12,322 results match your criteria Drugs and Chemicals


Recent Chemical Approaches for Site-specific Conjugation of Native Antibodies: Technologies toward Next Generation Antibody-Drug Conjugates.

Authors:
Kei Yamada Yuji Ito

Chembiochem 2019 Apr 11. Epub 2019 Apr 11.

Kagoshima Daigaku, JAPAN.

Antibody-drug conjugates (ADCs), which consist of three components- antibody, linker, and payload, can function as "magic bullets". These conjugates offer the ability to target drug delivery to specific cells, based on cell-specific recognition and the binding of an antigen by a monoclonal antibody (mAb). In particular, by delivering a cytotoxic payload to cancer cells, ADCs are expected to provide a breakthrough in oncology treatments by providing a way to increase efficacy and decrease toxicity in comparison with traditional chemotherapeutic treatments. Read More

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http://dx.doi.org/10.1002/cbic.201900178DOI Listing
April 2019
1 Read

Curcumin: Total-Scale Analysis of the Scientific Literature.

Molecules 2019 Apr 9;24(7). Epub 2019 Apr 9.

The Institute of Genetics and Animal Breeding, Polish Academy of Sciences, Jastrzębiec, 05-552 Magdalenka, Poland.

The current study aimed to provide a comprehensive bibliometric overview of the literature on curcumin, complementing the previous reviews and meta-analyses on its potential health benefits. Bibliometric data for the current analysis were extracted from the Web of Science Core Collection database, using the search string TOPIC=("curcumin*"), and analyzed by the VOSviewer software. The search yielded 18,036 manuscripts. Read More

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http://dx.doi.org/10.3390/molecules24071393DOI Listing
April 2019
6 Reads

Evaluation of the Radiosensitizing Potency of Bromelain for Radiation Therapy of 4T1 Breast Cancer Cells.

J Med Signals Sens 2019 Jan-Mar;9(1):68-74

Clinical Biochemistry Research Center, Basic Health Sciences Institute, Shahrekord University of Medical Sciences, Shahrekord, Iran.

Breast cancer (BC) remains the leading cause of death in women worldwide, despite the improvements of cancer screening and treatment methods. Recently, development of novel anticancer drugs for the improved prevention and treatment of BC is in the center of research. The anticancer effects of bromelain, as enzyme extract derived from the pineapples, contains chemicals that interfere with the growth of tumor cells. Read More

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http://dx.doi.org/10.4103/jmss.JMSS_25_18DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6419564PMC
April 2019
2 Reads

Smart Drug Release from Medical Devices.

J Pharmacol Exp Ther 2019 Apr 9. Epub 2019 Apr 9.

Universidade de Santiago de Compostela

Medical devices are becoming key players on health monitoring and treatment. Advances in materials science and electronics have paved the way to the design of advanced wearable, insertable and implantable medical devices suitable for the prevention and cure of diseases and the physical or functional replacement of damaged tissues or organs. However, intimate and prolonged contact of the medical devices with the human body increases the risks of adverse foreign-body reactions and biofilm formation. Read More

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http://dx.doi.org/10.1124/jpet.119.257220DOI Listing
April 2019
1 Read

Identification of the fungicide epoxiconazole by virtual screening and biological assessment as inhibitor of human 11β-hydroxylase and aldosterone synthase.

J Steroid Biochem Mol Biol 2019 Apr 6. Epub 2019 Apr 6.

Institute of Pharmacy / Pharmaceutical Chemistry and Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innrain 80-82, 6020, Innsbruck, Austria; Department of Medicinal and Pharmaceutical Chemistry, Institute of Pharmacy, Paracelsus Medical University, Strubergasse 22, 5020, Salzburg, Austria. Electronic address:

Humans are constantly exposed to a multitude of environmental chemicals that may disturb endocrine functions. It is crucial to identify such chemicals and uncover their mode-of-action to avoid adverse health effects. 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2) catalyze the formation of cortisol and aldosterone, respectively, in the adrenal cortex. Read More

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http://dx.doi.org/10.1016/j.jsbmb.2019.04.007DOI Listing
April 2019
3 Reads

Risk assessment of phthalates in pharmaceuticals.

J Toxicol Environ Health A 2019 Apr 8:1-10. Epub 2019 Apr 8.

a Division of Toxicology , College of Pharmacy, Sungkyunkwan University , Suwon , South Korea.

Phthalates are used for industrial plasticizers to impart flexibility and durability to polyvinyl chloride. Despite widespread use of phthalates, reported endocrine-disrupting properties raise safety concerns for consumers. Since phthalates are permitted as excipients in controlled-release capsules and enteric coatings, patients taking drugs containing these chemicals may potentially be at some health risk. Read More

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http://dx.doi.org/10.1080/15287394.2019.1598053DOI Listing
April 2019
4 Reads

Two-Step Separation of Chitin from Shrimp Shells Using Citric Acid and Deep Eutectic Solvents with the Assistance of Microwave.

Polymers (Basel) 2019 Mar 3;11(3). Epub 2019 Mar 3.

College of Food Science and Engineering, Ocean University of China, Qingdao 266003, China.

In this research, a two-step extraction approach was developed for chitin preparation from shrimp shells by utilizing citric acids and deep eutectic solvents (DESs), which effectively removed minerals and proteins. In the first step, minerals of shrimp shells were removed by citric acid, and the demineralization efficiency reached more than 98%. In the second step, the removal of protein was carried out using deep eutectic solvents with the assistance of microwave, and the deproteinization efficiency was more than 88%. Read More

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http://dx.doi.org/10.3390/polym11030409DOI Listing
March 2019
2 Reads

Use of passive sampling and high resolution mass spectrometry using a suspect screening approach to characterise emerging pollutants in contaminated groundwater and runoff.

Sci Total Environ 2019 Apr 1;672:253-263. Epub 2019 Apr 1.

Univ Lyon, CNRS, Université Claude Bernard Lyon 1, Institut des Sciences Analytiques, UMR 5280, 5 Rue de la Doua, F-69100 Villeurbanne, France. Electronic address:

Groundwater systems are being increasingly used to provide potable and other water supplies. Due to human activities, a range of organic pollutants is often detected in groundwater. One source of groundwater contamination is via stormwater infiltration basins, however, there is little information on the types of compounds present in these collection systems and their influence on the underlying groundwater. Read More

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http://dx.doi.org/10.1016/j.scitotenv.2019.03.489DOI Listing
April 2019
3 Reads

Identification of pharmacodynamic biomarker hypotheses through literature analysis with IBM Watson.

PLoS One 2019 8;14(4):e0214619. Epub 2019 Apr 8.

Merck KGaA, Frankfurter Straße, Darmstadt, Germany.

Background: Pharmacodynamic biomarkers are becoming increasingly valuable for assessing drug activity and target modulation in clinical trials. However, identifying quality biomarkers is challenging due to the increasing volume and heterogeneity of relevant data describing the biological networks that underlie disease mechanisms. A biological pathway network typically includes entities (e. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0214619PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6453528PMC
April 2019
5 Reads

Highly Variable Expression of CYP1A1 in Human Liver and Impact on Pharmacokinetics of Riociguat and Granisetron in Humans.

Chem Res Toxicol 2019 Apr 16. Epub 2019 Apr 16.

Bayer AG , Drug Metabolism and Pharmacokinetics, Research Center , Aprather Weg 18a , 42096 Wuppertal , Germany.

Cytochrome P450s (CYPs), a superfamily of enzymes, are involved in the biotransformation of endogenous and xenobiotic chemicals and mainly responsible for the metabolic clearance of widely prescribed drugs. Out of the 57 human isoforms, only a few, most notably CYP3A4, are considered to be important in this process. CYP1A1, one of the three isoforms of the CYP1 family, is widely believed to play an important role in the metabolism and activation of numerous procarcinogens, e. Read More

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http://dx.doi.org/10.1021/acs.chemrestox.8b00413DOI Listing
April 2019
3 Reads

Mechanistic Insights of Chemicals and Drugs as Risk Factors for Systemic Lupus Erythematosus.

Curr Med Chem 2019 Apr 4. Epub 2019 Apr 4.

Key Laboratory of Prevention and Management of Chronic Kidney Disease of Zhanjiang City, Affiliated Hospital of Guangdong Medical University, Zhanjiang 524001. China.

Systemic lupus erythematosus (SLE) is a chronic and relapsing heterogenous autoimmune disease that primarily affects women of reproductive age. Genetic and environmental risk factors are involved in the pathogenesis of SLE, and susceptibility genes have recently been identified. However, as gene therapy is far from clinical application, further investigation of environmental risk factors could reveal important therapeutic approaches. Read More

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http://dx.doi.org/10.2174/0929867326666190404140658DOI Listing
April 2019
2 Reads

Solution NMR to Quantify Mobility in Membranes: Diffusion, Protrusion, and Drug Transport Processes.

Authors:
Emiko Okamura

Chem Pharm Bull (Tokyo) 2019 ;67(4):308-315

Faculty of Pharmaceutical Sciences, Himeji Dokkyo University.

Lipid bilayer membranes are soft, fluid, and dynamic architecture where molecules are constantly moving and thermally fluctuating under physiological conditions. In this review, a strategy to quantify molecular dynamics in membranes is introduced by utilizing solution-state NMR spectroscopy as a versatile, noninvasive technique. The dynamics involves lateral diffusion and protrusion motion, in parallel and vertical direction to the membrane surface. Read More

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http://dx.doi.org/10.1248/cpb.c18-00946DOI Listing
January 2019
1 Read

Harmonized methodology to assess chronic dietary exposure to residues from compounds used as pesticide and veterinary drug.

Crit Rev Toxicol 2019 Mar 28:1-10. Epub 2019 Mar 28.

l Food Safety , Organisation mondiale de la Sante , Geneve , Switzerland.

Risk assessments for pesticide and veterinary drug residues in food are performed respectively by the Joint FAO/WHO Expert Meeting on Pesticide Residues (JMPR) and the Joint FAO/WHO Expert Committee on Food Additives (JECFA). The models used by the two Committees to assess chronic dietary exposure are based on different data and assumptions which may be confusing, particularly for risk managers, when the same compound is used to treat plants and animals. This publication details the results of combined chronic dietary exposure assessments for eight compounds used both as pesticide and veterinary drugs. Read More

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http://dx.doi.org/10.1080/10408444.2019.1578729DOI Listing
March 2019
1 Read

Jaw Osteonecrosis Preceded by Dengue Fever - Possible Pathogenetic Mechanism.

J Orthop Case Rep 2018 Nov-Dec;8(6):9-12

Department of Oral Pathology and Microbiology, Government Dental College and Hospital, Dhanvantari Nagar, Ghati Campus, Aurangabad, Maharashtra, India.

Introduction: Osteonecrosis of jaw (ONJ) is a debilitating condition which can lead to compromised dentition. Various causes for ONJ are suggested in the literature such as drugs, trauma, radiation, chemicals, bacterial, and fungal infections. Knowing etiology for particular case of ONJ is important to prevent further progression of this debilitating condition. Read More

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http://dx.doi.org/10.13107/jocr.2250-0685.1234DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6424322PMC
March 2019
1 Read

In Silico Drug-Target Profiling.

Methods Mol Biol 2019 ;1953:89-103

BioCIS UFR Pharmacie UMR CNRS 8076, Université Paris Saclay, Orsay, France.

Pharmacological science is trying to establish the link between chemicals, targets, and disease-related phenotypes. A plethora of chemical proteomics and structural data have been generated, thanks to the target-based approach that has dominated drug discovery at the turn of the century. There is an invaluable source of information for in silico target profiling. Read More

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http://dx.doi.org/10.1007/978-1-4939-9145-7_6DOI Listing
January 2019
1 Read

Network Pharmacology Analysis of in Gene-Phenotype.

Evid Based Complement Alternat Med 2019 17;2019:1368371. Epub 2019 Feb 17.

Department of Neurosurgery, The First Affiliated Hospital of China Medical University, NanJing Bei Road, Heping District, Shenyang, 110001, LiaoNing Province, China.

is known as Huci in traditional Chinese medicine. It contains a component having anthraquinone-like structure which is a part of the many used anticancer drugs. This study was to collect the evidence of disease-modulatory activities of Huci by analyzing the published literature on the chemicals and drugs. Read More

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https://www.hindawi.com/journals/ecam/2019/1368371/
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http://dx.doi.org/10.1155/2019/1368371DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6398045PMC
February 2019
5 Reads

Poisoning in Israel: Annual Report of the Israel Poison Information Center, 2017.

Isr Med Assoc J 2019 Mar;21(3):175-182

Maryland Poison Center, Department of Pharmacy Practice and Science, University of Maryland School of Pharmacy, Baltimore, MD, USA.

Background: The Israel Poison Information Center (IPIC), Rambam Health Care Campus, provides 24-hour telephone consultations on clinical toxicology and drug and reproductive toxicology. It participates in research, teaching and regulatory activities, and provides laboratory services. In 2014, nurse specialists in poison information joined the IPIC. Read More

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March 2019
1 Read
0.903 Impact Factor

Zwitterionic pH-responsive hyaluronic acid polymer micelles for delivery of doxorubicin.

Colloids Surf B Biointerfaces 2019 Mar 4;178:412-420. Epub 2019 Mar 4.

State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024, PR China. Electronic address:

As zwitterionic polymers show great promise in drug delivery, hyaluronic acid (HA) was deacetylated and grafted with dodecylamine to prepare a pH-sensitive zwitterionic polymer dHAD used as a carrier for antitumor drugs. The polymer was negatively charged at pH 7.4 and became positive at pH 6. Read More

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http://dx.doi.org/10.1016/j.colsurfb.2019.03.007DOI Listing
March 2019
3 Reads

Scrutinizing the interactions between bisphenol analogues and plasma proteins: Insights from biomimetic liquid chromatography, molecular docking simulations and in silico predictions.

Environ Toxicol Pharmacol 2019 Mar 9;68:148-154. Epub 2019 Mar 9.

Pharm-Analysis & Bio-Pharm Laboratory, Department of Pharmacy, School of Medicine and Surgery, University of Naples Federico II, Via D. Montesano, 49, I-80131, Naples, Italy; Consorzio Interuniversitario INBB, Viale Medaglie d'Oro, 305, I-00136, Rome, Italy. Electronic address:

The interactions between human serum albumin (HSA) and α- acid glycoprotein (AGP), the main plasma proteins binding drugs/xenobiotics, and some endocrine disrupting chemicals (EDCs), such as bisphenol A (BPA) and some of its structural analogues, bisphenol S (BPS), bisphenol F (BPF), bisphenol E (BPE), bisphenol B (BPB), bisphenol AF (BPAF), bisphenol A diglycidyl ether (BADGE) and bisphenol M (BPM), were characterized by biomimetic liquid chromatography (LC). The interactions between bisphenols (BPs) and either HSA or AGP protein was found to be non-specific and essentially lipophilicity-driven. To get more information on the binding of BPs and plasma proteins, in silico predictions and molecular docking simulations were exploited, and the results achieved in silico were compared to those observed in vitro. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S13826689193001
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http://dx.doi.org/10.1016/j.etap.2019.02.008DOI Listing
March 2019
5 Reads

Marine natural products as source of new drugs: a patent review (2015-2018).

Expert Opin Ther Pat 2019 Apr 3;29(4):283-309. Epub 2019 Apr 3.

a CSIR Unit for Research and Development of Information Products (CSIR-URDIP) , Pune , India.

Introduction: Natural products from plants, animals, microbes, and minerals have long been a traditional source for the treatment of human diseases. In the past decades, research on natural products for the pharmaceutical industry had declined due to numerous challenges. However, the recent developments in analytical technology, spectroscopy, and high-throughput screening have tremendously revived natural product drug discovery, including contribution from marine-based drugs. Read More

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http://dx.doi.org/10.1080/13543776.2019.1598972DOI Listing
April 2019
1 Read

Cytostatics as hazardous chemicals in healthcare workers' environment.

Int J Occup Med Environ Health 2019 Apr 19;32(2):141-159. Epub 2019 Mar 19.

Nofer Institute of Occupational Medicine, Łódź, Poland (Department of Chemical Safety).

Cytostatics not only induce significant side-effects in patients treated oncologically but also pose a threat to the health of occupationally exposed healthcare workers: pharmacists, physicians, nurses and other personnel. Since the 1970s numerous reports from various countries have documented the contamination of working areas with cytostatics and the presence of drugs/metabolites in the urine or blood of healthcare employees, which directly indicates the occurrence of occupational exposure to these drugs. In Poland the significant scale of occupational exposure to cytostatics is also confirmed by the data collected in the central register of occupational carcinogens/mutagens kept by the Nofer Institute of Occupational Medicine. Read More

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http://dx.doi.org/10.13075/ijomeh.1896.01248DOI Listing
April 2019
3 Reads

Safety considerations for working with animal models involving human health hazards.

Animal Model Exp Med 2018 Jun 28;1(2):91-99. Epub 2018 Jul 28.

Animal Resources Alcon Research and Development Fort Worth TX USA.

A human health hazard may constitute a variety of hazards that are encountered in an animal facility. Health hazards include physical, chemical, radioactive, or biological hazards such as cage and rack washers, chemicals used for cleaning and disinfection, experimental drugs or biologics, radioactive isotopes, zoonotic diseases, allergens, experimental infectious agents, or biological toxins. This article will focus on experimental infectious agents and biological toxins (biohazards) that are hazardous to both animals and humans and require biological containment (biocontainment) to prevent their inadvertent release into the environment. Read More

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http://dx.doi.org/10.1002/ame2.12019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6388071PMC
June 2018
1 Read

Human three-dimensional in vitro model of hepatic zonation to predict zonal hepatotoxicity.

J Biol Eng 2019 6;13:22. Epub 2019 Mar 6.

2Department of Predictive Toxicology, Korea Institute of Toxicology (KIT), Daejeon, 34114 Republic of Korea.

Background: Various hepatic models mimicking liver lobules have been investigated to evaluate the potential hepatotoxic effects of chemicals and drugs, but in vitro hepatic models of zonal hepatotoxicity have not yet been established. Herein, we developed a three-dimensional (3D) hepatic zonal channel to evaluate zone-specific hepatotoxicity. Based on the perivenous zone-3-like cytochrome P450 (CYP) expression patterns in metabolically active HepaRG cells treated with CHIR99021 (CHIR), which is an inducer of Wnt/β-catenin signaling, this culture model represents a novel tool for exploring hepatic zonation. Read More

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http://dx.doi.org/10.1186/s13036-019-0148-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6404355PMC
March 2019
1 Read

Developmental Expression of the Cytosolic Sulfotransferases in Human Liver.

Drug Metab Dispos 2019 Mar 18. Epub 2019 Mar 18.

Wayne State University;

The liver is the predominant organ of metabolism for many endogenous and foreign chemicals. Cytosolic sulfotransferases (SULTs) catalyze the sulfonation of drugs and other xenobiotics, as well as hormones, neurotransmitters, and sterols, with consequences that include enhanced drug elimination, hormone inactivation, and pro-carcinogen bioactivation. SULTs are classified into six gene families, but only SULT1 and SULT2 enzymes are expressed in human liver. Read More

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http://dx.doi.org/10.1124/dmd.119.086363DOI Listing
March 2019
1 Read
3.252 Impact Factor

Novel palladium (II) complexes with tetradentate thiosemicarbazones. Synthesis, characterization, in vitro cytotoxicity and xanthine oxidase inhibition.

Invest New Drugs 2019 Mar 14. Epub 2019 Mar 14.

Department of Chemistry, Engineering Faculty, Istanbul University-Cerrahpasa, 34320, Avcilar, Istanbul, Turkey.

In vitro cytotoxicity and xanthine oxidase inhibition capabilities were investigated for five palladium (II) chelate complexes. The palladium complexes were synthesized by starting from S-alkyl-thiosemicarbazones where the alkyl component is methyl, ethyl, propyl or butyl. The solid complexes are characterized by elemental analysis and spectroscopic techniques (UV-visible, IR and 1H NMR). Read More

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http://link.springer.com/10.1007/s10637-019-00751-1
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http://dx.doi.org/10.1007/s10637-019-00751-1DOI Listing
March 2019
5 Reads

Versatile fluorescence detection of microRNA based on novel DNA hydrogel-amplified signal probes coupled with DNA walker amplification.

Chem Commun (Camb) 2019 Apr 14;55(27):3919-3922. Epub 2019 Mar 14.

Key Laboratory of Optic-electric Sensing and Analytical Chemistry for Life Science, MOE, Shandong Key Laboratory of Biochemical Analysis, Key Laboratory of Analytical Chemistry for Life Science in Universities of Shandong, College of Chemistry and Molecular Engineering, Qingdao University of Science and Technology, Qingdao 266042, P. R. China.

A novel DNA hydrogel-amplified versatile fluorescence platform combined with hybridization chain reaction (HCR) and DNA walking multiple amplification was developed for ultrasensitive detection of miRNA. The DNA hydrogel was loaded with large amounts of SYBR Green (SG) I dyes or CdTe quantum dots (QDs) to assemble versatile signal probes. Read More

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http://dx.doi.org/10.1039/c9cc00565jDOI Listing
April 2019
2 Reads

[Psychiatric and addictologic complications of new synthetic products].

Rev Prat 2018 Jun;68(6):676-679

Service de psychiatrie et d'addictologie, hôpital universitaire Paul-Brousse (AP-HP), Université Paris-Sud, CESP, Villejuif, France.

Psychiatric and addictologic complications of new synthetic products. New synthetic products (NSP) have completely changed the current scene of addictions. Also known as designer drugs, legal highs, herbal highs, bath salts, plant fertilizers, incense, research chemicals, they have made their emergence on the drug market in the late 1990s. Read More

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June 2018
1 Read

The Acid/Base Profile of a Large Food Chemical Database.

Mol Inform 2019 Mar 12. Epub 2019 Mar 12.

Department of Pharmacy, School of Chemistry, Universidad Nacional Autónoma de México, Avenida Universidad 3000, Mexico City, 04510, Mexico.

Molecular acid/base properties have a significant influence on membrane permeation, metabolism, absorption, and affinity for biological targets. In particular, ionizable groups are critical in the strength of target-molecule interactions, pharmacokinetics, and toxicity. In this study, we estimated the acid/base properties of the food chemicals from FooDB, a public compound collection with more than 22,000 compounds. Read More

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http://dx.doi.org/10.1002/minf.201800171DOI Listing
March 2019
1 Read

Membrane transporter data to support kinetically-informed chemical risk assessment using non-animal methods: Scientific and regulatory perspectives.

Environ Int 2019 May 8;126:659-671. Epub 2019 Mar 8.

Univ Rennes, Inserm, EHESP, Irset (Institut de recherche en santé, environment et travail), UMR_S 1085, F-35000 Rennes, France.

Humans are continuously exposed to low levels of thousands of industrial chemicals, most of which are poorly characterised in terms of their potential toxicity. The new paradigm in chemical risk assessment (CRA) aims to rely on animal-free testing, with kinetics being a key determinant of toxicity when moving from traditional animal studies to integrated in vitro-in silico approaches. In a kinetically informed CRA, membrane transporters, which have been intensively studied during drug development, are an essential piece of information. Read More

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http://dx.doi.org/10.1016/j.envint.2019.03.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6441651PMC
May 2019
1 Read

Small Molecules: The Past or the Future in Drug Innovation?

Met Ions Life Sci 2019 Jan;19

With the impressive development of molecular life sciences, one may have the feeling that biopharmaceuticals will dominate the world of drug design and production. This is partly due to the evolution of pharmaceutical industry, especially since the 1980s. As a matter of fact, small molecules are still dominating the field of drug innovation, in contradiction with claims predicting their downfall and the exponential raise of biopharmaceuticals. Read More

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http://dx.doi.org/10.1515/9783110527872-008DOI Listing
January 2019
6 Reads

Kidney Pathophysiology, Toxicology, and Drug-Induced Injury in Drug Development.

Authors:
Zaher A Radi

Int J Toxicol 2019 Mar 7:1091581819831701. Epub 2019 Mar 7.

1 Pfizer Worldwide Research and Development, Drug Safety R&D, Cambridge, MA, USA.

Anatomically, the kidneys are paired, bean-shaped (in most mammals), excretory organs that lie in the retroperitoneum. High blood flow to the kidneys, together with high oxygen consumption, makes them more vulnerable to exposure, via the circulation, and subsequent injury related to high concentrations of xenobiotics and chemicals. In preclinical drug development and safety assessment of new investigational drugs, changes in kidney structure and/or function following drug administration in experimental laboratory animals need to be put in context with interspecies differences in kidney functional anatomy, physiology, spontaneous pathologies, and toxicopathological responses to injury. Read More

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http://dx.doi.org/10.1177/1091581819831701DOI Listing
March 2019
2 Reads

Honey bee (Apis mellifera) exposomes and dysregulated metabolic pathways associated with Nosema ceranae infection.

PLoS One 2019 7;14(3):e0213249. Epub 2019 Mar 7.

Life Science and Chemical Analysis Group, Agilent Technologies, Santa Clara, CA, United States of America.

Honey bee (Apis mellifera) health has been severely impacted by multiple environmental stressors including parasitic infection, pesticide exposure, and poor nutrition. The decline in bee health is therefore a complex multifactorial problem which requires a holistic investigative approach. Within the exposome paradigm, the combined exposure to the environment, drugs, food, and individuals' internal biochemistry affects health in positive and negative ways. Read More

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http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0213249PLOS
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6405199PMC
March 2019
4 Reads

Immune Pathomechanism and Classification of Drug Hypersensitivity.

Authors:
Werner J Pichler

Allergy 2019 Mar 6. Epub 2019 Mar 6.

ADR-AC GmbH, Holligenstr 91, 3008, Bern.

Drug hypersensitivity reactions (DHR) are based on distinct mechanisms and are clinically heterogeneous. Taking into account that also off target activities of drugs may lead to stimulations of immune or inflammatory cells, three forms of DHR were discriminated: The allergic-immune mechanism relies on the covalent binding of drugs/chemicals to proteins, which thereby form new antigens, to which a humoral and/or cellular immune response can develop. In IgE mediated drug allergies a possible tolerance mechanism to the drug during sensitization and the need of a covalent hapten-carrier link for initiation, but not for elicitation of IgE-mediated reactions are discussed. Read More

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http://doi.wiley.com/10.1111/all.13765
Publisher Site
http://dx.doi.org/10.1111/all.13765DOI Listing
March 2019
5 Reads

The Beneficial and Debilitating Effects of Environmental and Microbial Toxins, Drugs, Organic Solvents and Heavy Metals on the Onset and Progression of Multiple Sclerosis.

Toxins (Basel) 2019 Mar 5;11(3). Epub 2019 Mar 5.

Department of Clinical Sciences, College of Medicine, and the Immuno-Oncology group, Sharjah Institute for Medical Research (SIMR), University of Sharjah, Sharjah P.O. Box 27272, United Arab Emirates.

Multiple sclerosis (MS), a chronic inflammatory disease of the central nervous system is common amongst young adults, leading to major personal and socioeconomic burdens. However, it is still considered complex and challenging to understand and treat, in spite of the efforts made to explain its etiopathology. Despite the discovery of many genetic and environmental factors that might be related to its etiology, no clear answer was found about the causes of the illness and neither about the detailed mechanism of these environmental triggers that make individuals susceptible to MS. Read More

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http://dx.doi.org/10.3390/toxins11030147DOI Listing

(De)Toxifying the Epigenetic Code.

Chem Res Toxicol 2019 Mar 18. Epub 2019 Mar 18.

Chemical Biology Program , Memorial Sloan Kettering Cancer Center , New York 10044 , New York , United States.

Cells are continuously subjected to an array of reactive/toxic chemical species which are produced both endogenously through metabolic pathways and taken up exogenously by diet and exposure to drugs or toxins. As a result, proteins often undergo non-enzymatic covalent modifications (NECMs) by these species, which can alter protein structure, function, stability, and binding partner affinity. NECMs accumulate over time and are linked to various diseases such as Alzheimer's disease, cancer, and diabetes. Read More

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http://dx.doi.org/10.1021/acs.chemrestox.9b00013DOI Listing
March 2019
4 Reads

Rational Optimization and Action Mechanism of Novel Imidazole (or Imidazolium)-Labeled 1,3,4-Oxadiazole Thioethers as Promising Antibacterial Agents against Plant Bacterial Diseases.

J Agric Food Chem 2019 Apr 15;67(13):3535-3545. Epub 2019 Mar 15.

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education , Center for R&D of Fine Chemicals of Guizhou University , Guiyang , 550025 , China.

The emergence and widespread occurrence of plant bacterial diseases that cause global production constraints have become major challenges to agriculture worldwide. To promote the discovery and development of new bactericides, imidazole-labeled 1,3,4-oxadiazole thioethers were first fabricated by integrating the crucially bioactive scaffolds of the imidazole motif and 1,3,4-oxadiazole skeleton in a single molecular architecture. Subsequently, a superior antibacterial compound A was gradually discovered possessing excellent competence against plant pathogens Xanthomonas oryzae pv oryzae and Xanthomonas axonopodis pv citri with EC values of 0. Read More

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http://dx.doi.org/10.1021/acs.jafc.8b06242DOI Listing
April 2019
1 Read

A highly sensitive and versatile chiral sensor based on a top-gate organic field effect transistor functionalized with thiolated β-cyclodextrin.

Analyst 2019 Apr;144(8):2611-2617

School of Chemical Engineering and Technology, Tianjin Engineering Research Center of Functional Fine Chemicals, Tianjin University, Tianjin 300072, China.

The discrimination of chirality by field effect transistors (FETs) is a great challenge because enantiomers possess exactly identical charge and hence chiral recognition is solely related to spatial effects, while the working principle of most FET sensors is based on the intrinsic charge of analytes. In this work, a chiral organic field effect transistor (COFET) with a self-assembled thiolated β-cyclodextrin (SH-β-CD) monolayer modified gold top-gate electrode is developed to afford rapid, highly sensitive and real-time chiral discrimination for various enantiomers. Well-defined sensing results are achieved for diverse acidic enantiomers with the lowest detection concentration (LDC) of 10-12 M. Read More

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http://dx.doi.org/10.1039/c8an02339eDOI Listing
April 2019
5 Reads

Whole Cell Actinobacteria as Biocatalysts.

Front Microbiol 2019 18;10:77. Epub 2019 Feb 18.

College of Medicine and Public Health, Medical Biotechnology, Flinders University, Bedford Park, SA, Australia.

Production of fuels, therapeutic drugs, chemicals, and biomaterials using sustainable biological processes have received renewed attention due to increasing environmental concerns. Despite having high industrial output, most of the current chemical processes are associated with environmentally undesirable by-products which escalate the cost of downstream processing. Compared to chemical processes, whole cell biocatalysts offer several advantages including high selectivity, catalytic efficiency, milder operational conditions and low impact on the environment, making this approach the current choice for synthesis and manufacturing of different industrial products. Read More

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https://www.frontiersin.org/article/10.3389/fmicb.2019.00077
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http://dx.doi.org/10.3389/fmicb.2019.00077DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6387938PMC
February 2019
6 Reads

International Control Efforts to Curb the Global Production and Trafficking of Fentanyl and Other Synthetic Opioids.

J Addict Nurs 2019 Jan/Mar;30(1):71-76

Katherine Smith Fornili, DNP, MPH, RN, CARN, FIAAN, Assistant Professor, University of Maryland School of Nursing-Baltimore, Department of Family & Community Health, Baltimore, MD.

The purpose of this Policy Watch column is to provide a brief overview of the global problems associated with the illicit production and trafficking of synthetic opioids as well as international efforts and policy approaches designed to curb them. An in-depth evaluation of drug control efforts of many different nations is important for a comprehensive analysis. However, because of the vast amount of information available, this column is limited to cooperative global control efforts, not efforts specific to any one nation. Read More

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http://dx.doi.org/10.1097/JAN.0000000000000269DOI Listing
March 2019
2 Reads

The Impact of Immune Interventions: A Systems Biology Strategy for Predicting Adverse and Beneficial Immune Effects.

Front Immunol 2019 15;10:231. Epub 2019 Feb 15.

TNO, Zeist, Netherlands.

Despite scientific advances it remains difficult to predict the risk and benefit balance of immune interventions. Since a few years, network models have been built based on comprehensive datasets at multiple molecular/cellular levels (genes, gene products, metabolic intermediates, macromolecules, cells) to illuminate functional and structural relationships. Here we used a systems biology approach to identify key immune pathways involved in immune health endpoints and rank crucial candidate biomarkers to predict adverse and beneficial effects of nutritional immune interventions. Read More

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https://www.frontiersin.org/article/10.3389/fimmu.2019.00231
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http://dx.doi.org/10.3389/fimmu.2019.00231DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6384242PMC
February 2019
5 Reads

[Function of Sacran as an Artificial Skin Barrier and the Development of Skincare Products].

Yakugaku Zasshi 2019 ;139(3):371-379

DAITO KASEI KOGYO CO., LTD.

Sacran, a large molecular-weight polysaccharide isolated from algae, is composed of 11 types of saccharides, including sulfate and carboxylic acid groups. Because of its unique structure, sacran can form a gel-like sheet in the presence of polyols such as 1,3-butanediol. In addition, those sacran gel-like sheets prevent the evaporation of water and the penetration of chemicals. Read More

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http://dx.doi.org/10.1248/yakushi.18-00177-3DOI Listing
March 2019
4 Reads

A retrospective study of poisoning deaths from forensic autopsy cases in northeast China (Liaoning).

J Forensic Leg Med 2019 Apr 21;63:7-10. Epub 2019 Feb 21.

School of Forensic Medicine, China Medical University, Shenyang 110122, China. Electronic address:

Acute poisoning is a public health threat that leads to morbidity and mortality worldwide. In this retrospective study, we evaluated autopsies from deaths caused by acute poisoning from 2008 to 2017 at the School of Forensic Medicine, China Medical University (SFMCMU) in the Liaoning Province, northeast China. A total of 140 poisoning deaths were investigated and the demographic characteristics, causes and manner of death, toxics category were analyzed. Read More

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http://dx.doi.org/10.1016/j.jflm.2019.02.008DOI Listing
April 2019
3 Reads
0.989 Impact Factor

Discovery and synthesis of 2-amino-1-methyl-1H-imidazol-4(5H)-ones as GPCR ligands; an approach to develop breast cancer drugs via GPCR associated PAR1 and PI3Kinase inhibition mechanism.

Bioorg Chem 2019 May 22;86:641-651. Epub 2019 Feb 22.

Sai Supreme Chemicals, Gummidipoondi, Chennai 601201, Tamil Nadu, India.

Efforts were taken to synthesis and characterize 2-amino-1-methyl-1H-imidazole-4(5H)-one derivatives (4a-u) through a four-step reaction. The achieved compounds in remarkable yield have characterized through standard analytical techniques such as FTIR, LC-MS, NMR, HRMS, and elemental analysis. Present study mainly aimed to evaluate 4a-u as G protein-coupled receptors (GPCR). Read More

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http://dx.doi.org/10.1016/j.bioorg.2019.02.048DOI Listing
May 2019
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Rational design of allosteric modulators of the aromatase enzyme: An unprecedented therapeutic strategy to fight breast cancer.

Eur J Med Chem 2019 Apr 13;168:253-262. Epub 2019 Feb 13.

CNR-IOM-Democritos c/o International School for Advanced Studies (SISSA), Trieste, Italy. Electronic address:

Estrogens play a key role in cellular proliferation of estrogen-receptor-positive (ER+) breast cancers (BCs). Suppression of estrogen production by competitive inhibitors of the enzyme aromatase (AIs) is currently one of the most effective therapies against ER + BC. Yet, the development of acquired resistance, after prolonged treatments with AIs, represents a clinical major concern. Read More

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http://dx.doi.org/10.1016/j.ejmech.2019.02.045DOI Listing
April 2019
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Identification of Compounds That Inhibit Estrogen-Related Receptor Alpha Signaling Using High-Throughput Screening Assays.

Molecules 2019 Feb 27;24(5). Epub 2019 Feb 27.

National Center for Advancing Translational Sciences, National Institutes of Health (NIH), Bethesda, MD 20814, USA.

The nuclear receptor, estrogen-related receptor alpha (ERRα; NR3B1), plays a pivotal role in energy homeostasis. Its expression fluctuates with the demands of energy production in various tissues. When paired with the peroxisome proliferator-activated receptor γ coactivator 1α (PGC-1α), the PGC/ERR pathway regulates a host of genes that participate in metabolic signaling networks and in mitochondrial oxidative respiration. Read More

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http://dx.doi.org/10.3390/molecules24050841DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6429183PMC
February 2019
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In silico analysis identified miRNA‑based therapeutic agents against glioblastoma multiforme.

Oncol Rep 2019 Apr 19;41(4):2194-2208. Epub 2019 Feb 19.

Department of Pathology, First Affiliated Hospital of Guangxi Medical University, Nanning, Guangxi Zhuang Autonomous Region 530021, P.R. China.

MicroRNAs (miRNAs or miRs) contribute to the development of various malignant neoplasms, including glioblastoma multiforme (GBM). The present study aimed to explore the pathogenesis of GBM and to identify latent therapeutic agents for patients with GBM, based on an in silico analysis. Gene chips that provide miRNA expression profiling in GBM were obtained from the Gene Expression Omnibus (GEO) database. Read More

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http://www.spandidos-publications.com/10.3892/or.2019.7022
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http://dx.doi.org/10.3892/or.2019.7022DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6412522PMC
April 2019
5 Reads

Re-purposing is needed for beneficial bugs, not for the drugs.

Int Microbiol 2019 Mar 11;22(1):1-6. Epub 2018 Dec 11.

National Collection of Industrial Microorganisms (NCIM), CSIR-National Chemical Laboratory, Pashan Road, Pune, MH, 411,008, India.

Between 150 and 200 species of plants, insects, birds or mammals go extinct every day. We do not have any idea what the global extinction rate for microorganisms is. What is clear is that we have already lost a maximum number of the microbes that used to live in and on our skins. Read More

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http://dx.doi.org/10.1007/s10123-018-00049-xDOI Listing
March 2019
2 Reads

Multiple comparisons of three different sources of biomaterials in the application of tumor tissue engineering in vitro and in vivo.

Int J Biol Macromol 2019 Jun 23;130:166-176. Epub 2019 Feb 23.

State Key Laboratory of Fine Chemicals, Dalian R&D Center for Stem Cell and Tissue Engineering, Dalian University of Technology, Dalian 116024, China. Electronic address:

Potential anti-cancer drugs are frequently of low efficacy in clinics due to the lack of predictive models or the insufficient employment of existing preclinical test systems. Three-dimensional (3D) in vitro engineered tumor models can better predict the efficacy of novel drugs by reproducing the in vivo tumor microenvironment. In this study, three sources of scaffolds (decellularized lung scaffold, chitosan/gelatin scaffold, and poly-L-lactic acid scaffold) incorporated with breast cancer cells (MCF-7, 4T1) were bioengineered as a platform to study in vitro solid tumor development. Read More

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http://dx.doi.org/10.1016/j.ijbiomac.2019.02.136DOI Listing
June 2019
3 Reads

Effect of pH and Ionic Strength on the Solubility of Quinoline: Back-to-Basics.

AAPS PharmSciTech 2019 Feb 25;20(3):124. Epub 2019 Feb 25.

Department of Pharmacy Practice and Science, College of Pharmacy, University of Arizona, Tucson, Arizona, 85721, USA.

The interest of quinoline as a contaminant agent and as scaffold for the development of new therapeutic agent warrants to revisit the pH-solubility behavior of quinoline (Q) and quinoline derivatives (Q-derivatives) with possible salting-out effect. Q is a weak base with potential hazard upon exposure that may be occupational by inhalation or ingestion of or dermal exposure to particulates in certain industries; or simply by inhalation of cigarette smoke. In contrast, quinoline and its derivatives are useful in diverse therapeutic applications such as anticancer, antiseptic, antipyretic, antiviral, and antimalarial. Read More

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http://link.springer.com/10.1208/s12249-019-1336-9
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http://dx.doi.org/10.1208/s12249-019-1336-9DOI Listing
February 2019
7 Reads

Deep Neural Network Models for Predicting Chemically Induced Liver Toxicity Endpoints From Transcriptomic Responses.

Front Pharmacol 2019 5;10:42. Epub 2019 Feb 5.

Department of Defense Biotechnology High Performance Computing Software Applications Institute, Telemedicine and Advanced Technology Research Center, United States Army Medical Research and Materiel Command, Frederick, MD, United States.

Improving the accuracy of toxicity prediction models for liver injuries is a key element in evaluating the safety of drugs and chemicals. Mechanism-based information derived from expression (transcriptomic) data, in combination with machine-learning methods, promises to improve the accuracy and robustness of current toxicity prediction models. Deep neural networks (DNNs) have the advantage of automatically assembling the relevant features from a large number of input features. Read More

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http://dx.doi.org/10.3389/fphar.2019.00042DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6370634PMC
February 2019
2 Reads