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https://www.readbyqxmd.com/read/28095746/targeting-of-herbal-bioactives-through-folate-receptors-a-novel-concept-to-enhance-intracellular-drug-delivery-in-cancer-therapy
#1
Anshita Gupta, Chanchal Deep Kaur, Shailendra Saraf, Swarnlata Saraf
Targeted drug delivery through folate receptor (FR) has emerged as a most biocompatible, target oriented, and non-immunogenic cargoes for the delivery of anticancer drugs. FRs are highly overexpressed in many tumor cells (like ovarian, lung, breast, kidney, brain, endometrial, and colon cancer), and targeting them through conjugates bearing specific ligand with encapsulated nanodrug moiety is undoubtedly, a promising approach toward tumor targeting. Folate, being an endogenous ligand, can be exploited well to affect various cellular events occurring during the progress of tumor, in a more natural and definite way...
January 17, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/28094532/preclinical-comparison-of-albumin-binding-radiofolates-impact-of-linker-entities-on-the-in-vitro-and-in-vivo-properties
#2
Klaudia Siwowska, Stephanie Haller, Francesca Bortoli, Martina Benešová, Viola Groehn, Peter Bernhardt, Roger Schibli, Cristina Müller
Tumor targeting with folic acid radioconjugates has been proposed as a promising strategy for radionuclide therapy of folate receptor α (FR)-positive cancer. Recently, it was shown that modification of radiofolates with an albumin-binding entity increased the tumor-to-kidney ratios of accumulated radioactivity in mice. The goal of this study was to evaluate the lead compound cm10 and compare it with new albumin-binding folate conjugates. Compound cm12 was designed with a long spacer consisting of a PEG-11 entity, and compound cm13 contained a short alkane chain between the albumin-binding moiety and folic acid...
January 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28089786/3-carboxyphenylboronic-acid-modified-carboxymethyl-chitosan-nanoparticles-for-improved-tumor-targeting-and-inhibitory
#3
Xin Wang, Bing Wei, Xu Cheng, Jun Wang, Rupei Tang
Carboxymethyl chitosan-based nanoparticles (CM NPs) were prepared, and were further modified with a tumor-homing ligand (3-carboxyphenylboronic acid, 3-CPBA) to give tumor-targeting nanoparticles (CB NPs). Particle sizes were measured by dynamic light scattering, while the morphology was observed via transmission electron microscopy and scanning electronic microscope. The results show that CM and CB NPs are spherical-like, and kinetically stable in various conditions. Doxorubicin (DOX) as a model drug was successfully encapsulated to give CM-DOX and CB-DOX NPs...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088584/proton-pump-inhibition-and-cancer-therapeutics-a-specific-tumor-targeting-or-it-is-a-phenomenon-secondary-to-a-systemic-buffering
#4
REVIEW
Enrico Spugnini, Stefano Fais
One of the unsolved mysteries in oncology includes the strategies that cancer cells adopt to cope with an adverse microenvironment. However, we knew, from the Warburg's discovery that through their metabolism based on sugar fermentation, cancer cells acidify their microenvironment and this progressive acidification induces a selective pressure, leading to the development of very malignant cells entirely armed to survive in the hostile microenvironment generated by their own metabolism. In the last decades a primordial role for proton exchangers has been supported as a key tumor advantage in facing off the acidic milieu...
January 11, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28080053/lipid-drug-conjugate-for-enhancing-drug-delivery
#5
Danielle Irby, Chengan Du, Feng Li
Lipid-drug conjugates (LDCs) are drug molecules that have been covalently modified with lipids. The conjugation of lipids to drug molecules increases lipophilicity and also changes other properties of drugs. The conjugates demonstrate several advantages including improved oral bioavailability, improved targeting to the lymphatic system, enhanced tumor targeting, and reduced toxicity. Based on the chemical nature of drugs and lipids, various conjugation strategies and chemical linkers can be utilized to synthesize LDCs...
January 12, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28078380/imaging-features-of-hepatic-sarcomatous-carcinoma-on-computed-tomography-and-gadoxetic-acid-enhanced-magnetic-resonance-imaging
#6
Kyo-Won Gu, Young Kon Kim, Ji Hye Min, Sang Yun Ha, Woo Kyoung Jeong
PURPOSE: To determine the imaging features of hepatic sarcomatous carcinoma including sarcomatous intrahepatic cholangiocarcinoma (S-ICC) and sarcomatous hepatocellular carcinoma (S-HCC) on computed tomography (CT) and gadoxetic acid-enhanced magnetic resonance imaging (MRI). MATERIALS AND METHODS: Twenty-four patients with pathologically confirmed S-ICCs (n = 13), S-HCCs (n = 7), sarcomatous carcinoma (n = 2), carcinosarcoma (n = 1), and sarcomatous combined HCC-CC (n = 1) (size range 2...
January 12, 2017: Abdominal Radiology
https://www.readbyqxmd.com/read/28075466/co-delivery-of-doxorubicin-and-ph-sensitive-curcumin-prodrug-by-transferrin-targeted-nanoparticles-for-breast-cancer-treatment
#7
Tongxing Cui, Sihao Zhang, Hong Sun
The natural product curcumin and the chemotherapeutic agent doxorubicin have been used in the treatment of many cancers, including breast cancer. However, fast clearance and unspecific distribution in the body after intravenous injection are still challenges to be overcome by an ideal nano-sized drug delivery system in cancer treatment. In this study we design transferrin (Tf) decorated nanoparticles (NPs) to co-deliver CUR and DOX for breast cancer treatment. A pH-sensitive prodrug, transferrin-poly(ethylene glycol)-curcumin (Tf-PEG-CUR), was synthesized and used for the self‑assembling of NPs (Tf-PEG-CUR NPs)...
February 2017: Oncology Reports
https://www.readbyqxmd.com/read/28067257/enhanced-tumor-targeting-selectivity-by-modulating-bispecific-antibody-binding-affinity-and-format-valence
#8
Yariv Mazor, Kris F Sachsenmeier, Chunning Yang, Anna Hansen, Jessica Filderman, Kathy Mulgrew, Herren Wu, William F Dall'Acqua
Bispecific antibodies are considered attractive bio-therapeutic agents owing to their ability to target two distinct disease mediators. Cross-arm avidity targeting of antigen double-positive cancer cells over single-positive normal tissue is believed to enhance the therapeutic efficacy, restrict major escape mechanisms and increase tumor-targeting selectivity, leading to reduced systemic toxicity and improved therapeutic index. However, the interplay of factors regulating target selectivity is not well understood and often overlooked when developing clinically relevant bispecific therapeutics...
January 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28065935/two-birds-one-stone-dual-targeting-of-the-cancer-cell-surface-and-subcellular-mitochondria-by-the-galectin-3-binding-peptide-g3-c12
#9
Wei Sun, Lian Li, Qing-Qing Yang, Zhi-Rong Zhang, Yuan Huang
Active tumor-targeting approaches using specific ligands have drawn considerable attention over the years. However, a single ligand often fails to simultaneously target the cancer cell surface and subcellular organelles, which limits the maximum therapeutic efficacy of delivered drugs. We describe a polymeric delivery system modified with the G3-C12 peptide for sequential dual targeting. In this study, galectin-3-targeted G3-C12 peptide was conjugated onto the N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer for the delivery of D(KLAKLAK)2 (KLA) peptide...
January 9, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28064499/poly-glycerol-used-for-constructing-mixed-polymeric-micelles-as-t1-mri-contrast-agent-for-tumor-targeted-imaging
#10
Yi Cao, Min Liu, Kunchi Zhang, Guangyue Zu, Ye Kuang, Xiaoyan Tong, Dangsheng Xiong, Renjun Pei
There was much interest in the development of nanoscale delivery vehicles based on polymeric micelles to realize the diagnostic and therapeutic applications in biomedicine. Here, with the purpose of constructing a micellar magnetic resonance imaging (MRI) contrast agent (CA) with well biocompatibility and targeting specificity, two types of amphiphilic diblock polymers, mPEG-PG(DOTA(Gd))-b-PCL and FA-PEG-b-PCL, were synthesized to form mixed micelles by coassembly. The nanostructure of the resulting micellar system consisted of poly(caprolactone) (PCL) as core and poly(glycerol) (PG) and poly(ethylene glycol) (PEG) as shell, simultaneously modified with DOTA(Gd) chelates and folic acid (FA), which afforded functions of MRI contrast enhancement and tumor targeting...
January 9, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28063352/a-tumor-targeted-activatable-phthalocyanine-tetrapeptide-doxorubicin-conjugate-for-synergistic-chemo-photodynamic-therapy
#11
Mei-Rong Ke, Shao-Fang Chen, Xiao-Hui Peng, Qiao-Feng Zheng, Bi-Yuan Zheng, Chih-Kuang Yeh, Jian-Dong Huang
Chemo-photodynamic therapy is a promising strategy for cancer treatments. However, it remains a challenge to develop a chemo-photodynamic therapeutic agent with little side effect, high tumor-targeting, and efficient synergistic effect simultaneously. Herein, we report a zinc(II) phthalocyanine (ZnPc)-doxorubicin (DOX) prodrug linked with a fibroblast activation protein (FAP)-responsive short peptide with the sequence of Thr-Ser-Gly-Pro for chemo-photodynamic therapy. In the conjugate, both photosensitizing activity of ZnPc and cytotoxicity of DOX are inhibited obviously...
December 29, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28062698/monoclonal-antibodies-against-epidermal-growth-factor-receptor-acquire-an-ability-to-kill-tumor-cells-through-complement-activation-by-mutations-that-selectively-facilitate-the-hexamerization-of-igg-on-opsonized-cells
#12
Annalina Tammen, Stefanie Derer, Ralf Schwanbeck, Thies Rösner, Anna Kretschmer, Frank J Beurskens, Janine Schuurman, Paul W H I Parren, Thomas Valerius
Triggering of the complement cascade induces tumor cell lysis via complement-dependent cytotoxicity (CDC) and attracts and activates cytotoxic cells. It therefore represents an attractive mechanism for mAb in cancer immunotherapy development. The classical complement pathway is initiated by IgG molecules that have assembled into ordered hexamers after binding their Ag on the tumor cell surface. The requirements for CDC are further impacted by factors such as Ab epitope, valency, and affinity. Thus, mAb against well-validated solid tumor targets, such as the epidermal growth factor receptor (EGFR) that effectively induces complement activation and CDC, are highly sought after...
January 6, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28060891/performance-of-89zr-labeled-rituximab-pet-as-an-imaging-biomarker-to-assess-cd20-targeting-a-pilot-study-in-patients-with-relapsed-refractory-diffuse-large-b-cell-lymphoma
#13
Yvonne W S Jauw, Josée M Zijlstra, Daphne de Jong, Danielle J Vugts, Sonja Zweegman, Otto S Hoekstra, Guus A M S van Dongen, Marc C Huisman
PURPOSE: Treatment of patients with diffuse large B cell lymphoma (DLBCL) includes rituximab, an anti-CD20 monoclonal antibody (mAb). Insufficient tumor targeting might cause therapy failure. Tumor uptake of 89Zirconium (89Zr)-mAb is a potential imaging biomarker for tumor targeting, since it depends on target antigen expression and accessibility. The aim of this pilot study was to describe the performance of 89Zr-labeled-rituximab-PET to assess CD20 targeting in patients with relapsed/refractory DLBCL...
2017: PloS One
https://www.readbyqxmd.com/read/28058834/ph-dependent-transmembrane-activity-of-peptide-functionalized-gold-nanostars-for-computed-tomography-photoacoustic-imaging-and-photothermal-therapy
#14
Ying Tian, Yunlei Zhang, Zhaogang Teng, Wei Tian, Song Luo, Xiang Kong, Xiaodan Su, Yuxia Tang, Shouju Wang, Guangming Lu
Progress in multifunctional nanomaterials for tumor therapy mostly depends on the development of tumor-targeting delivery strategies. One approach is to explore a pH-responsive strategy to target the slightly acidic solid tumor microenvironment. A novel class of pH (low) insertion peptides (pHLIPs) with pH-dependent transmembrane activity can fold and rapidly insert into the lipid bilayer of tumor cells triggered by acidity, facilitating the cellular internalization of nanomaterials synchronously. Here, we innovatively decorated gold nanostars (GNSs) with pHLIPs (GNS-pHLIP) to improve their targeting ability and photothermal therapeutic (PTT) efficiency...
January 6, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28057464/graphene-quantum-dots-for-cancer-targeted-drug-delivery
#15
Daniela Iannazzo, Alessandro Pistone, Marina Salamò, Signorino Galvagno, Roberto Romeo, Salvatore V Giofré, Caterina Branca, Giuseppa Visalli, Angela Di Pietro
A biocompatible and cell traceable drug delivery system Graphene Quantum Dots (GQD) based, for the targeted delivery of the DNA intercalating drug doxorubicin (DOX) to cancer cells, is here reported. Highly dispersible and water soluble GQD, synthesized by acidic oxidation and exfoliation of multi-walled carbon nanotubes (MWCNT), were covalently linked to the tumor targeting module biotin (BTN), able to efficiently recognize biotin receptors over-expressed on cancer cells and loaded with DOX. Biological test performed on A549 cells reported a very low toxicity of the synthesized carrier (GQD and GQD-BTN)...
January 2, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28051996/full-preclinical-validation-of-the-123i-labeled-anti-psma-antibody-fragment-scfvd2b-for-prostate-cancer-imaging
#16
Barbara Frigerio, Gerben Franssen, Elena Luison, Alessandro Satta, Ettore Seregni, Marco Colombatti, Giulio Fracasso, Riccardo Valdagni, Delia Mezzanzanica, Otto Boerman, Silvana Canevari, Mariangela Figini
PURPOSE: In the context of prostate cancer (PCa) imaging, the aim of this study was to optimize (in vitro) the specificity and assess preclinically (in vivo) the tumor targeting properties of the 123I-scFvD2B antibody specific for prostate-specific membrane antigen (PSMA). EXPERIMENTAL DESIGN: The 123I-labeling conditions of the antibody fragment scFvD2B, produced in an eukaryotic system under GMP-compliant conditions, were optimized and assessed for purity and immunoreactivity...
December 30, 2016: Oncotarget
https://www.readbyqxmd.com/read/28050231/treatment-of-patients-with-refractory-metastatic-cancer-according-to-molecular-profiling-on-tumor-tissue-in-the-clinical-routine-an-interim-analysis-of-the-onco-t-profile-project
#17
Andreas Seeber, Guenther Gastl, Christian Ensinger, Gilbert Spizzo, Wolfgang Willenbacher, Florian Kocher, Christoph Leitner, Ella Willenbacher, Arno Amann, Normann Steiner, Wolfgang Eisterer, Andreas Voss, Kenneth Russell, Heinz Zwierzina
INTRODUCTION: Patients with refractory metastatic cancer have been shown to benefit from molecular profiling of tumor tissue. The ONCO-T-PROFILE project was launched in March 2014 at the Innsbruck Medical University. Within 2 years our project aims to recruit 110 patients with stage IV cancer refractory to standard therapy. Our data presented here are based on an interim-analysis. METHODS: Tumor tissue specimens were submitted for molecular profiling to the certified laboratory (Caris Life Science, USA)...
September 2016: Genes & Cancer
https://www.readbyqxmd.com/read/28048809/mo-d-brc-01-memorial-lecture
#18
B Fraass
Treatment planning is a central part of radiation therapy, including delineation in tumor volumes and critical organs, setting treatment goals of prescription doses to the tumor targets and tolerance doses to the critical organs, and finally generation of treatment plans to meet the treatment goals. National groups like RTOG have led the effort to standardize treatment goals of the prescription doses to the tumor targets and tolerance doses to the critical organs based on accumulated knowledge from decades of abundant clinical trial experience...
June 2016: Medical Physics
https://www.readbyqxmd.com/read/28048786/mo-d-brc-04-multiple-criteria-optimization-planning
#19
J Donaghue
Treatment planning is a central part of radiation therapy, including delineation in tumor volumes and critical organs, setting treatment goals of prescription doses to the tumor targets and tolerance doses to the critical organs, and finally generation of treatment plans to meet the treatment goals. National groups like RTOG have led the effort to standardize treatment goals of the prescription doses to the tumor targets and tolerance doses to the critical organs based on accumulated knowledge from decades of abundant clinical trial experience...
June 2016: Medical Physics
https://www.readbyqxmd.com/read/28048586/th-ab-206-00-challenges-and-opportunities-for-nuclear-medicine-theranostics
#20
Osama Mawlawi
In the past few decades, the field of nuclear medicine has made long strides with the continued advancement of related sciences and engineering and the availability of diagnostic and therapeutic radionuclides. Leveraging these advancements while combining the advantages of therapeutic and diagnostic radionuclides into one radiopharmaceutical has also created a new subfield "theranostics" in nuclear medicine that has the potential to further propel the field into the future. This session is composed of two talks; one focused on the physics principles of theranostics from properties of beta and alpha emitting radionuclides to dosimetric models and quantification; while the second describes preclinical and clinical applications of theranostics and discusses the challenges and opportunities of bringing them to the clinic...
June 2016: Medical Physics
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