Author: Jessica.F

Hu, Xiafei published the artcileConstruction of peptide macrocycles via radical-mediated intramolecular C-H alkylations, SDS of cas: 2418-95-3, the publication is Organic Letters (2021), 23(3), 716-721, database is CAplus and MEDLINE.

Enzyme-catalyzed radical-mediated C-H functionalization reactions allow nature to create natural products of unusual three-dimensional structures from simple linear peptide precursors. In comparison, chemist’s ability to harness radical C-H functionalization reactions for synthesis of complex peptides remains limited. In this work, new methods have been developed to construct peptide macrocycles via radical-mediated intramol. C-H alkylation reactions under photoredox catalysis. Linear peptide precursors equipped with a C-terminal N-(acyloxy)phthalimide ester can cyclize with the α C-H bond of N-terminal glycine or aryl C-H bond of N-heteroarene capping units in high yield and selectivity under mild conditions. The strategy uses the C-H cyclization step to incorporate lysine, homolysine, and various heteroarene-derived amino acid linchpins into peptide macrocycles, enabling convergent and flexible synthesis of complex peptide macrocycles from simple building blocks.

Organic Letters published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, SDS of cas: 2418-95-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Meng, Xu published the artcileNBS-mediated aziridination between styrenes and amides under transition metal-free conditions, Product Details of C7H5Cl2NO, the publication is Journal of Heterocyclic Chemistry (2014), 51(4), 937-942, database is CAplus.

An efficient and simple protocol for N-bromosuccinimide (NBS)-mediated aziridination of styrenes using amides as the nitrenoid source was developed. This aziridination affords the desired products in moderate to good yields without using transition metal catalyst under very mild reaction condition.

Journal of Heterocyclic Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Product Details of C7H5Cl2NO.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wang, Siqi published the artcilePiPo: random copolymers of C- with N-substituted glycines, Product Details of C11H22N2O4, the publication is Polymer Chemistry (2022), 13(3), 383-387, database is CAplus.

Random copolymers of C- with N-substituted glycines (PiPo) were synthesized by carrying out a statistical copolymerization of N-phenyloxycarbonyl-C-substituted glycine (NPC) monomers with N-phenyloxycarbonyl-N-substituted glycine (NNPC) monomers. The copolymerization kinetics were analyzed in detail. The solubility of PiPo was found to highly depend on the compositions of the peptide and peptoid repeat units.

Polymer Chemistry published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C8H6ClF3, Product Details of C11H22N2O4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Ma, Chunying published the artcileA practical and total synthesis of pasireotide: Synthesis of cyclic hexapeptide via a three-component condensation, Synthetic Route of 2418-95-3, the publication is Molecules (2019), 24(11), 2185, database is CAplus and MEDLINE.

Pasireotide is a multi-receptor ligand somatostatin analog approved for medical treatment of Cushing’s disease and acromegaly. The liquid-phase total synthesis of pasireotide-a 18-membered cyclic hexapeptide-was achieved by the 3 + 2 + 1 strategy, and the Pro¹ -Phe⁶ peptide bond was selected as the final cyclization position. Two key fragments were simply synthesized using N,O-bis(trimethylsilyl)acetamide/N-hydroxysuccinimide ester (BSA/NHS) as coupling agents, and processes of the two key fragments were simple without any chromatog. purification The current synthesis method is easily scalable and produces the target peptide with an overall yield of 15%.

Molecules published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Synthetic Route of 2418-95-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wu, Yueming published the artcileSuperfast and Water-Insensitive Polymerization on α-Amino Acid N-Carboxyanhydrides to Prepare Polypeptides Using Tetraalkylammonium Carboxylate as the Initiator, Application In Synthesis of 2418-95-3, the publication is Angewandte Chemie, International Edition (2021), 60(50), 26063-26071, database is CAplus and MEDLINE.

We design the tetraalkylammonium carboxylate-initiated superfast polymerization on α-amino acid N-carboxyanhydrides (NCA) for efficient synthesis of polypeptides. Carboxylates, as a new class of initiator for NCA polymerization, can initiate the superfast NCA polymerization without the need of extra catalysts and the polymerization can be operated in open vessels at ambient condition without the use of glove box. Tetraalkylammonium carboxylate-initiated polymerization on NCA easily affords block copolymers with at least 15 blocks. Moreover, this method avoids tedious purification steps and enables direct polymerization on crude NCAs in aqueous environments to prepare polypeptides and one-pot synthesis of polypeptide nanoparticles. These advantages and the mild polymerization condition of tetraalkylammonium carboxylate-initiated NCA polymerization imply its great potential in functional exploration and application of polypeptides.

Angewandte Chemie, International Edition published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C5H6BNO2, Application In Synthesis of 2418-95-3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wang, Bing published the artcileROS-responsive amphiphilic block copolymer-drug conjugate: Design, synthesis and potential as an efficient drug delivery system via a positive feedback strategy, Related Products of amides-buliding-blocks, the publication is Chemical Engineering Journal (Amsterdam, Netherlands) (2021), 131453, database is CAplus.

Reactive oxygen species (ROS)-responsive drug delivery systems for cancer treatment often suffer insufficient drug release. Herein, we developed a ROS-responsive amphiphilic block copolymer-drug conjugate, TA-CA-Prodrug, based on a pos. feedback strategy to address this issue. Cinnamaldehyde (CA), a ROS-generation agent, was modified as a ROS-responsive linker in the copolymer to connect hydrophilic and hydrophobic segments and conjugate an anti-tumor drug (PTX) to the main copolymeric chain. A pH-sensitive moiety (DPA) was also incorporated to the copolymer. This amphiphilic prodrug self-assembled into micelles at a particle size of around 150 nm with a neg. zeta potential. ROS-responsive release of PTX and CA was confirmed after TA-CA-Prodrug was incubated with H₂O₂, and the drug release rate was dependent on the concentration of H₂O₂. After endocytosis into tumor cells, TA-CA-Prodrug were mainly colocalized with mitochondria owing to the charge reversal after protonation of DPA moieties of TA-CA-Prodrug in an acidic intracellular environment (i.e., pH ≤ 6.2). A relatively high level of ROS around the mitochondria induced simultaneous release of CA and PTX from the prodrug. Then, ROS-generation was triggered by released CA, which in turn enhanced PTX release and PTX-mediated cell cycle arrest, thus resulting in remarkable apoptosis of tumor cells after treatment with TA-CA-Prodrug compared with control groups (TK-Prodrug and Prodrug). Due to a cascaded ROS-feedback strategy, i.v. injection of TA-CA-Prodrug into mice bearing 4 T1 tumors led to a greater tumor inhibition efficacy than control groups, and no obvious side effects were confirmed from negligible changes in body weight as well as H&E stained major organs of mice. Therefore, this block copolymer-drug conjugate could enhance intracellular ROS production for efficient drug release and augment its anti-tumor effect.

Chemical Engineering Journal (Amsterdam, Netherlands) published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C12H10FeO4, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Day, Christopher R. published the artcileHigh-throughput single-molecule screen for small-molecule perturbation of splicing and transcription kinetics, SDS of cas: 380315-80-0, the publication is Methods (Amsterdam, Netherlands) (2016), 59-68, database is CAplus and MEDLINE.

In eukaryotes, mRNA synthesis is catalyzed by RNA polymerase II and involves several distinct steps, including transcript initiation, elongation, cleavage, and transcript release. Splicing of RNA can occur during (co-transcriptional) or after (post-transcriptional) RNA synthesis. Thus, RNA synthesis and processing occurs through the concerted activity of dozens of enzymes, each of which is potentially susceptible to perturbation by small mols. However, there are few, if any, high-throughput screening strategies for identifying drugs which perturb a specific step in RNA synthesis and processing. Here we have developed a high-throughput fluorescence microscopy approach in single cells to screen for inhibitors of specific enzymic steps in RNA synthesis and processing. By utilizing the high affinity interaction between bacteriophage capsid proteins (MS2, PP7) and RNA stem loops, we are able to fluorescently label the intron and exon of a β-globin reporter gene in human cells. This approach allows one to measure the kinetics of transcription, splicing and release in both fixed and living cells using a tractable, genetically encoded assay in a stable cell line. We tested this reagent in a targeted screen of mols. that target chromatin readers and writers and identified three compounds that slow transcription elongation without changing transcription initiation.

Methods (Amsterdam, Netherlands) published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C20H23N3O2S, SDS of cas: 380315-80-0.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Day, Christopher R. published the artcileHigh-throughput single-molecule screen for small-molecule perturbation of splicing and transcription kinetics, Product Details of C25H34N4O2S, the publication is Methods (Amsterdam, Netherlands) (2016), 59-68, database is CAplus and MEDLINE.

In eukaryotes, mRNA synthesis is catalyzed by RNA polymerase II and involves several distinct steps, including transcript initiation, elongation, cleavage, and transcript release. Splicing of RNA can occur during (co-transcriptional) or after (post-transcriptional) RNA synthesis. Thus, RNA synthesis and processing occurs through the concerted activity of dozens of enzymes, each of which is potentially susceptible to perturbation by small mols. However, there are few, if any, high-throughput screening strategies for identifying drugs which perturb a specific step in RNA synthesis and processing. Here we have developed a high-throughput fluorescence microscopy approach in single cells to screen for inhibitors of specific enzymic steps in RNA synthesis and processing. By utilizing the high affinity interaction between bacteriophage capsid proteins (MS2, PP7) and RNA stem loops, we are able to fluorescently label the intron and exon of a β-globin reporter gene in human cells. This approach allows one to measure the kinetics of transcription, splicing and release in both fixed and living cells using a tractable, genetically encoded assay in a stable cell line. We tested this reagent in a targeted screen of mols. that target chromatin readers and writers and identified three compounds that slow transcription elongation without changing transcription initiation.

Methods (Amsterdam, Netherlands) published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, Product Details of C25H34N4O2S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Chen, Yu-Fon published the artcileTRAIL encapsulated to polypeptide-crosslinked nanogel exhibits increased anti-inflammatory activities in Klebsiella pneumoniae-induced sepsis treatment, Formula: C11H22N2O4, the publication is Materials Science & Engineering, C: Materials for Biological Applications (2019), 85-95, database is CAplus and MEDLINE.

Bacterial infections are often treated inadequately. Sepsis, being one of its most severe forms, is a multi-layered, life-threatening syndrome induced by rampant immune responses, like cytokine storms, that leads to high morbidity and death of infected patients. Particularly, the current increment in resistant bacterial strains and the lack of creative antibiotics to counter such menace are central reasons to the worsening of the situation. To avoid the said crisis, the antimicrobial peptides (AMPs) were used to target cell wall components, such as lipopolysaccharides (LPS), seems to have the most promise. These combine the ability of broad-spectrum bactericidal activity with low potential for induction of resistance. Inhibition of cytokine storms induced by activated immune cells has been considered a feasible treatment for in sepsis. One of the therapeutic approaches widely utilized in inducing apoptosis in inflammatory cells is the use of tumor necrosis factor (TNF)-related apoptosis-inducing ligands (TRAIL), which trigger an extrinsic apoptotic pathway via death receptors. Herein, we report TRAIL encapsulated in a bactericidal polypeptide-crosslinked nanogel that suppressed Klebsiella pneumoniae infection and overactive macrophages. Of interest, nanogel and TRAIL-nanogel treatments were more toxic towards LPS-activated cells than to naive cells in cell viability assays. Treatment with TRAIL-nanogel significantly prolonged survival in septic mice and reduced bacterial numbers in circulation. As such, TRAIL-nanogel may be promising as a therapeutic agent for treating bacteria-infected diseases.

Materials Science & Engineering, C: Materials for Biological Applications published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Formula: C11H22N2O4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Jiang, Yan published the artcileElucidation of SIRT-1/PGC-1α-associated mitochondrial dysfunction and autophagy in nonalcoholic fatty liver disease, Category: amides-buliding-blocks, the publication is Lipids in Health and Disease (2021), 20(1), 40, database is CAplus and MEDLINE.

Nonalcoholic fatty liver disease (NAFLD) can lead to chronic liver diseases associated with mitochondrial damages. However, the exact mechanisms involved in the etiol. of the disease are not clear. To gain new insights, the changes affecting sirtuin 1 (SIRT-1) during liver fat accumulation was investigated in a NAFLD mouse model. In addition, the in vitro research investigated the regulation operated by SIRT-1 on mitochondrial structures, biogenesis, functions, and autophagy. In mice NAFLD, high-fat-diet (HFD) increased body weight gain, upregulated serum total cholesterol, triglycerides, aspartate aminotransferase, alanine aminotransferase, blood glucose, insulin levels, and liver malondialdehyde, and decreased liver superoxide dismutase activity. In liver, the levels of SIRT-1 and peroxisome proliferator-activated receptor-gamma coactivator -1α (PGC-1α) decreased. The expression of peroxisome proliferator-activated receptor-α and Beclin-1 proteins was also reduced, while p62/SQSTM1 expression increased. These results demonstrated SIRT-1 impairment in mouse NAFLD. In a well-established NAFLD cell model, exposure of the HepG2 hepatocyte cell line to oleic acid (OA) for 48 h caused viability reduction, apoptosis, lipid accumulation, and reactive oxygen species production Disturbance of SIRT-1 expression affected mitochondria. Pre-treatment with Tenovin-6, a SIRT-1 inhibitor, aggravated the effect of OA on hepG2, while this effect was reversed by CAY10602, a SIRT-1 activator. Further investigation demonstrated that SIRT-1 activity was involved in mitochondrial biogenesis through PGC-1α and participated to the balance of autophagy regulatory proteins. In conclusion, in high-fat conditions, SIRT-1 regulates multiple cellular properties by influencing on mitochondrial physiol. and lipid autophagy via the PGC-1α pathway. The SIRT-1/PGC-1α pathway could be targeted to develop new NAFLD therapeutic strategies.

Lipids in Health and Disease published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics