165729-83-9Relevant academic research and scientific papers
Miktoarm star conjugated multifunctional gold nanoshells: Synthesis and an evaluation of biocompatibility and cellular uptake
Ng, Vanessa W. K.,Avti, Pramod K.,Bedard, Mathieu,Lam, Tina,Rouleau, Leonie,Tardif, Jean-Claude,Rheaume, Eric,Lesage, Frederic,Kakkar, Ashok
, p. 6334 - 6344 (2014)
A simple and highly versatile click chemistry based synthetic strategy to develop an ABC type miktoarm star ligand that is conjugated to gold nanoshells (GNS) is reported. The surface functionalized multifunctional GNS contain lipoic acid (LA) as a model
Kinetically Controlled Sequential Growth of Surface-Grafted Chiral Supramolecular Copolymers
Frisch, Hendrik,Fritz, Eva-Corinna,Stricker, Friedrich,Schmüser, Lars,Spitzer, Daniel,Weidner, Tobias,Ravoo, Bart Jan,Besenius, Pol
, p. 7242 - 7246 (2016)
We report a facile strategy to grow supramolecular copolymers on Au surfaces by successively exposing a surface-anchored monomer to solutions of oppositely charged peptide comonomers. Charge regulation on the active chain end of the polymer sufficiently slows down the kinetics of the self-assembly process to produce kinetically trapped copolymers at near-neutral pH. We thereby achieve architectural control at three levels: The β-sheet sequences direct the polymerization away from the surface, the height of the supramolecular copolymer brushes is well-controlled by the stepwise nature of the alternating copolymer growth, and 2D spatial resolution is realized by using micropatterned initiating monomers. The programmable nature of the resulting architectures renders this concept attractive for the development of customized biomaterials or chiral interfaces for optoelectronics and sensor applications.
Targeting Colorectal Cancer with Conjugates of a Glucose Transporter Inhibitor and 5-Fluorouracil
Chang, Chun-Kai,Chiu, Pei-Fang,Yang, Hui-Yi,Juang, Yu-Pu,Lai, Yen-Hsun,Lin, Tzung-Sheng,Hsu, Lih-Ching,Yu, Linda Chia-Hui,Liang, Pi-Hui
supporting information, p. 4450 - 4461 (2021/05/06)
Overexpression of glucose transporters (GLUTs) in colorectal cancer cells is associated with 5-fluorouracil (1, 5-FU) resistance and poor clinical outcomes. We designed and synthesized a novel GLUT-targeting drug conjugate, triggered by glutathione in the tumor microenvironment, that releases 5-FU and GLUTs inhibitor (phlorizin (2) and phloretin (3)). Using an orthotopic colorectal cancer mice model, we showed that the conjugate exhibited better antitumor efficacy than 5-FU, with much lower exposure of 5-FU during treatment and without significant side effects. Our study establishes a GLUT-targeting theranostic incorporating a disulfide linker between the targeting module and cytotoxic payload as a potential antitumor therapy.
ANTIFOLATE-CARRYING NANOPARTICLES AND THEIR USE IN MEDICINE
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Paragraph 36; 38, (2020/07/07)
The present invention provides a nanoparticle comprising: a core comprising a metal and/or a semiconductor; and a plurality of ligands covalently linked to the core, wherein said ligands comprise: (i) at least one dilution ligand comprising a carbohydrate, glutathione or an ethylene glycol-containing moiety; and (ii) a ligand of the formula D-L1-Z-L2, wherein D comprises an antifolate drug or folic acid, L1 comprises a first linker portion comprising a C2-C12 glycol and/or C2-C12 alkyl chain, L2 comprises a second linker portion comprising a C2-C12 glycol and/or C2-C12 alkyl chain, wherein L1 and L2 may be the same or different, and wherein Z represents a carbonyl-containing group linking L1 and L2, and wherein L2 is coupled to said core, Also provided are pharmaceutical compositions comprising such nanoparticles, medical uses thereof and methods for producing the nanoparticles.
NANOPARTICLE-BASED THERAPY OF INFLAMMATORY DISORDERS
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Page/Page column 32, (2020/07/07)
The present invention provides a nanoparticle comprising: a core comprising a metal and/or a semiconductor; and a plurality of ligands covalently linked to the core, wherein said ligands comprise: (i) at least one dilution ligand comprising a carbohydrate, glutathione or a polyethyleneglycol moiety; and (ii) a ligand of the formula MTX-L-, wherein MTX-L-represents methotrexate coupled to said core via a linker L. Also provided are pharmaceutical compositions of the nanoparticle, including gel formulations, and medical uses of the nanoparticle and pharmaceutical compositions, including for the treatment of an inflammatory or autoimmune disorder, such as psoriasis.
Homoallylglycine residues are superior precursors to orthogonally modified thioether containing polypeptides
Perlin, Pesach,Gharakhanian, Eric G.,Deming, Timothy J.
, p. 6196 - 6199 (2018/06/18)
Homoallylglycine N-carboxyanhydride, Hag NCA, monomers were synthesized and used to prepare polypeptides containing Hag segments with controllable lengths of up to 245 repeats. Poly(l-homoallylglycine), GHA, was found to adopt an α-helical conf
COMPOSITIONS AND METHODS FOR INDUCING IMMUNE TOLERANCE
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Paragraph 0327, (2019/01/08)
Several embodiments provided in the present disclosure relate to compositions that carry an antigen to which tolerance is desired, the antigen being coupled, bound, or otherwise joined to a targeting moiety, the targeting moiety configured to direct the composition to the liver of a subject. In several embodiments, the antigen in coupled to the targeting moiety by way of a polymeric linker. In several embodiments, the polymeric linker is configured to liberate the antigen in vivo. Methods of using the compositions to reduce and/or prevent unwanted immune responses against an antigen of interest are also provided.
NANOPARTICLES AND THEIR USE IN CANCER THERAPY
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Page/Page column 21, (2016/07/27)
The present invention provides a nanoparticle comprising a core comprising a metal; and a corona comprising a plurality of ligands covalently linked to the core, the plurality of ligands including at least a first species of ligand comprising an ethylene glycol portion and an amine group and at least a second species of ligand comprising a carbohydrate group, for use in a method of treating a cancer, particularly skin cancer, in a mammalian subject. Also disclosed are methods of treatment by administering the nanoparticles alone or in combination with radiotherapy.
Hetero-Click Conjugation of Oligonucleotides with Glycosides Using Bifunctional Phosphoramidites
Meyer, Albert,No?l, Mathieu,Vasseur, Jean-Jacques,Morvan, Fran?ois
supporting information, p. 2921 - 2927 (2015/05/04)
Two phosphoramidite derivatives, 1 and 2, each bearing two orthogonal functions: alkyne/thioacetyl or alkyne/tosyl, respectively, were synthesized and used to generate heteroglyco 5′-oligonucleotide conjugates. After coupling, the first conjugation was pe
Conjugation of multivalent ligands to gold nanoshells and designing a dual modality imaging probe
Bdard, Mathieu,Avti, Pramod K.,Lam, Tina,Rouleau, Lonie,Tardif, Jean-Claude,Rhaume, ric,Lesage, Frdric,Kakkar, Ashok
, p. 1788 - 1800 (2015/08/26)
Design and synthesis of branched tetraethylene glycol (TEG) based ligands for subsequent conjugation to gold nanoshells are reported. TEG enhances the aqueous solubility of hollow gold nanoshells (HAuNShs), and the branched architecture provides stability
