Category: 2591-17-5

Wang, Anni; Li, Xuewei; Ju, Yong; Chen, Dongying; Lu, Jianzhong published the artcile< Bioluminescence imaging of carbon monoxide in living cells based on a selective deiodination reaction>, Application In Synthesis of 2591-17-5, the main research area is bioluminescence imaging carbon monoxide deiodination.

D-Luciferin is a popular bioluminescent substrate of luciferase in the presence of ATP. It was used in luciferase-based bioluminescence imaging and cell-based high-throughput screening applications. Herein, the iodination of D-luciferin was undertaken and explored as a bioluminescence probe without the need for light excitation to sensitively trace and image carbon monoxide (CO) in liver cancer cells. The bioluminescent probe (7′-iodo-luciferin) exhibited excellent selectivity for CO detection in vitro. This new probe could image exogenous and endogenous CO in the luciferase-transfected cancer cells. This new probe might be used for evaluating the roles of CO in various biol. processes.

Analyst (Cambridge, United Kingdom) published new progress about Bioluminescent imaging. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application In Synthesis of 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Kim, Jun Hyeok; Bell, Laura J.; Wang, Xiao; Wimalasekera, Rinuckshi; Bastos, Hugo P.; Kelly, Krystyna A.; Hannah, Matthew A.; Webb, Alex A. R. published the artcile< Arabidopsis sirtuins and poly(ADP-ribose) polymerases regulate gene expression in the day but do not affect circadian rhythms>, SDS of cas: 2591-17-5, the main research area is Arabidopsis sirtuin PARP gene expression circadian oscillaton; Arabidopsis thaliana; Nicotinamide-adenine dinucleotide; circadian clock; poly(ADP-ribose) glycohydrolase; poly(ADP-ribose) polymerases; sirtuins.

Nicotinamide-adenine dinucleotide (NAD) is involved in redox homeostasis and acts as a substrate for NADases, including poly(ADP-ribose) polymerases (PARPs) that add poly(ADP-ribose) polymers to proteins and DNA, and sirtuins that deacetylate proteins. Nicotinamide, a byproduct of NADases increases circadian period in both plants and animals. In mammals, the effect of nicotinamide on circadian period might be mediated by the PARPs and sirtuins because they directly bind to core circadian oscillator genes. We have investigated whether PARPs and sirtuins contribute to the regulation of the circadian oscillator in Arabidopsis. We found no evidence that PARPs and sirtuins regulate the circadian oscillator of Arabidopsis or are involved in the response to nicotinamide. RNA-seq anal. indicated that PARPs regulate the expression of only a few genes, including FLOWERING LOCUS C. However, we found profound effects of reduced sirtuin 1 expression on gene expression during the day but not at night, and an embryo lethal phenotype in knockouts. Our results demonstrate that PARPs and sirtuins are not associated with NAD regulation of the circadian oscillator and that sirtuin 1 is associated with daytime regulation of gene expression.

Plant, Cell & Environment published new progress about Arabidopsis. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, SDS of cas: 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Ingram, Nicola; McVeigh, Laura E.; Abou-Saleh, Radwa H.; Maynard, Juliana; Peyman, Sally A.; McLaughlan, James R.; Fairclough, Michael; Marston, Gemma; Valleley, Elizabeth M. A.; Jimenez-Macias, Jorge L.; Charalambous, Antonia; Townley, William; Haddrick, Malcolm; Wierzbicki, Antonia; Wright, Alexander; Volpato, Milene; Simpson, Peter B.; Treanor, Darren E.; Thomson, Neil H.; Loadman, Paul M.; Bushby, Richard J.; Johnson, Benjamin R. G.; Jones, Pamela F.; Evans, J. Anthony; Freear, Steven; Markham, Alexander F.; Evans, Stephen D.; Coletta, P. Louise published the artcile< Ultrasound-triggered therapeutic microbubbles enhance the efficacy of cytotoxic drugs by increasing circulation and tumor drug accumulation and limiting bioavailability and toxicity in normal tissues>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is VEGFR2 SN38 liposome drug delivery circulation bioavailability colorectal cancer; Microbubble; VEGFR2; colorectal cancer; nanoformulation; ultrasound.

Most cancer patients receive chemotherapy at some stage of their treatment which makes improving the efficacy of cytotoxic drugs an ongoing and important goal. Despite large numbers of potent anti-cancer agents being developed, a major obstacle to clin. translation remains the inability to deliver therapeutic doses to a tumor without causing intolerable side effects. To address this problem, there has been intense interest in nanoformulations and targeted delivery to improve cancer outcomes. The aim of this work was to demonstrate how vascular endothelial growth factor receptor 2 (VEGFR2)-targeted, ultrasound-triggered delivery with therapeutic microbubbles (thMBs) could improve the therapeutic range of cytotoxic drugs. Methods: Using a microfluidic microbubble production platform, we generated thMBs comprising VEGFR2-targeted microbubbles with attached liposomal payloads for localised ultrasound-triggered delivery of irinotecan and SN38 in mouse models of colorectal cancer. I.v. injection into tumor-bearing mice was used to examine targeting efficiency and tumor pharmacodynamics. High-frequency ultrasound and bioluminescent imaging were used to visualise microbubbles in real-time. Tandem mass spectrometry (LC-MS/MS) was used to quantitate intratumoral drug delivery and tissue biodistribution. Finally, 89Zr PET radiotracing was used to compare biodistribution and tumor accumulation of ultrasound-triggered SN38 thMBs with VEGFR2-targeted SN38 liposomes alone. Results: ThMBs specifically bound VEGFR2 in vitro and significantly improved tumor responses to low dose irinotecan and SN38 in human colorectal cancer xenografts. An ultrasound trigger was essential to achieve the selective effects of thMBs as without it, thMBs failed to extend intratumoral drug delivery or demonstrate enhanced tumor responses. Sensitive LC-MS/MS quantification of drugs and their metabolites demonstrated that thMBs extended drug exposure in tumors but limited exposure in healthy tissues, not exposed to ultrasound, by persistent encapsulation of drug prior to elimination. 89Zr PET radiotracing showed that the percentage injected dose in tumors achieved with thMBs was twice that of VEGFR2-targeted SN38 liposomes alone. Conclusions: thMBs provide a generic platform for the targeted, ultrasound-triggered delivery of cytotoxic drugs by enhancing tumor responses to low dose drug delivery via combined effects on circulation, tumor drug accumulation and exposure and altered metabolism in normal tissues.

Theranostics published new progress about Bioavailability. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Yu, Mohan; Liu, Ya-Jun published the artcile< Same Luciferin in Different Luciferases Emitting Different-Color Light. A Theoretical Study on Beetle Bioluminescence>, Electric Literature of 2591-17-5, the main research area is luciferase bioluminescence luciferin Phrixotrix.

Bioluminescent beetles, firefly, click beetle, and railroad worm, naturally emit different-color light via the identical luciferin and bioluminescence (BL) mechanisms. Railroad worm especially emits two colors of light in its dorsal-lateral and cephalic lanterns. Four computational models of bioluminophore (oLu) in luciferases of red-emitting, yellow-green-emitting, red-emitting with addnl. loop, and red-emitting without C-terminal were built in this paper. To unveil the details of this luciferase effect at the mol. and electronic-state levels, second-order multiconfigurational perturbation calculations were performed following mol. dynamic simulations and time-dependent d. functional calculations for the above four oLu-luciferase systems. Via a systematic anal. on properties of oLu at the first singlet state (S1-oLu) in different luciferases, one clearly see the details of the microenvironment and secondary structure of luciferase affecting the excited-state property of S1-oLu, which ultimately result in the variant color of light emission. Typically, the increase in charge transfer of S1-oLu leads to the longer wavelength BL.

Journal of Chemical Theory and Computation published new progress about Bioluminescence. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Electric Literature of 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Saito-Moriya, Ryohei; Nakayama, Jun; Kamiya, Genta; Nobuo Kitada; Obata, Rika; Maki, Shojiro A.; Aoyama, Hiroshi published the artcile< How to select firefly luciferin analogues for in vivo imaging>, Application of C11H8N2O3S2, the main research area is review bioluminescence firefly luciferin analog imaging; bioluminescence imaging; high sensitivity; luciferase; luciferin analogue; multicolor; near-infrared light.

A review. Bioluminescence reactions are widely applied in optical in vivo imaging in the life science and medical fields. Such reactions produce light upon the oxidation of a luciferin (substrate) catalyzed by a luciferase (enzyme), and this bioluminescence enables the quantification of tumor cells and gene expression in animal models. Many researchers have developed single-color or multicolor bioluminescence systems based on artificial luciferin analogs and/or luciferase mutants, for application in vivo bioluminescence imaging (BLI). In the current review, we focus on the characteristics of firefly BLI technol. and discuss the development of luciferin analogs for high-resolution in vivo BLI. In addition, we discuss the novel luciferin analogs TokeOni and seMpai, which show potential as high-sensitivity in vivo BLI reagents.

International Journal of Molecular Sciences published new progress about Bioluminescent imaging. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Bazhin, Arkadiy A.; Sinisi, Riccardo; De Marchi, Umberto; Hermant, Aurelie; Sambiagio, Nicolas; Maric, Tamara; Budin, Ghyslain; Goun, Elena A. published the artcile< A bioluminescent probe for longitudinal monitoring of mitochondrial membrane potential>, Reference of 2591-17-5, the main research area is bioluminescent probe mitochondria membrane potential.

Mitochondrial membrane potential (ΔΨm) is a universal selective indicator of mitochondrial function and is known to play a central role in many human pathologies, such as diabetes mellitus, cancer and Alzheimer′s and Parkinson′s diseases. Here, the authors report the design, synthesis and several applications of mitochondria-activatable luciferin (MAL), a bioluminescent probe sensitive to ΔΨm, and partially to plasma membrane potential (ΔΨp), for non-invasive, longitudinal monitoring of ΔΨm in vitro and in vivo. The authors applied this new technol. to evaluate the aging-related change of ΔΨm in mice and showed that nicotinamide riboside (NR) reverts aging-related mitochondrial depolarization, revealing another important aspect of the mechanism of action of this potent biomol. In addition, the authors demonstrated application of the MAL probe for studies of brown adipose tissue (BAT) activation and non-invasive in vivo assessment of ΔΨm in animal cancer models, opening exciting opportunities for understanding the underlying mechanisms and for discovery of effective treatments for many human pathologies.

Nature Chemical Biology published new progress about Aging, animal. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Reference of 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Yang, Xingye; Qin, Xiaojun; Ji, Huimin; Du, Lupei; Li, Minyong published the artcile< Constructing firefly luciferin bioluminescence probes for in vivo imaging>, Application of C11H8N2O3S2, the main research area is .

Bioluminescence imaging (BLI) is a widely applied visual approach for real-time detecting many physiol. and pathol. processes in a variety of biol. systems. Based on the caging strategy, lots of bioluminescent probes have been well developed. While the targets react with recognizable groups, caged luciferins liberate luciferase substrates, which react with luciferase generating a bioluminescent response. Among the various bioluminescent systems, the most widely utilized bioluminescent system is the firefly luciferin system. The H and carboxylic acid of luciferin are critically caged sites. The introduced self-immolative linker extends the applications of probes. Firefly luciferin system probes have been successfully applied for analyzing physiol. processes, monitoring the environment, diagnosing diseases, screening candidate drugs, and evaluating the therapeutic effect. Here, we systematically review the general design strategies of firefly luciferin bioluminescence probes and their applications. Bioluminescence probes provide a new approach for facilitating investigation in a diverse range of fields. It inspires us to explore more robust light emission luciferin and novel design strategies to develop bioluminescent probes.

Organic & Biomolecular Chemistry published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Luo, Jinqiu; Yang, Jinfeng; Li, Guangjie; Yang, Sheng; Zhou, Yibo; Li, Jun-Bin; Huang, Ge; Hu, Yibo; Zou, Shuangfa; Zeng, Qinghai; Yang, Ronghua published the artcile< Noncovalently Caged Firefly Luciferins Enable Amplifiable Bioluminescence Sensing of Hyaluronidase-1 Activity in Vivo>, Product Details of C11H8N2O3S2, the main research area is noncovalently caged firefly luciferins bioluminescence sensor hyaluronidase 1; bioluminescence; enzymatic assay; hyaluronidase; in vivo bioimaging; nanosensor; signal amplification.

Hyaluronidase 1 (Hyal-1) is an important enzyme involved in intracellular hyaluronic acid (HA) catabolism for performing various physiol. functions, and its aberrant level is closely associated with many malignant diseases. Bioluminescence imaging is advantageous for monitoring Hyal-1 activity in vivo, but it remains challenging to design an available probe for differentiating Hyal-1 from other isoforms by a traditional strategy that covalently masks the firefly luciferase substrate. Herein, we, for the first time, present a noncovalently caging approach to construct a Hyal-1-specific bioluminogenic nanosensor by entrapping D-luciferin (D-Luc) inside the cholesterylamine-modified HA (CHA) nanoassembly to inhibit the bioluminescence production When encountered with intracellular Hyal-1, CHA could be fully dissembled to liberate multiple copies of the loaded D-Luc, thereby emitting light by the luciferase-catalyzed bioluminescence reaction. Because of its cascade signal amplification feature, D-Luc@CHA displayed a remarkable “”turn-on”” response (248-fold) to 5μg/mL Hyal-1 with a detection limit of 0.07 ng/mL. Importantly, bioluminescence imaging results validated that D-Luc@CHA could be competent for dynamically visualizing endogenous Hyal-1 changes in living cells and animals and possessed the capability of discriminating between normal and cancer cells, thus offering a promising toolbox to evaluate Hyal-1 roles in biol. processes as well as to diagnose Hyal-1-related diseases.

ACS Sensors published new progress about Bioluminescent imaging. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Product Details of C11H8N2O3S2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Lopez, Vittoria; Lee, Sang-Yong; Stephan, Holger; Mueller, Christa E. published the artcile< Recombinant expression of ecto-nucleotide pyrophosphatase/phosphodiesterase 4 (NPP4) and development of a luminescence-based assay to identify inhibitors>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is human ecto nucleotide pyrophosphatase phosphodiesterase NPP4 assay inhibitor polyphosphate; Antithrombotic drug; Assay development; Ectonucleotidase; High-throughput screening; Luminescence detection; NPP4 inhibitors; Recombinant enzyme expression.

Nucleotide pyrophosphatase/phosphodiesterase 4 (NPP4) is a membrane-bound enzyme that hydrolyzes extracellular diadenosine polyphosphates such as diadenosine triphosphate (Ap3A) and diadenosine tetraphosphate (Ap4A) yielding mononucleotides. NPP4 on the surface of endothelial cells was reported to promote platelet aggregation by hydrolyzing Ap3A to ADP, which activates pro-thrombotic G protein-coupled P2Y1 and P2Y12 receptors. Thus, NPP4 inhibitors have potential as novel antithrombotic drugs. In the present study we expressed soluble human NPP4 in Sf9 insect cells and established an enzyme assay using diadenosine tetraphosphate (Ap4A) as a substrate. The reaction product ATP was quantified by luciferin-luciferase reaction in a 96-well plate format. The sensitive method displayed a limit of detection (LOD) of 14.6 nM, and a Z′-factor of 0.68 indicating its suitability for high-throughput screening. The new assay was applied for studying enzyme kinetics and led to the identification of the first NPP4 inhibitors.

Analytical Biochemistry published new progress about Antithrombotics. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Helmer, Rebecca A.; Martinez-Zaguilan, Raul; Kaur, Gurvinder; Smith, Lisa A.; Dufour, Jannette M.; Chilton, Beverly S. published the artcile< Helicase-like transcription factor-deletion from the tumor microenvironment in a cell line-derived xenograft model of colorectal cancer reprogrammed the human transcriptome-S-nitroso-proteome to promote inflammation and redirect metastasis>, Category: thiazole, the main research area is helicase transcription factor colorectal cancer inflammation redirect metastasis.

Methylation of the HLTF gene in colorectal cancer (CRC) cells occurs more frequently in men than women. Progressive epigenetic silencing of HLTF in tumor cells is accompanied by negligible expression in the tumor microenvironment (TME). Cell line-derived xenografts (CDX) were established in control (Hltf+/+) and Hltf-deleted male Rag2-/-IL2rg-/- mice by direct orthotopic cell microinjection (OCMI) of HLTF+/+HCT116 Red-FLuc cells into the submucosa of the cecum. Combinatorial induction of IL6 and S100A8/A9 in the Hltf-deleted TME with ICAM-1and IL8 in the primary tumor activated a pos. feedback loop. The proinflammatory niche produced a major shift in CDX metastasis to peritoneal dissemination compared to controls. Inducible nitric oxide (iNOS) gene expression and transactivation of the iNOS-S100A8/A9 signaling complex in Hltf-deleted TME reprogrammed the human S-nitroso-proteome. POTEE, TRIM52 and UN45B were S-nitrosylated on the conserved I/L-X-C-X2-D/E motif indicative of iNOS-S100A8/A9-mediated S-nitrosylation. 2D-DIGE and protein identification by MALDI-TOF/TOF mass spectrometry authenticated S-nitrosylation of 53 individual cysteines in half-site motifs (I/L-X-C or C-X-X-D/E) in CDX tumors. POTEE in CDX tumors is both a general S-nitrosylation target and an iNOS-S100A8/A9 site-specific (Cys638) target in the Hltf-deleted TME. REL is an example of convergence of transcriptomic-S-nitroso-proteomic signaling. The gene is transcriptionally activated in CDX tumors with an Hltf-deleted TME, and REL-SNO (Cys143) was found in primary CDX tumors and all metastatic sites. Primary CDX tumors from Hltf-deleted TME shared 60% of their S-nitroso-proteome with all metastatic sites. Forty percent of SNO-proteins from primary CDX tumors were variably expressed at metastatic sites. Global S-nitrosylation of proteins in pathways related to cytoskeleton and motility was strongly implicated in the metastatic dissemination of CDX tumors. Hltf-deletion from the TME played a major role in the pathogenesis of inflammation and linked protein S-nitrosylation in primary CDX tumors with spatiotemporal continuity in metastatic progression when the tumor cells expressed HLTF.

PLoS One published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (POTEE). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica