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https://www.readbyqxmd.com/read/28444764/prospective-unbiased-experience-with-three-acellular-dermal-matrices-in-breast-reconstruction
#1
Edward I Chang, Jun Liu
BACKGROUND: The use of acellular dermal matrix (ADM) has become the standard of care in breast reconstruction. However, the majority of current studies are biased or combine large databases introducing inherent flaws. Here, we present a prospective single surgeon experience comparing three ADM. METHODS: All expander based breast reconstructions between 2014 and 2015 using ADM were included. RESULTS: Eighteen patients (32 breasts) underwent reconstruction using Flex Pliable, 15 patients (22 breasts) used Alloderm, and 14 patients (20 breasts) had Dermacell...
April 25, 2017: Journal of Surgical Oncology
https://www.readbyqxmd.com/read/28440049/analytical-based-methodologies-for-examining-the-in-vitro-absorption-distribution-metabolism-and-elimination-adme-of-silver-nanoparticles
#2
Sesha L A Paluri, John D Ryan, Nhi H Lam, Dhriti Nepal, Ioana E Sizemore
The clinical applications of silver nanoparticles (AgNPs) remain limited due to the lack of well-established methodologies for studying their nanokinetics. Hereby, the primary goal is to adapt a suite of analytical-based methodologies for examining the in vitro absorption, distribution, metabolism, and elimination of AgNPs. Vero 76 and HEK 293 cells are exposed to ≈10-nm spherical AgNPs(+) and AgNPs(-) at relevant concentrations (0-300 µg mL(-1) ) and times (4-48 h). Absorption: Inductively coupled plasma optical emission spectroscopy (ICP-OES) demonstrates that the two AgNP formulations are not bioequivalent...
April 25, 2017: Small
https://www.readbyqxmd.com/read/28438535/a-critical-view-on-in-vitro-analysis-of-p-glycoprotein-p-gp-transport-kinetics
#3
Lasse Saaby, Birger Brodin
Transport proteins expressed in the different barriers of the human body can have great implications on absorption, distribution and excretion of drug compounds. Inhibition or saturation of a transporter can potentially alter these ADME properties, and thereby also the pharmacokinetic profile and bioavailability of drug compounds. P-glycoprotein (P-gp, ABCB1), is an efflux transporter which is present in most of the barriers of the body, including the small intestine, the blood-brain barrier, the liver and the kidney...
April 21, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28431780/tolterodine-tartrate
#4
Gennady Ananchenko, Jasmina Novakovic
Tolterodine tartrate belongs to the family of muscarinic receptor antagonists and is indicated for the treatment of overactive urinary bladder syndrome. This chapter provides an overview of physical, analytical, and ADME profiles; highlights methods of chemical synthesis; and discusses stability of tolterodine as a free base and/or its l-tartrate salt in solution and in the solid state. The information presented in this chapter is based on the peer-reviewed literature, compendial reports (USP, EP), and authors' data...
2017: Profiles of Drug Substances, Excipients, and related Methodology
https://www.readbyqxmd.com/read/28431686/adm-guidance-ceramics-all-ceramic-multilayer-interfaces-in-dentistry
#5
Ulrich Lohbauer, Susanne S Scherrer, Alvaro Della Bona, Michael Tholey, Richard van Noort, Alessandro Vichi, J Robert Kelly, Paulo F Cesar
This guidance document describes the specific issues involved in dental multilayer ceramic systems. The material interactions with regard to specific thermal and mechanical properties are reviewed and the characteristics of dental tooth-shaped processing parameters (sintering, geometry, thickness ratio, etc.) are discussed. Several techniques for the measurement of bond quality and residual stresses are presented with a detailed discussion of advantages and disadvantages. In essence no single technique is able to describe adequately the all-ceramic interface...
April 18, 2017: Dental Materials: Official Publication of the Academy of Dental Materials
https://www.readbyqxmd.com/read/28430437/discovery-of-an-hcv-ns5b-replicase-palm-site-allosteric-inhibitor-bms-929075-advanced-to-phase-1-clinical-studies
#6
Kap-Sun Yeung, Brett R Beno, Kyle Parcella, John A Bender, Katherine A Grant-Young, Andrew Nickel, Prashantha Gunaga, Prakash Anjanappa, Rajesh Onkardas Bora, Kumaravel Selvakumar, Karen Rigat, Ying-Kai Wang, Mengping Liu, Julie A Lemm, Kathy Mosure, Steven Sheriff, Changhong Wan, Mark Witmer, Kevin Kish, Umesh M Hanumegowda, Xiaoliang Zhuo, Yue-Zhong Shu, Dawn Parker, Roy Haskell, Alicia Ng, Qi Gao, Elizabeth Colston, Joseph Raybon, Dennis M Grasela, Kenneth S Santone, Min Gao, Nicholas A Meanwell, Michael W Sinz, Matthew G Soars, Jay O Knipe, Susan B Roberts, John F Kadow
The hepatitis C virus NS5B replicase is a prime target for the development of direct-acting antiviral drugs for the treatment of chronic HCV infection. Inspired by the overlay of bound structures of three structurally distinct NS5B palm site allosteric inhibitors, the high throughput screening hit anthranilic acid 4, the known benzofuran analog 5 and the benzothiadiazine derivative 6, an optimization process utilizing the simple benzofuran template 7 as a starting point for a fragment growing approach was pursued...
April 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28429654/microrna-451-regulates-chemoresistance-in-renal-cell-carcinoma-by-targeting-atf-2-gene
#7
Xiang Sun, Longhua Lou, Kezhao Zhong, Lijuan Wan
Renal cell carcinoma (RCC) is a malignant tumor, which severely threatens human's life, moreover, the multi-drug resistance (MDR) under RCC undoubtedly strengthen the difficulties in the treatment. MiR-451 has been considered to play an important role in regulation of MDR in several cancers, but the role of it in MDR of RCC has not been explored. This study aims to explore the mechanism of miR-451 as a target to regulate chemotherapy resistance, which is crucial for further exploring novel therapy for RCC. Two human cell lines (ACHN and GRC-1) were performed in this study and adriamycin (ADM) was used to construct MDR cell lines...
January 1, 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28423019/design-synthesis-and-structure-activity-relationship-study-of-wollamide-b-a-new-potential-anti-tb-agent
#8
Henok Asfaw, Katja Laqua, Anna Maria Walkowska, Fraser Cunningham, Maria Santos Martinez-Martinez, Juan Carlos Cuevas-Zurita, Lluís Ballell-Pages, Peter Imming
Wollamide B is a cationic antimycobacterial cyclohexapeptide that exhibits activity against Mycobacterium bovis (M. bovis) (IC50 of 3.1 μM). Aiming to define its structural activity relationship (SAR), optimizing potency and pharmacokinetic properties, libraries of analogues were synthesized following a standard Fmoc-based solid phase peptide synthesis approach. The antimycobacterial activities of wollamide B and all the synthesized analogues were tested against Mycobacterium tuberculosis (Mtb) H37Rv. Parallely, in vitro drug metabolism and pharmacokinetic (ADME) profiling was done for the synthesized compounds to evaluate their drug likeness...
2017: PloS One
https://www.readbyqxmd.com/read/28420892/adenomyomatosis-concomitant-with-primary-gallbladder-carcinoma
#9
Tatsuya Morikawa, Takehiro Okabayashi, Yasuo Shima, Tatsuaki Sumiyoshi, Akihito Kozuki, Yuichi Saisaka, Teppei Tokumaru, Kenta Sui, Jun Iwata, Manabu Matsumoto, Sojiro Morita, Yutaka Nishioka
Some clinicians have proposed a relationship between gallbladder (GB) cancer and adenomyomatosis (ADM) of the gallbladder, although the latter condition is not considered to have malignant potential. We retrospectively reviewed the surgical pathology database of patients who underwent resection for ADM of the gallbladder at our institution from March 2005 to May 2015. In total, 624 patients underwent surgical resection of the gallbladder with Rokitansky-Aschoff sinuses. Of these cases, 93 were pathologically diagnosed with ADM of the gallbladder, with 44 (47...
April 2017: Acta Medica Okayama
https://www.readbyqxmd.com/read/28412404/development-of-human-biotransformation-qsars-and-application-for-pbt-assessment-refinement
#10
Ester Papa, Alessandro Sangion, Jon A Arnot, Paola Gramatica
Toxicokinetics heavily influence chemical toxicity as the result of Absorption, Distribution, Metabolism (Biotransformation) and Elimination (ADME) processes. Biotransformation (metabolism) reactions can lead to detoxification or, in some cases, bioactivation of parent compounds to more toxic chemicals. Moreover, biotransformation has been recognized as a key process determining chemical half-life in an organism and is thus a key determinant for bioaccumulation assessment for many chemicals. This study addresses the development of QSAR models for the prediction of in vivo whole body human biotransformation (metabolism) half-lives measured or empirically-derived for over 1000 chemicals, mainly represented by pharmaceuticals...
April 13, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28412087/pregestational-type-2-diabetes-mellitus-induces-cardiac-hypertrophy-in-the-murine-embryo-through-cardiac-remodeling-and-fibrosis
#11
Xue Lin, Penghua Yang, E Albert Reece, Peixin Yang
BACKGROUND: Cardiac hypertrophy is highly prevalent in patients with type 2 diabetes mellitus (T2DM). Experimental evidence has implied that pregnant women with T2DM and their children are at an increased risk of cardiovascular diseases. Our previous mouse model study has revealed that maternal T2DM induces structural heart defects in their offspring. OBJECTIVE: The present study aims to determine whether maternal T2DM induces embryonic heart hypertrophy in a murine model of diabetic embryopathy...
April 12, 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28411114/circulating-biologically-active-adrenomedullin-bio-adm-predicts-hemodynamic-support-requirement-and-mortality-during-sepsis
#12
Pietro Caironi, Roberto Latini, Joachim Struck, Oliver Hartmann, Andreas Bergmann, Giuseppe Maggio, Marco Cavana, Gianni Tognoni, Antonio Pesenti, Luciano Gattinoni, Serge Masson
BACKGROUND: The biological role of adrenomedullin, a hormone involved in hemodynamic homeostasis, is controversial in sepsis, since administration of either the peptide or an antibody against it may be beneficial. METHODS: Plasma bio-ADM was assessed on days 1, 2 and 7 after randomization of 956 patients with sepsis or septic shock to albumin or crystalloids for fluid resuscitation in the multicenter Albumin Italian Outcome Sepsis (ALBIOS) trial. We tested the association of bio-ADM and its time-dependent variation with fluid therapy, vasopressor administration, organ failures and mortality...
April 11, 2017: Chest
https://www.readbyqxmd.com/read/28410587/overview-of-cancer-incidence-and-mortality-among-people-living-with-hiv-aids-in-british-columbia-canada-implications-for-haart-use-and-nadm-development
#13
Connie G Chiu, Danielle Smith, Kate A Salters, Wendy Zhang, Steve Kanters, David Milan, Julio S G Montaner, Andy Coldman, Robert S Hogg, Sam M Wiseman
BACKGROUND: The objective of this study is to evaluate the incidence of non-AIDS defining malignancies (NADMs) among people living with HIV/AIDS (PLWHA) in British Columbia, focusing on clinical correlates, highly active antiretroviral therapy (HAART) use, and survival, in order to elucidate mechanisms for NADM development. METHODS: A retrospective population based analysis was carried out for individuals with HIV/AIDS that began their treatment between 1996 and 2008...
April 14, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28408876/effects-of-age-related-macular-degeneration-on-postural-sway
#14
Hortense Chatard, Laure Tepenier, Olivier Jankowski, Antoine Aussems, Alain Allieta, Talal Beydoun, Sawsen Salah, Maria P Bucci
Purpose: To compare the impact of unilateral vs. bilateral age-related macular degeneration (AMD) on postural sway, and the influence of different visual conditions. The hypothesis of our study was that the impact of AMD will be different between unilateral and bilateral AMD subjects compared to age-matched healthy elderly. Methods: Postural stability was measured with a platform (TechnoConcept®) in 10 elderly unilateral AMD subjects (mean age: 71.1 ± 4.6 years), 10 elderly bilateral AMD subjects (mean age: 70...
2017: Frontiers in Human Neuroscience
https://www.readbyqxmd.com/read/28407200/adrenomedullin-2-intermedin-a-putative-drug-candidate-for-treatment-of-cardiometabolic-diseases
#15
REVIEW
Song-Yang Zhang, Ming-Jiang Xu, Xian Wang
Adrenomedullin (ADM) 2/Intermedin (IMD) is a short peptide that belongs to the CGRP superfamily. Although it shares receptors with CGRP, ADM and amylin (AMY), ADM2 has significant and unique functions in the cardiovascular system. In the past decade, the cardiovascular effect of ADM2 has carefully been studied. In this review, progress in understanding ADM2's effects on the cardiovascular system as well as its protective role in cardiometabolic diseases are summarized.
April 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28405240/targeting-the-ubiquitin-conjugating-enzyme-e2d4-for-cancer-drug-discovery-a-structure-based-approach
#16
Vishwanath Ramatenki, Ramakrishna Dumpati, Rajender Vadija, Santhiprada Vellanki, Sarita Rajender Potlapally, Rohini Rondla, Uma Vuruputuri
Cancer progression is a global burden. The incidence and mortality now reach 30 million deaths per year. Several pathways of cancer are under investigation for the discovery of effective therapeutics. The present study highlights the structural details of the ubiquitin protein 'Ubiquitin-conjugating enzyme E2D4' (UBE2D4) for the novel lead structure identification in cancer drug discovery process. The evaluation of 3D structure of UBE2D4 was carried out using homology modelling techniques. The optimized structure was validated by standard computational protocols...
April 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28403781/design-synthesis-and-biological-evaluation-of-novel-1-3-thiazolidine-2-4-diones-as-anti-prostate-cancer-agents
#17
Ramakrishnan Elancheran, Kuppusamy Saravanan, Selvaraj Divakar, Sima Kumari, V Lenin Maruthanila, Senthamarikannan Kabilan, Muthaiah Ramanathan, Rajlakshmi Devi, Jibon Kotoky
Androgen receptor (AR) is an attractive target for the treatment of prostate cancer. Structural modification and molecular docking-based virtual screening approaches were imposed to identify the novel 1,3-thiazolidine-2,4-diones (TZDs) by using Schrödinger (Maestro 9.5). The best fit molecules (3-12 & 23-31) were synthesized and characterized using spectroscopic techniques, then in vitro antioxidant and anti-prostate cancer activities were evaluated. Further, the structure of the intermediate (18) was confirmed by single crystal XRD analysis...
April 12, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28402259/the-design-of-novel-inhibitors-for-treating-cancer-by-targeting-cdc25b-through-disruption-of-cdc25b-cdk2-cyclin-a-interaction-using-computational-approaches
#18
Hong-Lian Li, Ying Ma, Ying Ma, Yu Li, Xiu-Bo Chen, Wei-Li Dong, Run-Ling Wang
Cell division cycle 25B is a key cell cycle regulator and widely considered as potent clinical drug target for cancers. This research focused on identifying potential compounds in theory which are able to disrupt transient interactions between CDC25B and its CDK2/Cyclin A substrate.By using the method of ZDOCK and RDOCK, the most optimized 3D structure of CDK2/Cyclin A in complex with CDC25B was constructed and validated using two methods: 1) the superimposition of proteins; 2) analysis of the hydrogen bond distances of Arg 488(N1)-Asp 206(OD1), Arg 492(NE)-Asp 206(OD1), Arg 492(N1)-Asp 206(OD2) and Tyr 497(NE)-Asp 210(OD1)...
March 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/28400062/adm-guidance-ceramics-guidance-to-the-use-of-fractography-in-failure-analysis-of-brittle-materials
#19
Susanne S Scherrer, Ulrich Lohbauer, Alvaro Della Bona, Alessandro Vichi, Michael J Tholey, J Robert Kelly, Richard van Noort, Paulo Francisco Cesar
OBJECTIVES: To provide background information and guidance as to how to use fractography accurately, a powerful tool for failure analysis of dental ceramic structures. METHODS: An extended palette of qualitative and quantitative fractography is provided, both for in vivo and in vitro fracture surface analyses. As visual support, this guidance document will provide micrographs of typical critical ceramic processing flaws, differentiating between pre- versus post sintering cracks, grinding damage related failures and occlusal contact wear origins and of failures due to surface degradation...
April 8, 2017: Dental Materials: Official Publication of the Academy of Dental Materials
https://www.readbyqxmd.com/read/28399135/structure-based-comprehensive-modelling-spatial-fingerprints-mapping-and-adme-screening-of-curcumin-analogues-as-novel-alr2-inhibitors
#20
Sant Kumar Verma, Suresh Thareja
Aldose reductase (ALR2) inhibition is the most legitimate approach for the management of diabetic complications. The limited triumph in the drug development against ALR2 is mainly because of its close structural similarity with the other members of aldo-keto reductase (AKR) superfamily viz. ALR1, AKR1B10; and lipophilicity problem i.e. poor diffusion of synthetic aldose reductase inhibitors (ARIs) to target tissues. The literature evidenced that naturally occurring curcumin demonstrates relatively specific and non-competitive inhibition towards human recombinant ALR2 over ALR1 and AKR1B10; however β-diketone moiety of curcumin is a specific substrate for liver AKRs and accountable for it's rapid in vivo metabolism...
2017: PloS One
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