Tag: M.W=200-250

Kwak, Dong-Wook published the artcileLeukotriene B₄ receptors are necessary for the stimulation of NLRP3 inflammasome and IL-1β synthesis in neutrophil-dominant asthmatic airway inflammation, Safety of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Biomedicines (2021), 9(5), 535, database is CAplus and MEDLINE.

The stimulation of the NOD-, LRR- and pyrin domain-containing protein 3 (NLRP3) inflammasome and IL-1β synthesis are associated with chronic respiratory diseases such as neutrophildominant severe asthma. Leukotriene B₄ (LTB₄) is a principal chemoattractant mol. for neutrophil recruitment, and its receptors BLT1 and BLT2 have been suggested to contribute to neutrophildominant asthmatic airway inflammation. However, the relationship between BLT1/2 and NLRP3 in neutrophil-dominant asthmatic airway inflammation has not been previously studied. In the present study, we investigated whether BLT1/2 play any roles in stimulating the NLRP3 inflammasome and IL-1βsynthesis. The blockade of BLT1 or BLT2 clearly suppressed the stimulation of the NLRP3 inflammasome and IL-1β synthesis in house dust mite (HDM)/lipopolysaccharide (LPS)-induced neutrophilic airway inflammation. The enzymes 5-lipoxygenase and 12-lipoxygenase, which catalyze the synthesis of BLT1/2 ligands [LTB₄, 12(S)-hydroxyeicosatetraenoic acid (12(S)-HETE), and 12-hydroxyheptadecatreinoic acid (12-HHT)], were also critically associated with the stimulation of NLRP3 and IL-1β synthesis. Together, our results suggest that the 5-/12-LOX-BLT1/2-linked cascade are necessary for the simulation of the NLRP3 inflammasome and IL-1β synthesis, thus contributing to HDM/LPS-induced neutrophil-dominant airway inflammation.

Biomedicines published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Safety of [(2-Hexylcyclopentylidene)amino]thiourea.

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

Monty, Olivier B. C. published the artcileHomogeneous and Functional Group Tolerant Ring-Closing Metathesis for DNA-Encoded Chemical Libraries, Related Products of amides-buliding-blocks, the publication is ACS Combinatorial Science (2020), 22(2), 80-88, database is CAplus and MEDLINE.

Reaction heterogeneity, poor pH control, and catalyst decomposition in the ring-closing metathesis (RCM) of DNA-chem. conjugates lead to poor yields of the cyclized products. Herein we address these issues with a RCM reaction system that includes a novel aqueous solvent combination to enable reaction homogeneity, an acidic buffer system which masks traditionally problematic functional groups, and a decomposition-resistant catalyst which maximizes conversion to the cyclized product. Addnl., we provide a systematic study of the substrate scope of the on-DNA RCM reaction, a demonstration of its applicability to a single-substrate DNA-encoded chem. library that includes sequencing anal., and the first successful stapling of an unprotected on-DNA [i, i+4] peptide.

ACS Combinatorial Science 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, Related Products of amides-buliding-blocks.

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

Jonczyk, Andrzej published the artcileReactions of organic anions; LXXXV. Catalytic two-phase alkylation of cyanamide, Name: N,N-Dibenzylcyanamide, the publication is Synthesis (1978), 882-3, database is CAplus.

R₂NCN (R = PhCH₂, H₂C:CHCH₂, Bu, Et, Me₂CHCH₂CH₂, Me₂CH, Me, MeOCH₂, BuOCH₂) were prepare by reaction of H₂NCN with RX (X = Cl, Br) in presence of Aliquat 336. The heterocycles I [Q = (CH₂)_n, n = 2, 3, 4; o-C₆H₄] were similarly prepared from H₂NCN and BrCH₂QCH₂Br.

Synthesis published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Name: N,N-Dibenzylcyanamide.

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

Mukaiyama, Teruaki published the artcileThe effects of substituents on the hydrolysis of substituted cyanamides in sulfuric acid solution, Category: amides-buliding-blocks, the publication is Bulletin of the Chemical Society of Japan (1954), 416-21, database is CAplus.

The following RR’NCN were prepared either from RR’NH and BrCN, or (where R and R’ are the same) from the corresponding halide and Na₂NCN [R, R’, b.p. (mm.) given, resp.]: Et, H, 94-5° (4); Bu, H, 117° (14); n-heptyl, H, nondistillable; iso-Pr, H, 108° (10); tert-Bu, H, 109-10° (11); allyl, H, 92° (3); Ph, H, -, m. 42°; Et, Et, 78° (16); Bu, Bu, 120-1° (16); iso-Pr, iso-Pr, 93-4° (25); allyl, allyl, 107-8° (18); PhCH₂, PhCH₂, m. 53.5°. The hydrolysis of 0.1M solutions of the RR’NCN in 3:1 dioxane-water containing 20% by weight of H₂SO₄ was followed kinetically by contraction in volume, measured with a dilatometer. All of the ureas thus produced were known compounds except N,N-diallylurea, m. 64° (from petr. ether). Tables of rate constants at different temperatures, activation energies, and entropies of activation are given for hydrolysis of the various cyanamides. The rate of reaction increases in the series: (iso-Pr)₂, Et₂, Ph, tert.-Bu, H₂, iso-Pr, Et, heptyl. From these results it is proposed that the rate-determining step in the hydrolysis mechanism is the protonation of the cyanamide bisulfate, RR’NC(:NH)OSO₃H, which is in turn dependent upon the basic strength of the cyanamide. This hypothesis is not in accord with the mechanism proposed by Kilpatrick (C.A. 41, 1916g).

Bulletin of the Chemical Society of Japan published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Category: amides-buliding-blocks.

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

McCutcheon, David C. published the artcilePhotoproximity Profiling of Protein-Protein Interactions in Cells, Recommanded Product: H-Lys(Boc)-OH, the publication is Journal of the American Chemical Society (2020), 142(1), 146-153, database is CAplus and MEDLINE.

We report a novel photoproximity protein interaction (PhotoPPI) profiling method to map protein-protein interactions in vitro and in live cells. This approach utilizes a bioorthogonal, multifunctional chem. probe that can be targeted to a genetically encoded protein of interest (POI) through a modular SNAP-Tag/benzylguanine covalent interaction. A first generation photoproximity probe, PP1, responds to 365 nm light to simultaneously cleave a central nitroveratryl linker and a peripheral diazirine group, resulting in diffusion of a highly reactive carbene nucleophile away from the POI. We demonstrate facile probe loading, and subsequent interaction- and light-dependent proximal labeling of a model protein-protein interaction (PPI) in vitro. Integration of the PhotoPPI workflow with quant. LC-MS/MS enabled unbiased interaction mapping for the redox regulated sensor protein, KEAP1, for the first time in live cells. We validated known and novel interactions between KEAP1 and the proteins PGAM5 and HK2, among others, under basal cellular conditions. By contrast, comparison of PhotoPPI profiles in cells experiencing metabolic or redox stress confirmed that KEAP1 sheds many basal interactions and becomes associated with known lysosomal trafficking and proteolytic proteins like SQSTM1, CTSD, and LGMN. Together, these data establish PhotoPPI as a method capable of tracking the dynamic subcellular and protein interaction “social network” of a redox-sensitive protein in cells with high temporal resolution

Journal of the American Chemical Society 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, Recommanded Product: H-Lys(Boc)-OH.

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

Kim, Byung-Seok published the artcilePd-Catalyzed Sequential C-C and C-N Bond Formations for the Synthesis of N-Heterocycles: Exploiting Protecting Group-Directed C-H Activation under Modified Reaction Conditions, Safety of (2-Pivalamidophenyl)boronic acid, the publication is Chemistry – An Asian Journal (2011), 6(8), 1952-1957, database is CAplus and MEDLINE.

A Pd-catalyzed domino olefination/conjugate addition reaction of N-Ts-2-arylanilines with activated olefins has been achieved at ambient temperature under the newly defined reaction conditions. This process highlighted the directing effect of the N-protecting group in C-H activation, displayed broad substrate scope with wide functional group compatibility; thus rendering a straightforward entry to a wide variety of N-heterocycles such as dihydrophenanthridines.

Chemistry – An Asian Journal published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Safety of (2-Pivalamidophenyl)boronic acid.

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

Min, Arim published the artcileNOX2-Derived ROS-Mediated Surface Translocation of BLT1 Is Essential for Exocytosis in Human Eosinophils Induced by LTB₄, Computed Properties of 321673-30-7, the publication is International Archives of Allergy and Immunology (2014), 165(1), 40-51, database is CAplus and MEDLINE.

Background: Leukotriene B₄ (LTB₄) is a proinflammatory lipid mediator that elicits eosinophil exocytosis, leading to allergic inflammation. However, the detailed intracellular signaling mechanisms of eosinophil exocytosis induced by LTB₄ are poorly understood. Herein, we report that NADPH oxidase (NOX)2-derived reactive oxygen species (ROS)-mediated BLT1 migration to the cell surface is required for exocytosis in human eosinophils induced by LTB₄. Methods: Peripheral blood eosinophils were purified and stimulated for up to 60 min with LTB₄. The signaling role of NOX2-derived ROS in BLT1-dependent exocytosis in LTB₄-stimulated eosinophils was investigated. Results: Stimulating eosinophils with LTB₄ induced intracellular ROS production and surface upregulation of the exocytosis marker protein CD63 via BLT1-mediated signaling. LTB₄ induced p47^phox phosphorylation and 91^phox expression required for NOX2 activation in a BLT1-dependent manner. Pretreatment with NOX2 inhibitors, but not mitochondria inhibitor, prevented LTB₄-induced ROS generation and exocytosis. At 30 min after stimulation with LTB₄, BLT1 expression at the cell surface was upregulated. LTB₄-triggered surface upregulation of BLT1 was also blocked by inhibition of ROS generation with NOX2 inhibitors. Moreover, stimulation for 30 min with LTB₄ resulted in the interaction of BLT1 with NOX2 by immunoprecipitation LTB₄-induced ROS generation, surface upregulation of BLT1 and exocytosis was also inhibited by pretreatment with a lipid raft disruptor, protein kinase C inhibitor, or Src kinase inhibitor. Conclusion: These results suggest that NOX2-derived ROS-mediated BLT1 trafficking to the cell surface plays a key role in the exocytosis of human eosinophils induced by LTB₄.

International Archives of Allergy and Immunology published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Computed Properties of 321673-30-7.

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

Min, Arim published the artcileBLT1-mediated O-GlcNAcylation is required for NOX2-dependent migration, exocytotic degranulation and IL-8 release of human mast cell induced by Trichomonas vaginalis-secreted LTB₄, Safety of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Microbes and Infection (2018), 20(6), 376-384, database is CAplus and MEDLINE.

Trichomonas vaginalis is a sexually-transmitted protozoan parasite that causes vaginitis and cervicitis. Although mast cell activation is important for provoking tissue inflammation during infection with parasites, information regarding the signaling mechanisms in mast cell activation and T. vaginalis infection is limited. O-linked N-acetylglucosamine (O-GlcNAc) is a post-translational modification of serine and threonine residues that functions as a critical regulator of intracellular signaling, regulated by O-GlcNAc transferase (OGT) and O-GlcNAcase (OGA). We investigated if O-GlcNAcylation was associated with mast cell activation induced by T. vaginalis-derived secretory products (TvSP). Modified TvSP collected from live trichomonads treated with the 5-lipooxygenase inhibitor AA861 inhibited migration of mast cells. This result suggested that mast cell migration was caused by stimulation of T. vaginalis-secreted leukotrienes. Using the BLT1 antagonist U75302 or BLT1 siRNA, we found that migration of mast cells was evoked via LTB₄ receptor (BLT1). Furthermore, TvSP induced protein O-GlcNAcylation and OGT expression in HMC-1 cells, which was prevented by transfection with BLT1 siRNA. TvSP-induced migration, ROS generation, CD63 expression and IL-8 release were significantly suppressed by pretreatment with OGT inhibitor ST045849 or OGT siRNA. These results suggested that BLT1-mediated OGlcNAcylation was important for mast cell activation during trichomoniasis.

Microbes and Infection published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Safety of [(2-Hexylcyclopentylidene)amino]thiourea.

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

Uddin, Mohib published the artcileResolvins: Natural agonists for resolution of pulmonary inflammation, Computed Properties of 321673-30-7, the publication is Progress in Lipid Research (2011), 50(1), 75-88, database is CAplus and MEDLINE.

A review. Inappropriate or excessive pulmonary inflammation can contribute to chronic lung diseases. In health, the resolution of inflammation is an active process that terminates inflammatory responses. The recent identification of endogenous lipid-derived mediators of resolution has provided a window to explore the pathobiol. of inflammatory disease and structural templates for the design of novel pro-resolving therapeutics. Resolvins (resolution-phase interaction products) are a family of pro-resolving mediators that are enzymically generated from essential omega-3 polyunsaturated fatty acids. Two mol. series of resolvins have been characterised, namely E- and D-series resolvins which possess distinct structural, biochem. and pharmacol. properties. Acting as agonists at specific receptors (CMKLR1, BLT1, ALX/FPR2 and GPR32), resolvins can signal for potent counter-regulatory effects on leukocyte functions, including preventing uncontrolled neutrophil swarming, decreasing the generation of cytokines, chemokines and reactive oxygen species and promoting clearance of apoptotic neutrophils from inflamed tissues. Hence, resolvins provide mechanisms for cytoprotection of host tissues to the potentially detrimental effects of unresolved inflammation. This review highlights recent exptl. findings in resolvin research, and the impact of these stereospecific mols. on the resolution of pulmonary inflammation and tissue catabasis.

Progress in Lipid Research published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C6H10F3NO, Computed Properties of 321673-30-7.

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

Ko, Wooseok published the artcileConstruction of bacterial cells with an active transport system for unnatural amino acids, Application In Synthesis of 2418-95-3, the publication is ACS Synthetic Biology (2019), 8(5), 1195-1203, database is CAplus and MEDLINE.

Engineered organisms with an expanded genetic code have attracted much attention in chem. and synthetic biol. research. In this work, engineered bacterial organisms with enhanced unnatural amino acid (UAA) uptake abilities were developed by screening periplasmic binding protein (PBP) mutants for recognition of UAAs. A FRET-based assay was used to identify a mutant PBP (LBP-AEL) with excellent binding affinity (K_d ≈ 500 nM) to multiple UAAs from 37 mutants. Bacterial cells expressing LBP-AEL showed up to 5-fold enhanced uptake of UAAs, which was determined by genetic incorporation of UAAs into a green fluorescent protein and measuring UAA concentration in cell lysates. To the best of our knowledge, this work is the first report of engineering cellular uptake of UAAs and could provide an impetus for designing advanced unnatural organisms with an expanded genetic code, which function with the efficiency comparable to that of natural organisms. The system would be useful to increase mutant protein yield from lower concentrations of UAAs for industrial and large-scale applications. In addition, the techniques used in this report such as the sensor design and the measurement of UAA concentration in cell lysates could be useful for other biochem. applications.

ACS Synthetic Biology 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, Application In Synthesis of 2418-95-3.

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