Tag: 300-400

On February 1, 2011, Cyrus, Kedra; Wehenkel, Marie; Choi, Eun-Young; Han, Hyeong-Jun; Lee, Hyosung; Swanson, Hollie; Kim, Kyung-Bo published an article.Application In Synthesis of Bis(2,5-dioxopyrrolidin-1-yl) glutarate The title of the article was Impact of linker length on the activity of PROTACs. And the article contained the following:

Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations, a small mol.-based novel technol. termed “PROteolysis TArgeting ChimeraS (PROTACs)” has been developed, targeting proteins for degradation at the post-translational level. Despite the promising potential of PROTACs to serve as mol. probes of complex signaling pathways, their design has not been generalized for broad application. Here, we present the first generalized approach for PROTAC design by fine-tuning the distance between the two participating partner proteins, the E3 ubiquitin ligase and the target protein. As such, we took a chem. approach to create estrogen receptor (ER)-α targeting PROTACs with varying linker lengths and the loss of the ER in cultured cells was monitored via western blot and fluorometric analyses. We found a significant effect of chain length on PROTAC efficacy, and, in this case, the optimum distance between the E3 recognition motif and the ligand was a 16 atom chain length. The information gathered from this experiment may offer a generalizable PROTAC design strategy to further the expansion of the PROTAC toolbox, opening new possibilities for the broad application of the PROTAC strategy in the study of multiple signaling pathways. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Application In Synthesis of Bis(2,5-dioxopyrrolidin-1-yl) glutarate

The Article related to protein linker length breast cancer protac western blot fluorometry, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Application In Synthesis of Bis(2,5-dioxopyrrolidin-1-yl) glutarate

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

Shimomura, Hiromi; Sanada, Kazuo published an article in 1980, the title of the article was Synthesis of DL-γ-carboxyglutamic acid.Computed Properties of 59524-07-1 And the article contains the following content:

DL-γ-Carboxyglutamic acid (I) was prepared from Z-DL-Ser(OTos)OBzl (II; Tos = 4-MeC6H4SO2) and Z-NH-C(=CH2)-CO2Bzl (III; Z = PhCH2O2C) through Z-NH-C[CH2(CO2Bzl)]2-CO2Bzl (IV). A reaction mixture of Z-DL-Ser-OBzl with Tos-Cl in absolute pyridine, was adsorbed on silica gel column and eluted with C6H6 to sep. 36% III and 34% II. II was added to a mixture of 50% NaH and CH2(CO2Bzl)2 in DMF under N2 to give 94% IV, which was also similarly prepared from III. IV in MeOH was hydrogenated in the presence of 10% Pd-C to give 62% I. I showed two peaks in amino acid anal., when it was eluted with buffer solutions of pH 1-3. The experimental process involved the reaction of Benzyl 2-(((benzyloxy)carbonyl)amino)acrylate(cas: 59524-07-1).Computed Properties of 59524-07-1

The Article related to carboxyglutamic acid, serinate aminoacrylate reaction, Synthesis of Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Computed Properties of 59524-07-1

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

Weinstein, Boris; Watrin, Kerry G.; Loie, H. Jeff; Martin, Joseph C. published an article in 1976, the title of the article was Amino acids and peptides. 44. Synthesis of DL-γ-carboxyglutamic acid, new amino acid.Application of 59524-07-1 And the article contains the following content:

Benzyl Nα-benzyloxycarbonyl-L-serinate was converted into the corresponding chloralaninate derivative and alkylation with dibenzyl malonate gave racemic tribenzyl Nα-benzyloxycarbonyl-1,1,2-ethanetricarboxylate via benzyl Nα-benzyloxycarbonyl-2-methyleneglycinate. Hydrogenolysis of the triester gave the desired amino acid. The experimental process involved the reaction of Benzyl 2-(((benzyloxy)carbonyl)amino)acrylate(cas: 59524-07-1).Application of 59524-07-1

The Article related to carboxyglutamic acid, glutamic acid carboxy, Synthesis of Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Application of 59524-07-1

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

van Dongen, Stijn F. M.; Janvore, Julie; van Berkel, Sander S.; Marie, Emmanuelle; Piel, Matthieu; Tribet, Christophe published an article in 2012, the title of the article was Reactive protein-repellent surfaces for the straightforward attachment of small molecules up to whole cells.Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate And the article contains the following content:

Here we present a readily accessible strategy for creating protein-resistant surfaces that contain azides, based on the spontaneous adsorption of a comb-like copolymer. Using a strain-promoted azide alkyne cycloaddition, we illustrate the single-step conjugation of various representatives of important applications, being the labeling with small organic mols., capture of nanoparticles, attachment of native enzymes at a controlled d., and finally control of cell adhesion. We thus demonstrate that advanced biomaterials can be created in two straightforward steps without requiring addnl. reagents, which should make this strategy a valuable tool for researchers in diverse fields. 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 protein repellent surface mol cell, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate

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

On November 1, 2015, Kukacka, Zdenek; Rosulek, Michal; Strohalm, Martin; Kavan, Daniel; Novak, Petr published an article.Application of 79642-50-5 The title of the article was Mapping protein structural changes by quantitative cross-linking. And the article contained the following:

Chem. crosslinking is a promising technol. for protein tertiary structure determination Though the data has low spatial resolution, it is possible to obtain it at physiol. conditions on proteins that are not amenable to standard high resolution techniques such as X-ray, NMR anal. and cryo-EM. Here we demonstrate the utilization of isotopically labeled chem. crosslinking to visualize protein conformation rearrangements. Since calmodulin exists in two distinct conformations (calcium-free and calcium-containing forms), we selected this protein for testing the potential and the limits of a new technique. After crosslinking of both calmodulin forms, the calcium-free and calcium-containing forms were mixed together and digested under different conditions and the products of proteolysis were monitored using high resolution mass spectrometry. Finally, the ratios of heavy/light cross-links were calculated by mMass open source platform. 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 protein mapping structural change quant cross linking, chemical cross-linking, mass spectrometry, protein structure design, proteolysis, quantification, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Application of 79642-50-5

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

Corbille, Anne-Gaelle; Neunlist, Michel; Derkinderen, Pascal published an article in 2016, the title of the article was Cross-linking for the analysis of α-synuclein in the enteric nervous system.Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate And the article contains the following content:

Since the observation that aggregated α-synuclein, the pathol. hallmark of Parkinson’s disease (PD), is found in the gut in almost all patients, it has been suggested that the enteric nervous system (ENS) could be a starting point for α-synuclein pathol. α-synuclein has long been thought to occur as a monomer in living cells, but recent studies reported that it instead exists as a tetramer in non-neuronal cells and in neurons. Given the possible key role of the ENS in PD pathophysiol., we undertook the current research to characterize the native state of α-synuclein in rat primary culture of ENS and in adult human healthy ENS. Using amine-reactive crosslinking, we showed that, by contrast to cell lines and brain neurons, α-synuclein exists primarily as a monomer in intact enteric neurons, suggesting that the native state of α-synuclein is different between the ENS and the brain. Our results provide new insights into the widely discussed concepts of α-synuclein aggregation and misfolding in PD and raise issue about the possible transmission of α-synuclein from the ENS to the brain. Aggregated α-synuclein is found in the gut in almost all Parkinson’s disease patients. We used amine-reactive crosslinking to study the native state of α-synuclein in the enteric nervous system (ENS). We showed that, by contrast to erythroid cells and brain neurons, α-synuclein exists primarily as a monomer in intact enteric neurons. Our results provide new insights into the possible role of the ENS in the pathophysiol. of Parkinson’s disease. 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 synuclein analysis crosslinking enteric nervous system brain human parkinson, parkinson’s disease, cross-linking, enteric nervous system, α-synuclein, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate

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

On October 12, 2020, Bacon, Kaitlyn; Blain, Abigail; Burroughs, Matthew; McArthrur, Nikki; Rao, Balaji M.; Menegatti, Stefano published an article.Name: Bis(2,5-dioxopyrrolidin-1-yl) glutarate The title of the article was Isolation of Chemically Cyclized Peptide Binders Using Yeast Surface Display. And the article contained the following:

Cyclic peptides with engineered protein-binding activity have gained increasing attention for use in therapeutic and biotechnol. applications. The authors describe the efficient isolation and characterization of cyclic peptide binders from genetically encoded combinatorial libraries using yeast surface display. Here, peptide cyclization is achieved by disuccinimidyl glutarate-mediated crosslinking of amine groups within a linear peptide sequence that is expressed as a yeast cell surface fusion. Using this approach, the authors first screened a library of cyclic heptapeptides using magnetic selection, followed by fluorescence activated cell sorting (FACS) to isolate binders for a model target (lysozyme) with low micromolar binding affinity (KD ~1.2-3.7μM). The isolated peptides bind lysozyme selectively and only when cyclized. Importantly, yeast surface displayed cyclic peptides can be used to efficiently obtain quant. estimates of binding affinity, circumventing the need for chem. synthesis of the selected peptides. Subsequently, to demonstrate broader applicability of the authors’ approach, the authors isolated cyclic heptapeptides that bind human interleukin-17 (IL-17) using yeast-displayed IL-17 as a target for magnetic selection, followed by FACS using recombinant IL-17. Mol. docking simulations and follow-up exptl. analyses identified a candidate cyclic peptide that likely binds IL-17 in its receptor binding region with moderate apparent affinity (KD ~300 nM). Taken together, the authors’ results show that yeast surface display can be used to efficiently isolate and characterize cyclic peptides generated by chem. modification from combinatorial libraries. 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 cyclized peptide binder yeast surface display, affinity ligands, cyclic peptides, interleukin-17 (il-17), library screening, yeast-display libraries, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Name: Bis(2,5-dioxopyrrolidin-1-yl) glutarate

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

On July 18, 1980, Miller, Marvin J. published an article.COA of Formula: C18H17NO4 The title of the article was Isourea-mediated preparation of dehydro amino acids. And the article contained the following:

Z-NHCH(CHROH)CO2R1 (I; Z = PhCH2O2C; R = H, R1 = Me, CH2Ph; R, = Me, R1 = CH2Ph) were dehydrated by carbodiimides R2N:C:NR3 (R2 = R3 = CHMe2, cyclohexyl; R2 = cyclohexyl, R3 = 2-morpholinoethyl) in the presence of CuCl catalyst to give 65-96.5% Z-NHCH(:CHR)CO2R1. Ac-Cys-OCH2Ph was treated with Me2CHN:C:NCHMe2 in the presence of CuCl to give AcNHC(:CH2)CO2CH2Ph, whereas this reaction in the absence of CuCl gave [AcNHCH(CO2CH2Ph)CH2]2S. I were prepared by treating Z-NHCH(CHROH)CO2H with O-alkylisourea derivatives The experimental process involved the reaction of Benzyl 2-(((benzyloxy)carbonyl)amino)acrylate(cas: 59524-07-1).COA of Formula: C18H17NO4

The Article related to dehydro amino acid, hydroxy amino acid dehydration carbodiimide, isourea reaction amino acid, Synthesis of Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.COA of Formula: C18H17NO4

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

On January 17, 2012, Rozbesky, Daniel; Man, Petr; Kavan, Daniel; Chmelik, Josef; Cerny, Jiri; Bezouska, Karel; Novak, Petr published an article.Recommanded Product: 79642-50-5 The title of the article was Chemical Cross-Linking and H/D Exchange for Fast Refinement of Protein Crystal Structure. And the article contained the following:

A combination of chem. crosslinking and hydrogen-deuterium exchange coupled to high resolution mass spectrometry was used to describe structural differences of NKR-P1A receptor. The loop region extended from the compact core in the crystal structure is closely attached to the protein core in solution The authors’ approach has potential to refine protein structures in solution within a few days and has very low sample consumption. 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 crosslinking hydrogen deuterium exchange protein structure refinement mass spectrometry, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Recommanded Product: 79642-50-5

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

On April 27, 2021, Yang, Xiaobao; Jiang, Biao; Tan, Wenfu; Xu, Zhongli; Luo, Jia; Wang, Juan; Yang, Jun; Zhang, Shaoqing published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of (aminonitrophenyl)sulfonylpiperazinylbenzamides as protein degradation agents. And the patent contained the following:

The present invention relates to the preparation of (aminonitrophenyl)sulfonylpiperazinylbenzamides, R1-A1-LIN-A2-R2, as protein degradation agents. In particular, R1-A1-LIN-A2-R2, wherein, R1 is 4-[[4-[[4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-cyclohexen-1-yl]methyl]piperazin-1-yl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl]-2-nitro-anilino]methyl]-1-piperidyl, 3-[[4-[[4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-cyclohexen-1-yl]methyl]piperazin-1-yl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzoyl]sulfamoyl]-2-nitro-anilino]methyl]-1-piperidyl, 3-(4-chlorophenyl)-2-[[4-[4-[[3-nitro-4-(tetrahydropyran-4-ylmethylamino)phenyl]sulfonylcarbamoyl]-3-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)phenyl]piperazin-1-yl]methyl]phenoxy, etc.; A1 does not exist or represents a carbonyl group; A2 does not exist or represents a carbonyl group. Further LIN does not exist or represents a (un)substituted linear or branched alkylene group, wherein the alkylene group is optionally selected from oxygen, the group consisting of an optionally substituted heterocyclyl or any combination thereof is interrupted, when LIN does not exist, one of A1 and A2 does not exist and the other represents a carbonyl group, and R2 is I and II, wherein the R3 group represents an ethylene group or a vinylene group or salt, enantiomer, stereoisomer, solvate, polymorph thereof, and application thereof for treating diseases, were prepared The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Category: esters-buliding-blocks

The Article related to aminonitrophenyl sulfonylpiperazinylbenzamide protein degradation agent preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazines and other aspects.Category: esters-buliding-blocks

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