# Photoactivation in Chemotherapeutic Compounds for Cancer Treatment: Opportunities Beyond Photodynamic Therapy

**Authors:** Simon Ngigi Mbugua, Eunice Adhiambo Nyawade

PMC · DOI: 10.1155/bca/7161202 · Bioinorganic Chemistry and Applications · 2026-03-08

## TL;DR

This paper reviews photoactivatable anticancer drugs that use light to control drug activity, offering benefits like reduced side effects and better targeting of tumors.

## Contribution

The paper provides a comprehensive review of photoactivatable anticancer compounds and their advantages over traditional chemotherapy.

## Key findings

- Photoactivatable drugs allow precise control of drug activity using light, reducing off-target effects.
- These compounds can overcome drug resistance and enable in situ monitoring of drug activation.
- The paper explores synthesis methods and effectiveness of various photoresponsive metal complexes.

## Abstract

Photoactivation is the stimulation or regulation of a chemical or a chemical process by utilizing light of specific wavelength that corresponds to an absorbance optimum of the agent being used and can penetrate into tissues. In cancer therapy, photoactivatable drugs utilize this phenomenon by allowing the temporal and spatial regulation of their cytotoxicity using irradiation. Therefore, in order to reduce the adverse effects of platinum medications, photoactivatable anticancer pharmaceuticals, which might be site‐activated in the tumour region, are a viable option. This paper summarizes different types of photoactivatable anticancer compounds that would produce an active version of a drug by the process of photouncaging. The mode of photoactivation and rationale for drug design are summarized. The effects of typical complexes on cellular pathways, photocytotoxicity and dark cytotoxicity are explored. When compared to traditional Pt(II) anticancer medications, photoactivatable anticancer compounds provide a number of benefits, including ability to overcome drug resistance, and in situ monitoring of drug accumulation and activation inside cells. This review also covers the design approaches, synthesis techniques, photoresponsiveness and antitumour effectiveness of various photochemotherapeutic compounds. Future developments and challenges in incorporating photoresponsive metal complexes are also covered. This detailed review aims at encouraging further thorough investigation into this intriguing area of study by offering a summary of current developments in the design and development of photoresponsive compounds for cancer treatment and future clinical prospects.

## Linked entities

- **Diseases:** cancer (MONDO:0004992)

## Full-text entities

- **Genes:** CA2 (carbonic anhydrase 2) [NCBI Gene 760] {aka CA-II, CAC, CAII, Car2, HEL-76, HEL-S-282}, UROD (uroporphyrinogen decarboxylase) [NCBI Gene 7389] {aka PCT, UPD}, CTSK (cathepsin K) [NCBI Gene 1513] {aka CTS02, CTSO, CTSO1, CTSO2, PKND, PYCD}, TP53 (tumor protein p53) [NCBI Gene 7157] {aka BCC7, BMFS5, LFS1, P53, TRP53}, RBBP6 (RB binding protein 6, ubiquitin ligase) [NCBI Gene 5930] {aka MY038, P2P-R, PACT, RBQ-1, SNAMA}, PTPA (protein phosphatase 2 phosphatase activator) [NCBI Gene 5524] {aka PARK25, PP2A, PPP2R4, PR53}, CTSB (cathepsin B) [NCBI Gene 1508] {aka APPS, CPSB, KWE, RECEUP}, PCNA (proliferating cell nuclear antigen) [NCBI Gene 5111] {aka ATLD2}
- **Diseases:** head and neck, cutaneous, bladder, lung, oesophageal cancers (MESH:D006258), neurotoxicity (MESH:D020258), lung cancer (MESH:D008175), Cancers (MESH:D009369), nonsmall cell lung cancer (MESH:D002289), squamous cell carcinoma, head and neck, esophageal and lung cancers (MESH:D000077195), hypoxia (MESH:D000860), proliferative disorders (MESH:D009220), carcinogenesis (MESH:D063646), hypoxic (MESH:D002534), phototoxicity (MESH:D017484), Cytotoxicity (MESH:D064420), irregular heart rhythms (MESH:D008599), osteoporosis (MESH:D010024), neutropenia (MESH:D009503), metastasis (MESH:D009362), bladder cancer (MESH:D001749), bacterial and fungal illnesses (MESH:D009181), basal cell carcinoma (MESH:D002280), necrosis (MESH:D009336), bile duct, bladder, liver, colon, pancreas, brain, ovarian and prostate cancers (MESH:D010051), cutaneous malignancies (MESH:C562393), bacterial infections (MESH:D001424), triple-negative (MESH:D064726), breast cancer (MESH:D001943)
- **Chemicals:** D-luciferin (MESH:C532924), acetonitrile (MESH:C032159), esters (MESH:D004952), polymer (MESH:D011108), polyelectrolyte (MESH:D000071228), carbon (MESH:D002244), nitrobenzene (MESH:C036077), azide (MESH:D001386), carboxylic acid (MESH:D002264), dinitrogen (MESH:D009584), Paclitaxel (MESH:D017239), P (MESH:D010758), 3MC (MESH:D008748), ureidopyrimidinone (MESH:C000710651), Oxygen (MESH:D010100), Thioether (MESH:D013440), Platinum (MESH:D010984), methionine (MESH:D008715), Metal (MESH:D008670), ibuprofen (MESH:D007052), Gold (MESH:D006046), singlet oxygen (MESH:D026082), odanacatib (MESH:C527128), oxaliplatin (MESH:D000077150), hydroxyl radical (MESH:D017665), 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene (MESH:C095489), tegafur (MESH:D005641), Sn (MESH:D014001), iron (MESH:D007501), aza-BODIPY (MESH:C000613417), 4,4'-dimethyl-2,2'-bipyridine (MESH:C560551), iridium (MESH:D007495), azobenzene (MESH:C009850), water (MESH:D014867), E (MESH:D004540), aspirin (MESH:D001241), amide (MESH:D000577), 2,2'-bipyridine (MESH:D015082), amine (MESH:D000588), phenanthroline (MESH:D010618), carbamates (MESH:D002219), heme (MESH:D006418), CR (MESH:D002857), doxorubicin (MESH:D004317), nitrile (MESH:D009570), haematoxylin (MESH:D006416), combretastatin A-4 (MESH:C058728), d6 (MESH:C036629), ruthenium (MESH:D012428), 5-fluorodeoxyuridine (MESH:D005467), H2O2 (MESH:D006861), porphyrin (MESH:D011166), cisplatin (MESH:D002945), 3,5-DMB (-), superoxide (MESH:D013481), H&amp;E (MESH:D006371), Dextran (MESH:D003911), Cur (MESH:D003474), Ce6 (MESH:C062985), ROS (MESH:D017382)
- **Species:** Mus musculus (house mouse, species) [taxon 10090], Homo sapiens (human, species) [taxon 9606], Bacteria Latreille et al. 1825 (Bacteria stick insect, genus) [taxon 629395]
- **Mutations:** A549R
- **Cell lines:** A549 — Homo sapiens (Human), Lung adenocarcinoma, Cancer cell line (CVCL_0023), L929 — Mus musculus (Mouse), Spontaneously immortalized cell line (CVCL_AR58), HepG2 — Homo sapiens (Human), Hepatoblastoma, Cancer cell line (CVCL_0027), MCF-7 — Homo sapiens (Human), Invasive breast carcinoma of no special type, Cancer cell line (CVCL_0031), HCT116 — Homo sapiens (Human), Colon carcinoma, Cancer cell line (CVCL_0291), MDA-MB-231 — Homo sapiens (Human), Breast adenocarcinoma, Cancer cell line (CVCL_0062), HeLa — Homo sapiens (Human), Human papillomavirus-related endocervical adenocarcinoma, Cancer cell line (CVCL_0030)

## Full text

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## Figures

11 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12968341/full.md

## References

187 references — full list in the complete paper: https://tomesphere.com/paper/PMC12968341/full.md

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Source: https://tomesphere.com/paper/PMC12968341