Month: December 2022

Caterino, Marco published the artcileSelective binding of a bioactive porphyrin-based photosensitizer to the G-quadruplex from the KRAS oncogene promoter, Computed Properties of 111-87-5, the main research area is cervical cancer KRAS porphyrin G quadruplex photosensitizer photodynamic therapy; Biophysics; Chlorins; G-quadruplex; Ligands; Photodynamic activity; Singlet oxygen generation.

The G-quadruplex-forming sequence within the KRAS proto-oncogene P1 promoter is a promising target for anticancer therapy. Porphyrin derivatives are among the most rewarding G-quadruplex binders. They can also behave as photosensitizers. Three water-soluble, pos. charged porphyrin-like compounds were synthesized and tested for their interaction with the KRAS G-quadruplex by CD, fluorescence, and mol. docking calculations For a comparison of ligands binding affinity and selectivity, TMPyP4 was taken as a reference One out of the three tested compounds proved biol. activity and selectivity for G-quadruplex over duplex DNA. It also showed to discriminate between different G-quadruplex topologies, with a preference for the parallel over antiparallel conformation. Mol. docking studies suggested a preferential binding to the 3′-end of the KRAS G-quadruplex driven through π-π stacking interactions. Biol. assays also revealed a good photodynamic-induced cytotoxicity on HeLa cells. The reported results show that these porphyrin-like compounds could actually give the basis for the development of G-quadruplex ligands with effective photodynamic-induced cytotoxicity on cancer cells. The possibility of obtaining photosensitizers with improved physico-chem. features and able to selectively target G-quadruplexes is a very interesting perspective to develop new therapeutic agents.

International Journal of Biological Macromolecules published new progress about Antitumor agents. 111-87-5 belongs to class alcohols-buliding-blocks, name is n-Octanol, and the molecular formula is C8H18O, Computed Properties of 111-87-5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Bueno, Maria J. published the artcileEssentiality of fatty acid synthase in the 2D to anchorage-independent growth transition in transforming cells, SDS of cas: 97-67-6, the main research area is embryonic fibroblast breast carcinoma epithelial cell FASN tumor growth.

Upregulation of fatty acid synthase (FASN) is a common event in cancer, although its mechanistic and potential therapeutic roles are not completely understood. In this study, we establish a key role of FASN during transformation. FASN is required for eliciting the anaplerotic shift of the Krebs cycle observed in cancer cells. However, its main role is to consume acetyl-CoA, which unlocks isocitrate dehydrogenase (IDH)-dependent reductive carboxylation, producing the reductive power necessary to quench reactive oxygen species (ROS) originated during the switch from two-dimensional (2D) to three-dimensional (3D) growth (a necessary hallmark of cancer). Upregulation of FASN elicits the 2D-to-3D switch; however, FASN’s synthetic product palmitate is dispensable for this process since cells satisfy their fatty acid requirements from the media. In vivo, genetic deletion or pharmacol. inhibition of FASN before oncogenic activation prevents tumor development and invasive growth. These results render FASN as a potential target for cancer prevention studies.

Nature Communications published new progress about Antitumor agents. 97-67-6 belongs to class alcohols-buliding-blocks, name is (S)-2-hydroxysuccinic acid, and the molecular formula is C4H6O5, SDS of cas: 97-67-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Rossiter, Nicholas J. published the artcileCRISPR screens in physiologic medium reveal conditionally essential genes in human cells, Formula: C4H6O5, the main research area is human essential gene physiol medium CRISPR screen; CRISPR; HPLM; conditional gene essentiality; gene-nutrient interaction; genetic screen; physiologic medium.

Forward genetic screens across hundreds of cancer cell lines have started to define the genetic dependencies of proliferating human cells and how these vary by genotype and lineage. Most screens, however, have been carried out in culture media that poorly reflect metabolite availability in human blood. Here, we performed CRISPR-based screens in traditional vs. human plasma-like medium (HPLM). Sets of conditionally essential genes in human cancer cell lines span several cellular processes and vary with both natural cell-intrinsic diversity and the combination of basal and serum components that comprise typical media. Notably, we traced the causes for each of three conditional CRISPR phenotypes to the availability of metabolites uniquely defined in HPLM vs. conventional media. Our findings reveal the profound impact of medium composition on gene essentiality in human cells, and also suggest general strategies for using genetic screens in HPLM to uncover new cancer vulnerabilities and gene-nutrient interactions.

Cell Metabolism published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (EIF3A). 97-67-6 belongs to class alcohols-buliding-blocks, name is (S)-2-hydroxysuccinic acid, and the molecular formula is C4H6O5, Formula: C4H6O5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Di Nottia, Michela published the artcileA homozygous MRPL24 mutation causes a complex movement disorder and affects the mitoribosome assembly, Recommanded Product: (S)-2-hydroxysuccinic acid, the main research area is movement disorder MRPL24 mutation mitoribosome; MRPL24; Mitochondrial disorders; Mitochondrial protein synthesis; Mitoribosomes; Molecular modeling; Movement disorder; Protein interactions; Zebrafish.

Mitochondrial ribosomal protein large 24 (MRPL24) is 1 of the 82 protein components of mitochondrial ribosomes, playing an essential role in the mitochondrial translation process. We report here on a baby girl with cerebellar atrophy, choreoathetosis of limbs and face, intellectual disability and a combined defect of complexes I and IV in muscle biopsy, caused by a homozygous missense mutation identified in MRPL24. The variant predicts a Leu91Pro substitution at an evolutionarily conserved site. Using human mutant cells and the zebrafish model, we demonstrated the pathol. role of the identified variant. In fact, in fibroblasts we observed a significant reduction of MRPL24 protein and of mitochondrial respiratory chain complex I and IV subunits, as well a markedly reduced synthesis of the mtDNA-encoded peptides. In zebrafish we demonstrated that the orthologue gene is expressed in metabolically active tissues, and that gene knockdown induced locomotion impairment, structural defects and low ATP production The motor phenotype was complemented by human WT but not mutant cRNA. Moreover, sucrose d. gradient fractionation showed perturbed assembly of large subunit mitoribosomal proteins, suggesting that the mutation leads to a conformational change in MRPL24, which is expected to cause an aberrant interaction of the protein with other components of the 39S mitoribosomal subunit.

Neurobiology of Disease published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (COXIV). 97-67-6 belongs to class alcohols-buliding-blocks, name is (S)-2-hydroxysuccinic acid, and the molecular formula is C4H6O5, Recommanded Product: (S)-2-hydroxysuccinic acid.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Liu, Mengdi published the artcileCyanobacteria blooms potentially enhance volatile organic compound (VOC) emissions from a eutrophic lake: Field and experimental evidence, Category: alcohols-buliding-blocks, the main research area is cyanobacteria bloom volatile organic compound emission eutrophic lake; Cyanobacteria blooms (CBBs); Eutrophic lake; Fluxes; Life stages; Volatile organic compounds (VOCs).

Eutrophication promotes massive cyanobacteria blooms (CBBs), leading to the release of volatile organic compounds (VOCs). To investigate the effects of cyanobacteria on VOC emissions, field campaigns were carried out in eutrophic Chaohu Lake at six sites with different microalgae densities during CBBs in summer 2019, and incubation experiments were performed in the laboratory The results showed that the lake water was the primary source of VOCs at six sampling sites in Chaohu Lake during CBBs, with an average total VOC flux of 81.2 ± 20.6 μg m-2 h-1. Alkanes were the most abundantly emitted VOCs, with a share of 23.1-63.7% of total emitted VOCs, followed by aromatics (16.6-46.3%). The fluxes of total VOCs were significantly greater at sites B and/or C than at site A in July, and at site B′ and/or C′ than at site A′ in August in Chaohu Lake. The fluxes of total VOCs from living and decayed cyanobacteria in the exptl. treatments were two orders of magnitude higher than the corresponding values in the control treatments in the laboratory incubation. Taken together, these results suggested that CBBs potentially enhanced VOC emissions from the eutrophic lake, and that cyanobacteria acted as an important source of VOCs. Addnl., non-methane hydrocarbons (i.e., alkanes, alkenes, and aromatics) predominated among the released VOCs during the stabilization and senescence stages, while oxygenated volatile organic compounds (i.e. alcs., aldehydes, ketones, esters, and furans) prevailed during the apoptosis stage and aromatics and volatile organic sulfur compounds predominated during the decomposition stage, suggesting that VOC emissions varied markedly at different life stages.

Environmental Research published new progress about Aldehydes Role: ANT (Analyte), POL (Pollutant), ANST (Analytical Study), OCCU (Occurrence). 505-10-2 belongs to class alcohols-buliding-blocks, name is 3-(Methylthio)propan-1-ol, and the molecular formula is C4H10OS, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Nguyen, Thuy published the artcileDiarylureas Containing 5-Membered Heterocycles as CB1 Receptor Allosteric Modulators: Design, Synthesis, and Pharmacological Evaluation, COA of Formula: C4H11NO2, the main research area is diarylurea heterocycle synthesis SAR cannabinoid CB1 receptor; CB1 receptor; PSNCBAM-1; allosteric modulators; diarylurea; five-membered heterocycles; structure−activity relationship.

Allosteric modulators have attracted significant interest as an alternate strategy to modulate CB1 receptor signaling for therapeutic benefits that may avoid the adverse effects associated with orthosteric ligands. Here we extended our previous structure-activity relationship studies on the diarylurea-based CB1 neg. allosteric modulators (NAMs) by introducing five-membered heterocycles to replace the 5-pyrrolidinylpyridinyl group in PSNCBAM-1 (1), one of the first generation CB1 allosteric modulators. Many of these compounds had comparable potency to 1 in blocking the CB1 agonist CP55,940 stimulated calcium mobilization and [35S]GTP-γ-S binding. Similar to 1, most compounds showed pos. cooperativity by increasing [3H]CP55,940 binding, consistent with the pos. allosteric modulator (PAM)-antagonist mechanism. Interestingly, these compounds exhibited differences in ability to increase specific binding of [3H]CP55,940 and decrease binding of the antagonist [3H]SR141716. In saturation binding studies, only increases in [3H]CP55,940 Bmax, but not Kd, were observed, suggesting that these compounds stabilize low affinity receptors into a high affinity state. Among the series, the 2-pyrrolyl analog (I) exhibited greater potency than 1 in the [35S]GTP-γ-S binding assay and significantly enhanced the maximum binding level in the [3H]CP5,5940 binding assay, indicating greater CB1 receptor affinity and/or cooperativity.

ACS Chemical Neuroscience published new progress about Central nervous system disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, COA of Formula: C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Li, Rui published the artcileTreatment of azole-containing industrial wastewater by the Fenton process, Synthetic Route of 110-99-6, the main research area is treatment azole containing industrial wastewater Fenton process.

Some semiconductor fabrication processes generate high-strength wastewater that may contain high concentrations of azoles, amines, hydrogen peroxide, organic, and inorganic co-contaminants, making the treatment of this wastewater challenging. In this study, the Fenton process was utilized for the treatment of 53 mM pyrazole and 34 mM 2-(2-aminoethoxy) ethanol (known as diglycolamine, DGA) in a lab-prepared aqueous mixture containing 3.5 M hydrogen peroxide and 16 mM inorganic fluoride. The effects of operational variables for the Fenton process, such as temperature (10, 18, or 25°C), iron dosing (32.3, 37.3, or 74.5 mM), and pH (2.5, 3.0, or 3.5), on the degradation rates were investigated. The chosen variables were then used to treat wastewater from a semiconductor fabrication facility. The Fenton process was effective in treating both the lab-prepared mixture and semiconductor industrial wastewater. The degradation of pyrazole and DGA yielded a range of byproducts including inorganic ions and organic acids.

Industrial & Engineering Chemistry Research published new progress about Catalytic wastewater decomposition. 110-99-6 belongs to class alcohols-buliding-blocks, name is 2,2′-Oxydiacetic acid, and the molecular formula is C4H6O5, Synthetic Route of 110-99-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Yasukata, Tatsuro published the artcilePractical Synthetic Method for the Preparation of Pyrone Diesters: An Efficient Synthetic Route for the Synthesis of Dolutegravir Sodium, Name: 2,2-Dimethoxyethanamine, the main research area is pyrone diester dolutegravir sodium synthesis.

A highly efficient and practical synthetic method for the preparation of pyrone diesters was established. The pyrone diester 3c (I) can be prepared from readily available starting materials on a multihundred gram scale. The pyrone diester 3c can easily be converted to dolutegravir sodium (II.Na). The synthetic route demonstrated herein provides an efficient and atom-economical synthetic method for preparing this potent anti-HIV agent.

Organic Process Research & Development published new progress about Atom economy. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Name: 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Al-Wahaibi, Lamya H. Naser published the artcileComparative study on the essential oils of Artemisia judaica and A. herba-alba from Saudi Arabia, Recommanded Product: rel-(1R,2R,4R)-1,7,7-Trimethylbicyclo[2.2.1]heptan-2-ol, the main research area is Artemisia Aspergillus Syncephalastrum Bacillis Pseudomonas essential oils Saudi Arabia.

The volatile chem. constituents derived from two Asteraceae species (Artemisia judaica and A. herba-alba) were analyzed and compared for the first time using gas chromatog. techniques (GC-MS, GC-FID, Co-GC, LRI determination, database and literature searches) on two different stationary phase columns (polar and nonpolar). This anal. led to the identification of a total of 110 and 81 components from whole plant (stems, leaves and flowers) oils of A. judaica and A. herba-alba resp. The major classes of compounds in both plants included oxygenated monoterpenes, sesquiterpenes and hydrocarbons. The prominent components in the oil of A. judaica were β-eudesmol, hexadecanoic acid, spathulenol, eudesma-4 (15),7-dien-1-β-ol, carvacrol and thymol which account for 67.3% of the total essential oils composition (96.7%). While the main oil constituents from A. herba-alba were piperitone, (E)-ethylcinnamate, (Z)-ethylcinnamate, thymol, isophrone which account for 78.0% of the total oil composition (99.6%). Comparison showed similar composition in thymol and spathulenol while in others major constituents, have opposite values. To the best of our knowledge, both plant species (A. judaica and A. herba-alba) from Saudi Arabia were considered for the first time in this study. In addition, the oils of these plants were screened for their bio-activities and were found to possess significant anti-microbial activities.

Arabian Journal of Chemistry published new progress about Antimicrobial agents. 124-76-5 belongs to class alcohols-buliding-blocks, name is rel-(1R,2R,4R)-1,7,7-Trimethylbicyclo[2.2.1]heptan-2-ol, and the molecular formula is C10H18O, Recommanded Product: rel-(1R,2R,4R)-1,7,7-Trimethylbicyclo[2.2.1]heptan-2-ol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Chen, Xiao-Tong published the artcileEffects of xingnaojing injection on adenosinergic transmission and orexin signaling in lateral hypothalamus of ethanol-induced coma rats, Synthetic Route of 124-76-5, the main research area is coma xingnaojing injection adenosinergic transmission orexin lateral hypothalamus.

Acute alc. exposure induces unconscious condition such as coma whose main phys. manifestation is the loss of righting reflex (LORR). Xingnaojing Injection (XNJI), which came from Chinese classic formula An Gong Niu Huang Pill, is widely used for consciousness disorders in China, such as coma. Although XNJI efficiently shortened the duration of LORR induced by acute ethanol, it remains unknown how XNJI acts on ethanol-induced coma (EIC). We performed experiments to examine the effects of XNJI on orexin and adenosine (AD) signaling in the lateral hypothalamic area (LHA) in EIC rats. Results showed that XNJI reduced the duration of LORR, which implied that XNJI promotes recovery form coma. Microdialysis data indicated that acute ethanol significantly increased AD release in the LHA but had no effect on orexin A levels. The qPCR results displayed a significant reduction in the Orexin-1 receptors (OX1R) expression with a concomitant increase in the A1 receptor (A1R) and equilibrative nucleoside transporter type 1 (ENT1) expression in EIC rats. In contrast, XNJI reduced the extracellular AD levels but orexin A levels remained unaffected. XNJI also counteracted the downregulation of the OX1R expression and upregulation of A1R and ENT1 expression caused by EIC. Based on these results, we suggest that XNJI promotes arousal by inhibiting adenosine neurotransmission via reducing AD level and the expression of A1R and ENT1.

BioMed Research International published new progress about Blumea balsamifera. 124-76-5 belongs to class alcohols-buliding-blocks, name is rel-(1R,2R,4R)-1,7,7-Trimethylbicyclo[2.2.1]heptan-2-ol, and the molecular formula is C10H18O, Synthetic Route of 124-76-5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts