOI:
10.1021/acs.orglett.8b03614

9. Molecular Initiating Events of Bisphenols on Androgen Receptor-Mediated Pathways Provide Guidelines for in Silico Screening and Design of Substitute Compounds

Author:
Chen, Qinchang; Wang, Xiaoxiang; Tan, Haoyue; Shi, Wei; Zhang, Xiaowei; Wei, Si; Giesy, John P.; Yu, Hongxia
Source:
Environmental science & technology letters 2019 v.6 no.4 pp. 205-210
ISSN:
2328-8930
Subject:
antagonists; hormone antagonists,   etc   ; agonists; androgen receptors; guidelines; hydrophobicity; in vitro studies; molecular dynamics; quantitative analysis; screening; simulation models;     Show all 11 Subjects
Abstract:
... Bisphenols (BPs) have the potential to interfere with the androgen receptor (AR). However, in silico screening and substitute design were difficult because little was known about the mechanisms by which BPs interfere with AR-mediated molecular initiating events (MIEs). Here, the AR disrupting effects and associated mechanisms of 15 BPs were evaluated by in vitro assays and molecular dynamics simul ...
DOI:
10.1021/acs.estlett.9b00073

10. Correction: Improving the inhibitory effect of CXCR4 peptide antagonist in tumor metastasis with an acetylated PAMAM dendrimer

Author:
Liu, Changliang; Duan, Hongyang; Zhao, Zijian; Li, Wenzhe; Ma, Lilusi; Fang, Xiaocui; Wang, Chen; Yang, Yanlian
Source:
RSC advances 2018 v.8 no.73 pp. 42253
ISSN:
2046-2069
Subject:
antagonists,   etc   ; CXCR4 receptor; dendrimers; metastasis; neoplasms;     Show all 5 Subjects
Abstract:
... Correction for ‘Improving the inhibitory effect of CXCR4 peptide antagonist in tumor metastasis with an acetylated PAMAM dendrimer’ by Changliang Liu et al., RSC Adv., 2018, 8, 39948–39956. ...
DOI:
10.1039/c8ra90102c

11. Divergent Reactivity of gem-Difluoro-enolates toward Nitrogen Electrophiles: Unorthodox Nitroso Aldol Reaction for Rapid Synthesis of α-Ketoamides

Author:
Reddy, Mallu Kesava; Ramakrishna, Isai; Baidya, Mahiuddin
Source:
Organic letters 2018 v.20 no.15 pp. 4610-4613
ISSN:
1523-7052
Subject:
antagonists,   etc   ; Lewis acids; amination; ketones; moieties; nitrogen;     Show all 6 Subjects
Abstract:
... An amination reaction of in situ generated gem-difluoro-enolates has been explored with electrophilic nitrogen sources. While their exposure to azodicarboxylates smoothly produced fluorinated α-amino ketones, reaction with nitrosoarenes (nitroso aldol reaction) furnished α-ketoamides in very high yields (up to 94%). The reaction is very fast (typically completed within 5 min) and scalable and tole ...
DOI:
10.1021/acs.orglett.8b01900

12. N-3 alkylation of uracils with unprotected amino alcohols using the Mitsunobu reaction

Author:
Lafitte, Guillaume; Beillard, Audrey; Chambon, Sandrine; Soulet, Catherine; Dumais, Laurence; Mouis, Grégoire; Fournier, Jean-François; Clary, Laurence; Bouix-Peter, Claire; Tomas, Loic; Harris, Craig S.
Source:
Tetrahedron letters 2018 v.59 no.3 pp. 256-259
ISSN:
0040-4039
Subject:
antagonists,   etc   ; alkylation; amino alcohols; chemical structure;     Show all 4 Subjects
Abstract:
... During our search for novel CGRP antagonists, we had great difficulty in accessing one of our key motifs. Herein, we communicate how we solved the problem by an unprecedented Mitsunobu alkylation using unprotected amino alcohols. ...
DOI:
10.1016/j.tetlet.2017.12.024

13. In silico binding of 4,4'‐bisphenols predicts in vitro estrogenic and antiandrogenic activity

Author:
Conroy‐Ben, Otakuye; Garcia, Isabel; Teske, Sondra S.
Source:
Environmental toxicology 2018 v.33 no.5 pp. 569-578
ISSN:
1520-4081
Subject:
antagonists; hormone antagonists,   etc   ; androgen receptors; binding capacity; bioassays; estradiol; hydrogen bonding; phenol; pollutants; testosterone; wastes;     Show all 11 Subjects
Abstract:
... Bisphenols, anthropogenic pollutants, leach from consumer products and have potential to be ingested and are excreted in waste. The endocrine disrupting effects of highly manufactured bisphenols (BPA, BPS, and BPF) are known, however the activities of others are not. Here, the estrogenic and androgenic activities of a series of 4,4'‐bisphenols that vary at the inter‐connecting bisphenol bridge wer ...
DOI:
10.1002/tox.22539

14. Long-term properties and end-of-life of polymers from renewable resources

Author:
Badia, J.D.; Gil-Castell, O.; Ribes-Greus, A.
Source:
Polymer Degradation and Stability 2017 v.137 pp. 35-57
ISSN:
0141-3910
Subject:
antagonists,   etc   ; durability; polymers; renewable resources;     Show all 4 Subjects
Abstract:
... The long-term properties and end-of-life of polymers are not antagonist issues. They actually are inherently linked by the duality between durability and degradation. The control of the service-to-disposal pathway at useful performance, along with low-impact disposal represents an added-value. Therefore, the routes of design, production, and discarding of bio-based polymers must be carefully strat ...
DOI:
10.1016/j.polymdegradstab.2017.01.002

15. Role of the lipoxin A4 receptor in the development of neutrophil extracellular traps in Leishmania infantum infection

Author:
Wei, Furong; Gong, Wenci; Wang, Junyun; Yang, Yuetao; Liu, Jianxiu; Wang, Yanjuan; Cao, Jianping
Source:
Parasites & vectors 2019 v.12 no.1 pp. 275
ISSN:
1756-3305
Subject:
antagonists,   etc   ; Leishmania infantum; extrusion; histones; inflammation; leishmaniasis; mechanism of action; neutrophils; promastigotes; therapeutics;     Show all 10 Subjects
Abstract:
... BACKGROUND: Neutrophils play an immunomodulatory role through the release of neutrophil extracellular traps (NETs). NETs are released in response to Leishmania infection, but the mechanism of NET extrusion has not been elucidated. The lipoxin A4 receptor on neutrophils is crucial for the inflammatory response and immune regulation of many diseases, including Leishmania infection. Therefore, in the ...
DOI:
10.1186/s13071-019-3530-8

16. Phagocytosis of live and dead Escherichia coli and Staphylococcus aureus in human whole blood is markedly reduced by combined inhibition of C5aR1 and CD14

Author:
Skjeflo, E.W.; Christiansen, D.; Landsem, A.; Stenvik, J.; Woodruff, T.M.; Espevik, T.; Nielsen, E.W.; Mollnes, T.E.
Source:
Molecular immunology 2019 v.112 pp. 131-139
ISSN:
0161-5890
Subject:
antagonists,   etc   ; Escherichia coli; Gram-positive bacteria; Staphylococcus aureus; complement; cytokines; flow cytometry; humans; inflammation; monocytes; phagocytosis;     Show all 11 Subjects
Abstract:
... Sepsis is a dysregulated host response to infection. The aim of this study was to investigate the effects of complement- and CD14 inhibition on phagocytosis of live and dead Gram-negative and Gram-positive bacteria in human whole blood.Lepirudin-anticoagulated blood was incubated with live or dead E. coli or S. aureus at 37 °C for 120 min with or without the C5aR1 antagonist PMX53 and/or anti-CD14 ...
DOI:
10.1016/j.molimm.2019.03.014

17. Simple minimally-invasive automatic antidote delivery device (A2D2) towards closed-loop reversal of opioid overdose

Author:
Dhowan, Bahar; Lim, Jongcheon; MacLean, Michael D.; Berman, Alycia G.; Kim, Min Ku; Yang, Qi; Linnes, Jacqueline; Lee, Chi Hwan; Goergen, Craig J.; Lee, Hyowon
Source:
Journal of controlled release 2019 v.306 pp. 130-137
ISSN:
0168-3659
Subject:
antagonists,   etc   ; antidotes; drug delivery systems; in vivo studies; magnetic fields; mice; naloxone; overdose; patients;     Show all 9 Subjects
Abstract:
... With approximately 48,000 attributed deaths in 2017, the opioid overdose is now the leading cause of death amongst Americans under the age of 50. The overdose process can be interrupted by the administration of naloxone, a safe and effective opiate antagonist that can reverse the effects of overdose and minimizing the delay in administering the antidote is critical in preventing permanent damage t ...
DOI:
10.1016/j.jconrel.2019.05.041

18. Deciphering the mode of action of pollutants impairing the fish larvae escape response with the vibrational startle response assay

Author:
Faria, Melissa; Bedrossiantz, Juliette; Prats, Eva; Rovira Garcia, Xavier; Gómez-Canela, Cristian; Piña, Benjamin; Raldúa, Demetrio
Source:
The Science of the total environment 2019 v.672 pp. 121-128
ISSN:
0048-9697
Subject:
antagonists,   etc   ; escape behavior; fish larvae; habituation; imidacloprid; mechanism of action; muscarine receptors; neurotoxicity; neurotransmitters; pollutants; scopolamine;     Show all 11 Subjects
Abstract:
... The escape response evoked by vibrational stimuli and its habituation, essential behaviors for fish larvae survival, can be altered by neurotoxic environmental pollutants commonly found in our aquatic ecosystems.In this study we have analyzed the suitability of the Vibrational Startle Response Assay (VSRA) to obtain mechanistic information about the mode of action (MoA) of the chemicals impairing ...
DOI:
10.1016/j.scitotenv.2019.03.469

19. Endogenous opioid modulation of food intake and body weight: Implications for opioid influences upon motivation and addiction

Author:
Bodnar, Richard J.
Source:
Peptides 2019 v.116 pp. 42-62
ISSN:
0196-9781
Subject:
antagonists,   etc   ; agonists; body weight; brain; drugs; exons; food intake; motivation; opioid peptides; receptors; rodents; weight control;     Show all 12 Subjects
Abstract:
... This review is part of a special issue dedicated to Opioid addiction, and examines the influential role of opioid peptides, opioid receptors and opiate drugs in mediating food intake and body weight control in rodents. This review postulates that opioid mediation of food intake was an example of “positive addictive” properties that provide motivational drives to maintain opioid-seeking behavior an ...
DOI:
10.1016/j.peptides.2019.04.008

20. Ligand discrimination during virtual screening of the CB1 cannabinoid receptor crystal structures following cross-docking and microsecond molecular dynamics simulations

Author:
Loo, Jason S. E.; Emtage, Abigail L.; Murali, Lahari; Lee, Sze Siew; Kueh, Alvina L. W.; Alexander, Stephen P. H.
Source:
RSC advances 2019 v.9 no.28 pp. 15949-15956
ISSN:
2046-2069
Subject:
antagonists,   etc   ; agonists; crystal structure; drugs; ligands; markets; molecular dynamics; prediction; screening; simulation models; therapeutics;     Show all 11 Subjects
Abstract:
... The therapeutic potential of the CB1 cannabinoid receptor remains underexploited with only a few synthetic ligands on the market. The crystal structures of both the inactive and active-state CB1 receptor have recently been solved, allowing for unprecedented opportunities in structure-based drug discovery applications such as virtual screening. In this study, we have investigated the virtual screen ...
DOI:
10.1039/c9ra01095e