Tag: M.W=100-150

Yalcin, Abdullah; Sarkici, Gulcin; Kolac, Umut Kerem published the artcile< PKR inhibitors suppress endoplasmic reticulum stress and subdue glucolipotoxicitymediated impairment of insulin secretion in pancreatic beta cells>, Related Products of 452-06-2, the main research area is pancreatic beta cell protein kinase R inhibitor endoplasmic reticulum; ER stress; protein kinase R; β cell degeneration; Type 2 diabetes.

Type 2 diabetes mellitus is characterized by insulin resistance and hypersecretion of insulin from the pancreas to compensate for decreased insulin sensitivity in the peripheral tissues. In later stages of the disease insulin-secreting beta cell degeneration commences and patients require insulin replacement therapy in order to accomplish proper regulation of their blood glucose. Endoplasmic reticulum (ER) stress in the beta cells is one of the factors contributing to this detrimental effect. Protein kinase R (PKR) is a cellular stress kinase activated by ER stress and contributing to degeneration of pancreatic islets. In order to determine whether inhibition of PKR activation by specific small mol. inhibitors of PKR ameliorates pancreatic insulin secretion capacity, we treated beta cells with two imidazole/oxindole-derived inhibitors of PKR kinase, imoxin (C16) and 2-aminopurine (2-AP), in the presence of ER stress. Our results demonstrate that PKR inhibition suppresses tunicamycin-mediated ER stress without altering the insulin production capacity of the cells. Palmitic acid-mediated suppression of insulin secretion, however, was subdued significantly by PKR inhibitor treatment through an ER stress-related mechanism. We suggest that PKR inhibitor treatment may be used to increase the insulin secretion capacity of the pancreas in later stages of diabetes.

Turkish Journal of Biology published new progress about Cell death. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Related Products of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Plasser, Felix; Gomez, Sandra; Menger, Maximilian F. S. J.; Mai, Sebastian; Gonzalez, Leticia published the artcile< Highly efficient surface hopping dynamics using a linear vibronic coupling model>, Category: imidazoles-derivatives, the main research area is surface hopping dynamics linear vibronic coupling model.

We report an implementation of the linear vibronic coupling (LVC) model within the surface hopping dynamics approach and present utilities for parameterizing this model in a blackbox fashion. This results in an extremely efficient method to obtain qual. and even semi-quant. information about the photodynamical behavior of a mol., and provides a new route toward benchmarking the results of surface hopping computations. The merits and applicability of the method are demonstrated in a number of applications. First, the method is applied to the SO2 mol. showing that it is possible to compute its absorption spectrum beyond the Condon approximation, and that all the main features and timescales of previous on-the-fly dynamics simulations of intersystem crossing are reproduced while reducing the computational effort by three orders of magnitude. The dynamics results are benchmarked against exact wavepacket propagations on the same LVC potentials and against a variation of the electronic structure level. Four addnl. test cases are presented to exemplify the broader applicability of the model. The photodynamics of the isomeric adenine and 2-aminopurine mols. are studied and it is shown that the LVC model correctly predicts ultrafast decay in the former and an extended excited-state lifetime in the latter. Futhermore, the method correctly predicts ultrafast intersystem crossing in the modified nucleobase 2-thiocytosine and its absence in 5-azacytosine while it fails to describe the ultrafast internal conversion to the ground state in the latter.

Physical Chemistry Chemical Physics published new progress about Absorption spectra. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Mandal, Paulami; De, Debojyoti; Yun, Kyunghee; Kim, Kyeong Kyu published the artcile< Improved differentiation of human adipose stem cells to insulin-producing β-like cells using PDFGR kinase inhibitor Tyrphostin9>, Related Products of 452-06-2, the main research area is human insulin PDFGR kinase inhibitor adipose stem cell; Adipose-derived stem cells; Diabetes mellitus; Differentiation; PDGFR inhibitor; β-cell.

Diabetes mellitus (DM) is a metabolic syndrome where insulin secretion or the response to insulin produced by the body is compromised. The only available long-term treatment is the transplantation of pancreas or islet for procuring β-cells. However, due to the shortage of β-cell sources from the tissues, differentiation of pluripotent stem cells or terminally differentiated cells into β-cell is proposed as an alternative strategy. Previously, human adipose-derived stem cells (ADSCs) were reported to be converted into β-like cells by a stepwise treatment of chems. and growth factors. However, due to the low conversion efficiency, the clin. application was not feasible. In this study, we developed a modified conversion protocol with improved yield and functionality, which is achieved by changing the culture method and addition of Tyrphostin9, a platelet-derived growth factor receptor (PDGFR) kinase inhibitor. Tyrphostin9 was identified from a cell-based chem. screening using the mCherry reporter under the control of the Pdx1 promoter. The β-like cells differentiated under the new protocol showed a 3.6-fold increase in the expression of Pdx1, a marker for pancreatic differentiation, as compared to the previous protocol. We propose that Tyrphostin9 contributes to the β-like cell differentiation by playing a dual role; enhancing the definitive endoderm generation by inhibiting the PI3K signaling and suppressing the taurine-mediated proliferation of definitive endoderm. Importantly, these differentiated cells responded well to low and high glucose stimulations compared to cells differentiated by the previous protocol, as confirmed by the 2.0-fold increase in the C-peptide release. As ADSCs are abundant, easily isolated, and autologous in nature, improved differentiation approaches to generate β-like cells from ADSCs would provide a better opportunity for treating diabetes.

Biochemical and Biophysical Research Communications published new progress about Diabetes mellitus. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Related Products of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Lund, Paul E.; Chatterjee, Surajit; Daher, May; Walter, Nils G. published the artcile< Protein unties the pseudoknot: S1-mediated unfolding of RNA higher order structure>, Electric Literature of 452-06-2, the main research area is proteinS1 pseudoknot unfolding RNA preQ1 riboswitch conformation modeling Escherichia.

Ribosomal protein S1 plays important roles in the translation initiation step of many Escherichia coli mRNAs, particularly those with weak Shine-Dalgarno sequences or structured 5′ UTRs, in addition to a variety of cellular processes beyond the ribosome. In all cases, the RNA-binding activity of S1 is a central feature of its function. While sequence determinants of S1 affinity and many elements of the interactions of S1 with simple secondary structures are known, mechanistic details of the protein’s interactions with RNAs of more complex secondary and tertiary structure are less understood. Here, we investigate the interaction of S1 with the well-characterized H-type pseudoknot of a class-I translational preQ1 riboswitch as a highly structured RNA model whose conformation and structural dynamics can be tuned by the addition of ligands of varying binding affinity, particularly preQ1, guanine, and 2,6-diaminopurine. Combining biochem. and single mol. fluorescence approaches, we show that S1 preferentially interacts with the less folded form of the pseudoknot and promotes a dynamic, partially unfolded conformation. The ability of S1 to unfold the RNA is inversely correlated with the structural stability of the pseudoknot. These mechanistic insights delineate the scope and limitations of S1-chaperoned unfolding of structured RNAs.

Nucleic Acids Research published new progress about 5′-Untranslated region Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Electric Literature of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Godefroi, E. F.; Loozen, H. J. J.; Luderer-Platje, J. Th. J. Mrs. published the artcile< Synthesis of 1,2-disubstituted imidazole-5-carboxaldehydes and-4,5-dicarboxaldehydes>, Application In Synthesis of 36947-69-0, the main research area is formylation imidazole; imidazotropones; imidazopyridazine; pyridazine imidazo.

1,2-Disubstituted imidazoles react with refluxing 37% CH2O in Ac2O-NaOAc buffer. Both 5-hydroxymethyl- and 4,5-bis(hydroxymethyl)imidazole derivatives are formed in 25-50% yields. Bis(hydroxymethylation) is favored by prolonged reaction and is dependent upon the nature of the C-2 substituent. Oxidation of the mono- and dihydroxymethylimidazoles by Pb(OAc)4 in pyridine affords the imidazole-mono- and -dicarboxaldehydes. A few reactions of 1-benzyl-2-isopropylimidazole-4,5-dicarboxaldehyde (I) with certain ketones and with hydrazine are described.

Recueil des Travaux Chimiques des Pays-Bas published new progress about 36947-69-0. 36947-69-0 belongs to class imidazoles-derivatives, and the molecular formula is C7H12N2, Application In Synthesis of 36947-69-0.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Lo, Chen-Yu; Gao, Yang published the artcile< DNA Polymerase-Parental DNA Interaction Is Essential for Helicase-Polymerase Coupling during Bacteriophage T7 DNA Replication>, Reference of 452-06-2, the main research area is bacteriophage T7 DNA replication polymerase helicase coupling; DNA replication; bacteriophage T7; helicase; polymerase.

DNA helicase and polymerase work cooperatively at the replication fork to perform leading-strand DNA synthesis. It was believed that the helicase migrates to the forefront of the replication fork where it unwinds the duplex to provide templates for DNA polymerases. However, the mol. basis of the helicase-polymerase coupling is not fully understood. The recently elucidated T7 replisome structure suggests that the helicase and polymerase sandwich parental DNA and each enzyme pulls a daughter strand in opposite directions. Interestingly, the T7 polymerase, but not the helicase, carries the parental DNA with a pos. charged cleft and stacks at the fork opening using a β-hairpin loop. Here, we created and characterized T7 polymerases each with a perturbed β-hairpin loop and pos. charged cleft. Mutations on both structural elements significantly reduced the strand-displacement synthesis by T7 polymerase but had only a minor effect on DNA synthesis performed against a linear DNA substrate. Moreover, the aforementioned mutations eliminated synergistic helicase-polymerase binding and unwinding at the DNA fork and processive fork progressions. Thus, our data suggested that T7 polymerase plays a dominant role in helicase-polymerase coupling and replisome progression.

International Journal of Molecular Sciences published new progress about Coliphage T7. 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Reference of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Pagano, Bruno; Iaccarino, Nunzia; Di Porzio, Anna; Randazzo, Antonio; Amato, Jussara published the artcile< Screening of DNA G-quadruplex stabilizing ligands by nano differential scanning fluorimetry>, Application In Synthesis of 452-06-2, the main research area is DNA G quadruplex stabilizing ligand nano differential scanning fluorimetry.

G-quadruplex (G4) nucleic acid structures are involved in a number of different diseases and their drug-induced stabilization is deemed to be a promising therapeutic approach. Herein is reported a proof of principle study on the use of nano differential scanning fluorimetry for a rapid and accurate anal. of G4-stabilizing ligands, exploiting the fluorescence properties of a 2-aminopurine modified G4-forming oligonucleotide.

Analyst (Cambridge, United Kingdom) published new progress about DNA Role: ANT (Analyte), BSU (Biological Study, Unclassified), ANST (Analytical Study), 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

Zhu, Mei; Dong, Biao; Zhang, Guo-Ning; Wang, Ju-Xian; Cen, Shan; Wang, Yu-Cheng published the artcile< Synthesis and biological evaluation of new HIV-1 protease inhibitors with purine bases as P2-ligands>, Reference of 452-06-2, the main research area is HIV1 protease inhibitor purine base derivative; Biological evaluation; HIV-1 protease inhibitors; Purine bases.

Introducing purine bases to P2-ligands might enhance the potency of Human Immunodeficiency Virus-1 (HIV-1) protease inhibitory because of the carbonyl and NH groups promoting the formation of extensive H-bonding interactions. In this work, thirty-three compounds are synthesized and evaluated, among which inhibitors 16a, 16f and 16j (I – III, resp.) containing N-2-(6-substituted-9H-purin-9-yl)acetamide as the P2-ligands along with 4-methoxylphenylsulfonamide as the P2′-ligand, display potent inhibitory effect on the activity of HIV-1 protease with IC50 43 nM, 42 nM and 68 nM in vitro, resp.

Bioorganic & Medicinal Chemistry Letters published new progress about AIDS (disease). 452-06-2 belongs to class imidazoles-derivatives, and the molecular formula is C5H5N5, Reference of 452-06-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Konishi, Hideyuki; Muto, Takashi; Ueda, Tsuyoshi; Yamada, Yayoi; Yamaguchi, Miyuki; Manabe, Kei published the artcile< Imidazole Derivatives as Accelerators for Ruthenium-Catalyzed Hydroesterification and Hydrocarbamoylation of Alkenes: Extensive Ligand Screening and Mechanistic Study>, Recommanded Product: 2-(tert-Butyl)-1H-imidazole, the main research area is imidazole derivative accelerator ruthenium catalyzed hydroesterification hydrocarbamoylation alkene mechanism.

Imidazole derivatives are effective ligands for promoting the [Ru3(CO)12]-catalyzed hydroesterification of alkenes using formates. Extensive ligand screening was performed to identify 2-hydroxymethylated imidazole as the optimal ligand. Neither carbon monoxide gas nor a directing group was required, and the reaction also showed a wide substrate generality. The Ru-imidazole catalyst system also promoted intramol. hydrocarbamoylation to afford lactams. A Ru-imidazole complex was unambiguously analyzed by x-ray crystallog., and it had a trinuclear structure derived from one [Ru3(CO)12] and two ligands. This complex was also successfully used for hydroesterification. The mechanism was examined in detail by using D- and 13C-labeled formates, indicating that the hydroesterification reaction proceeds by a decarbonylation-recarbonylation pathway.

ChemCatChem published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 36947-69-0 belongs to class imidazoles-derivatives, and the molecular formula is C7H12N2, Recommanded Product: 2-(tert-Butyl)-1H-imidazole.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Wang, Li-juan; Ren, Ming; Wang, Hou-xiu; Qiu, Jian-Ge; Jiang, BingHua; Zhang, Chun-yang published the artcile< Construction of a quencher-free cascade amplification system for highly specific and sensitive detection of serum circulating miRNAs>, Computed Properties of 452-06-2, the main research area is microRNA sequence strand displacement amplification blood human neoplasm diagnosis.

Circulating miRNAs are a newly emerging class of noninvasive biomarkers, and the accurate quantification of their expression is essential to the biol. research and early clinic diagnosis. Herein, we demonstrate the construction of a quencher-free cascade amplification system for highly sensitive detection of serum circulating miRNAs. The target miRNA can hybridize with the linear probe to induce the cyclic strand displacement amplification (SDA) (cycle I) for the production of the binding probes. The binding probe can subsequently react with the 2-aminopurine (2-AP)-hairpin probe to induce the recycling exonuclease cleavage of 2-AP-hairpin probes (cycle II), releasing the triggers and 2-AP mols. simultaneously. The released trigger can hybridize with the free linear probe to start new cycles I and II amplifications. Through multiple rounds of cascade amplifications, a large number of 2-AP mols. are released, generating an enhanced fluorescence signal. This method exhibits a large dynamic range of 8 orders of magnitude and a detection limit of 0.16 aM. It can differentiate a single-base mismatch in miR-486-5p, quantify miR-486-5p in lung cancer cells at various stages, and even discriminate the expressions of serum circulating miR-486-5p in healthy persons from that in nonsmall-cell lung carcinoma (NSCLC) patients. Moreover, this assay can be rapidly carried out in one step under isothermal condition in a label-free manner, holding promising applications in point-of-care diagnosis and prognosis of lung cancers.

Analytical Chemistry (Washington, DC, United States) published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (ARHGAP5). 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