PiF is a multimodal pancreatic β cell probe for both fluorescence and for PET (positron emission tomography). By simple tail vein injection, PiF stains pancreatic β cells specifically and PiF-injected pancreatic tissue even facilitated an antibody-free islet analysis within 2 h, dramatically accelerating the day-long histological procedure without any fixing and dehydration step. The low background of PiF in the liver allowed us to monitor the intraportal transplanted islets, which is the first in vivo visualization of transplanted human islets without a prelabeling of the islets. Finally, we could replace the built-in fluorine atom in PiF with radioactive 18F and successfully demonstrate in situ PET imaging for pancreatic islets.
J. Am. Chem. Soc., 2020
2
TiNIR selectively detects heme oxygenase 2 (HMOX2) as a novel biomarker for TIC, and enriches the functionally active TIC in human lung tumors. Through the photoacoustic property, TiNIR also visualizes lung TIC in the patient-derived xenograft (PDX) model. Furthermore, TiNIR can inhibit tumor growth by blocking the function of HMOX2, resulting in significantly increased survival rates of the cancer model mice.
J. Am. Chem. Soc., 2019
3
BacGO, a novel Gram‐positive bacterial probe, was developed from a library of fluorescent molecules with a boronic‐acid motif that binds to peptidoglycan on the Gram‐positive bacterial cell wall. BacGO can be used to identify Gram‐positive bacteria in diverse, highly complex samples, and is an attractive alternative to Gram staining.
Angew. Chem. Int. Ed. Engl., 2019
4
Using a thorough structure-activity relationships study, we developed CDr20, a high‐performance fluorogenic chemical probe that enables the visualization of microglia both in vitro and in vivo. Using a genome‐scale CRISPR‐Cas9 knockout screen, the UDP‐glucuronosyltransferase Ugt1a7c was identified as the target of CDr20. The glucuronidation of CDr20 by Ugt1a7c in microglia produces fluorescence.
Angew. Chem. Int. Ed., 2019
5
CDg16 is a small molecule probe specific for activated macrophages and can be applied to visualize inflammatory atherosclerotic plaques in vivo. Through a systematic transporter screen using a CRISPR activation library, we identify the orphan transporter Slc18b1/SLC18B1 as the gating target of CDg16.
Nat. Commun., 2019
6
The NIR zwitterionic elastin probe ElaNIR (elastin NIR) was discovered through fluorescent-image-based screening. The probe was successfully applied for in vitro, ex vivo, and in vivo imaging by various imaging modalities. Age-related elastin differences shown by in vivo fluorescent and photoacoustic imaging indicated that ElaNIR can be a potentially convenient tool for uncovering changes of elastin in live models.
Chem, 2018
7
TiY is the first TIC‐specific fluorescent chemical probe with the molecular target of vimentin, a marker for epithelial‐to‐mesenchymal transition (EMT). TiY selectively stains TICs over differentiated tumor cells or normal cells, and facilitates the visualization and enrichment of functionally active TICs from patient tumors. At high concentration, TiY shows anti‐TIC activity with low toxicity to non‐TICs.
Angew. Chem. Int. Ed. Engl., 2018
8
TP-β is a 2-glucosamine-based two-photon fluorescent probe, which is suitable for imaging of beta cells in live pancreatic islets from mice. Flow cytometry studies confirmed that TP-β is suitable for isolation of primary beta cells. Moreover, two-photon imaging of TP-β-stained pancreatic islets showed brightly stained beta cells in live islets. Insulin enzyme-linked immunosorbent assays revealed that TP-β has no effect on glucose-stimulated insulin secretion from the stained islet.
J. Am. Chem. Soc., 2017
9
The first TP live pancreatic islet imaging probe, TP-α (Two Photon-alpha), can selectively stain glucagon secreting alpha cells. In vitro fluorescence test showed that TP-α have direct interaction and appear glucagon with a significant fluorescence increase, but not with insulin or other hormones/analytes. Finally, TP-α was successfully applied for 3D imaging of live islets by staining alpha cell directly.
J. Am. Chem. Soc., 2015
10
CDg13, a new fluorescent substrate for the Abcg2 transporter, facilitated the isolation of neurogenic neural stem/progenitor cells (NSPCs) from embryonic mouse brain. The high sensitivity and selectivity of CDg13 to Abcg2 make the probe as a very useful tool to measure Abcg2 activity in live cells.