1313026-32-2Relevant academic research and scientific papers
Cell-Selective Delivery of MicroRNA with a MicroRNA–Peptide Conjugate Nanocomplex
Xiao, Xiao,Wang, Xingxing,Gao, Haidong,Chen, Xi,Li, Jinbo,Zhang, Yan
, p. 3845 - 3849 (2018)
Targeted delivery of microRNA (miRNA) into specific cells has been regarded as an efficient strategy to enhance miRNA-targeted therapeutics. However, concurrent delivery of therapeutic miRNAs into different target cells that is conducive to multi-target t
Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging
Jin, Xiangmei,Zhang, Jun,Jin, Xiaoyan,Liu, Lan,Tian, Xizhe
, p. 1514 - 1520 (2020/10/12)
In this work, a folate receptor (FR)-mediated dual-targeting drug delivery system was synthesized to improve the tumor-killing efficiency and inhibit the side effects of anticancer drugs. We designed and synthesized an FR-mediated fluorescence probe (FA-Rho) and FR-mediated cathepsin B-sensitive drug delivery system (FA-GFLG-SN38). FA-GFLG-SN38 is composed of the FR ligand (folic acid, FA), the tetrapeptide substrate for cathepsin B (GFLG), and an anticancer drug (SN38). The rhodamine B (Rho)-labeled probe FA-Rho is suitable for specific fluorescence imaging of SK-Hep-1 cells overexpressing FR and inactive in FR-negative A549 and 16-HBE cells. FA-GFLG-SN38 exhibited strong cytotoxicity against FR-overexpressing SK-Hep-1, HeLa, and Siha cells, with IC50 values of 2-3 μM, but had no effect on FR-negative A549 and 16-HBE cells. The experimental results show that the FA-CFLG-SN38 drug delivery system proposed by us can effectively inhibit tumor proliferation in vitro, and it can be adopted for the diagnostics of tumor tissues and provide a basis for effective tumor therapy.
ANANDAMIDE-MODIFIED NUCLEIC ACID MOLECULES
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, (2014/02/15)
The present invention refers to a conjugate comprising at least one polyunsaturated fatty acid residue, particularly an arachidonic acid residue, more particularly an anandamide (arachidonoyl ethanol amide) residue and covalently bound thereto at least on
NOVEL SELF-REACTIVE ARMS AND PRODRUGS COMPRISING SAME
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Paragraph 0314; 0315; 0316; 0317; 0318, (2013/06/26)
The present invention relates to a compound of general formula (I): in which: X is OH, NH2, NHOH or RNH, where R may be a linear or branched, saturated or unsaturated, C1-C10 alkyl radical,Y is H, or an electron-withdrawing group, in particular
CELLULAR RECOGNITION CONJUGATES AND METHODS OF USE FOR THE HISTOLOGICAL ANALYSIS OF CANCER TISSUE USING MALDI-MS IMAGING
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Page/Page column 51-52, (2013/03/26)
Disclosed are conjugates that can bind to one or more site on cancer cell surface, for example, surface proteins, compound specific receptors and carbohydrates that comprise the surface of specific cell types. The disclosed conjugates can thereby serve as
Click-modified anandamide siRNA enables delivery and gene silencing in neuronal and immune cells
Willibald, Julian,Harder, Johannes,Sparrer, Konstantin,Conzelmann, Karl-Klaus,Carell, Thomas
, p. 12330 - 12333 (2012/09/05)
Click chemistry of alkyne-modified RNA with different receptor ligand azides was used to prepare 3′-folate, 3′-cholesterol, and, as a new entity, 3′-anandamide-modified RNA in high yields and excellent purity. The anandamide-modified RNA shows surprisingly high transfection properties and enables the delivery of siRNA even into difficult-to-transfect RBL-2H3 cells which model neuronal uptake. Furthermore, the system was employed in human immune cells (BJAB), demonstrating silencing effects similar to those of a cationic, benchmark transfection reagent. In addition, the anandamide conjugates were found to be nontoxic. The reported chemistry and the described properties of the anandamide siRNA extend the possibilities of using siRNA-based gene silencing in neuronal and immune cells.
The first generation of β-galactosidase-responsive prodrugs designed for the selective treatment of solid tumors in prodrug monotherapy
Legigan, Thibaut,Clarhaut, Jonathan,Tranoy-Opalinski, Isabelle,Monvoisin, Arnaud,Renoux, Brigitte,Thomas, Mika?l,Le-Pape, Alain,Lerondel, Stéphanie,Papot, Sébastien
supporting information, p. 11606 - 11610 (2013/01/15)
Massive attack: Galactoside prodrugs have been designed that can be selectively activated by lysosomal β-galactosidase located inside cancer cells expressing a specific tumor-associated receptor. This efficient enzymatic process triggers a potent cytotoxic effect, releasing the potent antimitotic agent MMAE and allowing the destruction of both receptor-positive and surrounding receptor-negative tumor cells. Copyright
