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Journal articles on the topic 'Photoactivatable systems'

Author: Grafiati

Published: 11 January 2025

Last updated: 31 July 2025

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1

Raymo, Françisco M. "Photoactivatable Fluorophores." ISRN Physical Chemistry 2012 (September 17, 2012): 1–15. http://dx.doi.org/10.5402/2012/619251.

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Photoactivatable fluorophores switch from a nonemissive to an emissive state upon illumination at an activating wavelength and then emit after irradiation at an exciting wavelength. The interplay of such activation and excitation events can be exploited to switch fluorescence on in a defined region of space at a given interval of time. In turn, the spatiotemporal control of fluorescence translates into the opportunity to implement imaging and spectroscopic schemes that are not possible with conventional fluorophores. Specifically, photoactivatable fluorophores permit the monitoring of dynamic

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Nihongaki, Yuta, Yuichi Furuhata, Takahiro Otabe, Saki Hasegawa, Keitaro Yoshimoto, and Moritoshi Sato. "CRISPR–Cas9-based photoactivatable transcription systems to induce neuronal differentiation." Nature Methods 14, no. 10 (2017): 963–66. http://dx.doi.org/10.1038/nmeth.4430.

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Gil, Melina D., Silvestre Bongiovanni Abel, César A. Barbero, Natalia S. Paulucci, and Edith I. Yslas. "Low-Power NIR-Triggered Photothermal Inactivation of Pseudomonas aeruginosa with Polypyrrole Nanoparticles." Polymers 17, no. 11 (2025): 1442. https://doi.org/10.3390/polym17111442.

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Conducting polymer (CP) nanoparticles have emerged as innovative materials for biomedical applications, particularly due to their safe interaction with biological systems. This study focuses on the synthesis, morphological, and spectroscopic characterization of polypyrrole nanoparticles (PPy-NPs) as photoactivatable agents under near-infrared (NIR) radiation for the inactivation of pathogenic bacteria. We successfully synthesized uniform nanoparticles (~180 nm) with strong absorption in the NIR region. A comprehensive characterization was performed using electron microscopy, dynamic light scat

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Smith, Nichola A., and Peter J. Sadler. "Photoactivatable metal complexes: from theory to applications in biotechnology and medicine." Philosophical Transactions of the Royal Society A: Mathematical, Physical and Engineering Sciences 371, no. 1995 (2013): 20120519. http://dx.doi.org/10.1098/rsta.2012.0519.

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This short review highlights some of the exciting new experimental and theoretical developments in the field of photoactivatable metal complexes and their applications in biotechnology and medicine. The examples chosen are based on some of the presentations at the Royal Society Discussion Meeting in June 2012, many of which are featured in more detail in other articles in this issue. This is a young field. Even the photochemistry of well-known systems such as metal–carbonyl complexes is still being elucidated. Striking are the recent developments in theory and computation (e.g. time-dependent

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Snapp, E. L., and P. Lajoie. "Activating Photoactivatable Proteins with Laser Light to Visualize Membrane Systems and Membrane Traffic in Living Cells." Cold Spring Harbor Protocols 2011, no. 11 (2011): pdb.prot066571. http://dx.doi.org/10.1101/pdb.prot066571.

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Ivanskaya, E. V., M. I. Meschaninova, M. A. Vorobyeva, D. O. Zharkov, and D. S. Novopashina. "The approach to the preparation of cyclic photocleavable RNA for photoactivatable CRISPR/Cas9 System." Биоорганическая химия 50, no. 5 (2024): 622–35. https://doi.org/10.31857/s0132342324050051.

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The development of controllable gene editing systems on the base of CRISPR/Cas is an actually problem of modern molecular biology and genetic enginery. Interesting variant of solution of this problem is modification of guide RNA by introduction of photocleavable linkers. We developed the approach to the synthesis of cyclic photocleavable guide crRNA for the CRISPR/Cas9 system with photolinker on the base of 1-(2-nitrophenyl)-1,2-ethanediol (PL). Upon irradiation by UV-light these guide RNA are linearized and CRISPR/Cas9 system is activated. Two chemical methods to the cyclization of RNA were t

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Li, Huiying, Qiansen Zhang, Yiran Gu, et al. "Efficient photoactivatable Dre recombinase for cell type-specific spatiotemporal control of genome engineering in the mouse." Proceedings of the National Academy of Sciences 117, no. 52 (2020): 33426–35. http://dx.doi.org/10.1073/pnas.2003991117.

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Precise genetic engineering in specific cell types within an intact organism is intriguing yet challenging, especially in a spatiotemporal manner without the interference caused by chemical inducers. Here we engineered a photoactivatable Dre recombinase based on the identification of an optimal split site and demonstrated that it efficiently regulated transgene expression in mouse tissues spatiotemporally upon blue light illumination. Moreover, through a double-floxed inverted open reading frame strategy, we developed a Cre-activated light-inducible Dre (CALID) system. Taking advantage of well

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Valueva, Anastasia A., Ivan D. Shumov, Anna L. Kaysheva, et al. "Covalent Protein Immobilization onto Muscovite Mica Surface with a Photocrosslinker." Minerals 10, no. 5 (2020): 464. http://dx.doi.org/10.3390/min10050464.

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Muscovite mica with an amino silane-modified surface is commonly used as a substrate in atomic force microscopy (AFM) studies of biological macromolecules. Herein, the efficiency of two different protein immobilization strategies employing either (N-hydroxysuccinimide ester)-based crosslinker (DSP) or benzophenone-based photoactivatable crosslinker (SuccBB) has been compared using AFM and mass spectrometry analysis. Two proteins with different physicochemical properties—human serum albumin (HSA) and horseradish peroxidase enzyme protein (HRP)—have been used as model objects in the study. In th

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Maronde, Erik. "Cyclic Nucleotide (cNMP) Analogues: Past, Present and Future." International Journal of Molecular Sciences 22, no. 23 (2021): 12879. http://dx.doi.org/10.3390/ijms222312879.

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Cyclic nucleotides are important second messengers involved in cellular events, and analogues of this type of molecules are promising drug candidates. Some cyclic nucleotide analogues have become standard tools for the investigation of biochemical and physiological signal transduction pathways, such as the Rp-diastereomers of adenosine and guanosine 3′,5′-cyclic monophosphorothioate, which are competitive inhibitors of cAMP- and cGMP-dependent protein kinases. Next generation analogues exhibit a higher membrane permeability, increased resistance against degradation, and improved target specifi

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Ferenz, Nick P., and Patricia Wadsworth. "Prophase Microtubule Arrays Undergo Flux-like Behavior in Mammalian Cells." Molecular Biology of the Cell 18, no. 10 (2007): 3993–4002. http://dx.doi.org/10.1091/mbc.e07-05-0420.

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In higher eukaryotic cells, microtubules within metaphase and anaphase spindles undergo poleward flux, the slow, poleward movement of tubulin subunits through the spindle microtubule lattice. Although a number of studies have documented this phenomenon across a wide range of model systems, the possibility of poleward flux before nuclear envelope breakdown (NEB) has not been examined. Using a mammalian cell line expressing photoactivatable green fluorescent protein (GFP)-tubulin, we observe microtubule motion, both toward and away from centrosomes, at a wide range of rates (0.5–4.5 μm/min) in p

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Ben Mihoub, Amina, Ludivine Larue, Albert Moussaron, et al. "Use of Cyclodextrins in Anticancer Photodynamic Therapy Treatment." Molecules 23, no. 8 (2018): 1936. http://dx.doi.org/10.3390/molecules23081936.

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Photodynamic therapy (PDT) is mainly used to destroy cancerous cells; it combines the action of three components: a photoactivatable molecule or photosensitizer (PS), the light of an appropriate wavelength, and naturally occurring molecular oxygen. After light excitation of the PS, the excited PS then reacts with molecular oxygen to produce reactive oxygen species (ROS), leading to cellular damage. One of the drawbacks of PSs is their lack of solubility in water and body tissue fluids, thereby causing low bioavailability, drug-delivery efficiency, therapeutic efficacy, and ROS production. To i

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White, Paul, Amar Joshi, Patrice Rassam, et al. "Exploitation of an iron transporter for bacterial protein antibiotic import." Proceedings of the National Academy of Sciences 114, no. 45 (2017): 12051–56. http://dx.doi.org/10.1073/pnas.1713741114.

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Unlike their descendants, mitochondria and plastids, bacteria do not have dedicated protein import systems. However, paradoxically, import of protein bacteriocins, the mechanisms of which are poorly understood, underpins competition among pathogenic and commensal bacteria alike. Here, using X-ray crystallography, isothermal titration calorimetry, confocal fluorescence microscopy, and in vivo photoactivatable cross-linking of stalled translocation intermediates, we demonstrate how the iron transporter FpvAI in the opportunistic pathogen Pseudomonas aeruginosa is hijacked to translocate the bact

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Yamaguchi, Haruka, Masayasu Okada, Takuya Otani, et al. "Near-Infrared Photoimmunotherapy in Brain Tumors—An Unexplored Frontier." Pharmaceuticals 18, no. 5 (2025): 751. https://doi.org/10.3390/ph18050751.

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Near-infrared photoimmunotherapy (NIR-PIT) is a promising cancer treatment that uses near-infrared light to activate a conjugate of a monoclonal antibody (mAb) and a photoactivatable silica phthalocyanine dye (IRDye700DX: IR700). Unlike conventional photodynamic therapy (PDT), NIR-PIT selectively destroys targeted tumor cells while preserving the surrounding normal tissue and providing superior tissue penetration. Recently, NIR-PIT has been approved for the treatment of unresectable recurrent head and neck cancers in Japan. It induces highly selective cancer cell death; therefore, it is expect

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Jerng, Henry H., Jay M. Patel, Tamor A. Khan, Benjamin R. Arenkiel, and Paul J. Pfaffinger. "Light-regulated voltage-gated potassium channels for acute interrogation of channel function in neurons and behavior." PLOS ONE 16, no. 3 (2021): e0248688. http://dx.doi.org/10.1371/journal.pone.0248688.

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Voltage-gated potassium (Kv) channels regulate the membrane potential and conductance of excitable cells to control the firing rate and waveform of action potentials. Even though Kv channels have been intensely studied for over 70 year, surprisingly little is known about how specific channels expressed in various neurons and their functional properties impact neuronal network activity and behavior in vivo. Although many in vivo genetic manipulations of ion channels have been tried, interpretation of these results is complicated by powerful homeostatic plasticity mechanisms that act to maintain

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Vizoso, Miguel, Colin E. J. Pritchard, Lorenzo Bombardelli, et al. "A doxycycline- and light-inducible Cre recombinase mouse model for optogenetic genome editing." Nature Communications 13, no. 1 (2022). http://dx.doi.org/10.1038/s41467-022-33863-z.

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AbstractThe experimental need to engineer the genome both in time and space, has led to the development of several photoactivatable Cre recombinase systems. However, the combination of inefficient and non-intentional background recombination has prevented thus far the wide application of these systems in biological and biomedical research. Here, we engineer an optimized photoactivatable Cre recombinase system that we refer to as doxycycline- and light-inducible Cre recombinase (DiLiCre). Following extensive characterization in cancer cell and organoid systems, we generate a DiLiCre mouse line,

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Umeda, Yuki, Hao Zhu, Satoshi Yamaguchi, et al. "Photoactivatable Alkyne Tag for Photolabeling Biomolecules in Living Cells." ChemBioChem, May 14, 2025. https://doi.org/10.1002/cbic.202500190.

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Light‐induced molecular imaging methods have attracted considerable attention owing to their potential for monitoring changes in the localization of intracellular molecules, which can provide valuable insights into the molecular mechanisms of living systems. In this study, a photoactivatable alkyne tag is developed by modifying an unstable intermediate of the alkyne‐forming reaction with a photodegradable protecting group; the photodegradation triggers the conversion of the intermediate into a linear alkyne in an aqueous solution. The developed photoactivatable alkyne tag is incorporated into

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Qiu, Xujun, Eric Pohl, Andre Jung, et al. "Modulating the photolysis of aryl azides in supramolecular host to develop photoactivatable fluorophores." Chemical Communications, 2024. http://dx.doi.org/10.1039/d4cc03907f.

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Photolysis of aryl azides is a convenient method to approach more functionalized systems in chemical biology. Here,we present a set of photoactivatable aryl azides that undergo controlled reaction pathways within...

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Huang, Lili, Justin Shum, Lawrence Cho-Cheung Lee, Guang-Xi Xu, Peter Kam-Keung Leung, and Kenneth Kam-Wing Lo. "An iridium(III) monosulfur-substituted chlorotetrazine complex for cysteine conjugation, bioimaging and photoactivatable therapy." RSC Chemical Biology, 2025. https://doi.org/10.1039/d4cb00316k.

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Photoactivatable systems have received considerable attention in the development of diagnostics and therapeutics due to their noninvasive nature and precise spatiotemporal control. Of particular interest is the S,S-tetrazine unit, which...

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Zhang, Xiao, Yuxin Pan, Shoukai Kang, and Liangcai Gu. "Combinatorial Approaches for Efficient Design of Photoswitchable Protein-Protein Interactions as In Vivo Actuators." Frontiers in Bioengineering and Biotechnology 10 (February 8, 2022). http://dx.doi.org/10.3389/fbioe.2022.844405.

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Light switchable two-component protein dimerization systems offer versatile manipulation and dissection of cellular events in living systems. Over the past 20 years, the field has been driven by the discovery of photoreceptor-based interaction systems, the engineering of light-actuatable binder proteins, and the development of photoactivatable compounds as dimerization inducers. This perspective is to categorize mechanisms and design approaches of these dimerization systems, compare their advantages and limitations, and bridge them to emerging applications. Our goal is to identify new opportun

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20

Song, Kun-Long, Ricardo Meyrelles, Guillaume Pilet, Boris Maryasin, Maurice Médebielle, and Jérémy Merad. "Dication Disulfuranes as Photoactivatable Sources of Radical Organocatalysts." Angewandte Chemie, November 4, 2024. http://dx.doi.org/10.1002/ange.202419751.

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The recent development of photoredox and energy transfer catalysis has led to a significant expansion of visible light‐driven chemical transformations. These methods have demonstrated exceptional efficiency in converting a wide range of substrates into radical intermediates and generating open‐shell catalytic species. However, the simplification of catalytic systems and the direct generation of highly reactive radical organocatalysts through direct visible light irradiation from stable precatalysts remains largely an unrealized goal. This challenge is mainly due to the limited availability of

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Song, Kun-Long, Ricardo Meyrelles, Guillaume Pilet, Boris Maryasin, Maurice Médebielle, and Jérémy Merad. "Dication Disulfuranes as Photoactivatable Sources of Radical Organocatalysts." Angewandte Chemie International Edition, November 4, 2024. http://dx.doi.org/10.1002/anie.202419751.

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The recent development of photoredox and energy transfer catalysis has led to a significant expansion of visible light‐driven chemical transformations. These methods have demonstrated exceptional efficiency in converting a wide range of substrates into radical intermediates and generating open‐shell catalytic species. However, the simplification of catalytic systems and the direct generation of highly reactive radical organocatalysts through direct visible light irradiation from stable precatalysts remains largely an unrealized goal. This challenge is mainly due to the limited availability of

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22

Zhang, Lili, Mei Chen, Zhiqiang Wang, et al. "Spatiotemporal Regulation of Cell Fate in Living Systems Using Photoactivatable Artificial DNA Membraneless Organelles." ACS Central Science, May 21, 2024. http://dx.doi.org/10.1021/acscentsci.4c00380.

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23

Zhao, Hengzhi, Deyu Yi, Lele Li, Yuliang Zhao, and Mengyuan Li. "Modular Weaving DNAzyme in Skeleton of DNA Nanocages for Photoactivatable Catalytic Activity Regulation." Angewandte Chemie, March 22, 2024. http://dx.doi.org/10.1002/ange.202404064.

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AbstractDNAzymes exhibit tremendous application potentials in the field of biosensing and gene regulation due to its unique catalytic function. However, spatiotemporally controlled regulation of DNAzyme activity remains a daunting challenge, which may cause nonspecific signal leakage or gene silencing of the catalytic systems. Here, we report a photochemical approach via modular weaving active DNAzyme into the skeleton of tetrahedral DNA nanocages (TDN) for light‐triggered on‐demand liberation of DNAzyme and thus conditional control of gene regulation activity. We demonstrate that the direct e

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Zhao, Hengzhi, Deyu Yi, Lele Li, Yuliang Zhao, and Mengyuan Li. "Modular Weaving DNAzyme in Skeleton of DNA Nanocages for Photoactivatable Catalytic Activity Regulation." Angewandte Chemie International Edition, March 22, 2024. http://dx.doi.org/10.1002/anie.202404064.

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AbstractDNAzymes exhibit tremendous application potentials in the field of biosensing and gene regulation due to its unique catalytic function. However, spatiotemporally controlled regulation of DNAzyme activity remains a daunting challenge, which may cause nonspecific signal leakage or gene silencing of the catalytic systems. Here, we report a photochemical approach via modular weaving active DNAzyme into the skeleton of tetrahedral DNA nanocages (TDN) for light‐triggered on‐demand liberation of DNAzyme and thus conditional control of gene regulation activity. We demonstrate that the direct e

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De Santis, Riccardo, Fred Etoc, Edwin A. Rosado-Olivieri, and Ali H. Brivanlou. "Self-organization of human dorsal-ventral forebrain structures by light induced SHH." Nature Communications 12, no. 1 (2021). http://dx.doi.org/10.1038/s41467-021-26881-w.

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AbstractOrganizing centers secrete morphogens that specify the emergence of germ layers and the establishment of the body’s axes during embryogenesis. While traditional experimental embryology tools have been instrumental in dissecting the molecular aspects of organizers in model systems, they are impractical in human in-vitro model systems to dissect the relationships between signaling and fate along embryonic coordinates. To systematically study human embryonic organizer centers, we devised a collection of optogenetic ePiggyBac vectors to express a photoactivatable Cre-loxP recombinase, that

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Fedoryshchak, Roman O., Andrii Gorelik, Mengjie Shen, Maria M. Shchepinova, Inmaculada Perez-Dorado, and Edward William Tate. "Discovery of lipid-mediated protein-protein interactions in living cells using metabolic labeling with photoactivatable clickable probes." Chemical Science, 2023. http://dx.doi.org/10.1039/d2sc06116c.

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Protein-protein interactions (PPIs) are essential and pervasive regulatory elements in biology. Despite development of a range of techniques to probe PPIs in living systems, there is a dearth of approaches...

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Armin, Baumschlager Mustafa Khammash. "Synthetic Biological Approaches for Optogenetics and Tools for Transcriptional Light-Control in Bacteria." February 9, 2021. https://doi.org/10.1002/adbi.202000256.

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Light has become established as a tool not only to visualize and investigate  but also to steer biological systems. This review starts by discussing the unique features that make light such an effective control input in biology. It then gives an overview of how light-control came to progress, starting  with photoactivatable compounds and leading up to current genetic imple-  mentations using optogenetic approaches. The review then zooms in on  optogenetics, focusing on photosensitive proteins, which form the basis for  optogenetic engineering using synthetic biological

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Soleimany, Amir, Delaram Kargari Aghmiouni, Masomeh Amirikhah, Mohammad Ali Shokrgozar, Sepideh Khoee, and Bruno Sarmento. "Two‐Photon Mediated Cancer Therapy: A Comprehensive Review on Two‐Photon Photodynamic Therapy and Two‐Photon‐Activated Therapeutic Delivery Systems." Advanced Functional Materials, July 18, 2024. http://dx.doi.org/10.1002/adfm.202408594.

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AbstractTwo‐photon excitation (2PE) represents substantial advantages in biophotonics over traditional one‐photon excitation (1PE), offering enhanced spatial resolution and deeper tissue penetration capabilities. Since its introduction in the 1990s, two‐photon excited microscopy has spurred the rapid emergence of novel 2PE‐based applications, including photodynamic therapy (PDT) and the targeted release of biologically active agents. This review first elucidates the fundamental principles of 2PE before comprehensively examining the evolution of photosensitizers (PSs) for two‐photon PDT (2P‐PDT

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Bequet‐Ermoy, Etienne, Virginie Silvestre, Stéphane Cuenot, and Eléna Ishow. "Reversible Light‐Triggered Stretching of Small‐Molecule Photochromic Organic Nanoparticles." Small, July 12, 2024. http://dx.doi.org/10.1002/smll.202403912.

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AbstractFunctional organic nanomaterials are nowadays largely spread in the field of nanomedicine. In situ modulation of their morphology is thus expected to considerably impact their interactions with the surroundings. In this context, photoswitchable nanoparticles that are manufactured, amenable to extensive disassembling upon illumination in the visible, and reversible reshaping under UV exposure. Such reversibility turns to be strongly impaired for photochromic nanoparticles in close contact with a substrate. In situ atomic force microscopy investigations at the nanoscale actually reveal p

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Uji, Masanori, Jumpei Kondo, Chikako Hara‐Miyauchi, et al. "In Vivo Optogenetics Based on Heavy Metal‐Free Photon Upconversion Nanoparticles." Advanced Materials, September 23, 2024. http://dx.doi.org/10.1002/adma.202405509.

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AbstractPhoton upconversion (UC) from red or near‐infrared (NIR) light to blue light is promising for in vivo optogenetics. However, the examples of in vivo optogenetics have been limited to lanthanide inorganic UC nanoparticles, and there have been no examples of optogenetics without using heavy metals. Here the first example of in vivo optogenetics using biocompatible heavy metal‐free TTA‐UC nanoemulsions is shown. A new organic TADF sensitizer, a boron difluoride curcuminoid derivative modified with a bromo group, can promote intersystem crossing to the excited triplet state, significantly

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Bolonduro, Olurotimi A., Zijing Chen, Corey P. Fucetola, et al. "An Integrated Optogenetic and Bioelectronic Platform for Regulating Cardiomyocyte Function." Advanced Science, July 25, 2024. http://dx.doi.org/10.1002/advs.202402236.

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AbstractBioelectronic medicine is emerging as a powerful approach for restoring lost endogenous functions and addressing life‐altering maladies such as cardiac disorders. Systems that incorporate both modulation of cellular function and recording capabilities can enhance the utility of these approaches and their customization to the needs of each patient. Here is report an integrated optogenetic and bioelectronic platform for stable and long‐term stimulation and monitoring of cardiomyocyte function in vitro. Optical inputs are achieved through the expression of a photoactivatable adenylyl cycl

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Vogt, Arend, Raik Paulat, Daniel Parthier, et al. "Simultaneous spectral illumination of microplates for high-throughput optogenetics and photobiology." Biological Chemistry, September 23, 2024. http://dx.doi.org/10.1515/hsz-2023-0205.

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Abstract The biophysical characterization and engineering of optogenetic tools and photobiological systems has been hampered by the lack of efficient methods for spectral illumination of microplates for high-throughput analysis of action spectra. Current methods to determine action spectra only allow the sequential spectral illumination of individual wells. Here we present the open-source RainbowCap-system, which combines LEDs and optical filters in a standard 96-well microplate format for simultaneous and spectrally defined illumination. The RainbowCap provides equal photon flux for each wave

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Olivi, Lorenzo, Cleo Bagchus, Victor Pool, et al. "Live-cell imaging reveals the trade-off between target search flexibility and efficiency for Cas9 and Cas12a." Nucleic Acids Research, April 22, 2024. http://dx.doi.org/10.1093/nar/gkae283.

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Abstract CRISPR-Cas systems have widely been adopted as genome editing tools, with two frequently employed Cas nucleases being SpyCas9 and LbCas12a. Although both nucleases use RNA guides to find and cleave target DNA sites, the two enzymes differ in terms of protospacer-adjacent motif (PAM) requirements, guide architecture and cleavage mechanism. In the last years, rational engineering led to the creation of PAM-relaxed variants SpRYCas9 and impLbCas12a to broaden the targetable DNA space. By employing their catalytically inactive variants (dCas9/dCas12a), we quantified how the protein-specif

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Gabashvili, Anna N., Natalya A. Alexandrushkina, Elizaveta N. Mochalova, et al. "Internalization of transferrin-tagged Myxococcus xanthus encapsulins into mesenchymal stem cells." Experimental Biology and Medicine 249 (May 7, 2024). http://dx.doi.org/10.3389/ebm.2024.10055.

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Currently, various functionalized nanocarrier systems are extensively studied for targeted delivery of drugs, peptides, and nucleic acids. Joining the approaches of genetic and chemical engineering may produce novel carriers for precise targeting different cellular proteins, which is important for both therapy and diagnosis of various pathologies. Here we present the novel nanocontainers based on vectorized genetically encoded Myxococcus xanthus (Mx) encapsulin, confining a fluorescent photoactivatable mCherry (PAmCherry) protein. The shells of such encapsulins were modified using chemical con

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Cieslik, Patrick A., Simon Klingler, Mirja Nolff, and Jason P. Holland. "Radiolabelled 177Lu‐Bispidine‐Trastuzumab for Targeting Human Epidermal Growth Factor Receptor 2 Positive Cancers." Chemistry – A European Journal, December 8, 2023. http://dx.doi.org/10.1002/chem.202303805.

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Radioimmunotherapy (TRIT) is a promising alternative to conventional treatment options. Here, we present experimental work on the synthesis, radiochemistry, and in vivo performance of a lanthanide‐selective nonadentate bispidine ligand suitable for 177Lu3+ ion complexation. The ligand (bisp,1) was derivatised with a photoactivatable aryl azide (ArN3) group as a bioconjugation handle for light‐induced labelling of proteins. Quantitative radiosynthesis of [177Lu]Lu‐1+ was accomplished in 10 minutes at 40oC. Subsequent incubation [177Lu]Lu‐1+ with trastuzumab, followed by irradiation with light a

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