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https://www.readbyqxmd.com/read/28727908/leveraging-a-clinical-phase-ib-proof-of-concept-study-for-the-gpr40-agonist-mk-8666-in-patients-with-type-2-diabetes-for-model-informed-phase-ii-dose-selection
#1
A W Krug, P Vaddady, R A Railkar, B J Musser, J Cote, Agh Ederveen, D G Krefetz, E DeNoia, A L Free, L Morrow, M V Chakravarthy, E Kauh, D A Tatosian, P A Kothare
GPR40 mediates free fatty acid-induced insulin secretion in beta cells. We investigated the safety, pharmacokinetics, and glucose response of MK-8666, a partial GPR40 agonist, after once-daily multiple dosing in type 2 diabetes patients. This double-blind, multisite, parallel-group study randomized 63 patients (placebo, n = 18; 50 mg, n = 9; 150 mg, n = 18; 500 mg, n = 18) for 14-day treatment. The results showed no serious adverse effects or treatment-related hypoglycemia. One patient (150-mg group) showed mild-to-moderate transaminitis at the end of dosing...
July 20, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/28726743/the-effect-of-n-terminal-cyclization-on-the-function-of-the-hiv-entry-inhibitor-5p12-rantes
#2
Anna F Nguyen, Megan S Schill, Mike Jian, Patricia J LiWang
Despite effective treatment for those living with Human Immunodeficiency Virus (HIV), there are still two million new infections each year. Protein-based HIV entry inhibitors, being highly effective and specific, could be used to protect people from initial infection. One of the most promising of these for clinical use is 5P12-RANTES, a variant of the chemokine RANTES/CCL5. The N-terminal amino acid of 5P12-RANTES is glutamine (Gln; called Q0), a residue that is prone to spontaneous cyclization when at the N-terminus of a protein...
July 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28726003/chitooligosaccharides-modified-reduction-sensitive-liposomes-enhanced-cytoplasmic-drug-delivery-and-osteosarcomas-tumor-inhibition-in-animal-models
#3
Xuelei Yin, Yingying Chi, Chuanyou Guo, Shuaishuai Feng, Jinhu Liu, Kaoxiang Sun, Zimei Wu
PURPOSE: To investigate the potential of a reduction-sensitive and fusogenic liposomes, enabled by surface-coating with chotooligosaccharides (COS) via a disulfide linker, for tumor-targeted cytoplasmic drug delivery. METHODS: COS (MW2000-5000) were chemically tethered onto the liposomes through a disulfide linker (-SS-) to cholesterol (Chol). Doxorubicin (DOX) was actively loaded in the liposomes. Their reduction-sensitivities, cellular uptake, cytotoxicity, pharmacokinetics and antitumor efficacy were investigated...
July 19, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28725364/interspecific-variation-in-persistence-of-buried-weed-seeds-follows-trade-offs-among-physiological-chemical-and-physical-seed-defenses
#4
Adam S Davis, Xianhui Fu, Brian J Schutte, Mark A Berhow, James W Dalling
Soil seedbanks drive infestations of annual weeds, yet weed management focuses largely on seedling mortality. As weed seedbanks increasingly become reservoirs of herbicide resistance, species-specific seedbank management approaches will be essential to weed control. However, the development of seedbank management strategies can only develop from an understanding of how seed traits affect persistence.We quantified interspecific trade-offs among physiological, chemical, and physical traits of weed seeds and their persistence in the soil seedbank in a common garden study...
October 2016: Ecology and Evolution
https://www.readbyqxmd.com/read/28725138/comparative-assessment-of-saliva-and-plasma-for-drug-bioavailability-and-bioequivalence-studies-in-humans
#5
Nasir M Idkaidek
Aims: To study the pharmacokinetics of selected drugs in plasma and saliva matrixes in healthy human volunteers, and to suggest using non-invasive saliva sampling instead of plasma as a surrogate in bioavailability and bioequivalence (BA/BE) studies. Methods: Four different pilot BA/BE studies were done in 12-18 healthy humans. Saliva and plasma samples were collected for 3-5 half life values of metformin, tolterodine, rosuvastatin, and paracetamol after oral dosing. Saliva and plasma samples were assayed using LC-MSMS, and then pharmacokinetic parameters were calculated by non-compartmental analysis using Kinetica program...
July 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28724926/enhanced-anti-metastatic-and-anti-tumorigenic-efficacy-of-berbamine-loaded-lipid-nanoparticles-in-vivo
#6
Priyambada Parhi, Sujit Suklabaidya, Sanjeeb Kumar Sahoo
Research on metastasis is gaining momentum for effective cancer management. Berbamine (BBM) has the potency to act as a therapeutic in multiple cancers and cancer metastasis. However, the major limitation of the compound includes poor bioavailability at the tumor site due to short plasma half-life. Here, our major objective involved development of lipid based nanoparticles (NPs) loaded with BBM with an aim to circumvent the above problem. Moreover its, therapeutic potentiality was evaluated through various in vitro cellular studies and in vivo melanoma primary and experimental lung metastatic tumor model in C57BL/6 mice...
July 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28724693/new-peptide-inhibitor-of-dipeptidyl-peptidase-iv-emdb-1-extends-the-half-life-of-glp-2-and-attenuates-colitis-in-mice-after-topical-administration
#7
Maciej Salaga, Anna Mokrowiecka, Marta Zielinska, Ewa Malecka-Panas, Radzislaw Kordek, Elzbieta Kamysz, Jakub Fichna
Protease inhibition has become a new possible approach in the inflammatory bowel disease (IBD) therapy. A serine exopeptidase, dipeptidyl peptidase IV (DPP IV) is responsible for inactivation of incretine hormone, glucagon-like peptide 2 (GLP-2), a potent stimulator of intestinal epithelium regeneration and growth. Recently we showed that the novel peptide analog of endomorphin-2, EMDB-1 is a potent blocker of DPP IV and has an inhibitory effect on gastrointestinal (GI) smooth muscle contractility. The aim of this study was to characterize the anti-inflammatory effect and mechanism of action of EMDB-1 in the mouse GI tract...
July 19, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28724494/pharmacokinetics-of-a-novel-transdermal-fentanyl-solution-in-rhesus-macaques-macaca-mulatta
#8
Gregory W Salyards, Marie-Josee Lemoy, Heather K Knych, Ashley E Hill, Kari L Christe
Rhesus macaques (Macaca mulatta) are the most commonly used NHP biomedical model and experience both research and clinical procedures requiring analgesia. Opioids are a mainstay of analgesic therapy. A novel, transdermal fentanyl solution (TFS) has been developed as a long-acting, single-administration topical opioid and was reported to provide at least 4 d of effective plasma concentrations in beagles (Canis familiaris). To evaluate the pharmacokinetic profile of TFS in healthy adult rhesus macaques, we used a 2-period, 2-treatment crossover study of a single topical administration of 1...
July 1, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28724091/effect-of-environmental-conditions-on-the-degradation-of-florasulam-in-typical-soils-of-northern-china
#9
Wangcang Su, Hongle Xu, Hongdan Hao, Renhai Wu, Hengliang Wang, Chuantao Lu
The widespread use of florasulam in China makes residues from this herbicide in soil a serious concern due to their potential to pollute the soil environment and groundwater. Accelerating the degradation of these residues will reduce their pollution potential. In this study, we investigated the degradation and adsorption of florasulam in four typical soils in northern China and examined the degradation of florasulam in Inceptisols at different temperatures, soil moisture contents, and pH values, as well as the influence of microorganisms and the use of organic matter and biogas slurry as soil amendments...
May 2017: Journal of Environmental Quality
https://www.readbyqxmd.com/read/28722819/self-targeting-immune-transparent-plasma-protein-coated-nanocomplex-for-noninvasive-photothermal-anticancer-therapy
#10
Fwu-Long Mi, Thierry Burnouf, Shih-Yuan Lu, Yu-Jen Lu, Kun-Ying Lu, Yi-Cheng Ho, Chang-Yi Kuo, Er-Yuan Chuang
Cancer cells exhibit specific physiological differences compared to normal cells. Most surface membranes of cancer cells are characterized by high expression of given protein receptors, such as albumin, transferrin, and growth factors that are also present in the plasma of patients themselves, but are lacking on the surface of normal cells. These distinct features between cancer and normal cells can serve as a niche for developing specific treatment strategies. Near-infrared (NIR)-light-triggered therapy platforms are an interesting novel avenue for use in clinical nanomedicine...
July 2017: Advanced Healthcare Materials
https://www.readbyqxmd.com/read/28721611/bone-targeting-parathyroid-hormone-conjugates-outperform-unmodified-pth-in-the-anabolic-treatment-of-osteoporosis-in-rats
#11
Yang Yang, Ali Aghazadeh-Habashi, Arash Panahifar, Yuchin Wu, Krishna H Bhandari, Michael R Doschak
Synthetic parathyroid hormone (PTH) is clinically indicated for the treatment of osteoporosis, through its anabolic effects on parathyroid hormone receptors (PTHRs), located on osteoblast cells. However, the bioavailability of PTH for bone cells is restricted by the short half-life of PTH and the widespread distribution of PTHRs in non-skeletal tissues. To impart affinity for mineralized bone surfaces, bisphosphonate (BP)-mediated PTH analogues were synthesized, characterized, and evaluated in vitro and in vivo...
July 18, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28721592/construction-purification-and-characterization-of-a-homodimeric-granulocyte-colony-stimulating-factor
#12
Gitana Mickiene, Indre Dalgediene, Zilvinas Dapkunas, Gintautas Zvirblis, Henrikas Pesliakas, Algirdas Kaupinis, Mindaugas Valius, Edita Mistiniene, Milda Pleckaityte
Granulocyte colony-stimulating factor (G-CSF) has found widespread clinical application, and modified forms with improved biopharmaceutical properties have been marketed as well. PEGylation, the covalent modification of G-CSF with polyethylene glycol (PEG), has a beneficial effect on drug properties, but there are concerns connected to the immunogenicity of PEGylated compounds and bioaccumulation of the synthetic polymer. To overcome challenges connected with chemical modifications, we developed fusion proteins composed of two G-CSF molecules connected via different peptide linkers...
July 18, 2017: Molecular Biotechnology
https://www.readbyqxmd.com/read/28720966/biochemical-characterization-and-thermal-inactivation-of-polyphenol-oxidase-from-elephant-foot-yam-amorphophallus-paeoniifolius
#13
Anuradha Singh, Neeraj Wadhwa
Polyphenol oxidase from Amorphophallus corm was purified (5.54 fold) by acetone precipitation and ion exchange chromatography. Electrophoretic-blot analysis revealed that the molecular weight of enzyme is 40 kDa. Enzyme preferred catechol as substrate and showed optimum activity at pH 6 and 35 °C with Km of 17.56 mM and Vmax 0.023 U/ml/min. Thermal inactivation kinetics study showed that 5.68% inactivation was achieved at 75 °C within 40 min. The half-life time of PPO is between 126.00 and 32.54 min...
June 2017: Journal of Food Science and Technology
https://www.readbyqxmd.com/read/28719664/predicting-the-protein-half-life-in-tissue-from-its-cellular-properties
#14
Mahbubur Rahman, Rovshan G Sadygov
Protein half-life is an important feature of protein homeostasis (proteostasis). The increasing number of in vivo and in vitro studies using high throughput proteomics provide estimates of the protein half-lives in tissues and cells. However, protein half-lives in cells and tissues are different. Due to the resource requirements for researching tissues, more data is available from cellular studies than tissues. We have designed a multivariate linear model for predicting protein half-life in tissue from its cellular properties...
2017: PloS One
https://www.readbyqxmd.com/read/28719640/short-lived-long-non-coding-rnas-as-surrogate-indicators-for-chemical-exposure-and-linc00152-and-malat1-modulate-their-neighboring-genes
#15
Hidenori Tani, Sayaka Okuda, Kaoru Nakamura, Motohide Aoki, Tomonari Umemura
Whole transcriptome analyses have revealed a large number of novel long non-coding RNAs (lncRNAs). Although accumulating evidence demonstrates that lncRNAs play important roles in regulating gene expression, the detailed mechanisms of action of most lncRNAs remain unclear. We previously reported that a novel class of lncRNAs with a short half-life (t1/2 < 4 h) in HeLa cells, termed short-lived non-coding transcripts (SLiTs), are closely associated with physiological and pathological functions. In this study, we focused on 26 SLiTs and nuclear-enriched abundant lncRNA, MALAT1(t1/2 of 7...
2017: PloS One
https://www.readbyqxmd.com/read/28719152/a-first-in-human-phase-i-multicenter-open-label-dose-escalation-study-of-the-oral-raf-vegfr-2-inhibitor-raf265-in-locally-advanced-or-metastatic-melanoma-independent-from-braf-mutation-status
#16
Benjamin Izar, William Sharfman, F Stephen Hodi, Donald Lawrence, Keith T Flaherty, Ravi Amaravadi, Kevin B Kim, Igor Puzanov, Jeffrey Sosman, Reinhard Dummer, Simone M Goldinger, Lyhping Lam, Shefali Kakar, Zhongwen Tang, Oliver Krieter, David F McDermott, Michael B Atkins
To establish the maximum tolerated dose (MTD), dose-limiting toxicities (DLT), safety profile, and anti-tumor efficacy of RAF265. We conducted a multicenter, open-label, phase-I, dose-escalation trial of RAF265, an orally available RAF kinase/VEGFR-2 inhibitor, in patients with advanced or metastatic melanoma. Pharmacokinetic (PK) analysis, pharmacodynamics (PD) and tumor response assessment were conducted. We evaluated metabolic tumor response by 18[F]-fluorodeoxyglucose-positron-emission tomography (FDG-PET), tissue biomarkers using immunohistochemistry (IHC), and modulators of angiogenesis...
July 18, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28718021/evidence-for-photolytic-and-microbial-degradation-processes-in-the-dissipation-of-leptospermone-a-natural-%C3%AE-triketone-herbicide
#17
Sana Romdhane, Marion Devers-Lamrani, Fabrice Martin-Laurent, Amani Ben Jrad, Delphine Raviglione, Marie-Virginie Salvia, Pascale Besse-Hoggan, Franck E Dayan, Cédric Bertrand, Lise Barthelmebs
Bioherbicides appear as an ecofriendly alternative to synthetic herbicides, generally used for weed management, because they are supposed to have low side on human health and ecosystems. In this context, our work aims to study abiotic (i.e., photolysis) and biotic (i.e,. biodegradation) processes involved in the fate of leptospermone, a natural β-triketone herbicide, by combining chemical and microbiological approaches. Under controlled conditions, the photolysis of leptospermone was sensitive to pH. Leptospermone has a half-life of 72 h under simulated solar light irradiations...
July 17, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28717654/fusion-to-flaviviral-leader-peptide-targets-hiv-1-reverse-transcriptase-for-secretion-and-reduces-its-enzymatic-activity-and-ability-to-induce-oxidative-stress-but-has-no-major-effects-on-its-immunogenic-performance-in-dna-immunized-mice
#18
Anastasia Latanova, Stefan Petkov, Yulia Kuzmenko, Athina Kilpeläinen, Alexander Ivanov, Olga Smirnova, Olga Krotova, Sergey Korolev, Jorma Hinkula, Vadim Karpov, Maria Isaguliants, Elizaveta Starodubova
Reverse transcriptase (RT) is a key enzyme in viral replication and susceptibility to ART and a crucial target of immunotherapy against drug-resistant HIV-1. RT induces oxidative stress which undermines the attempts to make it immunogenic. We hypothesized that artificial secretion may reduce the stress and make RT more immunogenic. Inactivated multidrug-resistant RT (RT1.14opt-in) was N-terminally fused to the signal providing secretion of NS1 protein of TBEV (Ld) generating optimized inactivated Ld-carrying enzyme RT1...
2017: Journal of Immunology Research
https://www.readbyqxmd.com/read/28717351/serial-sampling-of-serum-protein-biomarkers-for-monitoring-human-traumatic-brain-injury-dynamics-a-systematic-review
#19
REVIEW
Eric Peter Thelin, Frederick Adam Zeiler, Ari Ercole, Stefania Mondello, András Büki, Bo-Michael Bellander, Adel Helmy, David K Menon, David W Nelson
BACKGROUND: The proteins S100B, neuron-specific enolase (NSE), glial fibrillary acidic protein (GFAP), ubiquitin carboxy-terminal hydrolase L1 (UCH-L1), and neurofilament light (NF-L) have been serially sampled in serum of patients suffering from traumatic brain injury (TBI) in order to assess injury severity and tissue fate. We review the current literature of serum level dynamics of these proteins following TBI and used the term "effective half-life" (t1/2) in order to describe the "fall" rate in serum...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28717204/a-drug-carrier-for-sustained-zero-order-release-of-peptide-therapeutics
#20
Ya-Nan Zhao, Xiaoyu Xu, Na Wen, Rui Song, Qingbin Meng, Ying Guan, Siqi Cheng, Danni Cao, Yansheng Dong, Jiankun Qie, Keliang Liu, Yongjun Zhang
Peptides have great potential as therapeutic agents, however, their clinic applications are severely hampered by their instability and short circulation half-life. Zero-order release carriers could not only extend the circulation lifetime of peptides, but also maintain the plasma drug level constant, and thus maximize their therapeutic efficacy and minimize their toxic effect. Here using PEGylated salmon calcitonin (PEG-sCT)/tannic acid (TA) film as an example, we demonstrated that hydrogen-bonded layer-by-layer films of a PEGylated peptide and a polyphenol could be a platform for zero-order peptide release...
July 17, 2017: Scientific Reports
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