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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. Ammonium hydroxide as the ultimate amino source for the synthesis of N-unprotected 3-tetrasubstituted aminooxindoles via catalyst-free direct amination

Author:
Yue, Jing; Ma, Xi-Tao; Liu, Xiong-Li; Wang, Jun-Xin; Liu, Xiong-Wei; Zhou, Ying
Source:
Green chemistry 2020 v.22 no.6 pp. 1837-1841
ISSN:
1463-9270
Subject:
antagonists,   etc   ; amination; ammonium hydroxide; cost effectiveness; green chemistry; primary amines;     Show all 6 Subjects
Abstract:
... The direct use of ammonium hydroxide in amination for the synthesis of primary amines is considered to be one of the major challenges in synthetic organic chemistry. Herein, the first example of catalyst-free direct amination of 3-halooxindoles with ammonium hydroxide to synthesize N-unprotected 3-tetrasubstituted aminooxindoles in high yields (up to 91% yield) is described. An enhancement of the ...
DOI:
10.1039/d0gc00130a

3. Reducing Treatment Burden in AMD

Author:
Apte, Rajendra S.
Source:
Cell 2020 v.180 no.6 pp. 1033
ISSN:
0092-8674
Subject:
antagonists,   etc   ; intraocular injection; vascular endothelial growth factor A;     Show all 3 Subjects
Abstract:
... VEGF-A antagonists have revolutionized wet AMD treatment. Several challenges remain including high treatment burden requiring repeated intraocular injections for persistent disease. Brolucizumab directly inhibits VEGF-A function, providing visual outcomes comparable to aflibercept (an FDA-approved VEGF-A antagonist). Anatomic retinal outcomes including retinal fluid, a marker of disease activity, ...
DOI:
10.1016/j.cell.2020.02.028

4. Geminin is required for Hox gene regulation to pattern the developing limb

Author:
Lewis, Emily M.A.; Sankar, Savita; Tong, Caili; Patterson, Ethan S.; Waller, Laura E.; Gontarz, Paul; Zhang, Bo; Ornitz, David M.; Kroll, Kristen L.
Source:
Developmental biology 2020 v.464 no.1 pp. 11-23
ISSN:
0012-1606
Subject:
antagonists,   etc   ; forelimbs; gene expression; hindlimbs; homeotic genes; models; mutants; transcription factors; vertebrates;     Show all 9 Subjects
Abstract:
... Development of the complex structure of the vertebrate limb requires carefully orchestrated interactions between multiple regulatory pathways and proteins. Among these, precise regulation of 5′ Hox transcription factor expression is essential for proper limb bud patterning and elaboration of distinct limb skeletal elements. Here, we identified Geminin (Gmnn) as a novel regulator of this process. A ...
DOI:
10.1016/j.ydbio.2020.05.007

5. Downregulation of GPR183 on infection restricts the early infection and intracellular replication of mycobacterium tuberculosis in macrophage

Author:
Tang, Jun; Shi, Ya'nan; Zhan, Lingjun; Qin, Chuan
Source:
Microbial pathogenesis 2020 v.145 pp. 104234
ISSN:
0882-4010
Subject:
antagonists,   etc   ; B-lymphocytes; Mycobacterium tuberculosis; T-lymphocytes; chemotaxis; ligands; macrophages; mutational analysis;     Show all 8 Subjects
Abstract:
... GPR183/EBI2 is a key chemotactic receptor for the positioning of B cells in lymphoid organs, and also for the migration of T cells and other immune cells. Here, we demonstrate that the downregulation of GPR183 in macrophage induced during Mtb infection restrains the bacterial early infection and intracellular replication. Overexpression of GPR183 or stimulation with its natural ligand favors Mtb r ...
DOI:
10.1016/j.micpath.2020.104234

6. BMP signaling plays a role in anterior-neural/head development, but not organizer activity, in the gastropod Crepidula fornicata

Author:
Lyons, Deirdre C.; Perry, Kimberly J.; Batzel, Grant; Henry, Jonathan Q.
Source:
Developmental biology 2020 v.463 no.2 pp. 135-157
ISSN:
0012-1606
Subject:
antagonists,   etc   ; Crepidula; evolution; ganglia; head; larvae; ligands; messenger RNA; ocelli; organoids; proteins; snails;     Show all 12 Subjects
Abstract:
... BMP signaling is involved in many aspects of metazoan development, with two of the most conserved functions being to pattern the dorsal-ventral axis and to specify neural versus epidermal fates. An active area of research within developmental biology asks how BMP signaling was modified over evolution to build disparate body plans. Animals belonging to the superclade Spiralia/Lophotrochozoa are exc ...
DOI:
10.1016/j.ydbio.2020.04.008

7. Endogenous oxytocin is essential for the buffering effects of pair housing against the increase in cocaine reward induced by social stress

Author:
Ferrer-Pérez, Carmen; Reguilón, Marina D.; Miñarro, José; Rodríguez-Arias, Marta
Source:
Physiology & behavior 2020 v.221 pp. 112913
ISSN:
0031-9384
Subject:
antagonists,   etc   ; cocaine; drugs; males; mice; oxytocin; pair housing; protective effect; psychosocial factors; social factors; therapeutics;     Show all 11 Subjects
Abstract:
... Social factors have a dual influence on addictive disorders. While social defeat stress in rodents increases the response to drug reward, positive social conditions, such as pair housing, increase stress resilience. The objective of the present study was to confirm whether oxytocin (OT) mediates this social buffering. To this end, male mice were housed in pairs and administered the OT receptor ant ...
DOI:
10.1016/j.physbeh.2020.112913

8. Angiotensin-(1-7) receptor Mas antagonist (A779) influenced gliosis and reduced synaptic density in the spinal cord after peripheral axotomy

Author:
Assis, Alex Dias; Mascarenhas, Fernanda Naves Araújo do Prado; Araújo, Fernanda de Assis; Santos, Robson Augusto Souza; Zanon, Renata Graciele
Source:
Peptides 2020 v.129 pp. 170329
ISSN:
0196-9781
Subject:
antagonists,   etc   ; Schwann cells; astrocytes; nerve tissue; neurons; peptides; rodents; spinal cord;     Show all 8 Subjects
Abstract:
... The peptide angiotensin-(1-7) [Ang (1-7)] and its receptor Mas are involved in controlling arterial pressure and display actions on the nervous system. In a previous study, our laboratory showed that A779 [(peptidyl antagonist of the Ang-(1–7)] treatment had a negative effect following a lesion of the sciatic nerve, possibly by delaying the responses of Schwann cells, resulting in a decreased axon ...
DOI:
10.1016/j.peptides.2020.170329

9. 5-HT2A receptor-mediated PKCδ phosphorylation is critical for serotonergic impairments induced by p-chloroamphetamine in mice

Author:
Phan, Dieu Hien; Shin, Eun-Joo; Sharma, Naveen; Hoang Yen, Tran Phi; Dang, Duy-Khanh; Lee, Yong Sup; Lee, Yu Jeung; Nah, Seung-Yeol; Cheong, Jae Hoon; Jeong, Ji Hoon; Kim, Hyoung-Chun
Source:
Food and chemical toxicology 2020 v.141 pp. 111395
ISSN:
0278-6915
Subject:
antagonists,   etc   ; amphetamine; enzyme inhibitors; gene expression; genes; mice; neurotoxicity; phosphorylation; protein kinase C; toxicology;     Show all 10 Subjects
Abstract:
... p-Chloroamphetamine (PCA), an amphetamine derivative, has been shown to induce serotonergic toxicity. However, the precise mechanism of serotonergic toxicity induced by PCA remains unclear. In this study, PCA treatment (20 mg/kg, i.p.) did not significantly change 5-HT₁A receptor gene expression, but significantly increased 5-HT₂A receptor gene expression. Furthermore, 5-HT₂A receptor antagonist M ...
DOI:
10.1016/j.fct.2020.111395

10. Ecotoxicological equilibria of triclosan in Microtox, XenoScreen YES/YAS, Caco2, HEPG2 and liposomal systems are affected by the occurrence of other pharmaceutical and personal care emerging contaminants

Author:
Miro, Manuel; Oliver, Miquel; Kudłak, Błażej; Wieczerzak, Monika; Reis, Salette; Lima, Sofia A.C.; Segundo, Marcela A.; Miró, Manuel
Source:
The Science of the total environment 2020 v.719 pp. 137358
ISSN:
0048-9697
Subject:
antagonists,   etc   ; antagonism; diclofenac; ecotoxicology; human cell lines; methylparaben; models; toxicity; toxicity testing; triclosan;     Show all 10 Subjects
Abstract:
... Contaminants of emerging concern may be considered as any chemicals or factors whose unintended continuous release and persistence in the environment may lead to any observable undesirable response of living beings. Still not much is known on reciprocal toxicological impact of given chemicals when present in binary or more complex mixtures. In this work, an attempt was thus undertaken to study the ...
DOI:
10.1016/j.scitotenv.2020.137358

11. Improved synthesis of sterically encumbered heteroaromatic biaryls from aromatic β-keto esters

Author:
Rosen, Brandon R.; Ul Sharif, Ehesan; Miles, Dillon H.; Chan, Nicholas S.; Leleti, Manmohan R.; Powers, Jay P.
Source:
Tetrahedron letters 2020 v.61 no.20 pp. 151855
ISSN:
0040-4039
Subject:
antagonists,   etc   ; aromatic compounds; chemical structure; chromatography; condensation reactions; esters; guanidines; heterocyclic compounds;     Show all 8 Subjects
Abstract:
... A protocol for the synthesis of hindered 4-aryl 2-aminopyrimidines from β–keto esters is described. The process employs trifluoroethanol as an essential additive to promote the guanidine condensation reaction, enabling the synthesis of 25 aryl- and heteroaryl substituted aminopyrimidines in good yields and high purities with no column chromatography. The conditions described herein are readily sca ...
DOI:
10.1016/j.tetlet.2020.151855

12. Cytokine release syndrome in severe COVID-19: interleukin-6 receptor antagonist tocilizumab may be the key to reduce mortality

Author:
Zhang, Chi; Wu, Zhao; Li, Jia-Wen; Zhao, Hong; Wang, Gui-Qiang
Source:
International journal of antimicrobial agents 2020 v.55 no.5 pp. 105954
ISSN:
0924-8579
Subject:
antagonists,   etc   ; Coronavirus infections; death; drugs; interleukin-6; mortality; patients; people; signal transduction; viral pneumonia; China;     Show all 11 Subjects
Abstract:
... Since December 2019, a viral pneumonia, named coronavirus disease 2019 (COVID-19), from Wuhan, China, has swept the world. Although the case fatality rate is not high, the number of people infected is large and there is still a large number of patients dying. With the collation and publication of more and more clinical data, a large number of data suggest that there are mild or severe cytokine sto ...
DOI:
10.1016/j.ijantimicag.2020.105954
PubMed:
32234467
PubMed Central:
PMC7118634

13. Triterpene Glycosides Isolated from the Edible Sea Cucumber Bohadschia vitiensis and Their Antagonistic Activity against Transient Receptor Potential Ankyrin 1

Author:
Choi, Hansol; Oh, Chulhong; Hyun, JeongMi; Yang, Jeungeun; Song, Myung Jin; Lee, Hyi-Seung; Lee, Yeon-Ju
Source:
Journal of agricultural and food chemistry 2020 v.68 no.19 pp. 5349-5355
ISSN:
1520-5118
Subject:
antagonists,   etc   ; Bohadschia; analgesics; glycosides; inhibitory concentration 50; invertebrates; ion channels; pain; screening; triterpenoids;     Show all 10 Subjects
Abstract:
... Transient receptor potential ankyrin 1 (TRPA1) is a cation channel that plays a critical role in the occurrence and transmission of pain. By screening 393 marine invertebrate extracts for their antagonistic activity against TRPA1, it was found that the extract of the edible sea cucumber Bohadschia vitiensis had a remarkable potency. Bioassay-guided separation of the extract resulted in the isolati ...
DOI:
10.1021/acs.jafc.0c00847

14. Heparan sulfate proteoglycans regulate BMP signalling during neural crest induction

Author:
Pegge, James; Tatsinkam, Arnold Junior; Rider, Christopher C.; Bell, Esther
Source:
Developmental biology 2020 v.460 no.2 pp. 108-114
ISSN:
0012-1606
Subject:
antagonists,   etc   ; Xenopus laevis; bone morphogenetic proteins; ectoderm; heparan sulfate; mechanism of action; neural crest; proteoglycans;     Show all 8 Subjects
Abstract:
... Bone morphogenetic protein (BMP) signalling is key to many developmental processes, including early regionalisation of the ectoderm. The neural crest is induced here by a combination of BMP and Wnt signals from nearby tissues with many secreted factors contributing to its initial specification at the neural plate border. Gremlin 1 (Grem1) is a secreted BMP antagonist expressed in the neural crest ...
DOI:
10.1016/j.ydbio.2019.12.015
PubMed:
31883440
PubMed Central:
PMC7196931

15. Structural dynamics of the GluK3-kainate receptor neurotransmitter binding domains revealed by cryo-EM

Author:
Kumari, Jyoti; Bendre, Ameya D.; Bhosale, Sumedha; Vinnakota, Rajesh; Burada, Ananth P.; Tria, Giancarlo; Ravelli, Raimond B.G.; Peters, Peter J.; Joshi, Manali; Kumar, Janesh
Source:
International journal of biological macromolecules 2020 v.149 pp. 1051-1058
ISSN:
0141-8130
Subject:
antagonists,   etc   ; agonists; electron microscopy; functional properties; glutamate receptors; molecular dynamics; neurotransmitters; physiology; simulation models; synapse;     Show all 10 Subjects
Abstract:
... Kainate receptors belong to the ionotropic glutamate receptor family and play critical roles in the regulation of synaptic networks. The kainate receptor subunit GluK3 has unique functional properties and contributes to presynaptic facilitation at the hippocampal mossy fiber synapses along with roles at the post-synapses. To gain structural insights into the unique functional properties and dynami ...
DOI:
10.1016/j.ijbiomac.2020.01.282

16. A reduction of primary cilia but not hedgehog signaling disrupts morphogenesis in testicular organoids

Author:
Goldsmith, Taylor M.; Sakib, Sadman; Webster, Dennis; Carlson, Daniel F.; Van der Hoorn, Frans; Dobrinski, Ina
Source:
Cell and tissue research 2020 v.380 no.1 pp. 191-200
ISSN:
0302-766X
Subject:
antagonists,   etc   ; Sertoli cells; cilia; cyclopamine; gene editing; gene silencing; mammals; morphogenesis; organoids; signal transduction; somatic cells;     Show all 11 Subjects
Abstract:
... Most mammalian cells possess a single, non-motile primary cilium that plays an important role in mediating cellular signaling pathways, such as Hedgehog (Hh) signaling. Primary cilia are present on testicular somatic cells and demonstrate a temporal expression during development; however, their role in testicular morphogenesis is not well characterized. To investigate the role of primary cilia and ...
DOI:
10.1007/s00441-019-03121-8

17. Melanin-concentrating hormone (MCH) in the median raphe nucleus: Fibers, receptors and cellular effects

Author:
Pascovich, Claudia; Lagos, Patricia; Urbanavicius, Jessika; Devera, Andrea; Rivas, Mayda; Costa, Alicia; López Hill, Ximena; Falconi, Atilio; Scorza, Cecilia; Torterolo, Pablo
Source:
Peptides 2020 v.126 pp. 170249
ISSN:
0196-9781
Subject:
antagonists,   etc   ; cats; fluorescent dyes; mental depression; neurons; pathophysiology; rats; receptors; rhodamines; sleep; urethane;     Show all 11 Subjects
Abstract:
... Serotonergic neurons of the median raphe nucleus (MnR) and hypothalamic melanin-concentrating hormone (MCH)-containing neurons, have been involved in the control of REM sleep and mood.In the present study, we examined in rats and cats the anatomical relationship between MCH-containing fibers and MnR neurons, as well as the presence of MCHergic receptors in these neurons. In addition, by means of i ...
DOI:
10.1016/j.peptides.2019.170249

18. Sulfadiazine Masquerading as a Natural Product from Scilla madeirensis (Scilloideae)

Author:
Robertson, Luke P.; Moodie, Lindon W. K.; Holland, Darren C.; Jandér, K. Charlotte; Göransson, Ulf
Source:
Journal of natural products 2020 v.83 no.4 pp. 1305-1308
ISSN:
1520-6025
Subject:
antagonists,   etc   ; Scilla madeirensis; alkaloids; antibiotics; bioactive properties; biosynthesis; bulbs; nuclear magnetic resonance spectroscopy; phylogeny; sulfadiazine;     Show all 10 Subjects
Abstract:
... The structure of 2,4-(4′-aminobenzenamine)pyrimidine (1), a pyrimidine alkaloid previously isolated from the bulbs of Scilla madeirensis (Asparagaceae, synonym Autonoë madeirensis), has been revised. These conclusions were met via comparison of reported NMR and EIMS data with those obtained from synthetic standards. The corrected structure is the antibiotic sulfadiazine (2), which has likely been ...
DOI:
10.1021/acs.jnatprod.0c00163

19. Modified synthesis of the peptidomimetic natriuretic peptide receptor-C antagonist M372049

Author:
Porter, Jacob D.; Lindeman, Sergey V.; Dockendorff, Chris
Source:
Tetrahedron letters 2020 v.61 no.12 pp. 151654
ISSN:
0040-4039
Subject:
antagonists,   etc   ; chemical reactions; crystal structure; hypertension; lactams; natriuretic peptide receptors; natriuretic peptides; sodium; stereochemistry;     Show all 9 Subjects
Abstract:
... The Natriuretic Peptide Receptors (NPRs) regulate vascular sodium levels and have been of significant interest for the potential treatment of hypertension and related cardiovascular complications. The peptidomimetic antagonist M372049 is a valuable probe for the study of NPR-C signaling, unfortunately it is presently not commercially available. Described is a detailed protocol for its synthesis th ...
DOI:
10.1016/j.tetlet.2020.151654
PubMed:
32153307
PubMed Central:
PMC7062365

20. Melanin-like nanoparticles loaded with an angiotensin antagonist for an improved photothermal cancer therapy

Author:
Zhou, Zhengjie; Yan, Yang; Zhang, Qiang; Cheng, Yiyun
Source:
Biomaterials science 2020 v.8 no.6 pp. 1658-1668
ISSN:
2047-4849
Subject:
antagonists,   etc   ; acidity; blood; cancer therapy; collagen; in vivo studies; nanoparticles; neoplasms; transforming growth factor beta 1;     Show all 9 Subjects
Abstract:
... An abnormal tumor growth induces solid stress in tumors, thus reducing blood perfusion. As a result, the impaired blood perfusion, with dense interstitial matrix in tumors significantly reduces the penetration and efficacy of nanotherapeutics. In this study, we have developed a losartan-loaded polydopamine nanoparticle (PLST) for the enhanced delivery of nanoparticles to tumors and improved photot ...
DOI:
10.1039/c9bm01843c