title: Target-selective phototherapy using a ligand-based photosensitizer for type 2 cannabinoid receptor.
abstract: Phototherapy is a powerful, noninvasive approach for cancer treatment, with several agents currently in clinical use. Despite the progress and promise, most current phototherapy agents have serious side effects as they can lead to damage to healthy tissue, even when the photosensitizers are fused to targeting molecules due to nonspecific light activation of the unbound photosensitizer. To overcome these limitations, we developed a phototherapy agent that combines a functional ligand and a near infrared phthalocyanine dye. Our target is type 2 cannabinoid receptor (CB2R), considered an attractive therapeutic target for phototherapy given it is overexpressed by many types of cancers that are located at a surface or can be reached by an endoscope. We show that our CB2R-targeted phototherapy agent, IR700DX-mbc94, is specific for CB2R and effective only when bound to the target receptor. Overall, this opens up the opportunity for development of an alternative treatment option for CB2R-positive cancers.
authors.affiliation: Department of Radiology, University of Pittsburgh, 100 Technology Drive, Pittsburgh, PA 15219, USA; Department of Diagnostic Radiology, First Hospital of Medical School, Xi'an Jiaotong University, 277 Yanta West Road, 710061 Xi'an, PRC.
authors.forename: Shaojuan
authors.initials: S
authors.lastname: Zhang
authors.affiliation: Department of Radiology, University of Pittsburgh, 100 Technology Drive, Pittsburgh, PA 15219, USA; Department of Radiology, Eastern Hepatobiliary Surgery Hospital, Second Military Medical University, 225 Changhai Road, 200438 Shanghai, PRC.
authors.forename: Ningyang
authors.initials: N
authors.lastname: Jia
authors.affiliation: Department of Radiology, University of Pittsburgh, 100 Technology Drive, Pittsburgh, PA 15219, USA.
authors.forename: Pin
authors.initials: P
authors.lastname: Shao
authors.affiliation: Department of Pharmaceutical Sciences, Computational Chemical Genomics Screening Center, School of Pharmacy and Drug Discovery Institute, University of Pittsburgh, Pittsburgh, PA 15213, USA.
authors.forename: Qin
authors.initials: Q
authors.lastname: Tong
authors.affiliation: Department of Pharmaceutical Sciences, Computational Chemical Genomics Screening Center, School of Pharmacy and Drug Discovery Institute, University of Pittsburgh, Pittsburgh, PA 15213, USA.
authors.forename: Xiang-Qun
authors.initials: XQ
authors.lastname: Xie
authors.affiliation: Department of Radiology, University of Pittsburgh, 100 Technology Drive, Pittsburgh, PA 15219, USA; University of Pittsburgh Cancer Institute, 5150 Centre Avenue, Pittsburgh, PA 15232, USA. Electronic address: baim@upmc.edu.
authors.forename: Mingfeng
authors.initials: M
authors.lastname: Bai
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D007211:Indoles / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology / Q000627:therapeutic use; D008024:Ligands; D051379:Mice; D008856:Microscopy, Fluorescence; D009369:Neoplasms / Q000378:metabolism / Q000473:pathology / Q000628:therapy; D017646:Organosilicon Compounds / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology / Q000627:therapeutic use; D017319:Photosensitizing Agents / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology / Q000627:therapeutic use; D010789:Phototherapy; D011485:Protein Binding; D043885:Receptor, Cannabinoid, CB2 / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: C000593031:IR700DX-mbc94; D007211:Indoles; D008024:Ligands; D017646:Organosilicon Compounds; D017319:Photosensitizing Agents; D043885:Receptor, Cannabinoid, CB2