Category: 882847-32-7

Gardiner, James published the artcileβ-peptide conjugates: Syntheses and CD and NMR investigations of β/α-chimeric peptides, of a DPA-β-decapeptide, and of a PEGylated β-heptapeptide, Related Products of esters-buliding-blocks, the main research area is chimeric peptide dipicolinic acid solid phase synthesis; PEGylated heptapeptide solid phase synthesis; peptide solution mol structure CD NMR helical conformation.

β3-Peptides consisting of six, seven, and ten homologated proteinogenic amino acid residues have been attached to an α-heptapeptide (all D-amino acid residues), to a hexaethylene glycol chain (PEGylation), and to dipicolinic acid (DPA derivative, DPA = dipicolinic acid), resp. The conjugation of the β-peptides with the second component was carried out through the N-termini in all three cases. According to NMR anal. (CD3OH solutions), the (M)-314-helical structure of the β-peptidic segments was unscathed in all three chimeric compounds The α-peptidic section of the α/β-peptide was unstructured, and so was the oligoethylene glycol chain in the PEGylated compound Thus, neither does the appendage influence the β-peptidic secondary structure, nor does the latter cause any order in the attached oligomers to be observed by this method of anal. A similar conclusion may be drawn from CD spectra. These results bode well for the development of delivery systems involving β-peptides.

Helvetica Chimica Acta published new progress about Amino acids Role: RCT (Reactant), RACT (Reactant or Reagent). 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, Related Products of esters-buliding-blocks.

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

Fischer, Gabriel published the artcileOptimized solid phase-assisted synthesis of dendrons applicable as scaffolds for radiolabeled bioactive multivalent compounds intended for molecular imaging, Category: esters-buliding-blocks, the main research area is radiosynthesis dendron scaffold mol imaging radiotracer PET.

Dendritic structures, being highly homogeneous and sym., represent ideal scaffolds for the multimerization of bioactive mols. and thus enable the synthesis of compounds of high valency which are e.g., applicable in radiolabeled form as multivalent radiotracers for in vivo imaging. As the commonly applied solution phase synthesis of dendritic scaffolds is cumbersome and time-consuming, a synthesis strategy was developed that allows for the efficient assembly of acid amide bond-based highly modular dendrons on solid support via standard Fmoc solid phase peptide synthesis protocols. The obtained dendritic structures comprised up to 16 maleimide functionalities and were derivatized on solid support with the chelating agent DOTA. The functionalized dendrons furthermore could be efficiently reacted with structurally variable model thiol-bearing bioactive mols. via click chem. and finally radiolabeled with 68Ga. Thus, this solid phase-assisted dendron synthesis approach enable s the fast and straightforward assembly of bioactive multivalent constructs for example applicable as radiotracers for in vivo imaging with Positron Emission Tomog. (PET).

Molecules published new progress about Dimers Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, Category: esters-buliding-blocks.

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

Farrow, Blake published the artcileEpitope Targeting of Tertiary Protein Structure Enables Target-Guided Synthesis of a Potent In-Cell Inhibitor of Botulinum Neurotoxin, COA of Formula: C28H37NO9, the main research area is tertiary protein target guided indium cell inhibitor botulinum neurotoxin; botulinum neurotoxin; combinatorial screening; epitope targeting; peptides; target-guided synthesis.

Botulinum neurotoxin (BoNT) serotype A is the most lethal known toxin and has an occluded structure, which prevents direct inhibition of its active site before it enters the cytosol. Target-guided synthesis by in situ click chem. is combined with synthetic epitope targeting to exploit the tertiary structure of the BoNT protein as a landscape for assembling a competitive inhibitor. A substrate-mimicking peptide macrocycle is used as a direct inhibitor of BoNT. An epitope-targeting in situ click screen is utilized to identify a second peptide macrocycle ligand that binds to an epitope that, in the folded BoNT structure, is active-site-adjacent. A second in situ click screen identifies a mol. bridge between the two macrocycles. The resulting divalent inhibitor exhibits an in vitro inhibition constant of 165 pM against the BoNT/A catalytic chain. The inhibitor is carried into cells by the intact holotoxin, and demonstrates protection and rescue of BoNT intoxication in a human neuron model.

Angewandte Chemie, International Edition published new progress about Cytosol. 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, COA of Formula: C28H37NO9.

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

Alavi, Seyed Ebrahim published the artcileOptimized Methods for the Production and Bioconjugation of Site-Specific, Alkyne-Modified Glucagon-Like Peptide-1 (GLP-1) Analogs to Azide-Modified Delivery Platforms Using Copper-Catalyzed Alkyne-Azide Cycloaddition, Application of 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, the main research area is glucagon like peptide 1 analog alkyne azide cycloaddition.

This study aimed to develop and optimize chemistries to produce alkyne-modified glucagon-like peptide-1(7-36)-amide (GLP-1(7-36)-NH2) libraries, which could be rapidly and efficiently conjugated to other components and screened to identify compounds with the best drug delivery properties, as potential treatments for type 2 diabetes or obesity. For this purpose, the Lys26 (K26) side-chain, and the amino (N)- and carboxy (C)-termini of a dipeptidyl peptidase 4 (DPPIV)-resistant GLP-1 sequence (GLP-1(7-36;A8G)-NH2), were modified with an alkyne (4-pentynoic acid or propiolic acid). These analogs were characterized with respect to human GLP-1 receptor (hGLP-1R) agonist activity, effects on cell viability and human serum stability, revealing that these modifications maintained low (N-terminal; EC50 1.5 x 10-9 M) to subnanomolar (C-terminal and K26, ~4 x 10-10 M) agonist activity toward hGLP-1, had no effect on cell viability, and for the N-terminal and K26 modifications, increased human serum proteolytic stability (t1/2 > 24 h). Copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction conditions were investigated using the C-terminal modified GLP-1 analog and an azide-modified model lipid peptide, with respect to the effects of altering the azide/alkyne ratio, cosolvents, temperature, reducing agents, Cu(I)-stabilizing ligand, copper source, and the concentrations of reagents/reactants, in order to identify general conditions that provide fast reactions and high yields. A 1:2 azide-alkyne (lipid:GLP-1 peptide) and 4:1 sodium ascorbate/copper sulfate molar ratio in 65% volume/volume DMSO-water at room temperature, in the absence of Cu(I)-stabilizing ligands (THPTA or L-histidine) and buffers (phosphate, pH 7), provided the best yields. This work reports a library of characterized GLP-1 analogs and chemistries for their attachment to other species, providing useful tools to improve GLP-1 delivery and pharmacol. (e.g., through conjugation to other species that lower blood glucose, increase the duration of action, or enable delivery via a nonparenteral route).

Bioconjugate Chemistry published new progress about Buffers. 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, Application of 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid.

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

Deyle, Kaycie M. published the artcileA protein-targeting strategy used to develop a selective inhibitor of the E17K point mutation in the PH domain of Akt1, HPLC of Formula: 882847-32-7, the main research area is protein Akt1 inhibitor E17K mutation PH domain PIP3 peptide.

Ligands that can bind selectively to proteins with single amino-acid point mutations offer the potential to detect or treat an abnormal protein in the presence of the wild type (WT). However, it is difficult to develop a selective ligand if the point mutation is not associated with an addressable location, such as a binding pocket. Here we report an all-chem. synthetic epitope-targeting strategy that we used to discover a 5-mer peptide with selectivity for the E17K-transforming point mutation in the pleckstrin homol. domain of the Akt1 oncoprotein. A fragment of Akt1 that contained the E17K mutation and an I19[propargylglycine] substitution was synthesized to form an addressable synthetic epitope. Azide-presenting peptides that clicked covalently onto this alkyne-presenting epitope were selected from a library using in situ screening. One peptide exhibits a 10:1 in vitro selectivity for the oncoprotein relative to the WT, with a similar selectivity in cells. This 5-mer peptide was expanded into a larger ligand that selectively blocks the E17K Akt1 interaction with its PIP3 (phosphatidylinositol (3,4,5)-trisphosphate) substrate.

Nature Chemistry published new progress about Epitopes. 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, HPLC of Formula: 882847-32-7.

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

Aplander, Karolina published the artcileMolecular Wipes: Application to Epidemic Keratoconjuctivitis, COA of Formula: C28H37NO9, the main research area is topical skin wipe keratoconjunctivitis pentacosadiynoic acid polyethylene glycol.

Epidemic keratoconjunctivitis (EKC) is a severe disease of the eye, caused by members of the Adenoviridae (Ad) family, with symptoms such as keratitis, conjunctivitis, pain, edema, and reduced vision that may last for months or years. There are no vaccines or antiviral drugs available to prevent or treat EKC. It was found previously that EKC-causing Ads use sialic acid as a cellular receptor and demonstrated that soluble, sialic acid-containing mols. can prevent infection. In this study, multivalent sialic acid constructs based on 10,12-pentacosadiynoic acid (PDA) have been synthesized, and these constructs are shown to be efficient inhibitors of Ad binding (IC50 = 0.9 μM) and Ad infectivity (IC50 = 0.7 μM). The mechanism of action is to aggregate virus particles and thereby prevent them from binding to ocular cells. Such formulations may be used for topical treatment of adenovirus-caused EKC.

Journal of Medicinal Chemistry published new progress about Adenoviridae. 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, COA of Formula: C28H37NO9.

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

Yang, Yilei published the artcileDesign, synthesis, and biological characterization of novel PEG-linked dimeric modulators for CXCR4, Product Details of C28H37NO9, the main research area is polyethylene glycol dimeric peptide preparation CXCR4 modulator; CXCR4; Dimeric ligands; PEG.

CXCR4 dimerization has been widely demonstrated both biol. and structurally. This paper mainly focused on the development of structure-based dimeric ligands that target CXCL12-CXCR4 interaction and signaling. This study presents the design and synthesis of a series of [PEG]n linked dimeric ligands of CXCR4 based on the knowledge of the homodimeric crystal structure of CXCR4 and the authors’ well established platform of chem. and bioassays for CXCR4. These new ligands include [PEG]n linked homodimeric or heterodimeric peptides consisting of either two DV3-derived moieties (where DV3 is an all-D-amino acid analog of N-terminal modules of 1-10 (V3) residues of vMIP-II) or hybrids of DV3 moieties and CXCL121-8. Among a total of 24 peptide ligands, four antagonists and three agonists showed good CXCR4 binding affinity, with IC50 values of <50 nM and <800 nM, resp. Chemotaxis and calcium mobilization assays with SUP-T1 cells further identified two promising lead modulators of CXCR4: ligand 4 ((DV3-PEG3)2K), a [PEG3]2 linked homodimeric DV3, was an effective CXCR4 antagonist (IC50 = 22 nM); and ligand 21 (DV3-PEG3-K-(PEG3-CXCL121-8)), a [PEG3]2 linked heterodimeric DV3-CXCL121-8, was an effective CXCR4 agonist (IC50 = 407 nM). These dimeric CXCR4 modulators represent new mol. probes and therapeutics that effectively modulate CXCL12-CXCR4 interaction and function. Bioorganic & Medicinal Chemistry published new progress about Cell migration. 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, Product Details of C28H37NO9.

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

Stefanick, Jared F. published the artcileA Systematic Analysis of Peptide Linker Length and Liposomal Polyethylene Glycol Coating on Cellular Uptake of Peptide-Targeted Liposomes, Recommanded Product: 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, the main research area is peptide linker liposome polyethylene glycol coating cell uptake targeting.

PEGylated liposomes are attractive pharmaceutical nanocarriers; however, literature reports of ligand-targeted nanoparticles have not consistently shown successful results. Here, we employed a multifaceted synthetic strategy to prepare peptide-targeted liposomal nanoparticles with high purity, reproducibility, and precisely controlled stoichiometry of functionalities to evaluate the role of liposomal PEG coating, peptide EG-linker length, and peptide valency on cellular uptake in a systematic manner. We analyzed these parameters in two distinct disease models where the liposomes were functionalized with either HER2- or VLA-4-antagonistic peptides to target HER2-overexpressing breast cancer cells or VLA-4-overexpressing myeloma cells, resp. When targeting peptides were tethered to nanoparticles with an EG45 (∼PEG2000) linker in a manner similar to a more traditional formulation, their cellular uptake was not enhanced compared to non-targeted versions regardless of the liposomal PEG coating used. Conversely, reduction of the liposomal PEG to PEG350 and the peptide linker to EG12 dramatically enhanced cellular uptake by âˆ? fold and âˆ?00 fold in the breast cancer and multiple myeloma cells, resp. Uptake efficiency reached a maximum and a plateau with âˆ?% peptide d. in both disease models. Taken together, these results demonstrate the significance of using the right design elements such as the appropriate peptide EG-linker length in coordination with the appropriate liposomal PEG coating and optimal ligand d. in efficient cellular uptake of liposomal nanoparticles.

ACS Nano published new progress about Antitumor agents. 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, Recommanded Product: 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid.

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

Zhang, Chi published the artcileSite-Selective Cysteine-Cyclooctyne Conjugation, Computed Properties of 882847-32-7, the main research area is cysteine cyclooctyne conjugation DBCO tag peptide; bioconjugation; bioorthogonal chemistry; cysteine-cyclooctyne reaction; dibenzocyclooctyne; protein modification.

The authors report a site-selective cysteine-cyclooctyne conjugation reaction between a seven-residue peptide tag (DBCO-tag, Leu-Cys-Tyr-Pro-Trp-Val-Tyr) at the N or C terminus of a peptide or protein and various aza-dibenzocyclooctyne (DBCO) reagents. Compared to a cysteine peptide control, the DBCO-tag increases the rate of the thiol-yne reaction 220-fold, thereby enabling selective conjugation of DBCO-tag to DBCO-linked fluorescent probes, affinity tags, and cytotoxic drug mols. Fusion of DBCO-tag with the protein of interest enables regioselective cysteine modification on proteins that contain multiple endogenous cysteines; these examples include green fluorescent protein and the antibody trastuzumab. Short peptide tags can aid in accelerating bond-forming reactions that are often slow to non-existent in water.

Angewandte Chemie, International Edition published new progress about Enhanced green fluorescent proteins Role: BSU (Biological Study, Unclassified), PEP (Physical, Engineering or Chemical Process), BIOL (Biological Study), PROC (Process) (fusion protein with DCBO-tag). 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, Computed Properties of 882847-32-7.

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

Stefanick, Jared F. published the artcileEnhancement of Antibody Selectivity via Bicyclic Complex Formation, Quality Control of 882847-32-7, the main research area is antibody antigen bicyclic complex.

This study describes a strategy where antibody selectivity for high antigen-d. surfaces is enhanced by forming a thermodynamically stable bicyclic complex. The bicyclic complex was formed via multivalent interactions of the antibody with a synthetic trivalent mimotope at a 3:2 molar ratio. Complex formation was analyzed using dynamic light scattering and anal. ultracentrifugation, showing a hydrodynamic radius of ∼22 nm and a calculated mol. weight of 397 kDa, depicting a trimeric complex formation. The complex has high thermodn. stability and results in a 10-fold higher binding affinity for the trivalent mimotope (Kd = 0.14 μM) compared to the monovalent mimotope (Kd = 1.4 μM). As bicyclic complexes, the antibodies showed ∼18% binding of the monomeric form to low antigen-d. surfaces. At high antigen-d., antibody binding was equal whether delivered as a complex or a monomer. These results establish bicyclic complex selectivity for high antigen-d. surfaces and suggest a potential method to enhance therapeutic antibody selectivity for diseased cells.

Journal of Physical Chemistry Letters published new progress about Cell. 882847-32-7 belongs to class esters-buliding-blocks, name is 1-(9H-Fluoren-9-yl)-3-oxo-2,7,10,13,16,19-hexaoxa-4-azadocosan-22-oic acid, and the molecular formula is C28H37NO9, Quality Control of 882847-32-7.

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