The TSPO Ligands MGV-1 and 2-Cl-MGV-1 Differentially Inhibit the Cigarette Smoke-Induced Cytotoxicity to H1299 Lung Cancer Cells

Zeineh, Nidal; Nagler, Rafael M.; Gabay, Martín; Obeid, Fadi; Kahana, Meygal; Weizman, Abraham; Gavish, Moshe

doi:10.3390/biology10050395

Cited by 2 publications

(2 citation statements)

References 52 publications

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“…27,28 2-Cl-MGV-1 also inhibited cigarette smoke-induced cytotoxicity to H1299 lung cancer cells through prevention of ATP synthase reversal, ROS generation, depolarization of the mitochondrial membrane, and elevation in LDH. 29 Furthermore, MGV-1 promoted differentiation of progenitor cells to mature neurons and weeded out non-differentiating progenitor cells. 17 Further, our previous study suggested that 2-Cl-MGV-1 reduced neuronal apoptosis by inhibiting the mitochondrial-dependent pathway.…”

Section: Discussionmentioning

confidence: 99%

Enhanced angiogenesis in the thalamus induced by a novel TSPO ligand ameliorates cognitive deficits after focal cortical infarction

Chen,

Veenman,

Liao

et al. 2023

J Cereb Blood Flow Metab

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Neuronal loss in the ipsilateral thalamus after focal cortical infarction participates in post-stroke cognitive deficits, and enhanced angiogenesis in the thalamus is expected to reduce neuronal damage. We hypothesize that novel translocator protein (TSPO) ligand, 2-Cl-MGV-1, can promote angiogenesis, attenuate neuronal loss in the thalamus, and ameliorate post-stroke cognitive deficits. Cortical infarction was induced by distal middle cerebral artery occlusion (dMCAO) in stroke-prone renovascular hypertensive rats. 2-Cl-MGV-1 or dimethyl sulfoxide was administered 24 h after dMCAO and then for 6 or 13 days. Spatial learning and memory were assessed using the Morris water maze. Neuronal loss, TSPO expression, angiogenesis, and intrinsic pathway were determined by immunofluorescence and immunoblotting 7 and 14 days after dMCAO. Cortical infarction caused post-stroke cognitive deficits and secondary neuronal loss with gliosis in the ipsilateral thalamus within 14 days of dMCAO. Increased angiogenesis and elevated expression of vascular TSPO were detected in the ipsilateral thalamus, and treatment with 2-Cl-MGV-1 enhanced angiogenesis by stimulating the PI3K-AKT-mTOR pathway. The effects of 2-Cl-MGV-1 on angiogenesis coincided with reduced neuronal loss in the thalamus and contributed to improvements in post-stroke cognitive deficits. Our findings suggest that 2-Cl-MGV-1 stimulates angiogenesis, ameliorates neuronal loss in the thalamus, and improves post-stroke cognitive deficits.

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Section: Discussionmentioning

confidence: 99%

Enhanced angiogenesis in the thalamus induced by a novel TSPO ligand ameliorates cognitive deficits after focal cortical infarction

Chen,

Veenman,

Liao

et al. 2023

J Cereb Blood Flow Metab

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“…Therefore, treatment with MGV-1 and 2-Cl-MGV-1 was helpful in preventing TSPO-associated lung cancer. 92 …”

Section: Lung Cancermentioning

confidence: 99%

Translocator Protein 18 kDa (TSPO): A Promising Molecular Target for Image-Guided Surgery of Solid Cancers

Wongso,

Kurniawan,

Setiadi

et al. 2023

Adv Pharm Bull

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Translocator protein 18-kDa, broadly known as TSPO, is a mitochondrial membrane protein, previously identified as the peripheral benzodiazepine receptor (PBR). TSPO involves in a broad number of biochemical events, such as steroidogenesis, mitochondrial cholesterol transport, cell survival and death, cell proliferation, and carcinogenesis. Several investigations have reported the roles of TSPO in various types of cancers, including colorectal cancer, brain cancer, melanoma, breast cancer, prostate cancer, and lung cancer. It was found that TSPO is upregulated in cancer cells, and it appears that its expression is parallel with an aggressive phenotype and/or poor prognosis. As a consequence, there is great potential for developing diagnostic and prognostic tools targeting the TSPO. In this regard, several radioligands targeting the TSPO have been identified, and some of the candidates have advanced to clinical trials. In recent years, image-guided surgery using hybrid probes bearing radioactive and fluorescence molecules has demonstrated promising outcomes in animal and human studies, and thus might serve as a valuable surgical navigator during cancer surgery. In general, current hybrid probes are built from various molecular platforms, including small molecules, nanoparticles, and antibodies. Although several TSPO-targeted imaging probes have been developed, their development for image-guided surgery of cancers is scarce. This review highlights recent findings of the involvement of TSPO in carcinogenesis, and provides a new perspective on the potential application of TSPO-targeted hybrid probes for image-guided surgery.

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The TSPO Ligands MGV-1 and 2-Cl-MGV-1 Differentially Inhibit the Cigarette Smoke-Induced Cytotoxicity to H1299 Lung Cancer Cells

Cited by 2 publications

References 52 publications

Enhanced angiogenesis in the thalamus induced by a novel TSPO ligand ameliorates cognitive deficits after focal cortical infarction

Enhanced angiogenesis in the thalamus induced by a novel TSPO ligand ameliorates cognitive deficits after focal cortical infarction

Translocator Protein 18 kDa (TSPO): A Promising Molecular Target for Image-Guided Surgery of Solid Cancers

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