Month: October 2022

Jiang, Ming-jie; Chen, Yi-yun; Dai, Juan-juan; Gu, Dian-na; Mei, Zhu; Liu, Fu-rao; Huang, Qian; Tian, Ling published the artcile< Dying tumor cell-derived exosomal miR-194-5p potentiates survival and repopulation of tumor repopulating cells upon radiotherapy in pancreatic cancer>, Product Details of C30H30Cl2N6O2, the main research area is pancreatic cancer miR1945p proliferation DNA damage; Aspirin; DNA damage response; Exosome; Pancreatic cancer; Radiotherapy; Tumor repopulating cell; Tumor repopulation; microRNA.

Tumor repopulation is a major cause of radiotherapy failure. However, TRCs also suffer DNA damage after radiotherapy, and might undergo mitotic catastrophe under the stimulation of proliferative factors released by dying cells. Hence, we intend to find out how these paradoxical biol. processes coordinated to potentiate tumor repopulation after radiotherapy. Tumor repopulation models in vitro and in vivo were used for evaluating the therapy response and dissecting underlying mechanisms. RNA-seq was performed to find out the signaling changes and identify the significantly changed miRNAs. qPCR, western blot, IHC, FACS, colony formation assay, etc. were carried out to analyze the mols. and cells. Exosomes derived from dying tumor cells induced G1/S arrest and promoted DNA damage response to potentiate survival of TRCs through delivering miR-194-5p, which further modulated E2F3 expression. Moreover, exosomal miR-194-5p alleviated the harmful effects of oncogenic HMGA2 under radiotherapy. After a latent time, dying tumor cells further released a large amount of PGE2 to boost proliferation of the recovered TRCs, and orchestrated the repopulation cascades. Of note, low-dose aspirin was found to suppress pancreatic cancer repopulation upon radiation via inhibiting secretion of exosomes and PGE2. Exosomal miR-194-5p enhanced DNA damage response in TRCs to potentiate tumor repopulation. Combined use of aspirin and radiotherapy might benefit pancreatic cancer patients.

Molecular Cancer published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (TAZ). 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Product Details of C30H30Cl2N6O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Eslamloo, Khalil; Ghorbani, Atefeh; Xue, Xi; Inkpen, Sabrina M.; Larijani, Mani; Rise, Matthew L. published the artcile< Characterization and transcript expression analyses of atlantic cod viperin.>, Application In Synthesis of 452-06-2, the main research area is Gadus viperin transcript expression immune response; Gadus morhua; dsRNA; inhibition of antiviral responses; qPCR; rsad2; teleost ISGs.

Viperin is a key antiviral effector in immune responses of vertebrates including the Atlantic cod (Gadus morhua). Using cloning, sequencing and gene expression analyses, we characterized the Atlantic cod viperin at the nucleotide and hypothetical amino acid levels, regulating factors were investigated. Using computational modeling, we show that the Atlantic cod Viperin forms similar overall protein architecture compared to mammalian Viperins. qPCR revealed that viperin is a weakly expressed transcript during embryonic development of Atlantic cod. In adults, the highest constitutive expression of viperin transcript was found in blood compared with 18 other tissues. Using isolated macrophages and synthetic dsRNA stimulation, we tested various immune inhibitors to determine the possible regulating pathways of Atlantic cod viperin. Atlantic cod viperin showed a comparable pIC induction to other well-known antiviral genes (e.g., interferon gamma and interferon-stimulated gene 15-1) in response to various immune inhibitors. The pIC induction of Atlantic cod viperin was significantly inhibited with 2-Aminopurine, Chloroquine, SB202190, and Ruxolitinib. Therefore, endosomal-TLR-mediated pIC recognition and signal transducers downstream of the TLR-dependent pathway may activate the gene expression response of Atlantic cod viperin. Also, these results suggest that antiviral responses of Atlantic cod viperin may be transcriptionally regulated through the interferon-activated pathway.

Frontiers in Immunology published new progress about Activating transcription factors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Application In Synthesis of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Lin, Fang; Wang, Hao; Liu, Wei; Li, Jing published the artcile< Zero-dimensional ionic antimony halide inorganic-organic hybrid with strong greenish yellow emission>, Recommanded Product: 1-carboxymethyl-3-methylimidazolium chloride, the main research area is ionic antimony halide inorganic organic hybrid greenish yellow emission; crystallog ionic antimony halide inorganic organic hybrid.

Here, we reported a new zero-dimensional ionic antimony halide inorganic-organic hybrid structure, H3SbBr6(L)6 (L = 2-(3-methyl-1H-imidazol-3-ium-1-yl)acetate). The inorganic component is a mol. SbBr63- anion with an octaheral geometry for the metal. Each individual anion is surrounded by six organic ligands. The compound emits bright green-yellow light with high quantum efficiency (IQY = 55% at λex = 360 nm). Combined with its low toxicity and high stability, the title compound serves as a good example of lighting phosphors based on antimony halide hybrid materials.

Journal of Materials Chemistry C: Materials for Optical and Electronic Devices published new progress about Band structure. 700370-07-6 belongs to class imidazoles-derivatives, and the molecular formula is C6H9ClN2O2, Recommanded Product: 1-carboxymethyl-3-methylimidazolium chloride.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Shi, Fei; Deng, Zheng; Zhou, Zheng; Jiang, Bo; Jiang, Chen-Yi; Zhao, Rui-Zhe; Sun, Feng; Cui, Di; Sun, Meng-Hao; Sun, Qian; Wang, Xing-Jie; Wu, Qi; Xia, Shu-Jie; Han, Bang-Min published the artcile< Heat injured stromal cells-derived exosomal EGFR enhances prostatic wound healing after thulium laser resection through EMT and NF-κB signaling>, Computed Properties of 6823-69-4, the main research area is thulium nuclearfactor Epithelial mesenchymal transition epidermalgrowth factorreceptor stromalcell woundhealing; benign prostatic hyperplasia (BPH); epidermal growth factor receptor (EGFR); exosome; nuclear factor-kappa B (NF-κB); shallow heat injury; wound healing.

This study investigated shallow heat injury to prostate stromal fibroblasts and epithelial cells and their interaction to regulate the wound healing and the underlying mol. events. Prostate stromal fibroblasts and epithelial cells were cultured individually or cocultured and subjected to shallow heat injury for assessments of cell proliferation, migration, apoptosis, cell cycle distribution, and gene expression. The supernatant of heat-injured WPMY-1 cells was collected for exosome extraction and assessments. Furthermore, beagle dogs received thulium laser resection of the prostate (TmLRP) and randomly divided into Gefitinib, GW4869, and control treatment for the histol. anal., tissue re-epithelialization, and epidermal growth factor receptor (EGFR) expression on the prostatic wound surface. Immunofluorescence was to evaluate p63-pos. basal progenitor cell trans-differentiation and macrophage polarization and ELISA was to detect cytokine levels in beagles’ urine. Shallow heat injury caused these cells to enter a stressed state and enhanced their crosstalk. The prostate stromal fibroblasts produced and secreted more exosomal-EGFR and other cytokines and chemokines after shallow heat injury, resulting in increased proliferation and migration of prostate epithelial cells during wound healing. The wound healing of the canine prostatic urethra following the TmLRP procedure was slower in the Gefitinib and GW4869 treatment group than in the control group of animals. Immunofluorescence and ELISA showed that reduced EGFR expression interrupted macrophage polarization but increased the inflammatory response. Shallow heat injury was able to promote the interaction of prostate stromal cells with prostate epithelial cells to enhance wound healing. Stromal-derived exosomal-EGFR plays a crucial role in the balance of the macrophage polarization and prostatic wound healing.

Prostate (Hoboken, NJ, United States) published new progress about Apoptosis. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Computed Properties of 6823-69-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Inoue, Hiroo; Hayashi, Shigeki; Imoto, Eiji published the artcile< Electrical conductivity of heterocyclic compounds. Molecular complexes of phenazine>, Application In Synthesis of 1003-21-0, the main research area is .

The composition, color, and m.p. of mol. complexes of the salt type prepared from phenazine hydro-chloride (I) or methosulfate and pyrene (II) or p-hydroquinone (III) varied with drying conditions. Thus, the N content and resistivity increased and the Cl content and m.p. decreased with increased drying times over P2O5 at reduced pressure. The ultraviolet spectra of I-II in a KBr pellet showed an absorption band at ∼620 mμ. The electron spin resonance spectra showed an unpaired electron localized on the N atom of II. The salt-type mol. complexes had a lower resistivity than the non-salt type. Thus, the sp. resistivities of I-III and II-III were 3 × 1011 and 3 × 1015 ohm-cm., res.

Bulletin of the Chemical Society of Japan published new progress about Heterocyclic compounds. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Application In Synthesis of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Linciano, Pasquale; Sorbi, Claudia; Comitato, Antonella; Lesniak, Anna; Bujalska-Zadrozny, Magdalena; Pawlowska, Agata; Bielenica, Anna; Orzelska-Gorka, Jolanta; Kedzierska, Ewa; Biala, Grazyna; Ronsisvalle, Simone; Limoncella, Silvia; Casarini, Livio; Cichero, Elena; Fossa, Paola; Satala, Grzegorz; Bojarski, Andrzej J.; Brasili, Livio; Bardoni, Rita; Franchini, Silvia published the artcile< Identification of a Potent and Selective 5-HT1A Receptor Agonist with In Vitro and In Vivo Antinociceptive Activity>, Safety of 5-Bromo-1-methyl-1H-imidazole, the main research area is pain 5HT1A receptor agonist preparation analgesic; 5-HT1AR agonists; Serotonin receptors; behavioral profiling; mice; pain.

Opioids are the gold standard drugs for the treatment of acute and chronic severe pain, although their serious side effects constitute a big limitation. In the search for new and safer drugs, 5-HT1AR agonists are emerging as potential candidates in pain relief therapy. In this work, we evaluated the affinity and activity of enantiomers of the two newly synthesized, potent 5-HT1AR agonists N-[(2,2-diphenyl-1,3-dioxolan-4-yl)methyl]-2-[2-(pyridin-4-yl)phenoxy]ethan-1-ammonium hydrogenoxalate (rac-1) and N-((2,2-diphenyl-1,3-dioxolan-4-yl)methyl)-2-(2-(1-methyl-1H-imidazol-5-yl)phenoxy)ethan-1-ammonium hydrogenoxalate (rac-2) in vitro and in vivo. The role of chirality in the interaction with 5-HT1AR was evaluated by mol. docking. The activity of the rac-1 was tested in mouse models of acute pain (hot plate) and severe tonic nociceptive stimulation (intraplantar formalin test). Rac-1 was active in the formalin test with a reduction in paw licking in both phases at 10 mg/kg, and its effect was abolished by the selective 5-HT1AR antagonist, WAY-100635. The eutomer (S)-1, but not the racemate, was active during the hot plate test at 10 and 20 mg/kg, and this effect was abolished by 30 min treatment with WAY-100635 at 30 min. Similarly to 8-OH-DPAT, (S)-1 evoked a slow outward current and depressed spontaneous glutamatergic transmission in superficial dorsal horn neurons, more effectively than rac-1. The eutomer (S)-1 showed promising developability properties, such as high selectivity over 5-HT subtypes, no interaction with the μ receptors, and low hepato- and cardiotoxicity. Therefore, (S)-1 may represent a potential candidate for the treatment of acute and chronic pain without having the adverse effects that are commonly associated with the classic opioid drugs.

ACS Chemical Neuroscience published new progress about 5-HT1A agonists. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Safety of 5-Bromo-1-methyl-1H-imidazole.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Amaudrut, Jerome; Argiriadi, Maria A.; Barth, Martine; Breinlinger, Eric C.; Bressac, Didier; Broqua, Pierre; Calderwood, David J.; Chatar, Mohamed; Cusack, Kevin P.; Gauld, Stephen B.; Jacquet, Sebastien; Kamath, Rajesh V.; Kort, Michael E.; Lepais, Valerie; Luccarini, Jean-Michel; Masson, Philippe; Montalbetti, Christian; Mounier, Laurent; Potin, Dominique; Poupardin, Olivia; Rouaud, Sylvie; Spitzer, Luc; Wallace, Craig D. published the artcile< Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists>, Category: imidazoles-derivatives, the main research area is RORgamma agonist IL17 nuclear hormone receptor SAR; IL-17; Nuclear hormone receptor; RORγt inverse agonist; SAR; Th17 cells.

A high-throughput screen against Inventiva’s compound library using a Gal4/RORγ-LBD luciferase reporter gene assay led to the discovery of a new series of quinoline sulfonamides as RORγ inhibitors, eventually giving rise to a lead compound having an interesting in vivo profile after oral administration. This lead was evaluated in a target engagement model in mouse, where it reduced IL-17 cytokine production after immune challenge. It also proved to be active in a multiple sclerosis model (EAE) where it reduced the disease score. The synthesis, structure activity relationship (SAR) and biol. activity of these derivatives is described herein.

Bioorganic & Medicinal Chemistry Letters published new progress about Autoimmune disease. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

You, Jie; Wu, Wenyu; Lu, Mengxin; Xie, Yanghao; Miao, Rui; Gu, Misi; Xi, Dong; Yan, Weiming; Wu, Di; Wang, Xiaojing; Chen, Tao; Ning, Qin; Han, Meifang published the artcile< Hepatic exosomes with declined MiR -27b-3p trigger RIG-I / TBK1 signal pathway in macrophages>, Synthetic Route of 6823-69-4, the main research area is miR27b3p RIGI TBK1 macrophage hepatic exosome signaling pathway; HBsAg; exosome; host immune; interferon alpha; miR-27b-3p.

Evidence suggests that interferon alpha (IFNα) plays an essential role in decreasing the HBsAg quantification and elevating the rate of clin. cure in chronic hepatitis B (CHB). However, the mechanisms underlying the effects of the exosomes on the expression of host genes in IFNα treatment remain unclear. CHB patients with IFNα treatment were divided into responders and non-responders according to the degree of HBsAg decline. Through microRNA sequencing and a series of mol. biol. methods, the key microRNAs in serum exosomes associated with clin. antiviral response of Peg-IFNα treatment in nucleotide analog-treated CHB patients were investigated. The roles of exosomal miRNAs on the IFNα signal pathway were explored in macrophages. MicroRNA sequencing and RT-qPCR assays confirmed six distinctly declined miRNAs in serum exosomes of responders at week 12 compared with levels at baseline. Exosomes with declined miR27b-3p in the serum of Peg-IFNα-treated responders activated phosphorylation of interferon regulatory factor 3/7 (IRF3/7) in IFNα synthesis pathway in macrophages. However, miR-27b-3p overexpression in HepAD38 cells suppressed IFNα synthesis in macrophages, resulting in insufficient ability to eliminate HBV, whereas the inhibitory effect could be blocked by inhibitors of exosomes release. Luciferase assay showed miR-27b-3p directly suppressed retinoic acid-inducible gene I (RIG-I) and TANK-binding kinase 1 (TBK1) expressions, and these effects could be abrogated in mutation experiments In IFNα treatment, exosomes with declined miR-27b-3p triggered activation of RIG-I/TBK1 signalling in macrophages against HBV. Serum exosomal miR-27-3p might represent a potential biomarker for patients with CHB.

Liver International published new progress about Antiviral agents. 6823-69-4 belongs to class imidazoles-derivatives, and the molecular formula is C30H30Cl2N6O2, Synthetic Route of 6823-69-4.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Mashiach, Daniel; Bacasen, Erin Mae; Singh, Sunjum; Kao, Timothy; Yaramada, Lekha; Mishail, Daniel; Singh, Summer; Miller, Jeffrey H. published the artcile< Enhanced characterization of the thyA system for mutational analysis in Escherichia coli: Defining mutationally ""hot"" regions of the gene>, Computed Properties of 452-06-2, the main research area is Escherichia thyA system mutation; Catalog; Cisplatin; Hotspots; Mutation; thyA system.

We have extensively characterized base substitution mutations in the 795 base pair (bp) long E. coli thyA gene to define as many of the base substitution mutational sites that inactivate the gene as possible. The resulting catalog of mutational sites constitutes a system with up to 5 times as many sites for monitoring each of the six base substitution mutations as the widely used rpoB/Rifr system. We have defined 75 sites for the G:C -> A:T transition, 68 sites for the G:C -> T:A transversion, 53 sites for the G:C -> C:G transversion, 49 sites for the A:T -> G:C transition, 39 sites for the A:T -> T:A transversion, and 59 sites for the A:T -> C:G transversion. This allows for the examination of mutational spectra using a more detailed probe of known mutations, while still allowing one to compare the number of repeated occurrences at specific sites. We have examined several mutagens and mutators with this system, and show its utility by looking at the spectrum of cisplatin, that has a single hotspot, underscoring the value of having as large an array of sites as possible at which one can monitor repeat occurrences. The resulting graphs suggest that there are “”hot”” regions at intervals, and this may reflect aspects of secondary structures, of the higher order structure of the chromosome, or perhaps the nucleoid structure of the chromosome plus histone-like protein complexes.

Mutation Research, Fundamental and Molecular Mechanisms of Mutagenesis published new progress about Chromosome. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Computed Properties of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Butler, Richard Noel published the artcile< Proton nuclear magnetic resonance spectra of aryl and mono- and disubstituted N-methylazoles>, Synthetic Route of 1003-21-0, the main research area is NMR methylazole; pyrazole tetrazole imidazole NMR.

Proton NMR spectra of substituted azoles, e.g., methylpyrrole, imidazoles, pyrazoles, etc., are compared. The influence of the azole ring on the chem. shifts of phenyl protons is discussed. A correlation between N-Me chem. shifts and the structural characteristics of the N-Me group in mono- and disubstituted azoles is noted.

Canadian Journal of Chemistry published new progress about Molecular structure-property relationship. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Synthetic Route of 1003-21-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem