TSPO Ligand-Methotrexate Prodrug Conjugates: Design, Synthesis, and Biological Evaluation

TSPO Ligand-Methotrexate Prodrug Conjugates: Design, Synthesis, and Biological Evaluation

The 18-kDa translocator protein (TSPO) is a potential mitochondrial target for drug delivery to tumors overexpressing TSPO, including brain cancers, and selective TSPO ligands have been successfully used to selectively deliver drugs into the target. Methotrexate (MTX) is an anticancer drug of choice...

Full description

Bibliographic Details
Main Authors:	Valentino Laquintana, Nunzio Denora, Annalisa Cutrignelli, Mara Perrone, Rosa Maria Iacobazzi, Cosimo Annese, Antonio Lopalco, Angela Assunta Lopedota, Massimo Franco
Format:	Article
Language:	English
Published:	MDPI AG 2016-06-01
Series:	International Journal of Molecular Sciences
Subjects:	translocator protein methotrexate TSPO-ligand bio-conjugate glioma
Online Access:	http://www.mdpi.com/1422-0067/17/6/967

Similar Items

Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels
by: Antonio Lopalco, et al.
Published: (2018-04-01)

An Updated View of Translocator Protein (TSPO)
by: Nunzio Denora, et al.
Published: (2017-12-01)

Synthesis and Evaluation of Tricarbonyl 99mTc-Labeled 2-(4-Chloro)phenyl-imidazo[1,2-a]pyridine Analogs as Novel SPECT Imaging Radiotracer for TSPO-Rich Cancer
by: Ji Young Choi, et al.
Published: (2016-07-01)

Synthesis, Characterization, and Cytotoxicity of the First Oxaliplatin Pt(IV) Derivative Having a TSPO Ligand in the Axial Position
by: Salvatore Savino, et al.
Published: (2016-06-01)

Efficaciousness of Low Affinity Compared to High Affinity TSPO Ligands in the Inhibition of Hypoxic Mitochondrial Cellular Damage Induced by Cobalt Chloride in Human Lung H1299 Cells
by: Nidal Zeineh, et al.
Published: (2020-05-01)

Structure-to-function relationships of bacterial translocator protein (TSPO): a focus on Pseudomonas
by: Charlène eLeneveu-Jenvrin, et al.
Published: (2014-11-01)

Green Fluorescent Terbium (III) Complex Doped Silica Nanoparticles for TSPO Targeting
by: Elisabetta Fanizza, et al.
Published: (2019-06-01)

TSPO: An Evolutionarily Conserved Protein with Elusive Functions
by: Frederick Bonsack, et al.
Published: (2018-06-01)

The protective effect of the TSPO ligands 2,4-Di-Cl-MGV-1, CB86, and CB204 against LPS-induced M1 pro-inflammatory activation of microglia
by: Sheelu Monga, et al.
Published: (2020-05-01)

Etudes des protéines membranaires TSPO
by: Sénicourt, Lucile
Published: (2016)

Translocator Protein (TSPO)
Published: (2018)

TSPO in a murine model of Sandhoff disease: presymptomatic marker of neurodegeneration and disease pathophysiology
by: Meredith K. Loth, et al.
Published: (2016-01-01)

Evaluation of methotrexate-conjugated gadolinium(III) for cancer diagnosis and treatment
by: Xu D, et al.
Published: (2018-10-01)

Tetrapyrroles as Endogenous TSPO Ligands in Eukaryotes and Prokaryotes: Comparisons with Synthetic Ligands
by: Leo Veenman, et al.
Published: (2016-06-01)

Production et caractérisation structurale et fonctionnelle de la protéine membranaire recombinante TSPO
by: Iatmanen, Soria
Published: (2014)

Regulation of Translocator Protein 18 kDa (TSPO) Expression in Rat and Human Male Germ Cells
by: Gurpreet Manku, et al.
Published: (2016-09-01)

VDAC1 and the TSPO: Expression, Interactions, and Associated Functions in Health and Disease States
by: Varda Shoshan-Barmatz, et al.
Published: (2019-07-01)

In Vivo TSPO Signal and Neuroinflammation in Alzheimer’s Disease
by: Benjamin B. Tournier, et al.
Published: (2020-08-01)

The Role of Translocator Protein TSPO in Hallmarks of Glioblastoma
by: Laura-Marie Ammer, et al.
Published: (2020-10-01)

Patterns of Mitochondrial TSPO Binding in Cerebral Small Vessel Disease: An in vivo PET Study With Neuropathological Comparison
by: Paul Wright, et al.
Published: (2020-10-01)

Increased transcription of TSPO, HDAC2, and HDAC6 in the amygdala of males with alcohol use disorder
by: Luana Martins De Carvalho, et al.
Published: (2021-02-01)

Characterization of the High-Affinity Drug Ligand Binding Site of Mouse Recombinant TSPO
by: Soria Iatmanen-Harbi, et al.
Published: (2019-03-01)

A new prodrug and bioactivity evaluation of methotrexate based on Chitosan
by: Mohsin Omar Mohammed, et al.
Published: (2020-06-01)

Transferrin Functionalized Liposomes Loading Dopamine HCl: Development and Permeability Studies across an In Vitro Model of Human Blood–Brain Barrier
by: Antonio Lopalco, et al.
Published: (2018-03-01)

Impact of Cholesterol on the Stability of Monomeric and Dimeric Forms of the Translocator Protein TSPO: A Molecular Simulation Study
by: Zeineb Si Chaib, et al.
Published: (2020-09-01)

Development of a novel radioligand for imaging 18-kD translocator protein (TSPO) in a rat model of Parkinson’s disease
by: Chun-Yi Wu, et al.
Published: (2019-09-01)

The TSPO Ligands MGV-1 and 2-Cl-MGV-1 Differentially Inhibit the Cigarette Smoke-Induced Cytotoxicity to H1299 Lung Cancer Cells
by: Nidal Zeineh, et al.
Published: (2021-05-01)

TSPO: an emerging role in appetite for a therapeutically promising biomarker
by: Joshua Wang, et al.
Published: (2021-08-01)

Paeoniflorin elicits the anti-proliferative effects on glioma cell via targeting translocator protein 18 KDa
by: Zhuo-wei Gao, et al.
Published: (2021-01-01)

Induction of ATP Release, PPIX Transport, and Cholesterol Uptake by Human Red Blood Cells Using a New Family of TSPO Ligands
by: Irene Marginedas-Freixa, et al.
Published: (2018-10-01)

In vitro and pilot in vivo imaging of 18 kDa translocator protein (TSPO) in inflammatory vascular disease
by: Romain Schollhammer, et al.
Published: (2021-05-01)

Translocator Protein 18 kDa (TSPO) Deficiency Inhibits Microglial Activation and Impairs Mitochondrial Function
by: Rumeng Yao, et al.
Published: (2020-06-01)

Efeitos dos ligantes de TSPO sobre a migração leucocitária: participação de receptores de glicorticóides
by: Camila Bento de Lima
Published: (2012)

Efeitos dos ligantes de TSPO sobre a migração leucocitária: participação de receptores de glicorticóides
by: Lima, Camila Bento de
Published: (2012)

Translocator protein (TSPO) and stress cascades in mouse models of psychosis with inflammatory disturbances
by: Fukudome, Daisuke
Published: (2020)

Synthesis and Preliminary Anticancer Evaluation of 6-Mercaptopurine –Methotrexate Conjugate as Possible Mutual Prodrug
by: Asmaa S. Al-Darraji, et al.
Published: (2019-06-01)

Recent developments on PET radiotracers for TSPO and their applications in neuroimaging
by: Lingling Zhang, et al.
Published: (2021-02-01)

The Synthesis and Preliminary Anticancer Evaluation of 6-Mercaptopurine -Methotrexate Conjugate as Possible Mutual Prodrug
by: Asmaa Safwan Al-darraji, et al.
Published: (2019-06-01)

The Efficacy of the Novel TSPO Ligands 2-Cl-MGV-1 and 2,4-Di-Cl-MGV-1 Compared to the Classical TSPO Ligand PK 11195 to Counteract the Release of Chemokines from LPS-Stimulated BV-2 Microglial Cells
by: Sheelu Monga, et al.
Published: (2020-09-01)

Downregulation of Mitochondrial TSPO Inhibits Mitophagy and Reduces Enucleation during Human Terminal Erythropoiesis
by: Martina Moras, et al.
Published: (2020-11-01)