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https://www.readbyqxmd.com/read/29332233/pilot-study-of-serial-flt-and-fdg-pet-ct-imaging-to-monitor-response-to-neoadjuvant-chemoradiotherapy-of-esophageal-adenocarcinoma-correlation-with-histopathologic-response
#1
Victor H Gerbaudo, Joseph H Killoran, Chun K Kim, Jason L Hornick, Jonathan A Nowak, Peter C Enzinger, Harvey J Mamon
OBJECTIVE: The aim of this prospective pilot study was to investigate the potential of serial FLT-PET/CT compared to FDG-PET/CT to provide an early indication of esophageal cancer response to concurrent neoadjuvant chemoradiation therapy. METHODS: Five patients with biopsy-proven esophageal adenocarcinomas underwent neoadjuvant chemoradiation (Tx) prior to minimally invasive esophagectomy. The presence of residual tumor was classified histologically using the Mandard et al...
January 13, 2018: Annals of Nuclear Medicine
https://www.readbyqxmd.com/read/29331754/synthesis-and-bioevaluation-and-doking-study-of-1h-pyrrolo-2-3-b-pyridine-derivatives-bearing-aromatic-hydrazone-moiety-as-c-met-inhibitors
#2
Wenhui Wang, Shan Xu, Yongli Duan, Xiaobo Liu, Xiaojing Li, Caolin Wang, Bingbing Zhao, Pengwu Zheng, Wufu Zhu
Two series of aromatic hydrazone derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety (7a-r, 8a-i, 12a-b, 13a-c, 16a-d and 17a-e) were designed, synthesized and evaluated for the IC50 values against four cancer cell lines (A549, HepG2, MCF-7and PC-3). Two selected compounds (7c and 17e) were further evaluated for the activity against c-Met, Flt-3, VEGFR-2 and EGFR kinases. The data indicated that targets compounds were selective for c-Met kinase. And the most promising compound 7c was further studied in terms of dose-dependent, time-dependent and cell apoptosis...
December 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29327227/structural-characterization-of-a-novel-full-length-transcript-promoter-from-horseradish-latent-virus-hrlv-and-its-transcriptional-regulation-by-multiple-stress-responsive-transcription-factors
#3
Ahamed Khan, Ankita Shrestha, Kashyap Bhuyan, Indu B Maiti, Nrisingha Dey
The promoter fragment described in this study can be employed for strong transgene expression under both biotic and abiotic stress conditions. Plant-infecting Caulimoviruses have evolved multiple regulatory mechanisms to address various environmental stimuli during the course of evolution. One such mechanism involves the retention of discrete stress responsive cis-elements which are required for their survival and host-specificity. Here we describe the characterization of a novel Caulimoviral promoter isolated from Horseradish Latent Virus (HRLV) and its regulation by multiple stress responsive Transcription factors (TFs) namely DREB1, AREB1 and TGA1a...
January 11, 2018: Plant Molecular Biology
https://www.readbyqxmd.com/read/29325127/inhibiting-trophoblast-par-1-overexpression-suppresses-sflt-1-induced-anti-angiogenesis-and-abnormal-vascular-remodeling-a-possible-therapeutic-approach-for-preeclampsia
#4
Yin Zhao, YanFang Zheng, XiaoXia Liu, QingQing Luo, Di Wu, XiaoPing Liu, Li Zou
STUDY QUESTION: Is it possible to improve vascular remodeling by inhibiting the excessive expression of protease activated receptor 1 (PAR-1) in trophoblast of abnormal placenta? SUMMARY ANSWER: Inhibition of trophoblast PAR-1 overexpression may promote placental angiogenesis and vascular remodeling, offering an alternative therapeutic approach for preeclampsia. WHAT IS KNOWN ALREADY: PAR-1 is high-affinity receptor of thrombin. Thrombin increases sFlt-1 secretion in trophoblast via the activation of PAR-1...
January 9, 2018: Molecular Human Reproduction
https://www.readbyqxmd.com/read/29320922/co-emergence-of-specialized-endothelial-cells-from-embryonic-stem-cells
#5
Nicole Madfis, Zhiqiang Lin, Ashwath Kumar, Simone A Douglas, Manu O Platt, Yuhong Fan, Kara E McCloskey
A well-formed and robust vasculature is critical to the health of most organ systems in the body. However, the endothelial cells (ECs) forming the vasculature can exhibit a number of distinct functional subphenotypes like arterial or venous ECs, as well as angiogenic tip and stalk ECs. Here, we investigate the in vitro differentiation of EC subphenotypes from embryonic stem cells (ESCs) using. Using our staged induction methods and chemically-defined mediums, highly angiogenic EC subpopulations, as well as, less proliferative and less migratory EC subpopulations are derived...
January 10, 2018: Stem Cells and Development
https://www.readbyqxmd.com/read/29317165/discovery-of-novel-2-substituted-4-phenoxypyridine-derivatives-as-potential-antitumor-agents
#6
Yongli Duan, Shan Xu, Hehua Xiong, Linxiao Wang, Bingbing Zhao, Ping Wang, Caolin Wang, Yiqing Peng, Shifan Cai, Rong Luo, Pengwu Zheng, Qidong Tang
A series of 2-substituted-4-phenoxypyridine derivatives were designed, synthesized, and evaluated for their antiproliferative activity against 4 cancer cell lines (A549, HT-29, H460, and U87MG) in vitro. Most compounds showed moderate to excellent potency. Nine tyrosine kinases (c-Met, Flt-3, ALK, VEGFR-2, VEGFR-3, PDGFR-α, PDGFR-β, c-Kit, and EGFR) were used to evaluate the inhibitory activities with the most promising analogue 39, which showed the Flt-3/c-Met IC50 values of 2.18/2.61 nM. Structure-activity relationship studies indicated that n-Pr served as R1 group showed a higher preference, and stronger mono-EWGs on the phenyl ring (such as R2 = 4-F) was benefited to the potency...
December 29, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29288908/the-role-of-military-footwear-and-workload-on-ground-reaction-forces-during-a-simulated-lateral-ankle-sprain-mechanism
#7
Jeffrey D Simpson, Hunter DeBusk, Christopher Hill, Adam Knight, Harish Chander
BACKGROUND: Ankle sprains are a common orthopedic injury in military populations, which may be attributed to occupational demands and footwear. Minimalist military boots have become popular, but their influence on ground reaction force (GRF) attenuation capabilities during an ankle inversion perturbation are unknown. Therefore, the purpose of this study was to examine potential differences in GRFs during an ankle inversion perturbation in a standard issue (STN) and minimalist military boot (MIN) before and after a simulated military workload...
November 22, 2017: Foot
https://www.readbyqxmd.com/read/29248669/imaging-of-subclinical-haemopoiesis-after-stem-cell-transplantation-in-patients-with-haematological-malignancies-a-prospective-pilot-study
#8
Kirsten M Williams, Jennifer Holter-Chakrabarty, Liza Lindenberg, Quyen Duong, Sara K Vesely, Chuong T Nguyen, Joseph P Havlicek, Karen Kurdziel, Juan Gea-Banacloche, Frank I Lin, Daniele N Avila, George Selby, Christopher G Kanakry, Shibo Li, Teresa Scordino, Stephen Adler, Catherine M Bollard, Peter Choyke, Ronald E Gress
BACKGROUND: Haemopoietic stem-cell transplantation (HSCT) eradicates host haemopoiesis before venous infusion of haemopoietic stem cells (HSCs). The pathway to cellular recovery has been difficult to study in human beings because of risks associated with interventions during aplasia. We investigated whether 18F-fluorothymidine (18F-FLT) imaging was safe during allogenic HSCT and allowed visualisation of early cellular proliferation and detection of patterns of cellular engraftment after HSCT...
December 13, 2017: Lancet Haematology
https://www.readbyqxmd.com/read/29247446/correction-to-the-relationship-between-endogenous-thymidine-concentrations-and-18f-flt-uptake-in-a-range-of-preclinical-tumour-models
#9
Kathrin Heinzmann, Davina Jean Honess, David Yestin Lewis, Donna-Michelle Smith, Christopher Cawthorne, Heather Keen, Sandra Heskamp, Sonja Schelhaas, Timothy Howard Witney, Dmitry Soloviev, Kaye Janine Williams, Andreas Hans Jacobs, Eric Ofori Aboagye, John Richard Griffiths, Kevin Michael Brindle
Unfortunately, the original version of Figs. 4, 5 and 6b in the article [1] contained errors in the n numbers as indicated on the columns. Please note that column heights and error bars in the original figures and data in the ESM tables are correct and statistical tests are valid. These corrections do not affect any results or conclusions in this article.
December 15, 2017: EJNMMI Research
https://www.readbyqxmd.com/read/29235988/optimal-transformations-leading-to-normal-distributions-of-positron-emission-tomography-standardized-uptake-values
#10
Matthew Scarpelli, Jens Eickhoff, Enrique Cuna, Scott Perlman, Robert Jeraj
The statistical analysis of positron emission tomography (PET) standardized uptake value (SUV) measurements is challenging due to the skewed nature of SUV distributions. This limits utilization of powerful parametric statistical models for analyzing SUV measurements. An ad-hoc approach, which is frequently used in practice, is to blindly use a log transformation, which may or may not result in normal SUV distributions. This study sought to identify optimal transformations leading to normally distributed PET SUVs extracted from tumors and assess the effects of therapy on the optimal transformations...
December 13, 2017: Physics in Medicine and Biology
https://www.readbyqxmd.com/read/29218445/demonstration-of-nucleoside-transporter-activity-in-the-nose-to-brain-distribution-of-18f-fluorothymidine-using-pet-imaging
#11
Laura L Boles Ponto, Jiangeng Huang, Susan A Walsh, Michael R Acevedo, Christine Mundt, John Sunderland, Maureen Donovan
To evaluate the role of nucleoside transporters in the nose-to-brain uptake of [18F]fluorothymidine (FLT), an equilibrative nucleoside transporter (ENT1,2) and concentrative nucleoside transporter (CNT1-3) substrate, using PET to measure local tissue concentrations. Anesthetized Sprague-Dawley rats were administered FLT by intranasal (IN) instillation or tail-vein injection (IV). NBMPR (nitrobenzylmercaptopurine riboside), an ENT1 inhibitor, was administered either IN or intraperitoneally (IP). Dynamic PET imaging was performed for up to 40 min...
December 7, 2017: AAPS Journal
https://www.readbyqxmd.com/read/29218424/pharmacoimaging-of-blood-brain-barrier-permeable-fdg-and-impermeable-flt-substrates-after-intranasal-in-administration
#12
Laura L Boles Ponto, Susan Walsh, Jiangeng Huang, Christine Mundt, Katherine Thede-Reynolds, G Leonard Watkins, John Sunderland, Michael Acevedo, Maureen Donovan
To illustrate the use of imaging to quantify the transfer of materials from the nasal cavity to other anatomical compartments, specifically, transfer to the brain using the thymidine analogue, [18F]fluorothymidine (FLT), and the glucose analogue, [18F]fluorodeoxyglucose (FDG). Anesthetized rats were administered FLT or FDG by intranasal instillation (IN) or tail-vein injection (IV). PET/CT imaging was performed for up to 60 min. Volumes-of-interest (VOIs) for the olfactory bulb (OB) and the remaining brain were created on the CT and transferred to the co-registered dynamic PET...
December 7, 2017: AAPS Journal
https://www.readbyqxmd.com/read/29217733/sex-as-a-biological-variable-in-preclinical-imaging-research-initial-observations-with-18f-fluorothymidine
#13
Szeman Ruby Chan, Kelley Salem, Justin Jeffery, Ginny L Powers, Yongjun Yan, Kooresh I Shoghi, Aparna M Mahajan, Amy M Fowler
The study objective was to investigate whether sex influences 3'-deoxy-3'-[18F]fluorothymidine (18F-FLT) uptake and tissue distribution in mouse models of cancer. Methods:18F-FLT biodistribution was measured in three strains of male and female mice (129S6/SvEv, athymic nude, and BALB/c). 18F-Fluoro-2-deoxy-2-D-glucose (18F-FDG) biodistribution was performed for comparison. 18F-FLT uptake was also measured in female 129S6/SvEv mice bearing estrogen-dependent SSM3 mouse mammary tumors, male athymic nude mice bearing androgen-dependent CWR22 prostate cancer xenografts, and male and female athymic nude mice bearing estrogen-independent MDA-MB-231 human breast cancer xenografts...
December 7, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29203143/synthesis-and-bioevaluation-study-of-novel-n-methylpicolinamide-and-thienopyrimidine-derivatives-as-selectivity-c-met-kinase-inhibitors
#14
Linxiao Wang, Shan Xu, Xiuying Chen, Xiaobo Liu, Yongli Duan, Dejia Kong, Dandan Zhao, Pengwu Zheng, Qidong Tang, Wufu Zhu
Four series of N-methylpicolinamide moiety and thienopyrimidine moiety bearing pyridazinone were designed and synthesized and evaluated for the IC50 values against three cancer cell lines (A549, HepG2 and MCF-7) and some selected compounds were further evaluated for the activity against c-Met, Flt-3, VEGFR-2, c-Kit and EGFR kinases. Three compounds (35, 39 and 43) showed more active than positive control Foretinib against A549, HepG2 and MCF-7 cell lines. The most promising compound 43 showed superior activity against A549, HepG2 and MCF-7, with the IC50 values of 0...
November 26, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29198025/characteristics-of-polycyclic-aromatic-hydrocarbons-in-pm2-5-emitted-from-different-cooking-activities-in-china
#15
Yun-Chun Li, Jia-Qian Qiu, Man Shu, Steven Sai Hang Ho, Jun-Ji Cao, Ge-Hui Wang, Xian-Xiang Wang, Xiao-Qing Zhao
Nineteen polycyclic aromatic hydrocarbons (PAHs) in PM2.5 emitted from five different cooking activities were characterized, and their influencing factors were determined. The total quantified particle-bounded PAH concentrations (ΣPAHs) in the airs from the cooking activities were 4.2-36.5-fold higher than those in corresponding backgrounds. The highest ΣPAHs were seen in cafeteria frying (783 ± 499 ng/m3), followed by meat roasting (420 ± 191 ng/m3), fish roasting (210 ± 105 ng/m3), snack-street boiling (202 ± 230 ng/m3), and cafeteria boiling (150 ± 65 ng/m3)...
December 2, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29197731/synthesis-and-antiproliferative-activity-of-pyrrolo-2-3-b-pyridine-derivatives-bearing-the-1-8-naphthyridin-2-one-moiety
#16
Qidong Tang, Yongli Duan, Linxiao Wang, Min Wang, Yiqiang Ouyang, Caolin Wang, Han Mei, Sheng Tang, Yinhua Xiong, Pengwu Zheng, Ping Gong, Wufu Zhu
A series of pyrrolo[2,3-b]pyridine derivatives bearing the 1,8-naphthyridin-2-one moiety were synthesized, and evaluated for their antiproliferative activity against four cancer cell lines (HT-29, A549, H460, and U87MG) and six tyrosine kinases (c-Met, Flt-3, PDGFR-β, VEGFR-2, EGFR, and c-Kit) inhibitory activities in vitro. Most compounds showed moderate to excellent potency, with the most promising analogue 32 showing Flt-3/c-Met IC50 value of 1.16/1.92 nM. Structure-activity relationship studies indicated that the hydrogen atom served as R1 group was benefited to the potency, and mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring (such as R3 = 4-F) showed a higher preference for antiproliferative activity...
November 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29162137/potentiating-angiogenesis-arrest-in-vivo-via-laser-irradiation-of-peptide-functionalised-gold-nanoparticles
#17
Pedro Pedrosa, Amelie Heuer-Jungemann, Antonios G Kanaras, Alexandra R Fernandes, Pedro V Baptista
BACKGROUND: Anti-angiogenic therapy has great potential for cancer therapy with several FDA approved formulations but there are considerable side effects upon the normal blood vessels that decrease the potential application of such therapeutics. Chicken chorioallantoic membrane (CAM) has been used as a model to study angiogenesis in vivo. Using a CAM model, it had been previously shown that spherical gold nanoparticles functionalised with an anti-angiogenic peptide can humper neo-angiogenesis...
November 21, 2017: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/29149180/roles-of-vegf-flt-1-signaling-in-malignant-behaviors-of-oral-squamous-cell-carcinoma
#18
Ajiravudh Subarnbhesaj, Mutsumi Miyauchi, Chea Chanbora, Aki Mikuriya, Phuong Thao Nguyen, Hisako Furusho, Nurina Febriyanti Ayuningtyas, Minoru Fujita, Shigeaki Toratani, Masaaki Takechi, Shumpei Niida, Takashi Takata
BACKGROUND: Vascular endothelial growth factor (VEGF) is a highly specific signaling protein for vascular endothelial cells that plays a critical role in tumor growth and invasion through angiogenesis, and may contribute to cell migration and activation of pre-osteoclasts, osteoclasts and some tumor cells. OBJECTIVES: We aimed to clarify the detailed roles of VEGF-Flt-1 signaling in bone invasion of oral squamous cell carcinoma (OSCC) cells. RESULTS: Forty-two (42) of 54 cases with gingival SCC (77...
2017: PloS One
https://www.readbyqxmd.com/read/29145197/inflammatory-and-angiogenic-factors-linked-to-longitudinal-microvascular-changes-in-hemodialysis-patients-irrespective-of-treatment-dose-intensity
#19
Nicos Mitsides, Tom Cornelis, Natascha J H Broers, Nanada M P Diederen, Paul Brenchley, Nicole Heitink-Ter Braak, Frank M van der Sande, Casper G Schalkwijk, Jeroen P Kooman, Sandip Mitra
BACKGROUND: Cardiovascular disease is a major contributor to the poor outcomes observed in hemodialysis. We investigated the relationship between hemodialysis intensity and vascular parameters in high-dose (HDHD; >12hrs/week) and Conventional (CHD; ≤12hrs/week) hemodialysis intensity over a 6-month period. METHODS: We present the 6-month longitudinal analysis of a 2-year multicenter study investigating the effects of HDHD on cardiovascular parameters. We used pulse wave velocity, 24hr ambulatory blood pressure and sublingual dark field capillaroscopy measurements to assess macro- and microcirculation on 6-monthly basis...
November 16, 2017: Kidney & Blood Pressure Research
https://www.readbyqxmd.com/read/29143774/disrupting-vegf-vegfr1-interaction-de-novo-designed-linear-helical-peptides-to-mimic-the-vegf13-25-fragment
#20
Beatriz Balsera, M Ángeles Bonache, Marie Reille-Seroussi, Nathalie Gagey-Eilstein, Michel Vidal, Rosario González-Muñiz, María Jesús Pérez de Vega
The interaction between vascular endothelial growth factor (VEGF) and its receptors (VEGFR) has important implications in angiogenesis and cancer, which moved us to search for peptide derivatives able to block this protein-protein interaction. In a previous work we had described a collection of linear 13-mer peptides specially designed to adopt helical conformations (Ac-SSEEX⁵ARNX⁸AAX(12)N-NH₂), as well as the evaluation of seven library components for the inhibition of the interaction of VEGF with its Receptor 1 (VEGFR1)...
October 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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