Category: 79642-50-5

On July 31, 2019, Knewtson, Kelsey E.; Perera, Chamani; Hymel, David; Gao, Zhe; Lee, Molly M.; Peterson, Blake R. published an article.Computed Properties of 79642-50-5 The title of the article was Antibody-Drug Conjugate that Exhibits Synergistic Cytotoxicity with an Endosome-Disruptive Peptide. And the article contained the following:

Antibody-drug conjugates are an important class of cancer therapeutics. These agents generally bind a specific cell surface receptor, undergo receptor-mediated endocytosis, and enter the endosomal-lysosomal system, where the environment in these organelles facilitates the release of a membrane-permeable cytotoxin. By using a membrane-impermeable cytotoxin, we describe here a method that allows the cytotoxicity of an antibody conjugate to be triggered by co-administration with an endosome-disruptive peptide that exhibits low toxicity. This approach was validated by conjugation of an anionic derivative of the tubulin-binding cytotoxin colchinol Me ether to lysine residues of the HER2-targeting antibody trastuzumab (Herceptin) via a disulfide. When this antibody binds HER2 on SKBR3 breast cancer cells and undergoes endocytosis, the membrane-impermeable cytotoxin is released, but it becomes trapped in endosomes, resulting in relatively low cytotoxicity (IC50 > 1μM). However, co-administration with an essentially nontoxic (IC50 > 10μM) cholesterol-linked endosome-disruptive peptide promotes the release of this small mol. into the cytoplasm, conferring subnanomolar cytotoxic potency (IC50 = 0.11 ± 0.07 nM). Studies of a structurally related fluorophore conjugate revealed that the endosome-disruptive peptide does not substantially enhance cleavage of the disulfide (t1/2 = 8 ± 2 h) within endosomes, suggesting that the mechanism of endosomal escape involves the efflux of some small mols. without facilitating substantial influx of reduced glutathione. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Computed Properties of 79642-50-5

The Article related to cancer antibody drug conjugate synergistic cytotoxicity endosome disruptive peptide, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Computed Properties of 79642-50-5

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

On October 17, 2012, Bezouska, Karel; Kubinkova, Zuzana; Stribny, Jiri; Volfova, Barbora; Pompach, Petr; Kuzma, Marek; Sirova, Milada; Rihova, Blanka published an article.Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate The title of the article was Dimerization of an Immunoactivating Peptide Derived from Mycobacterial hsp65 Using N-Hydroxysuccinimide Based Bifunctional Reagents Is Critical for Its Antitumor Properties. And the article contained the following:

We have shown previously that a short pentapeptide derived from the mycobacterial heat shock protein hsp65 can be highly activating for the immune system based on its strong reactivity with the early activation antigen of lymphocytes CD69. Here, we investigated an optimal form of presentation of this antigen to the cells of the immune system. Four different forms of the dimerized heptapeptide LELTEGY, and of the control inactive dimerized heptapeptide LELLEGY that both contained an extra UV active glycine-tyrosine sequence, were prepared using dihydroxysuccinimidyl oxalate (DSO), dihydroxysuccinimidyl tartarate (DST), dihydroxysuccinimidyl glutarate (DSG), and dihydroxysuccinimidyl suberate (DSS), resp. Heptapeptides dimerized through DST and DSG linkers had optimal activity in CD69 precipitation assay. Moreover, dimerization of active heptapeptide resulted in a remarkable increase in its proliferation activity and production of cytokines in vitro. Furthermore, while DST and DSG dimerized heptapeptides both significantly enhanced the cytotoxicity of natural killer cells in vitro, only the DSG dimerized compound was active in suppressing growth of melanoma tumors in mice and in enhancing the cytotoxic activity of tumor infiltrating lymphocytes ex vivo. Thus, while the dimerization of the immunoactive peptide caused a dramatic increase in its immunoactivating properties, its in vivo anticancer properties were influenced by the chem. nature of linker used for its dimerization. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate

The Article related to hsp65 peptide dimerization hydroxysuccinimide linker antitumor immunomodulator, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate

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

On February 19, 2014, Bezouska, Karel; Kubinkova, Zuzana; Stribny, Jiri; Volfova, Barbora; Pompach, Petr; Kuzma, Marek; Sirova, Milada; Rihova, Blanka published an article.Recommanded Product: 79642-50-5 The title of the article was Dimerization of an Immunoactivating Peptide Derived from Mycobacterial hsp65 Using N-Hydroxysuccinimide Based Bifunctional Reagents Is Critical for Its Antitumor Properties [Retraction of document cited in CA157:510077]. And the article contained the following:

This article has been retracted with the agreement of the authors due to evidence of scientific misconduct on the part of the first author. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Recommanded Product: 79642-50-5

The Article related to retraction hsp65 peptide dimerization hydroxysuccinimide linker antitumor immunomodulator, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.Recommanded Product: 79642-50-5

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

Akin, Brandy L.; Jones, Larry R. published an article in 2012, the title of the article was Characterizing Phospholamban to Sarco(endo)plasmic Reticulum Ca2+-ATPase 2a (SERCA2a) Protein Binding Interactions in Human Cardiac Sarcoplasmic Reticulum Vesicles Using Chemical Cross-linking.Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) glutarate And the article contains the following content:

Chem. crosslinking was used to study protein binding interactions between native phospholamban (PLB) and SERCA2a in sarcoplasmic reticulum (SR) vesicles prepared from normal and failed human hearts. Lys27 of PLB was crosslinked to the Ca2+ pump at the cytoplasmic extension of M4 (at or near Lys328) with the homobifunctional crosslinker, disuccinimidyl glutarate (7.7 Å). Crosslinking was augmented by ATP but abolished by Ca2+ or thapsigargin, confirming in native SR vesicles that PLB binds preferentially to E2 (low Ca2+ affinity conformation of the Ca2+-ATPase) stabilized by ATP. To assess the functional effects of PLB binding on SERCA2a activity, the anti-PLB antibody, 2D12, was used to disrupt the phys. interactions between PLB and SERCA2a in SR vesicles. We observed a tight correlation between 2D12-induced inhibition of PLB crosslinking to SERCA2a and 2D12 stimulation of Ca2+-ATPase activity and Ca2+ transport. The results suggest that the inhibitory effect of PLB on Ca2+-ATPase activity in SR vesicles results from mutually exclusive binding of PLB and Ca2+ to the Ca2+ pump, requiring PLB dissociation for catalytic activation. Importantly, the same result was obtained with SR vesicles prepared from normal and failed human hearts; therefore, we conclude that PLB binding interactions with the Ca2+ pump are largely unchanged in failing myocardium. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) glutarate

The Article related to phospholamban sarcoplasmic reticulum calcium atpase heart sarcoplasmic vesicle crosslinking, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Recommanded Product: Bis(2,5-dioxopyrrolidin-1-yl) glutarate

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

Zhuang, Chen; Tao, Fu-Rong; Cui, Yue-Zhi published an article in 2016, the title of the article was Preparation and properties of gelatin films incorporated with N-hydroxysuccinimide-activated end-bit binary acid.Recommanded Product: 79642-50-5 And the article contains the following content:

A series of novel crosslinkers, N-hydroxysuccinimide (NHS)-activated end-bit binary acid (NHS- C4, C5, C6, C8, C10, C14), were synthesized to modify gelatin films and the crosslinking effects were compared. Homogeneous films with the exception of the film crosslinked by NHS-C14 were observed and the thickness was measured using a scanning electron microscope. The section feature influenced by different film-treatment conditions was also recorded. The differential scanning calorimetry results indicated higher thermal stability. The water contact angles confirmed enhanced hydrophobicity. NHS-C6, which was used as a probe crosslinker, exhibited the best crosslinking effect that the content of the free -NH2 achieved was the lowest out of all the crosslinkers. The biodegradation results of gelatin films modified by NHS-C6 exhibited better degradation-resistance and excellent stability. In addition, the optimal exptl. conditions were 45° C for 12 h when [NHS-C6]/[-NH2] = 2.5. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Recommanded Product: 79642-50-5

The Article related to hydroxysuccinimide binary acid preparation gelatin film property, Chemistry of Synthetic High Polymers: Chemical Transformation Of Polymers and other aspects.Recommanded Product: 79642-50-5

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

Hoshino, Ken-ichi; Nakajima, Tasuku; Matsuda, Takahiro; Sakai, Takamasa; Gong, Jian Ping published an article in 2018, the title of the article was Network elasticity of a model hydrogel as a function of swelling ratio: from shrinking to extreme swelling states.HPLC of Formula: 79642-50-5 And the article contains the following content:

In this work, we intended to investigate the relationship between the swelling ratio Q and Young’s modulus E of hydrogels from their contracted state to extreme swelling state and elucidate the underlining mol. mechanism. For this purpose, we used tetra-poly(ethylene glycol) (tetra-PEG) gel, whose network parameters are well known, as the polymer backbone, and we succeeded in tuning the swelling of the gel by a factor of 1500 times while maintaining the topol. structure of the network unchanged, using an approach combining a mol. stent method and a PEG dehydration method. A master curve of Q-E, independent of the method of obtaining Q, was obtained. Using the worm-like chain model, the exptl. determined master curve can be well reproduced. We also observed that the uniaxial stress-strain curve of the hydrogel can be well predicted by the worm-like chain model using the structure parameters determined from the fitting of the Q-E exptl. curve. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).HPLC of Formula: 79642-50-5

The Article related to tetraarm peg model hydrogel network elasticity swelling youngs modulus, Physical Properties of Synthetic High Polymers: Polymer Solutions and Gels and other aspects.HPLC of Formula: 79642-50-5

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

Imberdis, Thibaut; Fanning, Saranna; Newman, Andrew; Ramalingam, Nagendran; Dettmer, Ulf published an article in 2019, the title of the article was Studying α-synuclein conformation by intact-cell cross-linking.Application of 79642-50-5 And the article contains the following content:

β-Sheet-rich aggregates of α-synuclein (αS) are the hallmark neuropathol. of Parkinson’s disease (PD) and related synucleinopathies, whereas the native conformations of αS in healthy cells are under debate. Crosslinking analyses in intact cells detect a large portion of endogenous αS in apparent multimeric states, most notably as putative tetramers (αS60) that run around 60 kDa on SDS-PAGE, but also point at the dynamic nature of cellular αS states. Standardization of αS crosslinking methods will facilitate efforts to study the effects of genetic, pharmacol., and environmental factors on αS conformation. Here, we present detailed protocols for crosslinking cellular αS multimers in cultured cells and brain tissues. These protocols will benefit future studies aimed at characterizing αS conformation in its cellular environment, both at steady state and upon perturbation, be it chronic or acute. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Application of 79642-50-5

The Article related to parkinson disease alpha synuclein cell brain, chemical cross-linking, multimer, parkinson’s disease, protein homeostasis, tetramer, α-synuclein, Mammalian Pathological Biochemistry: Nervous System and Psychiatric Diseases and other aspects.Application of 79642-50-5

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

On February 28, 2022, Jayaraman, Vijay; Lee, D. John; Elad, Nadav; Vimer, Shay; Sharon, Michal; Fraser, James S.; Tawfik, Dan S. published an article.Product Details of 79642-50-5 The title of the article was A counter-enzyme complex regulates glutamate metabolism in Bacillus subtilis. And the article contained the following:

Abstract: Multi-enzyme assemblies composed of metabolic enzymes catalyzing sequential reactions are being increasingly studied. Here, we report the discovery of a 1.6 megadalton multi-enzyme complex from Bacillus subtilis composed of two enzymes catalyzing opposite (counter-enzymes) rather than sequential reactions: glutamate synthase (GltAB) and glutamate dehydrogenase (GudB), which make and break glutamate, resp. In vivo and in vitro studies show that the primary role of complex formation is to inhibit the activity of GudB. Using cryo-electron microscopy, we elucidated the structure of the complex and the mol. basis of inhibition of GudB by GltAB. The complex exhibits unusual oscillatory progress curves and is necessary for both planktonic growth, in glutamate-limiting conditions, and for biofilm growth, in glutamate-rich media. The regulation of a key metabolic enzyme by complexing with its counter enzyme may thus enable cell growth under fluctuating glutamate concentrations [graphic not available: see fulltext]. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Product Details of 79642-50-5

The Article related to bacillus glutamate metabolism gltab gudb, Microbial, Algal, and Fungal Biochemistry: Metabolism and Microbial Nutrition and other aspects.Product Details of 79642-50-5

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

On July 30, 2014, Han, Xu; Bian, Shudan; Liang, Yong; Houk, K. N.; Braunschweig, Adam B. published an article.Name: Bis(2,5-dioxopyrrolidin-1-yl) glutarate The title of the article was Reactions in Elastomeric Nanoreactors Reveal the Role of Force on the Kinetics of the Huisgen Reaction on Surfaces. And the article contained the following:

The force dependence of the copper-free Huisgen cycloaddition between an alkyne and a surface-bound azide was examined in elastomeric nanoreactors. These studies revealed that pressure and chain length are critical factors that determine the reaction rate. These experiments demonstrate the central role of pressure and surface structure on interfacial processes that are increasingly important in biol., materials science, and nanotechnol. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Name: Bis(2,5-dioxopyrrolidin-1-yl) glutarate

The Article related to elastomeric nanoreactor force kinetics huisgen surface, Physical Organic Chemistry: Ring Formation, Cleavage, Enlargement, and Contraction and other aspects.Name: Bis(2,5-dioxopyrrolidin-1-yl) glutarate

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

Yan, Qin; Zheng, Hong-Ning; Jiang, Chuan; Li, Kun; Xiao, Shou-Jun published an article in 2015, the title of the article was EDC/NHS activation mechanism of polymethacrylic acid: anhydride versus NHS-ester.Product Details of 79642-50-5 And the article contains the following content:

Polymer brushes of poly(methacrylic acid) (PMAA) and PMAA/PNIPAM (poly-N-isopropylacrylamide) copolymers were prepared on porous silicon for further investigation of the EDC/NHS (1-ethyl-3-(3-dimethylaminopropyl)carbodiimide/N-hydroxysuccinimide) activation mechanisms by IR spectroscopy. When the fragmentation degree of PMAA blocks in the copolymer is increased, the production of anhydride wanes from dominant to recessive, whereas a complementary product of the NHS-ester waxes from recessive to dominant. The Thorpe-Ingold effect was applied to explain the formation of anhydride: the gem-dialkyl groups of PMAA next to the carboxylic acids compress the acid side chains close to each other; thus, once the intermediate of O-acylisourea forms, it will be attacked by the intramol. neighboring acid much faster than any other nucleophiles such as NHS and water, and therefore the six-membered ring of the anhydride will be formed. All acid side chains in PMAA standing next to each other will form an anhydride, primarily due to the Thorpe-Ingold effect, unless they are sterically hindered, whereas only isolated acid side chains form the NHS-ester. The EDC/NHS activation results for four small mols. of dicarboxylic acids in aqueous media, namely, glutaric acid and 2,2-di-Me glutaric acid, which generate disuccinimidyl ester with high yield, and succinic acid and 2,2-di-Me succinic acid, which remain intact, can also be explained by the Thorpe-Ingold effect. A clear understanding of the EDC/NHS activation mechanisms of PMAA will take us a step closer for resolving the mechanistic ambiguity of the carbodiimide/additive coupling reactions for amide bond formation. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Product Details of 79642-50-5

The Article related to ethyldimethylaminopropylcarbodiimide hydroxysuccinimide activation mechanism polymethacrylic acid anhydride, Chemistry of Synthetic High Polymers: Monomers and Reagents Used In Polymerization and other aspects.Product Details of 79642-50-5

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