Table 1.
Recent applications of NPs targeting GPCR.
| Nanoparticles | Ligand/Antibody | GPCR | Function | Reference |
|---|---|---|---|---|
| Dendrimer | MRS2500 (antagonist) | P2Y(1) | Affinity to receptor (Ki 23 nM); Inhibiting ADP-promoted human platelet aggregation; Antithrombotic drug |
[46] |
| XAC (antagonist) | Adenosine receptor (A2AAR) | Affinity to receptor (Ki 3.7 nM); Treating Parkinson’s disease and asthma |
[81] | |
| CGS21680 (agonist) | Adenosine receptor (A2AAR) | Affinity to receptor (Ki 12 ± 6 nM); Activating adenylate cyclase and accumulating cAMP; Inhibiting ADP-promoted human platelet aggregation; Using short PEG chains in nanocarriers targeting ligand-receptor interactions |
[82] | |
| UDPGA-A3AR 3a-G4 PAMAM (agonist) |
Both Adenosine receptor (A3AR) and P2Y14 | Affinity to receptor (Ki 39.5 nM to A3AR); Inhibiting cAMP cumulation; Antithrombotic drug |
[46] | |
| DITC-APEC (agonist) |
Adenosine receptor (A2AAR) | Affinity to receptor (Ki 70 ± 3 nM); Inhibiting ADP-promoted human platelet aggregation; Antithrombotic drug |
[45] | |
| Quantum dots (QDs) | α-melanocyte-simulating hormone NDP and MT-II | Human melanocortin receptor (hMCR) | Specific marking of surface receptors; Single molecule imaging of GPCR; Multiplexing; Investigating GPCR localization and trafficking in live cells and in single molecule studies |
[83] |
| Deltorphin-II | Human δ-opioid receptor (hDOR) | |||
| ANGII | ANGIIReceptor | Monitoring ligand-receptor binding in live cells; Monitoring GPCR internalization; Detecting and labeling several GPCRs in living cells |
[53] | |
| BBN | BBN receptor | |||
| HaloTag ligand | Cyclic AMP receptor 1 (cAR1) | Single molecule imaging of GPCR; Using multi-colored, single molecule imaging to study membrane protein dynamics |
[56] | |
| Antibody against flag tag (HA) | Serotonin receptor subtype 1A (5-HT1A) | Monitoring internalization and endosomal trafficking; Identifying two distinct GPCR recycling pathways |
[59] | |
| ANGII | AGTR1 | Higher affinity to receptor than native ANGII; Multivalent ANGII-targeted NP-AGTR1 binding; Targeting tissues that overexpress AGTR1 |
[58] | |
| Adenosine | Adenosine receptor (A2AAR) | Studying the mobility of the receptor in neurons | [84] | |
| Antibody against flag tag (GFP) | Serotonin receptor subtype 1B (5-HT1B) | Monitoring receptor trafficking in rat hippocampal neurons; Suggesting alternative mechanism of mood regulation via GPCR |
[85] | |
| Antibody against flag tag (HA) | κ-opioid receptors (κ-ORs) | Displaying receptor affinity and specificity; Monitoring receptor trafficking; Detecting two receptors in one cell; Application in drug screening |
[86] | |
| Antibody against flag tag (GFP) | Adenosine receptor (A2AAR) | |||
| Antibody against flag tag (GFP) | Endothelin A receptor (ET(A)R) | Monitoring receptor intracellular translocation; Detecting intracellular targets (when conjugated with a cell penetrating agent) |
[87] | |
| Antibody against flag tag (HA) | Serotonin receptor (5-HT1A) | Single molecule imaging to monitor receptor trafficking; Understanding the mechanism of therapies targeting GPCR |
[59] | |
| Gold nanoparticle (AuNP) | Several AR agonists and antagonists | Adenosine receptor (AR) | Affinity to receptor (Ki 37 nM to A3AAR); Cancer diagnosing and treatment |
[73] |
| BBN | Gastrin-releasing peptide receptor (GRPR) | Monitoring receptor internalization; Cancer therapy and molecular imaging in vivo |
[74] | |
| Magnetic nanoparticle (MNP) | Anti-ETA antibody | Endothelin receptor (ETA) | Efficient receptor targeting; Bimodal contrast agent and imaging agent; Targeting tumor pathologies; Early Cancer diagnosing |
[32] |
| MG | Cholecystokinin-2 receptor (CCK2R) | Inducing cell death in cancer | [59] | |
| Elastin-like polypeptide (ELP) micelles | GRP | Gastrin-releasing peptide receptor (GRPR) | Specific receptor targeting; Delivering cytotoxic drugs to cancer |
[80] |
| Unmodified NPs | FSH | Follicle-Stimulating hormone receptor (FSHR) | Successfully delivering drug to lymph nodes; Reducing metastasis; Ovarian cancer therapy |
[79] |
| Nanorubies | Antibody against flag tag (HA) | μ-opioid receptor | Imaging functionality; Achieving real-time single molecule imaging on biological samples |
[88] |