36 results match your criteria targeting peg3

MTTL3 upregulates microRNA-1246 to promote occurrence and progression of NSCLC via targeting paternally expressed gene 3.

Mol Ther Nucleic Acids 2021 Jun 24;24:542-553. Epub 2021 Feb 24.

Department of Thoracocardiac Surgery, The Third Affiliated Hospital of Sun Yat-sen University, Guangzhou 510630, Guangdong, China.

Non-small cell lung cancer (NSCLC) is one of the major causes of morbidity and mortality worldwide. We aimed to investigate the role of N6-methyladenosine (m6A) methyltransferase-like 3 (METTL3) regulating microRNA-1246 (miR-1246) in the progression of NSCLC by targeting paternally expressed gene 3 (PEG3). METTL3, miR-1246, and PEG3 expression in tissues was assessed, and the predictive role of METTL3 in prognosis of patients with NSCLC was detected. Read More

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MiR-200a-3p Aggravates DOX-Induced Cardiotoxicity by Targeting PEG3 Through SIRT1/NF-κB Signal Pathway.

Cardiovasc Toxicol 2021 Apr 27;21(4):302-313. Epub 2021 Feb 27.

Department of Cardiovasology, Hunan Provincial People's Hospital, Changsha, Hunan, 410000, People's Republic of China.

Doxorubicin (DOX) is a widely used cytotoxic drug whose application is limited by its severe side effects. Little was known regarding how to offset its side effects. Therefore this study aims to explore the role of miR-200a-3p in DOX-induced cardiotoxicity and its possible mechanism. Read More

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Resveratrol and its Nanoparticle suppress Doxorubicin/Docetaxel-resistant anaplastic Thyroid Cancer Cells and .

Nanotheranostics 2021 1;5(2):143-154. Epub 2021 Jan 1.

South China University of Technology School of Medicine, Guangzhou 510006, P.R. China.

Docetaxel and doxorubicin combination has been widely used in anaplastic thyroid cancer/ATC treatment but often results in serious adverse effects and drug resistance. Resveratrol effectively inhibits ATC cell proliferation without affecting the corresponding normal cells, while its anti-ATC effects especially on the ones with docetaxel/doxorubicin-resistance have not been reported due to its low bioavailability. Nanoparticles with sustained-release and cancer-targeting features may overcome this therapeutic bottleneck. Read More

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January 2021

Functional Hybrid Molecules for the Visualization of Cancer: PESIN-Homodimers Combined with Multimodal Molecular Imaging Probes for Positron Emission Tomography and Optical Imaging: Suited for Tracking of GRPR-Positive Malignant Tissue*.

Chemistry 2020 Dec 28;26(69):16349-16356. Epub 2020 Oct 28.

Biomedical Chemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, Theodor-Kutzer-Ufer 1-3, 68167, Mannheim, Germany.

We describe multimodal imaging probes for gastrin-releasing peptide receptor (GRPR)-specific targeting suited for positron emission tomography and optical imaging (PET/OI), consisting of PESIN (PEG -BBN ) dimers connected to multimodal imaging subunits. These multimodal agents comprise a fluorescent dye for OI and the chelator ((1,4,7-triazacyclononane-4,7-diyl)diacetic acid-1-glutaric acid) (NODA-GA) for PET radiometal isotope labelling. Special focus was put on the influence of the used dyes on the properties of the whole bioconjugates. Read More

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December 2020

Novel multifunctional F-labelled PET tracer with prostate-specific membrane antigen-targeting and hypoxia-sensitive moieties.

Eur J Med Chem 2020 Mar 25;189:112099. Epub 2020 Jan 25.

Department of Nuclear Medicine, Molecular Imaging & Therapeutic Medicine Research Center, Biomedical Research Institute, Jeonbuk National University Medical School and Hospital, Jeonju, 54907, Republic of Korea; Research Institute of Clinical Medicine of Jeonbuk National University-Biomedical Research Institute of Jeonbuk National University Hospital, Jeonju, 54907, Republic of Korea. Electronic address:

Prostate cancer is one of the most frequently found cancers in men worldwide. Prostate-specific membrane antigen (PSMA) is typically highly expressed in prostate cancer, and the Glu-Urea-Lys (GUL) structure has recently received considerable attention as a key unit of PSMA-targeting agents. Additionally, one of the common characteristics of many solid tumors, such as prostate cancer, is hypoxia. Read More

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Targeting Phosphatidylethanolamine with Fluorine-18 Labeled Small Molecule Probe for Apoptosis Imaging.

Mol Imaging Biol 2020 08;22(4):914-923

Department of Nuclear Medicine and Medical Imaging, the First Affiliated Hospital, Sun Yat-sen University, Guangzhou, 510080, China.

Purpose: Externalization of phosphatidylethanolamine (PE) in dying cells makes the phospholipid an attractive target for apoptosis imaging. However, no ideal PE-targeted positron emission tomography (PET) radiotracer was developed. The goal of the study was to develop a novel PE-targeted radiopharmaceutical to imaging apoptosis. Read More

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Peptide-based targeted polymeric nanoparticles for siRNA delivery.

Nanotechnology 2019 Oct 11;30(41):415604. Epub 2019 Jul 11.

School of Chemistry and Molecular Biosciences, The University of Queensland, Brisbane, St. Lucia, QLD 4072, Australia. Department of Pharmaceutical Sciences and Center for Pharmaceutical Biotechnology and Nanomedicine, Northeastern University, 140 The Fenway, Boston, MA 02115, United States of America.

The development of polymer-based nanoparticulate delivery systems for siRNA is important for the clinical success of gene therapy. However, there are some major drawbacks that need to be overcome. Short interfering RNA (siRNA) has been investigated as a potential therapeutic drug to silence disease-associated genes, but its usage is limited due to the lack of effective and safe nanocarriers. Read More

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October 2019

Trans-allelic mutational effects at the Peg3 imprinted locus.

PLoS One 2018 18;13(10):e0206112. Epub 2018 Oct 18.

Department of Biological Sciences, Louisiana State University, Baton Rouge, LA, United States of America.

How one allele interacts with the other for the function of a gene is not well understood. In this study, we tested potential allelic interaction at the Peg3 imprinted locus with several mutant alleles targeting an Imprinting Control Region, the Peg3-DMR. According to the results, maternal deletion of the Peg3-DMR resulted in 2-fold up-regulation of two paternally expressed genes, Peg3 and Usp29. Read More

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Mitochondria-targeting BODIPY-loaded micelles as novel class of photosensitizer for photodynamic therapy.

Eur J Med Chem 2018 Sep 14;157:599-609. Epub 2018 Aug 14.

Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201301, China. Electronic address:

In this paper, a series of novel BODIPY-based photosensitizers have been designed and synthesized for photodynamic therapy. BODIPY3 was screened out as the most potential photosensitizer due to its excellent optical properties, high singlet oxygen efficiency and good photostability. However, as an organic photosensitizer, BODIPY3 still suffered from the drawbacks of insolubility and instability in aqueous system. Read More

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September 2018

Novel Cu Labeled RGD-BBN Heterotrimers for PET Imaging of Prostate Cancer.

Bioconjug Chem 2018 05 13;29(5):1595-1604. Epub 2018 Apr 13.

Molecular Imaging Program at Stanford (MIPS), Department of Radiology and Bio-X Program , Stanford University , Stanford , California 94305-5344 , United States.

Bombesin receptor 2 (BB) and integrin αβ receptor are privileged targets for molecular imaging of cancer because of their overexpression in a number of tumor tissues. The most recent developments in heterodimer-based radiopharmaceuticals concern BB- and integrin αβ-targeting compounds, consisting of bombesin (BBN) and cyclic arginine-glycine-aspartic acid peptides (RGD), connected through short length linkers. Molecular imaging probes based on RGD-BBN heterodimer design exhibit improved tumor targeting efficacy compared to the single-receptor targeting peptide monomers. Read More

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Positron Emission Tomography Imaging of Prostate Cancer with Ga-68-Labeled Gastrin-Releasing Peptide Receptor Agonist BBN and Antagonist RM26.

Bioconjug Chem 2018 02 9;29(2):410-419. Epub 2018 Jan 9.

Laboratory of Molecular Imaging and Nanomedicine, National Institute of Biomedical Imaging and Bioengineering (NIBIB), National Institutes of Health (NIH) , Bethesda, Maryland 20892, United States.

Radiolabeled bombesin (BBN) analogs have long been used for developing gastrin-releasing peptide receptor (GRPR) targeted imaging probes, and tracers with excellent in vivo performance including high tumor uptake, high contrast, and favorable pharmacokinetics are highly desired. In this study, we compared the Ga-labeled GRPR agonist (Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH, BBN) and antagonist (d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH, RM26) for the positron emission tomography (PET) imaging of prostate cancer. The in vitro stabilities, receptor binding, cell uptake, internalization, and efflux properties of the probes Ga-1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-Aca-BBN and Ga-NOTA-poly(ethylene glycol) (PEG)-RM26 were studied in PC-3 cells, and the in vivo GRPR targeting abilities and kinetics were investigated using PC-3 tumor xenografted mice. Read More

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February 2018

A dual-mediated liposomal drug delivery system targeting the brain: rational construction, integrity evaluation across the blood-brain barrier, and the transporting mechanism to glioma cells.

Int J Nanomedicine 2017 28;12:2407-2425. Epub 2017 Mar 28.

Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, Department of Pharmaceutics, School of Pharmaceutical Sciences.

As the global population ages, cancer rates increase worldwide, and degenerative diseases of the central nervous system (CNS), brain tumors, and inflammation threaten human health more frequently. We designed a dual-mediated (receptor-mediated and adsorption-mediated) liposome, named transferrin-cell penetrating peptide-sterically stabilized liposome (TF-CPP-SSL), to improve therapy for gliomas through combining molecular recognition of transferrin receptors (TF-Rs) on the blood-brain barrier (BBB) and glioma cells with the internalization and lysosomal escaping ability of CPP. Based on the systematic investigation of structure-activity relations on the cellular level, we constructed TF-CPP-SSL rationally by conjugating TF and CPP moieties to the liposomes via PEG and PEG, respectively, and found the optimum densities of TF and CPP were 1. Read More

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Improved positron emission tomography imaging of glioblastoma cancer using novel Ga-labeled peptides targeting the urokinase-type plasminogen activator receptor (uPAR).

Amino Acids 2017 06 18;49(6):1089-1100. Epub 2017 Mar 18.

Department of Radiology, School of Medicine, Stanford University, 1201 Welch Road, Lucas Center, P095, Mail Code 5484, Stanford, CA, 94305, USA.

The urokinase-type plasminogen activator receptor (uPAR) is overexpressed in several cancers including glioblastoma (GBM) and is an established biomarker for metastatic potential. The uPAR-targeting peptide AE105-NH (Ac-Asp-Cha-Phe-(D)Ser-(D)Arg-Tyr-Leu-Trp-Ser-CONH) is a promising candidate for non-invasive positron emission tomography (PET) imaging of uPAR. Despite the optimal physical properties of Ga for peptide-based PET imaging, low tumor uptakes have previously been reported using Ga-labeled AE105-NH-based tracers. Read More

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Re-programming pullulan for targeting and controlled release of doxorubicin to the hepatocellular carcinoma cells.

Eur J Pharm Sci 2017 May 10;103:104-115. Epub 2017 Feb 10.

Department of Pharmaceutical & Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy. Electronic address:

A novel bioconjugate for hepatocellular carcinoma (HCC) targeting was obtained by pullulan re-programming, which involves the backbone oxidation and conjugation of targeting peptide and doxorubicin (Doxo) through a releasable linker. Preliminary in vivo studies showed that the oxidation of 40 glucopyranose units (GPU) out of 100 remarkably reduced the pullulan unspecific liver tropism. This oxidized polymer was functionalized with PreS1 to selectively target the HCC and with rhodamine (Rhod) as label to perform in vitro cell up-take investigations. Read More

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Transcriptional Truncation of the Long Coding Imprinted Gene Usp29.

PLoS One 2016 21;11(6):e0158004. Epub 2016 Jun 21.

Department of Biological Sciences, Louisiana State University, Baton Rouge, LA 70803, United States of America.

Usp29 (Ubiquitin-specific protease 29) is a paternally expressed gene located upstream of another imprinted gene Peg3. In the current study, the transcription of this long coding gene spanning a 250-kb genomic distance was truncated using a knockin allele. According to the results, paternal transmission of the mutant allele resulted in reduced body and litter sizes whereas the maternal transmission caused no obvious effects. Read More

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AMD3100: A Versatile Platform for CXCR4 Targeting (68)Ga-Based Radiopharmaceuticals.

Bioconjug Chem 2016 Mar 3;27(3):752-61. Epub 2016 Mar 3.

Institut de Chimie Moléculaire de l'Université de Bourgogne, UMR6302, CNRS, Université Bourgogne Franche-Comté , F-21000 Dijon, France.

CXCR4 is a G protein-coupled receptor (GPCR), which is overexpressed in numerous diseases, particularly in multiple cancers. Therefore, this receptor represents a valuable target for imaging and therapeutic purposes. Among the different approaches, which were developed for CXCR4 imaging, a CXCR4 antagonist biscyclam system (AMD3100, also called Mozobil), currently used in the clinic for the mobilization of hematopoietic stem cells, was radiolabeled with different radiometals such as (62)Zn, (64)Cu, (67)Ga, or (99m)Tc. Read More

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Trim28 Haploinsufficiency Triggers Bi-stable Epigenetic Obesity.

Cell 2016 Jan;164(3):353-64

Max Planck Institute of Immunobiology and Epigenetics, Stübeweg 51, 79108 Freiburg, Germany. Electronic address:

More than one-half billion people are obese, and despite progress in genetic research, much of the heritability of obesity remains enigmatic. Here, we identify a Trim28-dependent network capable of triggering obesity in a non-Mendelian, "on/off" manner. Trim28(+/D9) mutant mice exhibit a bi-modal body-weight distribution, with isogenic animals randomly emerging as either normal or obese and few intermediates. Read More

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January 2016

Dual Functions of the RFTS Domain of Dnmt1 in Replication-Coupled DNA Methylation and in Protection of the Genome from Aberrant Methylation.

PLoS One 2015 18;10(9):e0137509. Epub 2015 Sep 18.

Laboratory of Epigenetics, Institute for Protein Research, Osaka University, Yamadaoka, Suita, Osaka, 565-0871, Japan.

In mammals, DNA methylation plays important roles in embryogenesis and terminal differentiation via regulation of the transcription-competent chromatin state. The methylation patterns are propagated to the next generation during replication by maintenance DNA methyltransferase, Dnmt1, in co-operation with Uhrf1. In the N-terminal regulatory region, Dnmt1 contains proliferating cell nuclear antigen (PCNA)-binding and replication foci targeting sequence (RFTS) domains, which are thought to contribute to maintenance methylation during replication. Read More

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Development and Preliminary Evaluation of TFIB, a New Bimodal Prosthetic Group for Bioactive Molecule Labeling.

ACS Med Chem Lett 2015 Feb 24;6(2):168-72. Epub 2014 Nov 24.

Clermont Université, Université d'Auvergne , Laboratoire d'Imagerie Moléculaire et Thérapie Vectorisée, BP 10448, F-63000 Clermont-Ferrand, France ; INSERM , U990, F-63005 Clermont-Ferrand, France ; Centre Jean Perrin , F-63011 Clermont-Ferrand, France.

The new readily available prosthetic group, tetrafluorophenyl 4-fluoro-3-iodobenzoate (TFIB), designed for both molecular imaging and targeted radionuclide therapy purposes was radiolabeled either with fluorine or iodine radionuclides with excellent radiochemical yields and purities. These radiolabeled tags were conjugated to N,N-diethylethylenediamine to give melanin-targeting radiotracers [ (125) I]9 and [ (18) F]9, which were successfully evaluated by PET and gamma scintigraphic imaging in B16F0 pigmented melanoma-bearing C57BL/6J mice. Then, radiolabeled [ (125) I]/[ (18) F]TFIB was used to tag tumor-targeting peptides (i. Read More

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February 2015

Divalent folate modification on PEG: an effective strategy for improving the cellular uptake and targetability of PEGylated polyamidoamine-polyethylenimine copolymer.

Mol Pharm 2015 Jan 16;12(1):240-52. Epub 2014 Dec 16.

Department of Pharmaceutical Science, Nanfang Hospital, Southern Medical University , Guangzhou 510515, P. R. China.

The stability and targeting ability of nanocarrier gene delivery systems are necessary conditions to ensure the good therapeutic effect and low nonspecific toxicity of cancer treatment. Poly(ethylene glycol) (PEG) has been widely applied for improving stability and as a spacer for linking ligands and nanocarriers to improve targetability. However, the cellular uptake and endosomal escape capacity of nanocarriers has been seriously harmed due to the introduction of PEG. Read More

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January 2015

Paternally expressed Peg3 controls maternally expressed Zim1 as a trans factor.

PLoS One 2014 29;9(9):e108596. Epub 2014 Sep 29.

Department of Biological Sciences, Louisiana State University, Baton Rouge, LA, United States of America.

The expression of two adjacent imprinted genes, Peg3 and Zim1, is inversely correlated: down-regulation of Peg3 coinciding with up-regulation of Zim1. The current study characterized this inverse correlation using a mutant allele targeting Peg3. According to the results, the mutation on the paternal allele of Peg3 resulted in a dramatic increase in the transcription levels of the maternal allele of Zim1, suggesting the involvement of unknown trans factors in this trans-allelic event. Read More

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November 2015

The effect of mini-PEG-based spacer length on binding and pharmacokinetic properties of a 68Ga-labeled NOTA-conjugated antagonistic analog of bombesin.

Molecules 2014 Jul 17;19(7):10455-72. Epub 2014 Jul 17.

Preclinical PET Platform, Department of Medicinal Chemistry, Faculty of Pharmacy, Uppsala University, Uppsala SE-751 23, Sweden.

The overexpression of gastrin-releasing peptide receptor (GRPR) in cancer can be used for peptide-receptor mediated radionuclide imaging and therapy. We have previously shown that an antagonist analog of bombesin RM26 conjugated to 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) via a diethyleneglycol (PEG2) spacer (NOTA-PEG2-RM26) and labeled with 68Ga can be used for imaging of GRPR-expressing tumors. In this study, we evaluated if a variation of mini-PEG spacer length can be used for optimization of targeting properties of the NOTA-conjugated RM26. Read More

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Metabolic exploitation of the sialic acid biosynthetic pathway to generate site-specifically labeled antibodies.

Glycobiology 2014 Jan 22;24(1):62-9. Epub 2013 Oct 22.

Department of Surgery, University of California Los Angeles.

Lack of a universal site-specific conjugation methodology for antibodies limits their potential to be developed as tumor-specific imaging agents or targeted therapeutics. A potential mechanism for site-specific conjugation involves utilization of the conserved N-glycosylation site in the CH2 domain. We sought to develop an antibody with an altered azido-sugar at this site whereby site-specific label could be added. Read More

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January 2014

2-Fluoropyridine prosthetic compounds for the 18F labeling of bombesin analogues.

Bioorg Med Chem Lett 2013 Jul 30;23(13):3920-6. Epub 2013 Apr 30.

TRIUMF, Nuclear Medicine Division, 4004 Wesbrook Mall, Vancouver, Canada BC V6T 2A3.

Acetylene-bearing 2-[(18)F]fluoropyridines [(18)F]FPy5yne and PEG-[(18)F]FPyKYNE were prepared via efficient nucleophilic heteroaromatic [(18)F]fluorination of their corresponding 2-trimethylammoniumpyrdinyl precursors. The prosthetic groups were conjugated to azide- and PEG3-modified bombesin(6-14) analogues via copper-catalyzed azide-alkyne cycloaddition couplings to yield mono- and di-mini-PEGylated ligands for PET imaging of the gastrin- releasing peptide receptor. The PEG3- and PEG2/PEG3-bearing (18)F peptides showed decreased lipophilicity relative to an analogous non-mini-PEGylated (18)F peptide. Read More

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Development of highly potent protease-activated receptor 2 agonists via synthetic lipid tethering.

FASEB J 2013 Apr 4;27(4):1498-510. Epub 2013 Jan 4.

Department of Physiology, Arizona Health Sciences Center, Tucson, AZ 85724-5030, USA.

Protease-activated receptor-2 (PAR₂) is a G-protein coupled receptor (GPCR) associated with a variety of pathologies. However, the therapeutic potential of PAR₂ is limited by a lack of potent and specific ligands. Following proteolytic cleavage, PAR₂ is activated through a tethered ligand. Read More

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Quantitative analysis and parametric imaging of 18F-labeled monomeric and dimeric RGD peptides using compartment model.

Mol Imaging Biol 2012 Dec;14(6):743-52

Department of Biomedical Engineering, Huazhong University of Science and Technology, 505 Bldg. D11, 1037 Luoyu Rd., Wuhan, Hubei, China 430074.

Purpose: Non-invasive PET imaging with radiolabeled RGD peptides for α(v)β(3) integrin targeting has become an important tool for tumor diagnosis and treatment monitoring in both pre-clinical and clinical studies. To better understand the molecular process and tracer pharmacokinetics, we introduced kinetic modeling in the investigation of (18)F-labeled RGD peptide monomer (18)F-FP-c(RGDyK) (denoted as (18)F-FPRGD) and dimer (18)F-FP-PEG3-E[c(RGDyK)](2) (denoted as (18)F-FPPRGD2).

Procedures: MDA-MB-435 tumor-bearing mice underwent 60 min dynamic PET scans following the injection of either (18)F-FPRGD or (18)F-FPPRGD2. Read More

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December 2012

The transcription factor ATF4 promotes skeletal myofiber atrophy during fasting.

Mol Endocrinol 2010 Apr 2;24(4):790-9. Epub 2010 Mar 2.

Department of Internal Medicine, Roy J. and Lucille A. Carver College of Medicine, The University of Iowa, Iowa City, Iowa 52242, USA.

Prolonged fasting alters skeletal muscle gene expression in a manner that promotes myofiber atrophy, but the underlying mechanisms are not fully understood. Here, we examined the potential role of activating transcription factor 4 (ATF4), a transcription factor with an evolutionarily ancient role in the cellular response to starvation. In mouse skeletal muscle, fasting increases the level of ATF4 mRNA. Read More

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Preparation, characterization and pharmacokinetics of folate receptor-targeted liposomes for docetaxel delivery.

J Nanosci Nanotechnol 2009 Mar;9(3):2155-61

Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.

A novel liposomal formulation of docetaxel targeting the folate receptor (FR) was synthesized and characterized. Liposomal formulations are less toxic and can provide longer systemic circulation time than the Tween 80 and ethanol based clinical formulation of docetaxel. Folate receptor-alpha (FR) is frequently over-expressed on epithelial cancer cells. Read More

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