Tag: M.W=250-300

Loretz, Carol; Ho, Ming-Chih David; Alam, Novera; Mitchell, Walter; Li, Albert P. published the artcile< Application of cryopreserved human intestinal mucosa and cryopreserved human enterocytes in the evaluation of herb-drug interactions: evaluation of CYP3A inhibitory potential of grapefruit juice and commercial formulations of twenty-nine herbal supplements>, Category: thiazole, the main research area is Application cryopreserved human intestinal mucosa drug interaction.

Com. formulations of 29 commonly used herbal supplements (HSs) and grapefruit juice were evaluated for drug interaction potential via quantification of their CYP3A inhibitory potential in two in vitro exptl. models of human small intestine, cryopreserved human intestinal mucosa (CHIM), and cryopreserved human enterocytes (CHEs). Two CYP3A substrates were used-in the studies with CHIM, CYP3A activity was quantified via liquid chromatog. tandem mass spectrometry quantification of midazolam 1′-hydroxylation, whereas in CHE, luciferin-IPA metabolism to luciferin was quantified by luminescence. Upon treatment of CHIM with the estimated lumen concentration of the HS upon each oral administration (manufacturers’ recommended dosage dissolved in 200 mL of culture medium), >80% CYP3A inhibition was observed for green tea extract, St. John’s wort, valerian root, horehound, and grapefruit juice. Less than 50% inhibition was observed for fenugreek, aloe vera, guarana, soy isoflavone, maca, echinacea, spirulina, evening primrose, milk thistle, cranberry, red yeast rice, rhodiola, ginkgo biloba, turmeric, curcumin, white kidney bean, garlic, cinnamon, saw palmetto berries, panax ginseng, black elderberry, wheat grass juice, flaxseed oil, black cohosh, and ginger root. The results were confirmed in a a dose-response study with HSs obtained from three suppliers for the four inhibitory HSs (green tea extract, horehound, St). John’s wort, valerian root and three representative noninhibitory HSs (black cohosh, black elderberry, echinacea). Similar results were obtained with the inhibitory HSs in CHE. The results illustrate that CHIM and CHE represent physiol. relevant in vitro exptl. models for the evaluation of drug interaction potential of herbal supplements. Based on the results, green tea extract, horehound, St. John’s wort, and valerian root may cause drug interactions with orally administered drugs that are CYP3A substrates, as was observed for grapefruit juice.

Drug Metabolism & Disposition published new progress about Allium sativum. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Category: thiazole.

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

Diaz, Rodrigo D.; Larrondo, Luis F. published the artcile< A circadian clock in Neurospora crassa functions during plant cell wall deconstruction>, Name: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is Neurospora cell wall circadian clock; Cellulose degradation; Clock Regulation; Luciferase real-time reporter.

Circadian clocks are autonomous timers that are believed to confer organisms a selective advantage by enabling processes to occur at appropriate times of the day. In the model fungus Neurospora crassa, 20-40% of its genes are reported to be under circadian regulation, as assayed in simple sugar media. Although it has been well-described that Neurospora efficiently deconstructs plant cell wall components, little is known regarding the status of the clock when Neurospora grows on cellulosic material, or whether such a clock has an impact on any of the genes involved in this process. Through luciferase-based reporters and fluorescent detection assays, we show that a clock is functioning when Neurospora grows on cellulose-containing wheat straw as the only carbon and nitrogen source. Addnl., we found that the major cellobiohydrolase encoding gene involved in plant cell wall deconstruction, cbh-1, is rhythmically regulated by the Neurospora clock, in a manner that depends on cellulose concentration and on the transcription factor CRE-1, known as a key player in carbon-catabolite repression in this fungus. Our findings are a step towards a more comprehensive understanding on how clock regulation modulates cellulose degradation, and thus Neurospora’s physiol.

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

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

Krasitskaya, Vasilisa V.; Bashmakova, Eugenia E.; Frank, Ludmila A. published the artcile< Coelenterazine-dependent luciferases as a powerful analytical tool for research and biomedical applications>, Synthetic Route of 2591-17-5, the main research area is review coelenterazine luciferase bioluminescent system; Ca2+-regulated photoprotein; analytical systems; bioluminescence; coelenterazine; luciferase.

A review. The functioning of bioluminescent systems in most of the known marine organisms is based on the oxidation reaction of the same substrate-coelenterazine (CTZ), catalyzed by luciferase. Despite the diversity in structures and the functioning mechanisms, these enzymes can be united into a common group called CTZ-dependent luciferases. Among these, there are two sharply different types of the system organization-Ca2+-regulated photoproteins and luciferases themselves that function in accordance with the classical enzyme-substrate kinetics. Along with deep and comprehensive fundamental research on these systems, approaches and methods of their practical use as highly sensitive reporters in analytics have been developed. The research aiming at the creation of artificial luciferases and synthetic CTZ analogs with new unique properties has led to the development of new exptl. anal. methods based on them. The com. availability of many ready-to-use assay systems based on CTZ-dependent luciferases is also important when choosing them by first-time-users. The development of anal. methods based on these bioluminescent systems is currently booming. The bioluminescent systems under consideration were successfully applied in various biol. research areas, which confirms them to be a powerful anal. tool. In this , we consider the main directions, results, and achievements in research involving these luciferases.

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

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

Zhang, Kuojun; Yao, Yiwu; Tu, Zhengchao; Liao, Chenzhong; Wang, Zhen; Qiu, Yatao; Chen, Dong; Hamilton, Dale J.; Li, Zheng; Jiang, Sheng published the artcile< Discovery of class I histone deacetylase inhibitors based on romidpesin with promising selectivity for cancer cells>, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is romidpesin class I histone deacetylase inhibitor cancer cell selectivity; antitumor; class I histone deacetylases; cyclic depsipeptides; inhibitor; structure–activity relationship.

Aim: Class I histone deacetylases (HDACs) are considered to be promising anticancer targets, but selective inhibition of class I HDAC isoforms remains a challenge. Methods & results: Previously, we obtained a selective class I HDAC inhibitor 9 based on a macrocyclic HDAC inhibitor Romidpesin. As our continuous efforts, a library of novel cyclicdepsipeptides based on 9 was established using a convergent synthesis strategy. The most active compounds 10, 16 and 19 selectively inhibit class I HDACs and exhibit promising nanomolar antiproliferative activities against several cancer cell lines with excellent selectivity toward cancer cells over normal cells. Besides, compound 10 demonstrates excellent antitumor effects in human prostate carcinoma PC3 xenograft models with no observed toxicity. Conclusion: These cyclicdepsipeptides show great therapeutic potential as novel anticancer agents for clin. translation.

Future Medicinal Chemistry published new progress about Antitumor agents. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

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

Li, Shufeng; Ruan, Zhiyang; Zhang, Hang; Xu, Haiwei published the artcile< Recent achievements of bioluminescence imaging based on firefly luciferin-luciferase system>, Electric Literature of 2591-17-5, the main research area is Bioluminescence imaging (BLI); Caged luciferins; Disease diagnosis and therapy; Firefly luciferin-luciferase system; Mutant luciferase-luciferin pairs.

Bioluminescence imaging (BLI) is a newly developed noninvasive visual approach which facilitates the understanding of a plethora of biol. processes in vitro and in vivo due to the high sensitivity, resolution and selectivity, low background signal, and the lack of external light excitation. BLI based on firefly luciferin-luciferase system has been widely used for the activity evaluation of tumor-specific enzymes, for the detection of diseases-related bioactive small mols. and metal ions, and for the diagnosis and therapy of diseases including the studies of drug transport, the research of immune response, and the evaluation of drug potency and tissue distribution. In this review, we highlight the recent achievements in luciferin derivatives with red-shifted emission spectra, mutant luciferase-luciferin pairs, and the diagnostic and therapeutic application of BLI based on firefly luciferin-luciferase system. The development and application of BLI will expand our knowledge of the occurrence and development of diseases and shed light on the diagnosis and treatment of various diseases.

European Journal of Medicinal Chemistry published new progress about 2591-17-5. 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

Kanou, Harumi; Nagasawa, Kouki; Ishii, Yuki; Chishima, Aya; Hayashi, Juri; Haga, Sanae; Sutherland, Kenneth; Ishikawa, Masayori; Ozaki, Michitaka; Shirato, Hiroki; Hamada, Kazuko; Hamada, Toshiyuki published the artcile< Period1 gene expression in the olfactory bulb and liver of freely moving streptozotocin-treated diabetic mouse>, Recommanded Product: (S)-2-(6-Hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid, the main research area is period1 gene expression olfactory bulb liver diabetes mellitus; Circadian rhythm; In vivo imaging; Luciferin; Period1.

Clock genes express circadian rhythms in most organs. These rhythms are organized throughout the whole body, regulated by the suprachiasmatic nucleus (SCN) in the brain. Disturbance of these clock gene expression rhythms is a risk factor for diseases such as obesity. In the present study, to explore the role of clock genes in developing diabetes, we examined the effect of streptozotocin (STZ)-induced high glucose on Period1 (Per1) gene expression rhythm in the liver and the olfactory bub (OB) in the brain. We found a drastic increase of Per1 expression in both tissues after STZ injection while blood glucose content was low. After a rapid expression peak, Per1 expression showed no rhythm. Associated with an increase of glucose content, behavior became arrhythmic. Finally, we succeeded in detecting an increase of Per1 expression in mice hair follicles on day 1 after STZ administration, before the onset of symptoms. These results show that elevated Per1 expression by STZ plays an important role in the aggravation of diabetes.

Biochemical and Biophysical Research Communications published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (Per1). 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

Ikeda, Yuma; Nomoto, Takahiro; Hiruta, Yuki; Nishiyama, Nobuhiro; Citterio, Daniel published the artcile< Ring-Fused Firefly Luciferins: Expanded Palette of Near-Infrared Emitting Bioluminescent Substrates>, Quality Control of 2591-17-5, the main research area is ring fused firefly luciferin near IR emitting bioluminescence substrate.

Firefly bioluminescence is broadly applied as a noninvasive imaging modality in the biomedical research field. One limitation in firefly bioluminescence imaging is the limited variety of luciferins emitting in the near-IR (NIR) region (650-900 nm), where tissue penetration is high. Herein, we describe a series of structure-inherent NIR emitting firefly luciferin analogs, NIRLucs, designed through a ring fusion strategy. This strategy resulted in pH-independent structure-inherent NIR emission with a native firefly luciferase, which was theor. supported by quantum chem. calculations of the oxidized form of each luciferin. When applied to cells, NIRLucs displayed dose-independent improved NIR emission even at low concentrations where the native D-luciferin substrate does not emit. Addnl., excellent blood retention and brighter photon flux (7-fold overall, 16-fold in the NIR spectral range) than in the case of D-luciferin have been observed with one of the NIRLucs in mice bearing s.c. tumors. We believe that these synthetic luciferins provide a solution to the longstanding limitation in the variety of NIR emitting luciferins and pave the way to the further development of NIR bioluminescence imaging platforms.

Analytical Chemistry (Washington, DC, United States) published new progress about Bioluminescence. 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

Yu, Xiaoling; Zhang, Bingbing; Shan, Guangsheng; Wu, Yue; Yang, Feng-Ling; Lei, Xinsheng published the artcile< Synthesis of the molecular hybrid inspired by Largazole and Psammaplin A>, SDS of cas: 96929-05-4, the main research area is macrocyclic depsipeptide hybrid thiol synthesis HDAC inhibitor antitumor agent; natural product largazole psammaplin A drug design; methylcysteine acylation cyclocondensation thiazole thiazoline hydrolysis; malic acid cyclocondensation trichloro ethanediol esterification amidation; macrolactamization protective group.

One important class of HDAC (histone deacetylation enzymes) inhibitors is the sulfur-containing marine natural products with structural diversity. Inspired by two structurally distinguishing examples, Largazole and Psammaplin A, which possess macrocyclic depsipeptide and simple linear amide scaffold resp., we designed one novel mol. hybrid by replacing the alkene moiety in Largazole with a semirigid amide bond. This hybrid compound has been synthesized from L-malic acid in 10 steps with an overall yield of 7%. The preliminary biol. assays suggest that the replacement of trans olefin moiety with amide bond will lead to an unbeneficial effect on the inhibition against HDACs.

Tetrahedron published new progress about (Fluorenylmethoxy)carbonyl group. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, SDS of cas: 96929-05-4.

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

Xiao, Yao; Peng, Jinrong; Liu, Qingya; Chen, Lijuan; Shi, Kun; Han, Ruxia; Yang, Qian; Zhong, Lin; Zha, Ruoyu; Qu, Ying; Qian, Zhiyong published the artcile< Ultrasmall CuS@BSA nanoparticles with mild photothermal conversion synergistically induce MSCs-differentiated fibroblast and improve skin regeneration>, Product Details of C11H8N2O3S2, the main research area is copper sulfide BSA nanoparticle MSC fibroblast skin regeneration; CuS@BSA; MSCs; differentiation; photothermal conversion; wound healing..

Mesenchymal stem cell (MSC)-based therapies have been used in skin regeneration due to their ability to differentiate into many cells, promote cytokine secretion and participate in collagen deposition. In this study, we concluded that a CuS@BSA nanoparticles exhibited similar potential in inducing MSCs differentiation to fibroblasts as Cu ions for wound healing. First, we verified the photothermal efficiency of CuS@BSA in vivo and vitro and had no cytotoxicity for MSCs when the temperature was controlled at 42°C by adjusting the power of irradiation at 980 nm. And then we detected the expression of vimentin in MSCs, which further directed the MSCs to fibroblasts through Western blotting and Immunofluorescence when treated with CuS@BSA or pre-heat at 42°C. In addition, we implanted MSCs into the Matrigel or electrospun PLA nanofiber membrane in vitro to evaluating the effect of heating or CuS@BSA on the morphol. change of MSCs by SEM. Finally, we evaluated improving skin regeneration by the combination of preheated-MSCs and CuS@BSA nanoparticles that were encapsulated in Matrigel. The CuS@BSA nanoparticles have good photothermal conversion efficiency. Not only CuS nanoparticles itself or after irradiation at 980 nm stimulated the expressioin of vimentin in MSCs. Besides, the CuS@BSA can promote cell proliferation as Cu ion through the expression of ERK. The combination of the CuS@BSA nanoparticles and thermal treatment synergistically improved the closure of an injured wound in an injured wound model. MSCs combined with CuS@BSA are a promising wound dressing for the reconstruction of full-thickness skin injuries.

Theranostics published new progress about Bioluminescence. 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

Stoneman, Michael R.; Raicu, Valerica published the artcile< Dielectric spectroscopy based detection of specific and nonspecific cellular mechanisms>, SDS of cas: 2591-17-5, the main research area is dielec spectroscopy GPCR ligand interaction intracellular transport; G protein-coupled receptor; GPCR; dielectric relaxation; dielectric spectroscopy; label-free detection; ligand binding.

Using radiofrequency dielec. spectroscopy, we have investigated the impact of the interaction between a G protein-coupled receptor (GPCR), the sterile2 α-factor receptor protein (Ste2), and its cognate agonist ligand, the α-factor pheromone, on the dielec. properties of the plasma membrane in living yeast cells (Saccharomyces cerevisiae). The dielec. properties of a cell suspension containing a saturating concentration of α-factor were measured over the frequency range 40 Hz-110 MHz and compared to the behavior of a similarly prepared suspension of cells in the absence of α-factor. A spherical three-shell model was used to determine the elec. phase parameters for the yeast cells in both types of suspensions. The relative permittivity of the plasma membrane showed a significant increase after exposure to α-factor (by 0.06 ± 0.05). The equivalent experiment performed on yeast cells lacking the ability to express Ste2 showed no change in plasma membrane permittivity. Interestingly, a large change also occurred to the elec. properties of the cellular interior after the addition of α-factor to the cell suspending medium, whether or not the cells were expressing Ste2. We present a number of different complementary experiments performed on the yeast to support these dielec. data and interpret the results in terms of specific cellular reactions to the presence of α-factor.

Sensors published new progress about Cell membrane. 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