Tag: M.W=250-300

Syed, Aisha J.; Anderson, James C. published the artcile< Applications of bioluminescence in biotechnology and beyond>, SDS of cas: 2591-17-5, the main research area is .

Bioluminescence is the fascinating natural phenomenon by which living creatures produce light. Bioluminescence occurs when the oxidation of a small-mol. luciferin is catalyzed by an enzyme luciferase to form an excited-state species that emits light. There are over 30 known bioluminescent systems but the luciferin-luciferase pairs of only 11 systems have been characterised to-date, while other novel systems are currently under investigation. The different luciferin-luciferase pairs have different light emission wavelengths and hence are suitable for various applications. The last decade or so has seen great advances in protein engineering, synthetic chem., and physics which have allowed luciferins and luciferases to reach previously uncharted applications. The bioluminescence reaction is now routinely used for gene assays, the detection of protein-protein interactions, high-throughput screening (HTS) in drug discovery, hygiene control, anal. of pollution in ecosystems and in vivo imaging in small mammals. Moving away from sensing and imaging, the more recent highlights of the applications of bioluminescence in biomedicine include the bioluminescence-induced photo-uncaging of small-mols., bioluminescence based photodynamic therapy (PDT) and the use of bioluminescence to control neurons. There has also been an increase in blue-sky research such as the engineering of various light emitting plants. This has led to lots of exciting multidisciplinary science across various disciplines. This review focuses on the past, present, and future applications of bioluminescence. We aim to make this review accessible to all chemists to understand how these applications were developed and what they rely upon, in simple understandable terms for a graduate chemist.

Chemical Society Reviews published new progress about 2591-17-5. 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

Kagiya, Go; Sato, Ayaka; Ogawa, Ryohei; Hatashita, Masanori; Kato, Mana; Kubo, Makoto; Kojima, Fumiaki; Kawakami, Fumitaka; Nishimura, Yukari; Abe, Naoya; Hyodo, Fuminori published the artcile< Real-time visualization of intratumoral necrosis using split-luciferase reconstitution by protein trans-splicing>, Quality Control of 2591-17-5, the main research area is intratumoral necrosis luciferase protein splicing; bioluminescent imaging; cell death; extein; intein; necrosis; necrosis imaging reporter; protein trans-splicing; split-luciferase reconstitution.

Necrosis, a form of cell death, occurs not only with the development of various diseases but also with a tumor tissue response to cancer treatment. Therefore, pursuing progress for cancer therapy through induction of necrosis may be one of the most effective approaches for cancer eradication. We herein describe the development of a real-time imaging system to visualize intratumoral necrosis. The system is composed of two types of cells expressing either one of two necrosis imaging reporters that consist of a DnaE intein sequence linking to one of two split-luciferase fragments. When necrosis occurs in a tumor composed of both of the cells, the two types of leaked reporters can reconstitute the enzymic activity as a result of protein trans-splicing and thereby emit bioluminescence in the presence of the substrate. This system, which was constructed with shrimp-derived luciferase, allowed in vitro imaging of necrosis. We further confirmed real-time imaging of intratumoral necrosis caused by phys. or chem. tissue disruption, validating its application in in vivo necrosis imaging. Thus, the constructed imaging system could be a powerful tool for the optimization of the therapeutic condition for cancer therapy and for the evaluation of novel anticancer drugs targeting necrosis.

Molecular Therapy–Oncolytics published new progress about Antitumor agents. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Quality Control of 2591-17-5.

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

Hettie, Kenneth S.; Teraphongphom, Nutte Tarn; Ertsey, Robert D.; Rosenthal, Eben L.; Chin, Frederick T. published the artcile< Targeting intracranial patient-derived glioblastoma (GBM) with a NIR-I fluorescent immunoconjugate for facilitating its image-guided resection>, Computed Properties of 2591-17-5, the main research area is glioblastoma human fluorescent immunoconjugate.

Glioblastoma multiforme (GBM) is the most aggressive form of primary brain tumor type and is associated with a high mortality rate borne out of such affording a survival rate of only 15 mo. GBM aggressiveness is associated with the overexpression of epidermal growth factor receptor (EGFR) and its mutants. Targeting GBM with therapeutics is challenging because the blood-brain barrier (BBB) permits primarily select small-mol. entities across its semipermeable blockade. However, recent preclin. data suggest that large biomols., such as the anti-EGFR antibody therapeutic, cetuximab, could be capable of bypassing the BBB despite the relative enormity of its size. As such, we set forth to establish the feasibility of utilizing an EGFR-targeting near-IR-I (NIR-I) fluorescent construct in the form of an immunoconjugate (cetuxmimab-IRDye800) to achieve visual differentiation between diseased brain tissue arising from a low-passage patient-derived GBM cell line (GBM39) and healthy brain tissue via utilizing orthotopic intracranial murine GBM39 tumor models for in vivo and ex vivo evaluation such that by doing so would establish proof of concept for ultimately facilitating its in vivo fluorescence-guided resection and ex vivo surgical back-table pathol. confirmation in the clinic. As anticipated, we were not capable of distinguishing between malignant tumor tissue and healthy tissue in resected intact and slices of whole brain ex vivo under white-light illumination (WLI) due to both the diseased tissue and healthy tissue appearing virtually identical to the unaided eye. However, we readily observed over an average 6-fold enhancement in the fluorescence emission in the resected intact whole brain ex vivo when performing NIR-I fluorescence imaging (FLI) on the cohort of GBM39 tumor models that were administered the immunoconjugate compared to controls. In all, we laid the initial groundwork for establishing that NIR-I fluorescent immunoconjugates (theranostics) such as cetuximab-IRDye800 can bypass the BBB to visually afford GBM39 tumor tissue differentiation for its image-guided surgical removal.

RSC Advances published new progress about Biochemical compounds Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Computed Properties of 2591-17-5.

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

Watanabe, Hiroaki; Yamaori, Satoshi; Kamijo, Shinobu; Aikawa, Kaori; Ohmori, Shigeru published the artcile< In vitro inhibitory effects of sesamin on CYP4F2 activity>, Formula: C11H8N2O3S2, the main research area is microsome CYP4F2 enzyme inhibition sesamin NADPH; CYP4F2; inactivation; inhibition; sesamin.

Sesamin is a major lignan in sesame seeds, and a recent meta-anal. of controlled trials indicated that sesamin intake decreases blood pressure. The antihypertensive effect of sesamin has been suggested to be due to sesamin-mediated suppression of 20-hydroxyeicosatetraenoic acid production catalyzed by CYP4F2. However, the detailed mechanism underlying inhibition of CYP4F2 function by sesamin remains unclear. In this study, the effects of sesamin on catalytic activity of CYP4F2 were investigated in vitro. Sesamin inhibited luciferin-4F2/3 O-dealkylase activity of recombinant human CYP4F2 with an IC50 value of 0.381μM. When preincubated in the presence of reduced NADP (NADPH) for 20 min, sesamin potentiated the inhibition of CYP4F2 activity. Moreover, kinetic anal. of the inactivation revealed that sesamin showed a preincubation time- and concentration-dependent inhibition of CYP4F2 activity yielding a maximal inactivation rate constant (kinact) value of 0.354 min-1 and half-maximal inhibitory concentration (KI) value of 1.12μM. The inactivation of CYP4F2 by sesamin required NADPH. These results indicated that sesamin is a mechanism-based inactivator of human CYP4F2.

Biological & Pharmaceutical Bulletin published new progress about Enzyme inhibition kinetics. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Formula: C11H8N2O3S2.

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

Wang, Fang I.; Ding, Gucci; Ng, Garmen S.; Dixon, S. Jeffrey; Chidiac, Peter published the artcile< Luciferase-based GloSensor cAMP assay: Temperature optimization and application to cell-based kinetic studies>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is luciferase glosensor cAMP assay temperature optimization kinetics drug discovery; Drug discovery; GPCRs; GloSensor; High-throughput screening; Optimization.

G protein-coupled receptors (GPCRs) are an important receptor superfamily and common therapeutic targets. The second messenger cyclic adenosine monophosphate (cAMP) is a key mediator in many GPCR signaling pathways. Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well as allosteric modulators. In this regard, luminescence-based biosensors have revolutionized our ability to monitor GPCR signaling kinetics. The GloSensor cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. However, it is crucial to optimize assay conditions such as temperature As well, it has not been reported whether the effects of temperature on biosensor activity are reversible. Here, we describe the temperature sensitivity and reversibility of the GloSensor cAMP assay, and which GloSensor version is optimal for measuring cytosolic cAMP. We also present a detailed protocol for monitoring cAMP levels in live cells expressing endogenous or exogenous GPCRs. Temperature optimization studies were carried out using HEK293H cells transiently transfected with the adenosine receptor A2a and the GloSensor plasmid (pGloSensor-20F or -22F). We found that preincubation and luminescence reading at room temperature were optimal as compared to higher temperatures As well, the GloSensor-22F biosensor had a superior signal-to-background ratio and the effect of temperature on biosensor activity was reversible. However, thermal instability of the biosensor may pose a problem for in vivo studies. Nevertheless, the GloSensor cAMP assay can be applied to analyze signaling by a wide range of GPCRs for drug discovery purposes.

Methods (Amsterdam, Netherlands) published new progress about Adenosine A2A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Zhao, Pei; Wu, Xiaokang; Li, Jie; Dong, Gaopan; Sun, Yingai; Ma, Zhao; Li, Minyong; Du, Lupei published the artcile< Discovery of alkene-conjugated luciferins for redshifted and improved bioluminescence imaging in vitro and in vivo>, Formula: C11H8N2O3S2, the main research area is .

The firefly luciferase system is the most extensively utilized bioluminescence system in the field of life science at the moment. In this work, we designed and synthesized a series of alkene-conjugated luciferins to develop new firefly bioluminescence substrates, and further evaluated their activities in vitro and in vivo. It is worth noting that the maximum biol. emission wavelength of novel luciferin analog AL3 ((S,E)-2-(6-hydroxy-5-(3-methoxy-3-oxoprop-1-en-1-yl)benzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) is 100 nm red-shifted compared with D-luciferin, while that of analog AL4 ((S,E)-2-(5-(2-cyanovinyl)-6-hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) is 75 nm red-shifted. The new substrate AL2 ((S,E)-2-(6-hydroxy-7-(3-methoxy-3-oxoprop-1-en-1-yl)benzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid) showed better bioluminescence performance in vivo.

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

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

Inouye, Satoshi; Nakamura, Mitsuhiro; Taguchi, Jumpei; Hosoya, Takamitsu published the artcile< Identification of a novel oxidation product from yellow fluorophore in the complex of apoPholasin and dehydrocoelenterazine>, Application of C11H8N2O3S2, the main research area is oxidation yellow fluorophore complex apoPholasin dehydrocoelenterazine; Coelenteramide; Coelenteramine; Coelenterazine; Photoproteins; Reactive oxygen.

The complex of the recombinant fusion protein of apoPholasin and glutathione S-transferase (GST-apoPholasin) with non-fluorescent dehydrocoelenterazine (dCTZ) (GST-apoPholasin/dCTZ complex) shows yellow fluorescence at 539 nm by excitation at 430 nm. The GST-apoPholasin/dCTZ complex with a fluorophore (dCTZ*) has considerably weak luminescence activity, converting slowly to a blue fluorescence protein with the emission peak at 430 nm. The main oxidation products from dCTZ* for blue fluorescence were identified as coelenteramine (CTM) and an unreported pyrazine derivative, 3-benzyl-5-(4-hydroxyphenyl)pyrazin-2(1H)-one (CTO) that was confirmed by chem. synthesis.

Bioorganic & Medicinal Chemistry Letters published new progress about Chimeric fusion proteins Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (GST-apoPholasin). 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

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

Ji, Xincai; Adams, Spencer T. Jr.; Miller, Stephen C. published the artcile< Bioluminescence imaging in mice with synthetic luciferin analogues>, Computed Properties of 2591-17-5, the main research area is review bioluminescence imaging synthetic luciferin analog transgenic mice; AAV; Coelenterazine; CycLuc1; FAAH; Firefly; GFAP; Luciferase; NanoLuc; PHP.eB; Transgenic.

A review. Luciferase enzymes from bioluminescent organisms can be expressed in mice, enabling these rodents to glow when treated with a corresponding luciferin substrate. Light emission occurs where the expression of the genetically-encoded luciferase overlaps with the biodistribution of the administered small mol. luciferin. Here we discuss differences between firefly luciferin analogs for bioluminescence imaging, focusing on transgenic and adeno-associated virus (AAV)-transduced mice.

Methods in Enzymology published new progress about Adeno-associated virus. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Computed Properties of 2591-17-5.

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

Choi, Sunju; Matta, Hittu; Gopalakrishnan, Ramakrishnan; Natarajan, Venkatesh; Gong, Songjie; Jeronimo, Alberto; Kuo, Wei-Ying; Bravo, Bryant; Chaudhary, Preet M. published the artcile< A novel thermostable beetle luciferase based cytotoxicity assay>, SDS of cas: 2591-17-5, the main research area is luciferase thermostability isolation beetle anticancer agent cytotoxicity.

Cytotoxicity assays are essential for the testing and development of novel immunotherapies for the treatment of cancer. We recently described a novel cytotoxicity assay, termed the Matador assay, which was based on marine luciferases and their engineered derivatives In this study, we describe the development of a new cytotoxicity assay termed ‘Matador-Glo assay’ which takes advantage of a thermostable variant of Click Beetle Luciferase (Luc146-1H2). Matador-Glo assay utilizes Luc146-1H2 and D-luciferin as the luciferase-substrate pair for luminescence detection. The assay involves ectopic over-expression of Luc146-1H2 in the cytosol of target cells of interest. Upon damage to the membrane integrity, the Luc146-1H2 is either released from the dead and dying cells or its activity is preferentially measured in dead and dying cells. We demonstrate that this assay is simple, fast, specific, sensitive, cost-efficient, and not labor-intensive. We further demonstrate that the Matador-Glo assay can be combined with the marine luciferase-based Matador assay to develop a dual luciferase assay for cell death detection. Finally, we demonstrate that the Luc146-1H2 expressing target cells can also be used for in vivo bioluminescence imaging applications.

Scientific Reports published new progress about Antitumor agents. 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

Kadota, Ayano; Moriguchi, Misato; Watanabe, Tadashi; Sekine, Yuichi; Nakamura, Shigeo; Yasuno, Takumi; Ohe, Tomoyuki; Mashino, Tadahiko; Fujimuro, Masahiro published the artcile< A pyridinium-type fullerene derivative suppresses primary effusion lymphoma cell viability via the downregulation of the Wnt signaling pathway through the destabilization of β-catenin>, Product Details of C11H8N2O3S2, the main research area is Wnt beta catenin pyridinium fullerene suppression primary effusion lymphoma; Kaposi’s sarcoma‑associated herpesvirus; Wnt signaling; fullerene; primary effusion lymphoma; pyridinium fullerene; β‑catenin.

Primary effusion lymphoma (PEL) is defined as a rare subtype of non-Hodgkin′s B cell lymphoma, which is caused by Kaposi′s sarcoma-associated herpesvirus (KSHV) in immunosuppressed patients. PEL is an aggressive type of lymphoma and is frequently resistant to conventional chemo- therapeutics. Therefore, the discovery of novel drug candidates for the treatment of PEL is of utmost importance. In order to discover potential novel anti-tumor compounds against PEL, the authors previously developed a pyrrolidinium-type fullerene derivative, 1,1,1′,1′-tetramethyl [60]fullerenodi- pyrrolidinium diiodide (derivative #1), which induced the apoptosis of PEL cells via caspase-9 activation. In the present study, the growth inhibitory effects of pyrrolidinium-type (derivatives #1 and #2), pyridinium-type (derivatives #3 and #5 to #9) and anilinium-type fullerene derivatives (derivative #4) against PEL cells were evaluated. This anal. revealed a pyridinium-type derivative (derivative #5; 3-5′-(ethoxycarbonyl)-1′,5′-dihydro-2′H-[5,6]fullereno-C60-Ih-[1,9-c] pyrrol-2′-yl-1-methylpyridinium iodide), which exhibited antitumor activity against PEL cells via the downregulation of Wnt/β-catenin signaling. Derivative #5 suppressed the viability of KSHV-infected PEL cells compared with KSHV-uninfected B-lymphoma cells. Furthermore, derivative #5 induced the destabilization of β-catenin and suppressed β-catenin-TCF4 transcriptional activity in PEL cells. It is known that the constitutive activation of Wnt/β-catenin signaling is essential for the growth of KSHV-infected cells. The Wnt/β-catenin activation in KSHV-infected cells is mediated by KSHV latency-associated nuclear antigen (LANA). The data demonstrated that derivative #5 increased β-catenin phosphorylation, which resulted in β-catenin polyubiquitination and subsequent degradation Thus, derivative #5 overcame LANA-mediated β-catenin stabilization. Furthermore, the administration of derivative #5 suppressed the development of PEL cells in the ascites of SCID mice with tumor xenografts derived from PEL cells. On the whole, these findings provide evidence that the pyridinium-type fullerene derivative #5 exhibits antitumor activity against PEL cells in vitro and in vivo. Thus, derivative #5 may be utilized as a novel therapeutic agent for the treatment of PEL.

Oncology Reports published new progress about Adenomatous polyposis coli proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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