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https://www.readbyqxmd.com/read/28549890/-18-f-labeled-indole-based-analogs-as-highly-selective-radioligands-for-imaging-sigma-2-receptors-in-the-brain
#1
Liang Wang, Jiajun Ye, Yingfang He, Winnie Deuther-Conrad, Jinming Zhang, Xiaojun Zhang, Mengchao Cui, Jörg Steinbach, Yiyun Huang, Peter Brust, Hongmei Jia
We have designed and synthesized a series of indole-based σ2 receptor ligands containing 5,6-dimethoxyisoindoline or 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline as pharmacophore. In vitro competition binding assays showed that all ten ligands possessed low nanomolar affinity (Ki=1.79-5.23nM) for σ2 receptors and high subtype selectivity (Ki (σ2)/Ki (σ1)=56-708). Moreover, they showed high selectivity for σ2 receptor over the vesicular acetylcholine transporter (>1000-fold). The corresponding radiotracers [(18)F]16 and [(18)F]21 were prepared by an efficient one-pot, two-step reaction sequence with a home-made automated synthesis module, with 10-15% radiochemical yield and radiochemical purity of >99%...
May 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28549836/heterogeneity-of-tumor-and-immune-cell-pd-l1-expression-and-lymphocyte-counts-in-surgical-nsclc-samples
#2
David Casadevall, Sergi Clavé, Álvaro Taus, Max Hardy-Werbin, Pedro Rocha, Marta Lorenzo, Silvia Menéndez, Marta Salido, Joan Albanell, Lara Pijuan, Edurne Arriola
BACKGROUND: Immune-checkpoint inhibitors against programmed cell death protein 1 (PD-1)/programmed death-ligand 1 (PD-L1) have shown remarkable therapeutic activity in non-small-cell lung cancer (NSCLC). However, biomarker-based patient selection remains a challenge. Our aim was to assess the heterogeneity of various immune markers between different tumor areas of surgically resected NSCLC specimens. MATERIALS AND METHODS: We included 94 adenocarcinoma (ADC) and 50 squamous cell carcinoma (SCC) specimens...
May 4, 2017: Clinical Lung Cancer
https://www.readbyqxmd.com/read/28545880/stepwise-preconditioning-enhances-mesenchymal-stem-cell-based-cartilage-regeneration-through-epigenetic-modification
#3
Sien Lin, Wayne Yuk Wai Lee, Liangliang Xu, Yujia Wang, Yuanfeng Chen, Kevin Ki Wai Ho, Ling Qin, Xiaohua Jiang, Liao Cui, Gang Li
OBJECTIVE: This study is to investigate the functions and underlying mechanisms of MSCs underwent stepwise preconditioning in chondrogenic medium before expansion, then further explore their therapeutic effects in a surgically induced OA model. METHODS: MSCs isolated from the adult rats expressing Green Fluorescence Protein (GFP) were incubated in basal medium or primed in chondrogenic medium before expansion. The multipotency including cell proliferation, differentiation, and survivability was compared between chondrogenic manipulated MSCs (M-MSCs) and untreated MSCs...
May 22, 2017: Osteoarthritis and Cartilage
https://www.readbyqxmd.com/read/28545525/rotational-alignment-of-femoral-component-with-different-methods-in-total-knee-arthroplasty-a-randomized-controlled-trial
#4
Joon Kyu Lee, Sahnghoon Lee, Sae Hyung Chun, Ki Tae Kim, Myung Chul Lee
BACKGROUND: Femoral component rotation (FCR) is one of the most important factors in total knee arthroplasty. In this prospective study, we used three different techniques for FCR and analyzed their accuracy with postoperative axial computed tomography (CT) images. We also evaluated effect of FCR to clinical outcome. METHODS: One hundred sixty-five patients were randomly allocated into three groups. In the measured resection group, FCR was set by externally rotating the axis 3° off the posterior femoral condylar axis...
May 25, 2017: BMC Musculoskeletal Disorders
https://www.readbyqxmd.com/read/28544659/intranasal-distribution-and-clearance-of-thermoreversible-gel-in-an-animal-model
#5
Ji Eun Choi, Ki Ryung Kim, Yangseop Noh, Won-Ho Chung, Yang-Sun Cho, Seung-Kyu Chung, Hun-Jong Dhong, Hyo Yeol Kim
BACKGROUND: Poloxamer 407 (P407) has been investigated for an intranasal drug delivery system. However, there is little known about the distribution and clearance of intranasally applied P407. The purpose of this study was to evaluate the distribution and clearance time of P407 in an animal model. METHODS: Five male pigs were administered the experimental solution (18% of P407 with 0.01% of fluorescein) and the control solution (normal saline with 0.01% of fluorescein) into their right and left nasal cavity, respectively...
May 23, 2017: International Forum of Allergy & Rhinology
https://www.readbyqxmd.com/read/28537566/intramural-gastric-hematoma-imitating-a-gastrointestinal-stromal-tumor-case-report-and-literature-review
#6
Arkadiusz Spychała, Piotr Nowaczyk, Aleksandra Budnicka, Ewa Antoniewicz, Dawid Murawa
The article presents a case report of a patient with an intramural gastric hematoma. Diagnostic examinations were suggestive of a suspected gastrointestinal stromal tumor Normal image was observed in gastroscopic examination while abdominal CT scan revealed a nodular lesion along the greater curvature of the stomach extending from the posterior wall and adjoining the pancreas and the spleen. The patient was qualified for surgical treatment. Laparotomy was performed followed by total gastric resection and Roux-en-Y reconstruction of the gastrointestinal tract...
April 30, 2017: Polski Przeglad Chirurgiczny
https://www.readbyqxmd.com/read/28537255/spin-orbit-torque-driven-skyrmion-dynamics-revealed-by-time-resolved-x-ray-microscopy
#7
Seonghoon Woo, Kyung Mee Song, Hee-Sung Han, Min-Seung Jung, Mi-Young Im, Ki-Suk Lee, Kun Soo Song, Peter Fischer, Jung-Il Hong, Jun Woo Choi, Byoung-Chul Min, Hyun Cheol Koo, Joonyeon Chang
Magnetic skyrmions are topologically protected spin textures with attractive properties suitable for high-density and low-power spintronic device applications. Much effort has been dedicated to understanding the dynamical behaviours of the magnetic skyrmions. However, experimental observation of the ultrafast dynamics of this chiral magnetic texture in real space, which is the hallmark of its quasiparticle nature, has so far remained elusive. Here, we report nanosecond-dynamics of a 100nm-diameter magnetic skyrmion during a current pulse application, using a time-resolved pump-probe soft X-ray imaging technique...
May 24, 2017: Nature Communications
https://www.readbyqxmd.com/read/28537066/optically-patternable-metamaterial-below-diffraction-limit
#8
Youngseop Lee, Sang-Gil Park, SeokJae Yoo, Minhee Kang, Sang Chul Jeon, Young-Su Kim, Q-Han Park, Ki-Hun Jeong
We report an optically patternable metamaterial (OPM) for ultraviolet nanolithography below the diffraction limit. The OPM features monolayered silver nanoislands embedded within a photosensitive polymer by using spin-coating of an ultrathin polymer, oblique angle deposition and solid-state embedment of silver nanoislands. This unique configuration simultaneously exhibits both negative effective permittivity and high image contrast in the ultraviolet range, which enables the surface plasmon excitation for the clear photolithographic definition of minimum feature size of 70 nm (< ~ λ/5) beyond the near-field zone...
May 24, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28536487/current-status-and-challenges-in-sentinel-node-navigation-surgery-for-early-gastric-cancer
#9
Bang Wool Eom, Young-Il Kim, Hong Man Yoon, Soo-Jeong Cho, Jong Yeul Lee, Chan Gyoo Kim, Soo Jin Kim, Ji Yoon Rho, Seok Ki Kim, Myeong-Cherl Kook, Young-Woo Kim, Keun Won Ryu
Although a number of feasibility studies for sentinel node (SN) concepts in gastric cancer have been conducted since 2000, there remains a debate regarding detailed detection techniques and oncological safety. Two important multicenter phase II clinical trials were performed in Japan that used different methods and reached different conclusions; one confirmed acceptable results with a false-negative rate of 7%, and the other showed an unacceptably high false-negative rate of 46.4%. The Sentinel Node Oriented Tailored Approach (SENORITA) trial is a multicenter randomized controlled phase III trial being performed in Korea...
April 2017: Chinese Journal of Cancer Research, Chung-kuo Yen Cheng Yen Chiu
https://www.readbyqxmd.com/read/28530802/discovery-of-n-5-fluoropyridin-2-yl-6-methyl-4-pyrimidin-5-yloxy-picolinamide-vu0424238-a-novel-negative-allosteric-modulator-of-metabotropic-glutamate-receptor-subtype-5-selected-for-clinical-evaluation
#10
Andrew S Felts, Alice L Rodriguez, Anna L Blobaum, Ryan D Morrison, Brittney S Bates, Analisa Thompson Gray, Jerri M Rook, Mohammed N Tantawy, Frank W Byers, Sichen Chang, Daryl F Venable, Vincent B Luscombe, Gilles D Tamagnan, Colleen M Niswender, J Scott Daniels, Carrie K Jones, P Jeffrey Conn, Craig W Lindsley, Kyle A Emmitte
Preclinical evidence in support of the potential utility of mGlu5 NAMs for the treatment of a variety of psychiatric and neurodegenerative disorders is extensive, and multiple such molecules have entered clinical trials. Despite some promising results from clinical studies, no small molecule mGlu5 NAM has yet to reach market. Here we present the discovery and evaluation of N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (27, VU0424238), a compound selected for clinical evaluation. Compound 27 is more than 900-fold selective for mGlu5 versus the other mGlu receptors, and binding studies established a Ki value of 4...
May 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28530280/visualization-of-vesicular-transport-from-the-endoplasmic-reticulum-to-lysosome-using-an-amidine-derived-two-photon-probe
#11
Hyo Won Lee, Myoung Ki Cho, Hye-Ri Kim, Chang Su Lim, Chulhun Kang, Hwan Myung Kim
We report an amidine-based small molecule two-photon fluorescent probe (ELP1) for monitoring vesicle transport from the ER to lysosome in live cells. Two-photon microscopy imaging studies indicated that this probe initially localized in the ER and subsequently transferred to lysosomal compartments through vesicular transport. These results may provide an effective tool for studying trafficking-related biology and pathology in real-time.
May 22, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28525908/mri-based-radiotherapy-planning-method-using-rigid-image-registration-technique-combined-with-outer-body-correction-scheme-a%C3%A2-feasibility-study
#12
Ki Mun Kang, Hoon Sik Choi, Bae Kwon Jeong, Jin Ho Song, In-Bong Ha, Yun Hee Lee, Chul Hang Kim, Hojin Jeong
An alternative pseudo CT generation method for magnetic resonance image (MRI)-based radiotherapy planning was investigated in the work. A pseudo CT was initially generated using the rigid image registration between the planning MRI and previously acquired diagnostic CT scan. The pseudo CT generated was then refined to have the same morphology with that of the referenced planning image scan by applying the outer body correction scheme. This method was applied to some sample of brain image data and the feasibility of the method was assessed by comparing dosimetry results with those from the current gold standard CT-based calculations...
May 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28524648/instantaneous-ph-boosted-functionalization-of-stellate-gold-nanoparticles-for-intracellular-imaging-of-mirna
#13
Jisun Ki, Eunji Jang, Seungmin Han, Moo-Kwang Shin, Byunghoon Kang, Yong-Min Huh, Seungjoo Haam
Various types of nanoprobes have recently been utilized to monitor living organisms by detecting and imaging intracellular biomarkers, such as microRNAs (miRs). We here present a simple one-pot method to prepare stellate gold nanoparticles functionalized with miR-detecting molecular beacons (SGNP-MBs); low pH conditions permitted the rapid-high loading of MBs on the surface of SGNPs. Compared to the conventional gold nanoparticle-based MBs, SGNPs carried a 4.5-fold higher load of MBs and exhibited a 6.4-fold higher cellular uptake...
May 19, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28516046/image-quality-assessment-of-a-1-5t-dedicated-magnetic-resonance-simulator-for-radiotherapy-with-a-flexible-radio-frequency-coil-setting-using-the-standard-american-college-of-radiology-magnetic-resonance-imaging-phantom-test
#14
Oi Lei Wong, Jing Yuan, Siu Ki Yu, Kin Yin Cheung
BACKGROUND: A flexible RF coil setting has to be used on an MR-simulator (MR-sim) in the head and neck simulation scan for radiotherapy (RT) purpose, while the image quality might be compromised due to the sub-optimized flexible coil compared to the normal diagnostic radiological (DR) head coil. In this study, we assessed the image quality of an MR-sim by conducting the standard American College of Radiology (ACR) MRI phantom test on a 1.5T MR-sim under RT-setting and comparing it to DR-setting...
April 2017: Quantitative Imaging in Medicine and Surgery
https://www.readbyqxmd.com/read/28507867/low-grade-cribriform-cystadenocarcinoma-a-review-of-the-literature-and-case-report
#15
Nao Wakabayashi, Hiroki Umezawa, Noriko M Matsumoto, Yoko Endo, Zenya Naito, Rei Ogawa
Low-grade cribriform cystadenocarcinoma (LGCCC) is a rare tumor of the salivary gland that most often arises from the parotid gland. A 51-year-old man developed a small mass on the right parotid gland 5 years ago. A preoperative magnetic resonance image showed abnormal intensity, an atypical characteristic for such a tumor; therefore, the diagnosis was difficult. Thus, a superficial parotidectomy was performed as a total excisional biopsy to remove the tumor. Histopathological analyses revealed that the tumor was composed of a single cyst comprising cells containing mucosal fluid, with proliferation of large cells...
April 2017: Plastic and Reconstructive Surgery. Global Open
https://www.readbyqxmd.com/read/28503470/falsely-elevated-postvoid-residual-urine-volume-in-uterine-myoma
#16
Tae Hee Kim, Hyo Sang Kim, Jung Wook Park, Oh Kyung Lim, Ki Deok Park, Ju Kang Lee
Precise measurement of postvoid residual (PVR) urine volume is a key factor in assessing patients with voiding dysfunction, including those with lower urinary tract problems. The safe and noninvasive ultrasound bladder scan is the preferred mode to measure PVR volume. However, this procedure has a false-positive rate up to 9%, in the presence of ovarian cysts, renal cysts, ascites, or uterine myoma with cystic degeneration. Until now, cystic lesions are known to cause false positivity in ultrasound bladder scanner...
April 2017: Annals of Rehabilitation Medicine
https://www.readbyqxmd.com/read/28501470/possibility-of-predicting-sert-occupancy-from-the-in-vitro-inhibition-constant-for-sert-the-clinically-relevant-plasma-concentration-of-unbound-drugs-and-their-profiles-for-substrates-of-transporters
#17
REVIEW
Masahiro Yahata, Koji Chiba, Takao Watanabe, Yuichi Sugiyama
Accurate prediction of target occupancy facilitates CNS drug development. In this review, we discuss the predictability of serotonin transporter (SERT) occupancy in human brain estimated from in vitro Ki values for human SERT and plasma concentrations of unbound drug (Cu,plasma) as well as the impact of drug transporters in the blood-brain barrier. First, the geometric means of in vitro Ki values were compared with the means of in vivo Ki values (Ki,u,plasma) which were calculated as Cu,plasma values at 50% occupancy of SERT obtained from previous clinical PET/SPECT imaging studies for 6 selective serotonin transporter reuptake inhibitors (SSRIs) and 3 serotonin norepinephrine reuptake inhibitors (SNRIs)...
May 10, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28498800/locally-applied-5-fluorouracil-loaded-slow-release-patch-prevents-pancreatic-cancer-growth-in-an-orthotopic-mouse-model
#18
In Kyong Shim, Hye-Jin Yi, Hee-Gyeong Yi, Chan Mi Lee, Yu Na Lee, Yeong-Jin Choi, Seong-Yun Jeong, Eunsung Jun, Robert M Hoffman, Dong-Woo Cho, Song Cheol Kim
To obtain improved efficacy against pancreatic cancer, we investigated the efficacy and safety of a locally-applied 5-fluorouracil (5-FU)-loaded polymeric patch on pancreatic tumors in an orthotopic nude-mouse model. The 5-FU-releasing polymeric patch was produced by 3D printing. After application of the patch, it released the drug slowly for 4 weeks, and suppressed BxPC-3 pancreas cancer growth. Luciferase imaging of BxPC3-Luc cells implanted in the pancreas was performed longitudinally. The drug patch delivered a 30...
April 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28493679/light-induced-fluorescence-modulation-of-quantum-dot-crystal-violet-conjugates-stochastic-off-on-off-cycles-for-multicolor-patterning-and-super-resolution
#19
Sungwook Jung, Joonhyuck Park, Jiwon Bang, Jae-Yeol Kim, Cheolhee Kim, Yongmoon Jeon, Seung Hwan Lee, Ho Jin, Sukyung Choi, Bomi Kim, Woo Jin Lee, Chan-Gi Pack, Jong-Bong Lee, Nam Ki Lee, Sungjee Kim
Photoswitching or modulation of quantum dots (QDs) can be promising for many fields that include display, memory, and super-resolution imaging. However, such modulations have mostly relied on photomodulations of conjugated molecules in QD vicinity, which typically require high power of high energy photons at UV. We report a visible light-induced facile modulation route for QD-dye conjugates. QD crystal violets conjugates (QD-CVs) were prepared and the crystal violet (CV) molecules on QD quenched the fluorescence efficiently...
May 25, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28493504/imaging-sonographic-findings-of-in-a-case-of-proliferating-trichilemmal-tumor-of-a-finger-a-case-report
#20
Ki Eon Kwon, Seon-Jeong Kim, Joo Hak Kim, Yoon Yang Jung, Noh Hyuck Park, Ji Yeon Park, Kyung A Kang, Soo Heui Baek
Proliferating trichilemmal tumor (PTT) is a rare tumor that originates from the outer root sheath of a hair follicle. About 90% of PTTs occur on the scalp. The sonographic findings of PTT in the subungual region have not been reported previously. In our case, sonography showed a heterogeneous mass containing echogenic foci with no detectable intratumoral vascularity. These echogenic foci probably represent keratin and cholesterol. © 2017 Wiley Periodicals, Inc. J Clin Ultrasound, 2017.
May 11, 2017: Journal of Clinical Ultrasound: JCU
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