TY - JOUR
T1 - Peptide-Conjugated Long-Lived Theranostic Imaging for Targeting GRPr in Cancer and Immune Cells
AU - Wang, Wanhe
AU - Wu, Ke Jia
AU - Vellaisamy, Kasipandi
AU - Leung, Chung Hang
AU - MA, Edmond Dik Lung
N1 - Funding Information:
We thank Hao Liu for HPLC checking. This work is supported by Hong Kong Baptist University (FRG2/17‐18/003), the Health and Medical Research Fund (HMRF/14150561), the National Natural Science Foundation of China (21775131), the Hong Kong Baptist University Century Club Sponsorship Scheme 2019, the Interdisciplinary Research Matching Scheme (RC‐IRMS/16‐17/03), Interdisciplinary Research Clusters Matching Scheme (RC‐IRCs/17‐18/03), Collaborative Research Fund (C5026‐16G), SKLEBA and HKBU Strategic Development Fund (SKLP_1920_P02), the Science and Technology Development Fund, Macau SAR (File no. 0072/2018/A2), the University of Macau (MYRG2019‐00002‐ICMS and MYRG2018‐00187‐ICMS).
PY - 2020/10/5
Y1 - 2020/10/5
N2 - 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.
AB - 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.
KW - gastrin-releasing peptide receptor (GRPr)
KW - peptide-conjugated transition-metal complexes
KW - theranostic agents
KW - time-resolved emission spectroscopy
UR - http://www.scopus.com/inward/record.url?scp=85089465375&partnerID=8YFLogxK
U2 - 10.1002/anie.202007920
DO - 10.1002/anie.202007920
M3 - Journal article
C2 - 32649787
AN - SCOPUS:85089465375
SN - 1433-7851
VL - 59
SP - 17897
EP - 17902
JO - Angewandte Chemie. International Edition
JF - Angewandte Chemie. International Edition
IS - 41
ER -
