Peptide‐Conjugated Long‐Lived Theranostic Imaging for Targeting GRPr in Cancer and Immune Cells

Abstract

Gastrin‐releasing peptide receptor (GRPr) plays proliferative and inflammatory roles in living systems. Here, we report a highly selective GRPr antagonist (JMV594)‐tethered iridium(III) complex for probing GRPr in living cancer cells and immune cells. This probe exhibited desirable photophysical properties and also displayed negligible cytotoxicity, overcoming the inherent toxicity of the iridium(III) complex. Its long emission lifetime enabled its luminescence signal to be readily distinguished from the interfering fluorescence of organic dyes by using a time‐resolved technique. This probe selectively visualized living cancer cells via specific binding to GRPr, while it also modulated the function of GRPr on TNF‐α secretion in immune cells. To our knowledge, this is the first peptide‐conjugated iridium(III) complex developed as a GRPr bioimaging probe and modulator of GRPr activity. This theranostic agent shows great potential at unmasking the diverse roles of GRPr in living systems.

A tandem activity-based sensing and labeling strategy enables imaging of transcellular hydrogen peroxide signaling

“…This gap in fundamental knowledge is due in part to limitations in chemical tools to visualize integrated H 2 O 2 activity that can retain spatial information over larger and/or more complex cell populations. Indeed, there have been recent elegant developments in sensing platforms and probe design (28)(29)(30)(31) (44)(45)(46)(47)(48) and do not provide a permanent signal.…”

Dissecting Prognosis Modules and Biomarkers in Glioblastoma Based on Weighted Gene Co-Expression Network Analysis

“…Besides, gastrin-releasing peptide receptor (GRPR) acts as proliferative and inflammatory factors in living systems. 46 The activation of GRPR promotes cell proliferation, whereas GRPR antagonists induce antiproliferative effects in both in vitro and in vivo experimental GBM models. In addition, according to the knockdown of GRPR induces senescence in GBM cells, GRPR have the potential to serve as a therapeutic target in brain tumors.…”

Aqueous emissive cyclometalated iridium photoreductants: synthesis, computational analysis and the photocatalytic reduction of 4-nitrophenol

“…Luminescent cyclometallated iridium complexes have received great attention in the last few decades because of their exciting photophysical property and enthralling applications in different fields of science and technology. [1][2][3][4][5] Such systems display properties such as high photostability, high quantum yield, and longer emission lifetime due to intersystem crossing (ISC), [6][7][8][9] resulting in their application as photocatalysts for organic transformation, [10][11][12][13][14][15][16][17][18][19][20] materials for organic light-emitting diodes (OLEDs), 16,21,22 light-emitting electrochemical cells (LEECs), 23 theranostic and bioimaging agents, [24][25][26][27][28][29][30][31][32][33] etc. The majority of the developed cyclometallated iridium systems are readily accessible in organic solvents.…”