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Showing 1 to 17 of 17 for “"Heterobifunctional"”.
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Synthesis and Characterization of Well-Defined Heterobifunctional Polyethers for Coating Magnetite and Their Applications in Biomedicine Resonance Imaging
Well-defined heterobifunctional homopolyethers and amphiphilic block copolyethers containing a variety of functionalities were designed, synthesized, and characterized via GPC and 1H NMR. These have included controlled molecular weight cholesterol-PEO-OH, mono- and trivinylsilyl-PEO-OH, …
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Enabling Synthesis Toward the Production of Biocompatible Magnetic Nanoparticles With Tailored Surface Properties
… carboxylic acid groups per chain was achieved. Heterobifunctional poly(ethylene oxide) (PEO) and poly(ethylene oxide-b-propylene oxide) (PEO-b-PPO) copolymers were synthesized utilizing heterobifunctional initiators to yield polymers having a hydroxyl group at one chain end and additional …
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Developing Computational Methods in Proximity Pharmacology for Enzyme Discovery, PROTAC Screening, and Conformational Space Exploration
… interaction between proteins. Later, heterobifunctional compounds consisting of two ligands connected by a linker demonstrated that E3 ligases could be chemically recruited to target proteins, inducing de novo protein-protein interactions and leading to target degradation. These …
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Synthesis and Characterization of Poly(lactide) Functional Oligomers and Block Copolymers
… with poly(L-lactide), (PLLA) homopolymer. Heterobifunctional PEO oligomers were directly prepared by initiating ethylene oxide with functional alcohols bearing vinylsilane, vinylether and maleimide moieties to provide appropriate end groups for conjugating targeting ligands. The polyethers …
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Preparation and Functionalization of Macromolecule-Metal and Metal Oxide Nanocomplexes for Biomedical Applications
… were prepared and utilized for the synthesis of heterobifunctional poly(ethylene oxide) oligomers with a free hydroxy group on one end and one to three vinylsilyl groups on the other end. The oligomers were further modified with carboxylic acids via ene-thiol addition reactions while preserving …
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Synthesis and Characterization of Novel Polyethers and Polypeptides for Use in Biomedicine and Magnetic Resonance Imaging
… glycidyl ether (EVGE), were synthesized. These heterobifunctional monomers were polymerizable via the epoxide groups and can be functionalized via thiol-ene reactions through the pendent vinyl groups. A series of amphiphilic block copolyethers based on poly(ethylene oxide) and poly(1,2-butylene …
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Bioorthogonal Tethering of Drug Fragments to Engineered G Protein-Coupled Receptors
… labeling of the engineered variants using heterobifunctional compounds containing bioorthogonal tethering groups linked to either a small-molecule fluorophore or a peptide. Bioorthogonal labeling of CCR5 in live cells using inverse electron demand Diels-Alder ligation was more specific and …
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Designed bifunctional proteins for induced degradation of androgen receptor in prostate cancer
… it to the ubiquitinproteasome pathway using heterobifunctional degrader molecules. Among others, consensus-designed tetratricopeptide repeat proteins (CTPRs) were deployed as artificial modular scaffolds, onto which AR- and E3 ligase-binding moieties were grafted to induce AR ubiquitination …
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SERS-based nanoparticle biodetection using carbohydrate-lectin interactions
… with a variety of thiol-based linker molecules. Heterobifunctional PEG (carboxyl/thiol) molecules were found to be most successful in preventing non-specific aggregation. The carboxylic acid functionality of the PEG molecules used allowed for subsequent coupling of a variety of carbohydrates to …
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The synthesis, characterization, and use of a protein-cysteine proteinase inhibitor complex for the study of endosome/lysosome fusion
… to bovine serum albumin (BSA) using the heterobifunctional crosslinking agent sulfo-SANPAH. This non-reducible cross-linked complex was used to characterize the inhibitory properties of the protein-inhibitor complex against cathepsins B, L, S and papain in vitro and in vivo.
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The Design, Synthesis and in vitro Evaluation of Proteolysis Targeting Chimeras (PROTACs) for the Degradation of Protein Arginine Methyltransferase 1
… PROTACs led to the isolation of a heterobifunctional molecule with the linker attached to the binding pharmacophore of the CRBN ligand. This molecule was found to degrade PRMT1 and is proposed to be a monomeric degrader that destabilises the structure of PRMT1 upon binding. This …
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Block and Graft Copolymers Containing Carboxylate or Phosphonate Anions
… functionalized PEO-b-PAA copolymers. First, heterobifunctional poly(ethylene oxide) (PEO) with three different molecular weights were synthesized. Modification on one of these afforded a PEO macroinitiator with a bromide on one end and a protected amine on the other end. ATRP polymerization …
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Design and development of a site specific protein patterning technique for use in a microfluidic antibody separation device
… involving the UV-initiated conjugation of a heterobifunctional linker, undecylenic acid N-Hydroxysuccinimde ester (UANHS), to a hydrogen terminated silicon surface was investigated. A photolithographic mask and phase mask were used to form micron and submicron UANHS motifs respectively, on …
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Synthesis and performance of novel supramolecular tools for single-particle cryogenic electron microscopy and drug and gene delivery
… utilizing organocatalytic ROP from a heterobifunctional PEG derivative. A facile and widely applicable synthetic procedure for the synthesis of cyclic amino-acid-N-carboxyanhydride monomers for synthesis of polypeptides utilizing tetrahydrofuran (THF) as solvent was developed and used …
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Novel Nucleic Acid Sensors for the Rapid Detection of Cryptosporidium Parvum
… be filled with up to 106 dye molecules. By using heterobifunctional linkers liposomes can be tagged with oligonucleotides, thereby enabling their use in nucleic acid hybridization assays. The developed test-strip provides an internal control. The limit of detection is 2.7 fmol/mL with a sample …
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Synthesis and Characterization of Novel Pol(arylene ethers) for Gas Separation and Water Desalination Membranes
… account of synthesis of monofunctional, heterobifunctional and telechelic poly(2-ethyl-2-oxazoline)s using different initiators including methyl triflate, activated alkyl halides (e.g., benzyl halides), and non-activated alkyl halides has been presented in this thesis. Endgroup …
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Induced Degradation of G-Protein-Coupled Receptors Through Proteolysis Targeting Chimeras
… targeting chimeras (PROTACs), which are heterobifunctional molecules where one end has a ligand for the protein-of-interest (POI), and the other end has an E3 ligase recruiting ligand. PROTACs take advantage of the ubiquitin-proteasome system (UPS) by forcing a POI in proximity to an E3 …