cRGD functionalized 2,1,3-benzothiadiazole (BTD)-containing two-photon absorbing red-emitter-conjugated amphiphilic poly(ethylene glycol)-block-poly(ε-caprolactone) for targeted bioimaging

Abstract

A two-photon absorbing (2PA) red emitter group was chemically conjugated onto amphiphilic poly(ethylene glycol)-block-poly(ε-caprolactone) (PEG-b-PCL) copolymers, and further grafted with cyclo(Arg-Gly-Asp) (cRGD) peptide to form micelle 1.

Smart MSN-Drug-Delivery System for Tumor Cell Targeting and Tumor Microenvironment Release

“…The invasive growth of tumors requires a large amount of nutrients, which promotes the formation of new blood vessels. Endogenous α v β 3 integrin transmembrane glycoprotein, considered as a marker of angiogenesis, is widely distributed on tumor neovascular. , Research findings indicate that the arginine-glycine-aspartate sequence (RGD) can combine with α v β 3 integrin to inhibit tumor angiogenesis and thus prevent tumor growth and metastasis. , The binding ability of the cyclic RGD peptide (cRGD) to α v β 3 integrin and the inhibition of tumor neovascularization have been shown to be stronger than those of linear RGD peptide. − Therefore, the functionalization of drug-delivery carriers with cRGD targeting ligand can effectively increase their retention effect and enrich on the tumor cell surface. − In addition, according to the literature, − folate receptor (FR) is highly expressed on the surface of most cancer cells to absorb folic acid (FA), which is required for the rapid growth of cancer cells. The introduction of FA into the carrier surface can increase the probability of the carrier being captured and internalized by cancer cells via the active targeting function.…”

Deciphering the Dynamics of Organic Nanoaggregates with AIEE Effect and Excited States: Lipophilic Benzothiadiazole Derivatives as Selective Cell Imaging Probes

“…Molecular 2,1,3-benzothiadiazole (BTD) derivatives have been successfully applied as bioimaging probes. − Several groups − have effectively tested the BTD derivatives as active and efficient bioprobes for bioimaging experiments, including us. − In spite of the successes renowned on the use of BTD luminophores, there is still much room for improvement and this new class of fluorophores has just begun to glow among the classical scaffolds, − such as coumarins, fluoresceins, cyanines, rhodamines, BODIPYs, and a few others. A small number of reports have investigated the AIEE (or AIE) effect for fluorescent BTD derivatives (see examples in Figure ), − but these studies are in general not focused to depict the dynamics (formation/break and intramolecular interactions) of this phenomenon and only a few properties (size and standard photophysical) of the organic nanoaggregates are routinely described.…”

Graphene nanoribbon-based supramolecular ensembles with dual-receptor targeting function for targeted photothermal tumor therapy

“…These selective properties of GNR-Man/PRGD for MDA-MB-321 cells was further confirmed through its evaluation with additional cancer cell lines. These include Hela cells (human cervical cell line), 51 MCF-7 cells (human breast cancer cell line) 52 and Hep-G2 cells (human hepatoma cell line), 53 all of which are reported to have a lower expression of the integrin α v β 3 receptor. Both GNR-Man/PRGD and GNR-Man were shown to have minimal phototoxicities for these chosen cell lines, which further supports the good selectivity of GNR-Man/PRGD and GNR-Man for MDA-MB-321 cells (Fig.…”