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. 2022 Nov 19;7:379. doi: 10.1038/s41392-022-01243-0

Table 1.

Overview of organelle-targeted therapeutic agents applied in cancer treatments

Organelle Targeted factors Toxins Intervention mechanism Therapy Others Models Ref.
Nucleus NLS peptide CPT prodrug DNA damage Chemotherapy In vitro 407
TAT/RGD peptide DOX/CS-6@ Erythrocyte membrane-encapsulated GOQDs DNA damage/VEGF expression ↓ Chemotherapy In vivo 87
TAT peptide DOX@MSNs DNA damage Chemotherapy Overcoming MDR In vitro 408
TAT peptide CPT@FMSN DNA damage Chemotherapy Charge-reversal strategy In vitro 409
Passive targeting DOX@PELA micelles DNA damage Chemotherapy Variable-size changeable strategy In vivo 410
R8NLS peptide H1 peptide@HPMA polymer Interference c-Myc DNA binding Chemotherapy Multi-stage targeting strategy In vivo 411
NLS peptide Gold nanorods DNA damage PTT In vivo 94
Passive targeting Hf-HI-4COOH polymer DNA damage PTT Low-temperature thermal ablation In vivo 412
Passive targeting Ir-Es complexes Nuclear damage PDT Irradiation improvement In vivo 413
TAT peptide Ce6@Upconversion-TiO2 Nanoparticles DNA replication disruption PDT Irradiation improvement In vivo 414
NLS peptide PpIX@Chimeric peptide nanoparticles DNA damage PDT Charge-reversal strategy In vivo 415
AS1411 aptamer Ce6@MOF nanoenzyme DNA damage PDT Overcoming hypoxia In vivo 416
NLS/CPP/RGD peptide ASO@PyTPE DNA interference/Bcl-2 ↓ Gene therapy In vitro 417
RGD-R8-PEG-HA pDNA@Fluorinated polymer PF33 DNA interference Gene therapy Multi-stage targeting strategy In vivo 418
Mitochondria TPP Resveratrol Prodrug Metabolism disruption Chemotherapy In vitro 419
TPP ATO/DOX Prodrug mtDNA damage/MMP↓ Chemotherapy Redox-responsive strategy In vivo 420
TPP DOX@Self-assembled cyanostilbene nanoparticles Unbalance of redox states/MMP↓ Chemotherapy In vivo 421
Organometallic rhenium complexes DOX Metabolism disruption/topoisomerase II ↓ Chemotherapy Overcoming MDR In vitro 215
TPP Cisplatin@PLGA-b-PEG nanoplatforms mtDNA damage Chemotherapy Overcoming MDR In vivo 422
PPh3 SOPs Mitochondrial dysfunction PTT ATOT strategy In vivo 423
Single-walled carbon nanotubes-chitosan nanoparticles MPTP PTT Charge-reversal strategy In vitro 424
ATO/IR820 @ Self-assembled nanodrugs Metabolism disruption/HSPs expression ↓ PTT Overcoming thermotolerance In vivo 425
CTPP CAT/Ce6 @ hollow silica nanoparticles Metabolism disruption/unbalance of redox states/mtDNA damage PDT Overcoming hypoxia In vivo 426
CyNH2 Acetylated lysine- CyNH2 MMP↓/unbalance of redox states PDT Imaging-guided PDT In vivo 427
UCNP@TiO2 NCs Unbalance of redox states/metabolism disruption PDT Irradiation improvement In vivo 428
Ir(III) complexes Ir(III) complexes Unbalance of redox states/metabolism disruption PDT Irradiation improvement In vitro 429
MLS pDNA@DQAplexes Initiation mtDNA transcription Gene therapy In vitro 210
R8 moieties ASO@MITO-Porter system Metabolism disruption Gene therapy In vitro 430
Lysosomes Endocytosis Iron(III)-activated iridium(III) prodrug Inducing Fe releasing/LMP Chemotherapy In vivo 431
Endocytosis PTX@PDA coated MS NPs LMP Chemotherapy In vivo 432
Endocytosis DOX@Sericin protein modified MSNs LMP Chemotherapy Overcoming MDR In vivo 433
Morpholine and cRGD Morpholine-cRGD peptide LMP PTT In vivo 434
FA Ruthenium nitrosyl donor LMP PDT NO and ROS synergistic PDT In vitro 435
Endocytosis BDP-688/P16FP@ Polymer micelles LMP PDT Imaging-guided PDT In vivo 436
Endocytosis BODIPY dyes@Polymer micelles LMP PDT PAI-guided PDT In vivo 437
Nucleus-Mitochondria-Lysosomes Endocytosis platinum-doped carbon nanoparticles Thermal damage to multi-organelles PTT Multiple-organelle synergistic strategy In vivo 438
Mitochondria-Lysosomes Endocytosis and TPP AIE-Mito-TPP & AlPcSNa4 LMP/metabolism disruption/ unbalance of redox states /mtDNA damage PDT Multiple-organelle synergistic strategy In vivo 439

ASO antisense oligonucleotide, ATO arsenic trioxide, ATOT strategy active tumor- and organelle-targeted theranostic strategy, AIE aggregation-induced emission, CPT camptothecin, CS-6 gamabufotalin, Ce6 chlorin e6, CAT catalase, CPP cell-penetrating peptide, DOX doxorubicin, DQAplexes cationic ‘bola-lipid’-based vesicles, FMSN folic acid modified magnetic mesoporous silica nanoparticles, GOQDs graphene oxide quantum dot,HPMA polymer N-(2-hydroxypropyl) methacrylamide polymer, Hf-HI-4COOH polymer heptamethine cyanine dye-based nanoscale coordination polymer, Ir-Es complexes terpyridine-based cyclometalated Iridium(iii) complexes, LMP lysosomal membrane permeabilization, MSNs mesoporous silica nanoparticles, MDR multidrug resistance, MMP mitochondrial membrane potential, MOF metal-organic framework, NLS nuclear localization signal, PELA micelles mPEG-PLA-ss-PEI-DMMA polymer micelles, PpIX alkylated protoporphyrin IX, pDNA plasmid DNA, PAI photoacoustic/optoacoustic imaging, PTT photothermal therapy, PDT photodynamic therapy, ROS reactive oxygen species, SOPs small-molecule organic photothermal agents, TPE two-photon excitation, UCNP upconversion nanoparticle, VEGF vascular endothelial growth factor