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Dongguk University

UniversitySeoul, Seoul, South Korea

Research output, citation impact, and the most-cited recent papers from Dongguk University (South Korea). Aggregated across the NobleBlocks index of 300M+ scholarly works.

Total works
28.3K
Citations
1.4M
h-index
306
i10-index
28.6K
Also known as
Dongguk University동국대학교

Top-cited papers from Dongguk University

Nano based drug delivery systems: recent developments and future prospects
Jayanta Kumar Patra, Gitishree Das, Leonardo Fernandes Fraceto, Estefânia Vangelie Ramos Campos +4 more
2018· Journal of Nanobiotechnology6.5Kdoi:10.1186/s12951-018-0392-8

Nanomedicine and nano delivery systems are a relatively new but rapidly developing science where materials in the nanoscale range are employed to serve as means of diagnostic tools or to deliver therapeutic agents to specific targeted sites in a controlled manner. Nanotechnology offers multiple benefits in treating chronic human diseases by site-specific, and target-oriented delivery of precise medicines. Recently, there are a number of outstanding applications of the nanomedicine (chemotherapeutic agents, biological agents, immunotherapeutic agents etc.) in the treatment of various diseases. The current review, presents an updated summary of recent advances in the field of nanomedicines and nano based drug delivery systems through comprehensive scrutiny of the discovery and application of nanomaterials in improving both the efficacy of novel and old drugs (e.g., natural products) and selective diagnosis through disease marker molecules. The opportunities and challenges of nanomedicines in drug delivery from synthetic/natural sources to their clinical applications are also discussed. In addition, we have included information regarding the trends and perspectives in nanomedicine area.

The Role of Tumor Necrosis Factor Alpha (TNF-α) in Autoimmune Disease and Current TNF-α Inhibitors in Therapeutics
Dan-in Jang, A-Hyeon Lee, Hye-Yoon Shin, Hyo-Ryeong Song +4 more
2021· International Journal of Molecular Sciences1.6Kdoi:10.3390/ijms22052719

Tumor necrosis factor alpha (TNF-α) was initially recognized as a factor that causes the necrosis of tumors, but it has been recently identified to have additional important functions as a pathological component of autoimmune diseases. TNF-α binds to two different receptors, which initiate signal transduction pathways. These pathways lead to various cellular responses, including cell survival, differentiation, and proliferation. However, the inappropriate or excessive activation of TNF-α signaling is associated with chronic inflammation and can eventually lead to the development of pathological complications such as autoimmune diseases. Understanding of the TNF-α signaling mechanism has been expanded and applied for the treatment of immune diseases, which has resulted in the development of effective therapeutic tools, including TNF-α inhibitors. Currently, clinically approved TNF-α inhibitors have shown noticeable potency in a variety of autoimmune diseases, and novel TNF-α signaling inhibitors are being clinically evaluated. In this review, we briefly introduce the impact of TNF-α signaling on autoimmune diseases and its inhibitors, which are used as therapeutic agents against autoimmune diseases.

Organic Light Detectors: Photodiodes and Phototransistors
Kang‐Jun Baeg, Maddalena Binda, Dario Natali, Mario Caironi +1 more
2013· Advanced Materials1.3Kdoi:10.1002/adma.201204979

While organic electronics is mostly dominated by light-emitting diodes, photovoltaic cells and transistors, optoelectronics properties peculiar to organic semiconductors make them interesting candidates for the development of innovative and disruptive applications also in the field of light signal detection. In fact, organic-based photoactive media combine effective light absorption in the region of the spectrum from ultraviolet to near-infrared with good photogeneration yield and low-temperature processability over large areas and on virtually every substrate, which might enable innovative optoelectronic systems to be targeted for instance in the field of imaging, optical communications or biomedical sensing. In this review, after a brief resume of photogeneration basics and of devices operation mechanisms, we offer a broad overview of recent progress in the field, focusing on photodiodes and phototransistors. As to the former device category, very interesting values for figures of merit such as photoconversion efficiency, speed and minimum detectable signal level have been attained, and even though the simultaneous optimization of all these relevant parameters is demonstrated in a limited number of papers, real applications are within reach for this technology, as it is testified by the increasing number of realizations going beyond the single-device level and tackling more complex optoelectronic systems. As to phototransistors, a more recent subject of study in the framework of organic electronics, despite a broad distribution in the reported performances, best photoresponsivities outperform amorphous silicon-based devices. This suggests that organic phototransistors have a large potential to be used in a variety of optoelectronic peculiar applications, such as a photo-sensor, opto-isolator, image sensor, optically controlled phase shifter, and opto-electronic switch and memory.

Aquaporins in the Kidney: From Molecules to Medicine
Søren Nielsen, Jørgen Frøkiær, David Marples, Tae‐Hwan Kwon +2 more
2002· Physiological Reviews1.2Kdoi:10.1152/physrev.00024.2001

The discovery of aquaporin-1 (AQP1) answered the long-standing biophysical question of how water specifically crosses biological membranes. In the kidney, at least seven aquaporins are expressed at distinct sites. AQP1 is extremely abundant in the proximal tubule and descending thin limb and is essential for urinary concentration. AQP2 is exclusively expressed in the principal cells of the connecting tubule and collecting duct and is the predominant vasopressin-regulated water channel. AQP3 and AQP4 are both present in the basolateral plasma membrane of collecting duct principal cells and represent exit pathways for water reabsorbed apically via AQP2. Studies in patients and transgenic mice have demonstrated that both AQP2 and AQP3 are essential for urinary concentration. Three additional aquaporins are present in the kidney. AQP6 is present in intracellular vesicles in collecting duct intercalated cells, and AQP8 is present intracellularly at low abundance in proximal tubules and collecting duct principal cells, but the physiological function of these two channels remains undefined. AQP7 is abundant in the brush border of proximal tubule cells and is likely to be involved in proximal tubule water reabsorption. Body water balance is tightly regulated by vasopressin, and multiple studies now have underscored the essential roles of AQP2 in this. Vasopressin regulates acutely the water permeability of the kidney collecting duct by trafficking of AQP2 from intracellular vesicles to the apical plasma membrane. The long-term adaptational changes in body water balance are controlled in part by regulated changes in AQP2 and AQP3 expression levels. Lack of functional AQP2 is seen in primary forms of diabetes insipidus, and reduced expression and targeting are seen in several diseases associated with urinary concentrating defects such as acquired nephrogenic diabetes insipidus, postobstructive polyuria, as well as acute and chronic renal failure. In contrast, in conditions with water retention such as severe congestive heart failure, pregnancy, and syndrome of inappropriate antidiuretic hormone secretion, both AQP2 expression levels and apical plasma membrane targetting are increased, suggesting a role for AQP2 in the development of water retention. Continued analysis of the aquaporins is providing detailed molecular insight into the fundamental physiology and pathophysiology of water balance and water balance disorders.

A survey on LPWA technology: LoRa and NB-IoT
Rashmi Sharan Sinha, Yiqiao Wei, Seung-Hoon Hwang
2017· ICT Express996doi:10.1016/j.icte.2017.03.004

By 2020, more than twenty five billion devices would be connected through wireless communications. In accordance with the rapid growth of the internet of things (IoT) market, low power wide area (LPWA) technologies have become popular. In various LPWA technologies, narrowband (NB)-IoT and long range (LoRa) are two leading technologies. In this paper, we provide a comprehensive survey on NB-IoT and LoRa as efficient solutions connecting the devices. It is shown that unlicensed LoRa has advantages in terms of battery lifetime, capacity, and cost. Meanwhile, licensed NB-IoT offers benefits in terms of QoS, latency, reliability, and range.

Structural Changes and Thermal Stability of Charged LiNi<sub><i>x</i></sub>Mn<sub><i>y</i></sub>Co<sub><i>z</i></sub>O<sub>2</sub> Cathode Materials Studied by Combined <i>In Situ</i> Time-Resolved XRD and Mass Spectroscopy
Seong‐Min Bak, Enyuan Hu, Yong‐Ning Zhou, Xiqian Yu +4 more
2014· ACS Applied Materials & Interfaces974doi:10.1021/am506712c

Thermal stability of charged LiNixMnyCozO2 (NMC, with x + y + z = 1, x:y:z = 4:3:3 (NMC433), 5:3:2 (NMC532), 6:2:2 (NMC622), and 8:1:1 (NMC811)) cathode materials is systematically studied using combined in situ time-resolved X-ray diffraction and mass spectroscopy (TR-XRD/MS) techniques upon heating up to 600 °C. The TR-XRD/MS results indicate that the content of Ni, Co, and Mn significantly affects both the structural changes and the oxygen release features during heating: the more Ni and less Co and Mn, the lower the onset temperature of the phase transition (i.e., thermal decomposition) and the larger amount of oxygen release. Interestingly, the NMC532 seems to be the optimized composition to maintain a reasonably good thermal stability, comparable to the low-nickel-content materials (e.g., NMC333 and NMC433), while having a high capacity close to the high-nickel-content materials (e.g., NMC811 and NMC622). The origin of the thermal decomposition of NMC cathode materials was elucidated by the changes in the oxidation states of each transition metal (TM) cations (i.e., Ni, Co, and Mn) and their site preferences during thermal decomposition. It is revealed that Mn ions mainly occupy the 3a octahedral sites of a layered structure (R3̅m) but Co ions prefer to migrate to the 8a tetrahedral sites of a spinel structure (Fd3̅m) during the thermal decomposition. Such element-dependent cation migration plays a very important role in the thermal stability of NMC cathode materials. The reasonably good thermal stability and high capacity characteristics of the NMC532 composition is originated from the well-balanced ratio of nickel content to manganese and cobalt contents. This systematic study provides insight into the rational design of NMC-based cathode materials with a desired balance between thermal stability and high energy density.

Characteristics of Gintonin-Mediated Membrane Depolarization of Pacemaker Activity in Cultured Interstitial Cells of Cajal
Byung Joo Kim, Joo‐Hyun Nam, Kyun Ha Kim, Myungsoo Joo +4 more
2014· Cellular Physiology and Biochemistry892doi:10.1159/000366306

BACKGROUND/AIMS: Ginseng regulates gastrointestinal (GI) motor activity but the underlying components and molecular mechanisms are unknown. We investigated the effect of gintonin, a novel ginseng-derived G protein-coupled lysophosphatidic acid (LPA) receptor ligand, on the pacemaker activity of the interstitial cells of Cajal (ICC) in murine small intestine and GI motility. MATERIALS AND METHODS: Enzymatic digestion was used to dissociate ICC from mouse small intestines. The whole-cell patch-clamp configuration was used to record pacemaker potentials and currents from cultured ICC in the absence or presence of gintonin. In vivo effects of gintonin on gastrointestinal (GI) motility were investigated by measuring the intestinal transit rate (ITR) of Evans blue in normal and streptozotocin (STZ)-induced diabetic mice. RESULTS: We investigated the effects of gintonin on pacemaker potentials and currents in cultured ICC from mouse small intestine. Gintonin caused membrane depolarization in current clamp mode but this action was blocked by Ki16425, an LPA1/3 receptor antagonist, and by the addition of GDPβS, a GTP-binding protein inhibitor, into the ICC. To study the gintonin signaling pathway, we examined the effects of U-73122, an active PLC inhibitor, and chelerythrine and calphostin, which inhibit PKC. All inhibitors blocked gintonin actions on pacemaker potentials, but not completely. Gintonin-mediated depolarization was lower in Ca(2+)-free than in Ca(2+)-containing external solutions and was blocked by thapsigargin. We found that, in ICC, gintonin also activated Ca(2+)-activated Cl(-) channels (TMEM16A, ANO1), but not TRPM7 channels. In vivo, gintonin (10-100 mg/kg, p.o.) not only significantly increased the ITR in normal mice but also ameliorated STZ-induced diabetic GI motility retardation in a dose-dependent manner. CONCLUSIONS: Gintonin-mediated membrane depolarization of pacemaker activity and ANO1 activation are coupled to the stimulation of GI contractility through LPA1/3 receptor signaling pathways in cultured murine ICC. Gintonin might be a ingredient responsible for ginseng-mediated GI tract modulations, and could be a novel candidate for development as a prokinetic agent that may prevent or alleviate GI motility dysfunctions in human patients.

Intrinsic Tryptophan Fluorescence in the Detection and Analysis of Proteins: A Focus on Förster Resonance Energy Transfer Techniques
Amar B. T. Ghisaidoobe, Sang M. Chung
2014· International Journal of Molecular Sciences887doi:10.3390/ijms151222518

Förster resonance energy transfer (FRET) occurs when the distance between a donor fluorophore and an acceptor is within 10 nm, and its application often necessitates fluorescent labeling of biological targets. However, covalent modification of biomolecules can inadvertently give rise to conformational and/or functional changes. This review describes the application of intrinsic protein fluorescence, predominantly derived from tryptophan (λ EX ≈ 280 nm, λ EM ≈ 350 nm), in protein-related research and mainly focuses on label-free FRET techniques. In terms of wavelength and intensity, tryptophan fluorescence is strongly influenced by its (or the proteinlocal environment, which, in addition to fluorescence quenching, has been applied to study protein conformational changes. Intrinsic Förster resonance energy transfer (iFRET), a recently developed technique, utilizes the intrinsic fluorescence of tryptophan in conjunction with target-specific fluorescent probes as FRET donors and acceptors, respectively, for real time detection of native proteins.

Benefaction of probiotics for human health: A review
Rout George Kerry, Jayanta Kumar Patra, Sushanto Gouda, Yooheon Park +2 more
2018· Journal of Food and Drug Analysis877doi:10.1016/j.jfda.2018.01.002

Humans are a unique reservoir of heterogeneous and vivacious group of microbes, which together forms the human-microbiome superorganism. Human gut serves as a home to over 100-1000 microbial species, which primarily modulate the host internal environment and thereby, play a major role in host health. This spectacular symbiotic relationship has attracted extensive research in this field. More specifically, these organisms play key roles in defense function, eupepsia along with catabolism and anabolism, and impact brain-gut responses. The emergence of microbiota with resistance and tolerance to existing conventional drugs and antibiotics has decreased the drug efficacies. Furthermore, the modern biotechnology mediated nano-encapsulated multiplex supplements appear to be high cost and inconvenient. Henceforth, a simple, low-cost, receptive and intrinsic approach to achieve health benefits is vital in the present era. Supplementation with probiotics, prebiotics, and synbiotics has shown promising results against various enteric pathogens due to their unique ability to compete with pathogenic microbiota for adhesion sites, to alienate pathogens or to stimulate, modulate and regulate the host's immune response by initiating the activation of specific genes in and outside the host intestinal tract. Probiotics have also been shown to regulate fat storage and stimulate intestinal angiogenesis. Hence, this study aims to underline the possible beneficial impact of probiotics for human health and medical sectors and for better lifestyle.

Endophytes: A Treasure House of Bioactive Compounds of Medicinal Importance
Sushanto Gouda, Gitishree Das, Sandeep K. Sen, Han‐Seung Shin +1 more
2016· Frontiers in Microbiology846doi:10.3389/fmicb.2016.01538

Endophytes are an endosymbiotic group of microorganisms that colonize in plants and microbes that can be readily isolated from any microbial or plant growth medium. They act as reservoirs of novel bioactive secondary metabolites, such as alkaloids, phenolic acids, quinones, steroids, saponins, tannins, and terpenoids that serve as a potential candidate for antimicrobial, anti-insect, anticancer and many more properties. While plant sources are being extensively explored for new chemical entities for therapeutic purposes, endophytic microbes also constitute an important source for drug discovery. This review aims to comprehend the contribution and uses of endophytes as an impending source of drugs against various forms of diseases and other possible medicinal use.

True Meaning of Pseudocapacitors and Their Performance Metrics: Asymmetric versus Hybrid Supercapacitors
Nilesh R. Chodankar, Hong Duc Pham, Ashok Kumar Nanjundan, Joseph F. S. Fernando +4 more
2020· Small822doi:10.1002/smll.202002806

The development of pseudocapacitive materials for energy-oriented applications has stimulated considerable interest in recent years due to their high energy-storing capacity with high power outputs. Nevertheless, the utilization of nanosized active materials in batteries leads to fast redox kinetics due to the improved surface area and short diffusion pathways, which shifts their electrochemical signatures from battery-like to the pseudocapacitive-like behavior. As a result, it becomes challenging to distinguish "pseudocapacitive" and "battery" materials. Such misconceptions have further impacted on the final device configurations. This Review is an earnest effort to clarify the confusion between the battery and pseudocapacitive materials by providing their true meanings and correct performance metrics. A method to distinguish battery-type and pseudocapacitive materials using the electrochemical signatures and quantitative kinetics analysis is outlined. Taking solid-state supercapacitors (SSCs, only polymer gel electrolytes) as an example, the distinction between asymmetric and hybrid supercapacitors is discussed. The state-of-the-art progress in the engineering of active materials is summarized, which will guide for the development of real-pseudocapacitive energy storage systems.

Dendritic Nanostructured Waste Copper Wires for High-Energy Alkaline Battery
Nilesh R. Chodankar, Su‐Hyeon Ji, Young‐Kyu Han, Do‐Heyoung Kim
2019· Nano-Micro Letters770doi:10.1007/s40820-019-0337-2

Abstract Rechargeable alkaline batteries (RABs) have received remarkable attention in the past decade for their high energy, low cost, safe operation, facile manufacture, and eco-friendly nature. To date, expensive electrode materials and current collectors were predominantly applied for RABs, which have limited their real-world efficacy. In the present work, we propose a scalable process to utilize electronic waste (e-waste) Cu wires as a cost-effective current collector for high-energy wire-type RABs. Initially, the vertically aligned CuO nanowires were prepared over the waste Cu wires via in situ alkaline corrosion. Then, both atomic-layer-deposited NiO and NiCo-hydroxide were applied to the CuO nanowires to form a uniform dendritic-structured NiCo-hydroxide/NiO/CuO/Cu electrode. When the prepared dendritic-structured electrode was applied to the RAB, it showed excellent electrochemical features, namely high-energy-density (82.42 Wh kg −1 ), excellent specific capacity (219 mAh g −1 ), and long-term cycling stability (94% capacity retention over 5000 cycles). The presented approach and material meet the requirements of a cost-effective, abundant, and highly efficient electrode for advanced eco-friendly RABs. More importantly, the present method provides an efficient path to recycle e-waste for value-added energy storage applications.

Person Recognition System Based on a Combination of Body Images from Visible Light and Thermal Cameras
Dat Nguyen, Hyung Hong, Ki Hyun Kim, Kang Park
2017· Sensors767doi:10.3390/s17030605

The human body contains identity information that can be used for the person recognition (verification/recognition) problem. In this paper, we propose a person recognition method using the information extracted from body images. Our research is novel in the following three ways compared to previous studies. First, we use the images of human body for recognizing individuals. To overcome the limitations of previous studies on body-based person recognition that use only visible light images for recognition, we use human body images captured by two different kinds of camera, including a visible light camera and a thermal camera. The use of two different kinds of body image helps us to reduce the effects of noise, background, and variation in the appearance of a human body. Second, we apply a state-of-the art method, called convolutional neural network (CNN) among various available methods, for image features extraction in order to overcome the limitations of traditional hand-designed image feature extraction methods. Finally, with the extracted image features from body images, the recognition task is performed by measuring the distance between the input and enrolled samples. The experimental results show that the proposed method is efficient for enhancing recognition accuracy compared to systems that use only visible light or thermal images of the human body.

Recent advances in polymeric drug delivery systems
Yong Kiel Sung, Sung Wan Kim
2020· Biomaterials Research708doi:10.1186/s40824-020-00190-7

BACKGROUND: Polymeric drug delivery systems have been achieved great development in the last two decades. Polymeric drug delivery has defined as a formulation or a device that enables the introduction of a therapeutic substance into the body. Biodegradable and bio-reducible polymers make the magic possible choice for lot of new drug delivery systems. The future prospects of the research for practical applications has required for the development in the field. MAIN BODY: Natural polymers such as arginine, chitosan, dextrin, polysaccharides, poly (glycolic acid), poly (lactic acid), and hyaluronic acid have been treated for polymeric drug delivery systems. Synthetic polymers such as poly (2-hydroxyethyl methacrylate), poly(N-isopropyl acrylamide)s, poly(ethylenimine)s, dendritic polymers, biodegradable and bio-absorbable polymers have been also discussed for polymeric drug delivery. Targeting polymeric drug delivery, biomimetic and bio-related polymeric systems, and drug-free macromolecular therapeutics have also treated for polymeric drug delivery. In polymeric gene delivery systems, virial vectors and non-virial vectors for gene delivery have briefly analyzed. The systems of non-virial vectors for gene delivery are polyethylenimine derivatives, polyethylenimine copolymers, and polyethylenimine conjugated bio-reducible polymers, and the systems of virial vectors are DNA conjugates and RNA conjugates for gene delivery. CONCLUSION: The development of polymeric drug delivery systems that have based on natural and synthetic polymers are rapidly emerging to pharmaceutical fields. The fruitful progresses have made in the application of biocompatible and bio-related copolymers and dendrimers to cancer treatment, including their use as delivery systems for potent anticancer drugs. Combining perspectives from the synthetic and biological fields will provide a new paradigm for the design of polymeric drug and gene delivery systems.

Pesticides in Drinking Water—A Review
Muhammad Syafrudin, Risky Ayu Kristanti, Adhi Yuniarto, Tony Hadibarata +4 more
2021· International Journal of Environmental Research and Public Health697doi:10.3390/ijerph18020468

The ubiquitous problem of pesticide in aquatic environment are receiving worldwide concern as pesticide tends to accumulate in the body of the aquatic organism and sediment soil, posing health risks to the human. Many pesticide formulations had introduced due to the rapid growth in the global pesticide market result from the wide use of pesticides in agricultural and non-agricultural sectors. The occurrence of pesticides in the water body is derived by the runoff from the agricultural field and industrial wastewater. Soluble pesticides were carried away by water molecules especially during the precipitation event by percolating downward into the soil layers and eventually reach surface waters and groundwater. Consequently, it degrades water quality and reduces the supply of clean water for potable water. Long-time exposure to the low concentration of pesticides had resulted in non-carcinogenic health risks. The conventional method of pesticide treatment processes encompasses coagulation-flocculation, adsorption, filtration and sedimentation, which rely on the phase transfer of pollutants. Those methods are often incurred with a relatively high operational cost and may cause secondary pollution such as sludge formation. Advanced oxidation processes (AOPs) are recognized as clean technologies for the treatment of water containing recalcitrant and bio-refractory pollutants such as pesticides. It has been adopted as recent water purification technology because of the thermodynamic viability and broad spectrum of applicability. This work provides a comprehensive review for occurrence of pesticide in the drinking water and its possible treatment.

An Overview of Carcinogenic Heavy Metal: Molecular Toxicity Mechanism and Prevention
Hyun Soo Kim, Yeo Jin Kim, Young Rok Seo
2015· Journal of Cancer Prevention674doi:10.15430/jcp.2015.20.4.232

Almost all heavy metals are serious toxicants as carcinogens. However, due to their chemical and physiological properties, heavy metals are useful in industrial areas including alloy, smelting and production of commercial products. Such applications increase the opportunity for heavy metal exposure. Waste from industrial processes is also a major source of environmental contamination and accumulation in the human body. Arsenic, cadmium, chromium, and nickel are classified as group 1 carcinogens by the International Agency for Research on Cancer, and are utilized commercially. In this review, we used molecular pathway analysis to understand the toxicity and carcinogenic mechanisms of these metals. Our analyzed data showed that above-mentioned metallic substances induce oxidative stress, DNA damage, and cell death processes, resulting in increase the risk of cancer and cancer-related diseases. Thus, we might think phytochelatin molecules and antioxidative phytochemical substances are helpful for prevention of heavy metal-induced cancer.

Application of Nanotechnology in Food Science: Perception and Overview
Trepti Singh, Shruti Shukla, Pradeep Kumar, Verinder Wahla +2 more
2017· Frontiers in Microbiology643doi:10.3389/fmicb.2017.01501

Recent innovations in nanotechnology have transformed a number of scientific and industrial areas including the food industry. Applications of nanotechnology have emerged with increasing need of nanoparticle uses in various fields of food science and food microbiology, including food processing, food packaging, functional food development, food safety, detection of foodborne pathogens, and shelf-life extension of food and/or food products. This review summarizes the potential of nanoparticles for their uses in the food industry in order to provide consumers a safe and contamination free food and to ensure the consumer acceptability of the food with enhanced functional properties. Aspects of application of nanotechnology in relation to increasing in food nutrition and organoleptic properties of foods have also been discussed briefly along with a few insights on safety issues and regulatory concerns on nano-processed food products.

ABC Transporters in Multidrug Resistance and Pharmacokinetics, and Strategies for Drug Development
Young Hee Choi, Ai‐Ming Yu
2014· Current Pharmaceutical Design636doi:10.2174/138161282005140214165212

Multidrug resistance (MDR) is a serious problem that hampers the success of cancer pharmacotherapy. A common mechanism is the overexpression of ATP-binding cassette (ABC) efflux transporters in cancer cells such as P-glycoprotein (P-gp/ABCB1), multidrug resistance-associated protein 1 (MRP1/ABCC1) and breast cancer resistance protein (BCRP/ABCG2) that limit the exposure to anticancer drugs. One way to overcome MDR is to develop ABC efflux transporter inhibitors to sensitize cancer cells to chemotherapeutic drugs. The complete clinical trials thus far have showen that those tested chemosensitizers only add limited or no benefits to cancer patients. Some MDR modulators are merely toxic, and others induce unwanted drug-drug interactions. Actually, many ABC transporters are also expressed abundantly in the gastrointestinal tract, liver, kidney, brain and other normal tissues, and they largely determine drug absorption, distribution and excretion, and affect the overall pharmacokinetic properties of drugs in humans. In addition, ABC transporters such as P-gp, MRP1 and BCRP co-expressed in tumors show a broad and overlapped specificity for substrates and MDR modulators. Thus reliable preclinical assays and models are required for the assessment of transporter-mediated flux and potential effects on pharmacokinetics in drug development. In this review, we provide an overview of the role of ABC efflux transporters in MDR and pharmacokinetics. Preclinical assays for the assessment of drug transport and development of MDR modulators are also discussed.

Efficacy and safety of canagliflozin monotherapy in subjects with type 2 diabetes mellitus inadequately controlled with diet and exercise
Kaj Stenlöf, William T. Cefalu, Kyung‐Ah Kim, Maria Alba +4 more
2012· Diabetes Obesity and Metabolism611doi:10.1111/dom.12054

AIMS: Canagliflozin is a sodium glucose co-transporter 2 inhibitor in development for type 2 diabetes mellitus (T2DM). The efficacy and safety of canagliflozin were evaluated in subjects with T2DM inadequately controlled with diet and exercise. METHODS: In this 26-week, randomized, double-blind, placebo-controlled, phase 3 trial, subjects (N = 584) received canagliflozin 100 or 300 mg or placebo once daily. Primary endpoint was the change from baseline in haemoglobin A1c (HbA1c) at week 26. Secondary endpoints included the proportion of subjects achieving HbA1c < 7.0%; change from baseline in fasting plasma glucose (FPG), 2-h postprandial glucose (PPG) and systolic blood pressure (BP); and percent change in body weight, high-density lipoprotein cholesterol (HDL-C) and triglycerides. Adverse events (AEs) were recorded throughout the study. RESULTS: At week 26, HbA1c was significantly reduced from baseline with canagliflozin 100 and 300 mg compared with placebo (-0.77, -1.03 and 0.14%, respectively; p < 0.001 for both). Both canagliflozin doses significantly decreased FPG, 2-h PPG, body weight and systolic BP (p < 0.001 for all), and increased HDL-C compared with placebo (p < 0.01 for both). Overall incidences of AEs were modestly higher with canagliflozin versus placebo; rates of serious AEs and AE-related discontinuations were low and similar across groups. Incidences of genital mycotic infections, urinary tract infections and osmotic diuresis-related AEs were higher with canagliflozin; these led to few discontinuations. The incidence of hypoglycaemia was low across groups. CONCLUSION: Canagliflozin treatment improved glycaemic control, reduced body weight and was generally well tolerated in subjects with T2DM inadequately controlled with diet and exercise.

A Thienoisoindigo-Naphthalene Polymer with Ultrahigh Mobility of 14.4 cm<sup>2</sup>/V·s That Substantially Exceeds Benchmark Values for Amorphous Silicon Semiconductors
Gyoungsik Kim, Seok‐Ju Kang, Gitish K. Dutta, Young‐Kyu Han +3 more
2014· Journal of the American Chemical Society601doi:10.1021/ja504537v

By considering the qualitative benefits associated with solution rheology and mechanical properties of polymer semiconductors, it is expected that polymer-based electronic devices will soon enter our daily lives as indispensable elements in a myriad of flexible and ultra low-cost flat panel displays. Despite more than a decade of research focused on designing and synthesizing state-of-the-art polymer semiconductors for improving charge transport characteristics, the current mobility values are still not sufficient for many practical applications. The confident mobility in excess of ∼10 cm(2)/V·s is the most important requirement for enabling the realization of the aforementioned near-future products. We report on an easily attainable donor-acceptor (D-A) polymer semiconductor: poly(thienoisoindigo-alt-naphthalene) (PTIIG-Np). An unprecedented mobility of 14.4 cm(2)/V·s, by using PTIIG-Np with a high-k gate dielectric poly(vinylidenefluoride-trifluoroethylene) (P(VDF-TrFE)), is achieved from a simple coating processing, which is of a magnitude that is very difficult to obtain with conventional TFTs by means of molecular engineering. This work, therefore, represents a major step toward truly viable plastic electronics.