Month: October 2022

Oberkersch, Roxana E.; Pontarin, Giovanna; Astone, Matteo; Spizzotin, Marianna; Arslanbaeva, Liaisan; Tosi, Giovanni; Panieri, Emiliano; Ricciardi, Sara; Allega, Maria Francesca; Brossa, Alessia; Grumati, Paolo; Bussolati, Benedetta; Biffo, Stefano; Tardito, Saverio; Santoro, Massimo M. published the artcile< Aspartate metabolism in endothelial cells activates the mTORC1 pathway to initiate translation during angiogenesis>, Computed Properties of 112-63-0, the main research area is endothelial cell angiogenesis mTORC1 aspartate metabolism translation; angiogenesis; aspartate metabolism; endothelial metabolism; mTOR signalling; tumor angiogenesis.

Angiogenesis, the active formation of new blood vessels from pre-existing ones, is a complex and demanding biol. process that plays an important role in physiol. as well as pathol. settings. Recent evidence supports cell metabolism as a critical regulator of angiogenesis. However, whether and how cell metabolism regulates endothelial growth factor receptor levels and nucleotide synthesis remains elusive. We here shown in both human cell lines and mouse models that during developmental and pathol. angiogenesis, endothelial cells (ECs) use glutaminolysis-derived glutamate to produce aspartate (Asp) via aspartate aminotransferase (AST/GOT). Asp leads to mTORC1 activation which, in turn, regulates endothelial translation machinery for VEGFR2 and FGFR1 synthesis. Asp-dependent mTORC1 pathway activation also regulates de novo pyrimidine synthesis in angiogenic ECs. These findings identify glutaminolysis-derived Asp as a regulator of mTORC1-dependent endothelial translation and pyrimidine synthesis. Our studies may help overcome anti-VEGF therapy resistance by targeting endothelial growth factor receptor translation.

Developmental Cell published new progress about Angiogenesis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Computed Properties of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Fonseca, Emanuella M. B.; Trivella, Daniela B. B.; Scorsato, Valeria; Dias, Mariana P.; Bazzo, Natalia L.; Mandapati, Kishore R.; de Oliveira, Fabio L.; Ferreira-Halder, Carmen V.; Pilli, Ronaldo A.; Miranda, Paulo C. M. L.; Aparicio, Ricardo published the artcile< Crystal structures of the apo form and a complex of human LMW-PTP with a phosphonic acid provide new evidence of a secondary site potentially related to the anchorage of natural substrates>, Electric Literature of 112-63-0, the main research area is phosphonic acid binding secondary site LMW phosphatase crystal structure; Anticancer drugs; Crystal structure; Enzyme kinetics; LMW-PTP; Phosphatase inhibitors; Structure-based drug design.

Low mol. weight protein tyrosine phosphatases (LMW-PTP, EC 3.1.3.48) are a family of single-domain enzymes with mol. weight up to 18 kDa, expressed in different tissues and considered attractive pharmacol. targets for cancer chemotherapy. Despite this, few LMW-PTP inhibitors have been described to date, and the structural information on LMW-PTP druggable binding sites is scarce. In this study, a small series of phosphonic acids were designed based on a new crystallog. structure of LMW-PTP complexed with benzylsulfonic acid, determined at 2.1 Å. In silico docking was used as a tool to interpret the structural and enzyme kinetics data, as well as to design new analogs. From the synthesized series, two compounds were found to act as competitive inhibitors, with inhibition constants of 0.124 and 0.047 mM. We also report the 2.4 Å structure of another complex in which LMW-PTP is bound to benzylphosphonic acid, and a structure of apo LMW-PTP determined at 2.3 Å resolution Although no appreciable conformation changes were observed, in the latter structures, amino acid residues from an expression tag were found bound to a hydrophobic region at the protein surface. This regions is neighbored by pos. charged residues, adjacent to the active site pocket, suggesting that this region might be not a mere artifact of crystal contacts but an indication of a possible anchoring region for the natural substrate-which is a phosphorylated protein.

Bioorganic & Medicinal Chemistry published new progress about Crystal structure. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Berthiaume, Sylvie L.; Bray, Brian L.; Hess, Petr; Liu, Yanzhou; Maddox, Michael L.; Muchowski, Joseph M.; Scheller, Markus E. published the artcile< Synthesis of 5-substituted pyrrole-2-carboxaldehydes. Part I. Generation of formal 5-lithiopyrrole-2-carboxaldehyde equivalents by bromine-lithium exchange of 2-bromo-6-(diisopropylamino)-1-azafulvene derivatives>, Formula: C8H9NO3, the main research area is azafulvene lithiated derivative; pyrrolecarboxaldehyde derivative.

The first known lithiated 1-azafulvene derivatives, e.g., I, were generated by a low-temperature bromine-lithium exchange procedure with tert-butyllithium. These lithio species show substantial stability at ≤-90°C because, at these temperatures, the sterically demanding 6-diisopropylamino moiety, unlike the dimethylamino group, completely inhibits nucleophilic addition to C-6. At higher temperatures, the addition of tert-butyllithium to C-6 is significant and it can become the dominant process. The lithio species I is a useful formal equivalent of 5-lithiopyrrole-2-carboxaldehyde since, on reaction with electrophilic reagents and subsequent hydrolysis, a wide variety of regiochem. pure 5-substituted pyrrole-2-carboxaldehydes is formed. The 6-dialkylamino-1-azafulvenes described herein exist predominantly or exclusively as the syn conformer in solution at room temperature This conformational preference is confirmed by a significant NOE effect between H-4 and H-6 in the parent diisopropylamino-substituted azafulvene. The origin of the syn conformational preference stems from a substantial contribution of the charge-separated form to the ground state structure of these compounds, a phenomenon that is strongly supported by variable temperature NMR measurements on 2-bromo-6-diisopropylamino-1-azafulvene.

Canadian Journal of Chemistry published new progress about Lithiation. 7126-50-3 belongs to class esters-buliding-blocks, and the molecular formula is C8H9NO3, Formula: C8H9NO3.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Ghersetti, S.; Giorgianni, S.; Minari, M.; Spunta, G. published the artcile< Far infrared features of quinoline N-oxides. Intramolecular vibrations and hydrogen bonding>, Synthetic Route of 112-63-0, the main research area is quinoline oxide phenol IR; hydrogen bond phenol quinoline oxide; complex phenol quinoline oxide.

The far ir spectra of quinoline N-oxide and its 2-, 3-, and 4-Me, -MeO, -Cl, and -Br derivatives at 40-400 cm-1 in CHCl3-CCl4 (1:1) in the absence and presence of PhOH were recorded and assigned. The strong bands at 160 and 320-40 cm-1 were assigned to an out-of-plane bending mode (γNO) and an in-plane bending vibration (βNO), resp. The stretching modes of the H bonding vibration of the complexes with PhOH were determined and were linearly related to those for pyridine N-oxides for the 3- and 4-substituted derivatives

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about Hydrogen bond. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Synthetic Route of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Park, Yuna; Maeng, Soohyun; Damdintogtokh, Tuvshinzaya; Oh, Hyejin; Bang, Minji; Bai, Jaewoo; Kim, Myung Kyum published the artcile< Microvirga splendida sp. nov., bacteria isolated from soil>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is Microvirga splendida bacteria soil; Methylobacteriaceae; Microvirga; Novel species; Taxonomy.

Two bacterial strains, BT325T and BT690, were isolated from soil samples collected in Korea. Both strains were Gram stain-neg., short rod-shaped, and formed light-pink colored colonies. The 16S rRNA sequence similarity of strains BT325T and BT690 shared a sequence similarity of 99.7%. Both strains shared the highest 16S rRNA gene similarity of 98.6% with Microvirga arabica SV2184PT, followed by Microvirga ossetica V5/3 M T (98.5% and 98.2%, resp.), Microvirga soli R491T (98.3% and 98.2%, resp.), Microvirga aerilata (98.2% and 98.08%, resp.), Microvirga makkahensis (98.08% and 97.8%, resp.). Phylogenetic analyses based on 16S rRNA gene sequences revealed that strain BT325Tand BT690 were positioned in a distinct lineage within the family Methylobacteriaceae (order Rhizobiales, class Alphaproteobacteria). The genome size of strain BT325T was 5,200,315 bp and the genomic DNA G + C content was 64.3 mol%. The sole respiratory quinone of strain BT325T was Q-10 and the predominant cellular fatty acids were summed feature 3 (C16:1ω7c/C16:1ω6c) and summed feature 8 (C18:1ω7c/C18:1ω6c). The major polar lipids were diphosphatidylglycerol, phosphatidylglycerol, phosphatidylethanolamine, and phosphatidylcholine. Polyphasic taxonomic anal. of biochem., chemotaxonomic, and phylogenetic analyses suggested that strains BT325T represents a novel bacterial species within the genus Microvirga, for which the name Microvirga splendida is proposed. The type strain of Microvirga splendida is BT325T (= KCTC 72406 T = NBRC 114847 T).

Antonie van Leeuwenhoek published new progress about 16S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Hechter, Oscar; Terada, Shigeyuki; Spitsberg, Vitaly; Nakahara, Tatsuo; Nakagawaga, S. Hase; Flouret, George published the artcile< Neurohypophyseal hormone-responsive renal adenylate cyclase. III. Relationship between affinity and intrinsic activity in neurohypophyseal hormones and structural analogs>, Synthetic Route of 112-63-0, the main research area is neurohyophyseal hormone structure activity; vasopressin receptor adenyl cyclase; oxytocin structure activity; kidney adenyl cyclase vasopressin.

Binding and adenylate cyclase [9012-42-4] activation with neurohypophyseal hormones (NHH) and synthetic analogs were examined in 2 bovine renal medullary membrane preparations The relation between binding affinity of NHH and 10 analogs (as determined by competitive binding studies with 3H-labeled 8-lysine vasopressin (I) [50-57-7] and adenylate cyclase activation) was studied in 1 membrane preparation under identical conditions where hormonal stimulation of cyclase was at steady state and binding was at (or near) equilibrium A linear relation was demonstrated between the neg. logs of peptide concentration required for half-maximal binding and for half-maximal enzyme activation (Ka). Study of adenylate cyclase activation by NHH analogs, with and without a preliminary preincubation, showed that the magnitude of enzyme stimulation achieved (percentage of Vmax relative to I) with certain low affinity analogs was increased when these peptides were assayed without preincubation (in the 0-10-min period) without significant influence on Ka. To maximize the magnitude of adenylate cyclase stimulation achieved with low affinity analogs, the relation between the apparent affinity and intrinsic activity of 30 NHH analogs was studied in a 2nd membrane, where adenylate cyclase was assayed without preincubation. It was found that the apparent affinity of NHH analogs may be decreased ∼5 orders of magnitude with only minimal (20%) reduction in intrinsic activity. With further decrease in affinity to a critical Ka value, there was an abrupt decrease in intrinsic activity so that peptides with Ka ∼ 2 × 10-4M were either weak partial agonists or competitive antagonists. The tripeptide tails of NHH were not necessary for adenylate cyclase activation. No single amino acid in the ring moieties was essential for biol. activity. Receptor-mediated enzyme activation apparently involves the cooperative interaction of multiple elements of the ring with complementary elements of the receptor, with Asn5 and Tyr2 of the peptide ring playing critical roles. Studies of [Nε-acylated Lys8]vasopressin analogs have revealed it is possible to introduce carboxyl functions in the Lys8 side chain with unexpectedly high retention of affinity. Retro-D analogs of [Gly7]deaminooxytocin and deaminotocinamide, with a free NH2 group, were weak partial agonists; N-formylation, resulting in charge removal, led to loss of agonistic activity with development of antagonistic activity. Structural differences between the bovine and porcine renal receptor have previously been established with respect to position 8 of the vasopressin mol. A 2nd species difference, involving the NH2 terminus of the peptide was also found. The NH2 terminus increased binding affinity in the porcine receptor but not in the bovine receptor where deaminopressinamide [35748-54-0] had a higher affinity than pressinamide [27759-18-8], and 1-deaminooxytocin [113-78-0] had a higher affinity than oxytocin [50-56-6].

Journal of Biological Chemistry published new progress about Cell membrane. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Synthetic Route of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Lee, Yujeong; Onishi, Yoshiyuki; McPherson, Lisa; Kietrys, Anna M.; Hebenbrock, Marian; Jun, Yong Woong; Das, Ishani; Adimoolam, Shanthi; Ji, Debin; Mohsen, Michael G.; Ford, James M.; Kool, Eric T. published the artcile< Enhancing Repair of Oxidative DNA Damage with Small-Molecule Activators of MTH1>, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is human mutant homolog activator preparation oxidative DNA damage repair.

Here, it is reported that selected tyrosine kinase (TK) inhibitors including nilotinib, employed clin. in the treatment of chronic myeloid leukemia, are activators of the repair enzyme Human MutT Homolog 1 (MTH1). MTH1 cleanses the oxidatively damaged cellular nucleotide pool by hydrolyzing the oxidized nucleotide 8-oxo-2′-deoxyguanosine (8-oxo-dG)TP, which is a highly mutagenic lesion when incorporated into DNA. Structural optimization of analogs of TK inhibitors resulted in compounds such as SU0448, which induces 1000 +/- 100% activation of MTH1 at 10μM and 410 +/- 60% at 5μM. The compounds are found to increase the activity of the endogenous enzyme, and at least one (SU0448) decreases levels of 8-oxo-dG in cellular DNA. The results suggest the possibility of using MTH1 activators to decrease the frequency of mutagenic nucleotides entering DNA, which may be a promising strategy to suppress tumorigenesis in individuals with elevated cancer risks.

ACS Chemical Biology published new progress about DNA base excision repair. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Recommanded Product: (9Z,12Z)-Methyl octadeca-9,12-dienoate.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Diantina, S.; McGill, C.; Millner, J.; Nadarajan, J.; Pritchard, H. W.; Colville, L.; Clavijo McCormick, A. published the artcile< Seed viability and fatty acid profiles of five orchid species before and after ageing>, Reference of 112-63-0, the main research area is seed viability fatty acid profile orchid species ageing; Epiphytic Dendrobium; fatty acid methyl esters (FAMEs); gas chromatography (GC); seed lipids; seed storage; terrestrial orchids.

Changes in seed lipid composition during ageing are associated with seed viability loss in many plant species. However, due to their small seed size, this has not been previously explored in orchids. We characterized and compared the seed viability and fatty acid profiles of five orchid species before and after ageing: one tropical epiphytic orchid from Indonesia (Dendrobium strebloceras), and four temperate species from New Zealand, D. cunninghamii (epiphytic), and Gastrodia cunninghamii, Pterostylis banksii and Thelymitra nervosa (terrestrial). Seeds were aged under controlled laboratory conditions (3-mo storage at 60% RH and 20°C). Seed viability was tested before and after ageing using tetrazolium chloride staining. Fatty acid Me esters from fresh and aged seeds were extracted through trans-esterification, and then analyzed using gas chromatog.-mass spectrometry. All species had high initial viability (>80%) and experienced significant viability loss after ageing. The saturated, polyunsaturated, monounsaturated and total fatty acid content decreased with ageing in all species, but this reduction was only significant for D. strebloceras, D. cunninghamii and G. cunninghamii. Our results suggest that fatty acid degradation is a typical response to ageing in orchids, albeit with species variation in magnitude, but the link between fatty acid degradation and viability was not elucidated. Pterostylis banksii exemplified this variation; it showed marked viability loss despite not having a significant reduction in its fatty acid content after ageing. More research is required to identify the effect of ageing on fatty acid composition in orchids, and its contribution to seed viability loss.

Plant Biology (Berlin, Germany) published new progress about Aging, plant. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Reference of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Feng, Wei; Zhang, Xing-Guo published the artcile< Organophosphine-free copper-catalyzed isothiocyanation of amines with sodium bromodifluoroacetate and sulfur>, Synthetic Route of 19241-24-8, the main research area is primary amine sodium bromodifluoroacetate sulfur copper iodide catalyst isothiocyanation; isothiocyanate preparation green chem.

A copper-catalyzed isothiocyanation of amines with sodium bromodifluoroacetate and sulfur in the absence of organophosphine was established. This approach represented a simple and efficient one-pot synthesis of isothiocyanates and features excellent functional group tolerance and the use of a cheap, safe and odorless sulfur source. This process could directly provided isothiocyanate analogous bioactive mols., thiocarbonyl-containing pesticides and facile construction of benzoxazole and benzimidazole frames.

Chemical Communications (Cambridge, United Kingdom) published new progress about Cyanation (isothio). 19241-24-8 belongs to class esters-buliding-blocks, and the molecular formula is C11H13NS, Synthetic Route of 19241-24-8.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Wozniak, Marian; Roszkiewicz, Witold published the artcile< Spectral data of substituted naphthyridines. V. The IR spectra of substituted 1,8-naphthyridines>, Computed Properties of 112-63-0, the main research area is IR naphthyridine derivative.

In general the IR spectra of 1,8-naphthyridines show a ring bending (skeletal) vibration at 690-740-cm-1, three adjacent H absorption at 750-795 and 810-885 cm-1, two adjacent H absorptions at 785-855 cm-1 and isolated H absorptions at 795-810 and 885-920 cm-1.

Zeszyty Naukowe Uniwersytetu Jagiellonskiego, Prace Chemiczne published new progress about IR spectra. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Computed Properties of 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics