Machine Learning in Quantitative Protein-Peptide Affinity Prediction: Implications for Therapeutic Peptide Design.
CONCLUSION: There is still a long way to go before establishment of general, reliable and efficient machine leaning-based protein-peptide affinity predictors. PMID: 30317994 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 12, 2018 Category: Drugs & Pharmacology Authors: Li Z, Miao Q, Yan F, Meng Y, Zhou P Tags: Curr Drug Metab Source Type: research

Advances and Application of a Novel Oral Anticoagulant in Specific Populations: Dabigatran Etexilate.
Abstract Dabigatran etexilate (DE) was approved by the FDA in 2010 to reduce the risk of stroke and systemic embolism in adults with non-valvular atrial fibrillation (NVAF). Compared with warfarin, a traditional anticoagulant drug, DE exhibits a shorter half-life, improved dose-effect relationship, fewer food and drug interactions, and can be taken orally without monitoring the conventional coagulation index. DE can also prevent or reduce the severity of adverse events, such as attenuated drug efficacy or bleeding. It is convenient for patients to take DE due to low levels of individual variation. We review the ph...
Source: Current Drug Metabolism - October 11, 2018 Category: Drugs & Pharmacology Authors: Xu D, Su C, Pan J Tags: Curr Drug Metab Source Type: research

The Development of Machine Learning Methods in Cell-Penetrating Peptides Identification: A Brief Review.
CONCLUSION: In this review, the last studies on CPP identification using machine learning method were reported. We also discussed the future development direction of CPP recognition with computational methods. PMID: 30317992 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 10, 2018 Category: Drugs & Pharmacology Authors: Wei HH, Yang W, Tang H, Lin H Tags: Curr Drug Metab Source Type: research

Drug-drug interactions of P-gp substrates unrelated to CYP metabolism.
Abstract In this decade, it is known that the role of several drug transporters is to act as a key player in drug disposition, and then they can affect clinical significances. Nevertheless, most of the drug-drug interaction (DDI) studies have been related to cytochrome P450s (CYPs), and these are followed by in vitro and in vivo drug-interactive reports on drug-transporters, which are accumulating. In addition, when both substrate drugs of CYPs and drug transporters (e.g., P-glycoprotein, P-gp) are related to DDIs, it remains that the mechanisms of DDIs will be quite ambiguous in assessing how much the CYPs and/or...
Source: Current Drug Metabolism - October 3, 2018 Category: Drugs & Pharmacology Authors: Akamine Y, Yasui-Furukori N, Uno T Tags: Curr Drug Metab Source Type: research

Survey of Drug Oxidation Activities in Liver and Intestine Microsomes of Individual Common Marmosets, a New Nonhuman Primate Animal Model.
CONCLUSION: The marmoset could be a model animal for humans with respect to the first-pass extraction of terfenadine and related substrates. These findings provide a foundation for understanding individual pharmacokinetic and toxicological results in nonhuman primates as preclinical models and will help to further support understanding of the molecular mechanisms of human P450 function. PMID: 30280664 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - October 3, 2018 Category: Drugs & Pharmacology Authors: Uehara S, Oshio T, Nakanishi K, Tomioka E, Suzuki M, Inoue T, Uno Y, Sasaki E, Yamazaki H Tags: Curr Drug Metab Source Type: research

A Review of Recent Advances and Research on Drug Target Identification Methods.
Abstract From a therapeutic viewpoint, understanding how drugs bind and regulate the functions of their target proteins to protect against disease is crucial. The identification of drug targets plays a significant role in drug discovery and in studying the mechanisms of diseases. The development of methods to identify drug targets has become a popular issue in this field of research. Originally, scientists used biological experiments to identify drug targets. However, recently, an increasing number of scientists use computational methods to identify drug targets. Although thousands of drug targets are estimated to...
Source: Current Drug Metabolism - September 24, 2018 Category: Drugs & Pharmacology Authors: Hu Y, Zhao T, Zhang N, Zhang Y, Cheng L Tags: Curr Drug Metab Source Type: research

A Review of Theranostics Applications and Toxicities of Carbon Nanomaterials.
CONCLUSION: In brief, this review article discusses the numerous theranostics applications and toxicities of CNMs. Biomolecules-functionalized oxygenated GO and CNTs are more efficacious than the other CNMs with abridged cellular toxicity. PMID: 30251600 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 24, 2018 Category: Drugs & Pharmacology Authors: Gupta N, Rai DB, Jangid AK, Kulhari H Tags: Curr Drug Metab Source Type: research

Influence of CYP3A and ABCB1 Single Nucleotide Polymorphisms on the Pharmacokinetics/Pharmacodynamics of Tacrolimus in pediatric patients.
Abstract Single nucleotide polymorphisms (SNPs) are the most common variants in many genes, which are also promising markers in relation to drug responses in pharmacogenomics studies. Tacrolimus is a primary immunosuppressant used for the prevention of organ rejection in pediatric organ transplantation. Tacrolimus, transported out of cells via P-glycoprotein (ABCB1), is also a metabolic substrate for cytochrome P450 (CYP) 3A enzymes, especially the CYP3A4 and the CYP3A5. The SNP of these genes have been studied extensively in adult population, but there is no systematic review in children. In this paper, we focus ...
Source: Current Drug Metabolism - September 24, 2018 Category: Drugs & Pharmacology Authors: Yang M, Wang M, Gui H, Mao C Tags: Curr Drug Metab Source Type: research

Replacing GHB with GBL in recreational settings: a new trend in chemsex.
CONCLUSIONS: GBL currently represents a growing public health issue since the substance relatively cheaper and easier to obtain than GHB. Improvement and implementation of laws and policies to place GBL under control are needed to limit its diffusion, the eventual health threat for users and its non -negligible abuse liability and dependence risk. PMID: 30251602 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 24, 2018 Category: Drugs & Pharmacology Authors: Busardo FP, Gottardi M, Tini A, Minutillo A, Marinelli E, Zaami S Tags: Curr Drug Metab Source Type: research

Cancer Nanotechnology: A New Revolution for Cancer Diagnosis and Therapy.
Conclusion- This review highlights various approaches of cancer nanotechnology in the advancement of cancer therapy. PMID: 30227814 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 18, 2018 Category: Drugs & Pharmacology Authors: Chaturvedi VK, Singh A, Singh VK, Singh MP Tags: Curr Drug Metab Source Type: research

The role of xenobiotic receptors on hepatic glycolipid metabolism.
Abstract PXR (pregnane X receptor) and CAR (constitutive androstane receptor) are termed as xenobiotic receptors, which are known as core factors in the regulation of the transcription of metabolic enzymes and drug transporters. However, accumulating evidence has shown that PXR and CAR exert their effects on energy metabolism through the regulation of gluconeogenesis, lipogenesis, and β-oxidation. Therefore, PXR and CAR may become new therapeutic targets for metabolic syndrome, including obesity and diabetes. In this review, we will summarize recent advances to show how xenobiotic receptors regulate energy me...
Source: Current Drug Metabolism - September 18, 2018 Category: Drugs & Pharmacology Authors: Chen K, Zhong J, Hu L, Li R, Duc Q, Cai J, Li Y, Gao Y, Cui X, Yang X, Wu X, Yao L, Dai J, Wang Y, Jin H Tags: Curr Drug Metab Source Type: research

Advanced Glycation End Products (AGEs), Glutathione and Breast Cancer: Factors, Mechanism and Therapeutic Interventions.
CONCLUSION: This review provides a strong platform to comprehend the etiology, mechanism and production of AGEs and glutathione along with the agents which can block their production, paving a way for the therapeutic intervention and an amicable solution to treat and manage breast cancer. PMID: 30207227 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 11, 2018 Category: Drugs & Pharmacology Authors: Sharma AK, Sharma VR, Gupta GK, Ashraf GM, Kamal MA Tags: Curr Drug Metab Source Type: research

Novel Nanoparticles for Tumor Targeting Drug Delivery.
PMID: 30187836 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - September 8, 2018 Category: Drugs & Pharmacology Authors: Gao H Tags: Curr Drug Metab Source Type: research

Targeting Virus-host Protein Interactions: Feature Extraction and Machine Learning Approaches.
We describe the pivotal and representative features extracted from relevant sources of biological data, mainly include sequence signatures, known domain interactions, protein motifs and protein structure information, which are the basis of the virus-host PPI prediction. We focus on state-of-the-art machine learning algorithms that are used to build binary prediction models for the classification of virus-host protein pairs and discuss their abilities, weakness and future directions. PMID: 30156155 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - August 29, 2018 Category: Drugs & Pharmacology Authors: Zheng N, Wang K, Zhan W, Deng L Tags: Curr Drug Metab Source Type: research

Molecular Design of Peptide-Fc Fusion Drugs.
Abstract Peptide-Fc fusion drugs are a category of biological therapeutics in which the Fc region of an antibody is genetically fused to a peptide of interest. In this review, we summarize the key steps in peptide-Fc fusion technology and stress the main computational resources, tools, and methods that have been used in the rational design of peptide-Fc fusion drugs. Additionally, open questions about the computer-aided molecular design of peptide-Fc are raised. Answers to these questions by future research will certainly help make the transition from peptide leads to drugs on the market quicker and cheaper. ...
Source: Current Drug Metabolism - August 20, 2018 Category: Drugs & Pharmacology Authors: Ning L, He B, Zhou P, Derda R, Huang J Tags: Curr Drug Metab Source Type: research

Recent advances in the machine learning-based drug-target interaction prediction.
This study provides the guide to the development of computational methods for the drug-target interaction prediction. PMID: 30129407 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - August 20, 2018 Category: Drugs & Pharmacology Authors: Zhang W, Lin W, Zhang D, Wang S, Shi J, Niu Y Tags: Curr Drug Metab Source Type: research

The Impact of Carboxylesterases in Drug Metabolism and Pharmacokinetics.
Abstract Carboxylesterases (CES) play a critical role in catalyzing hydrolysis of esters, amides, carbamates and thioesters, and bioconverting prodrugs and soft drugs. Human CES1 is one of the most highly expressed drug metabolizing enzymes in the liver, while human intestine only expresses CES2. The unique tissue distribution of CES enzymes provides great opportunities to design prodrugs or soft drugs for tissue targeting. CES enzymes have moderate to high inter-individual variability and exhibit low to no expression in the fetus, but increase substantially during the first few months of life. The CES genes are h...
Source: Current Drug Metabolism - August 20, 2018 Category: Drugs & Pharmacology Authors: Di L Tags: Curr Drug Metab Source Type: research

Survey of Machine Learning Techniques in Drug Discovery.
Abstract Drug discovery, which is the process of discovering new candidate medications, is very important for pharmaceutical industries. At its current stage, discovering new drugs is still an expensive and time-consuming process, requiring Phases I, II and III for clinical trials. Recently, machine learning techniques in Artificial Intelligence (AI), especially the deep learning techniques which allow a computational model to generate multiple layers, have been widely applied and achieved state-of-the-art performance in various fields, such as speech recognition, image classification, bioinformatics, etc. One pot...
Source: Current Drug Metabolism - August 19, 2018 Category: Drugs & Pharmacology Authors: Stephenson N, Shane E, Chase J, Rowland J, Ries D, Justice N, Zhang J, Chan L, Cao R Tags: Curr Drug Metab Source Type: research

Interindividual Variability in Drug Metabolizing Enzymes.
PMID: 30117390 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - August 17, 2018 Category: Drugs & Pharmacology Authors: Volpe DA Tags: Curr Drug Metab Source Type: research

Preclinical Pharmacokinetics of Triptolide: A Potential Antitumor Drug.
Abstract Triptolide, a bioactive component in Tripterygium wilfordii extracts, possess strong anti-proliferative activity on all 60-national cancer institute (NCI) cancer cell lines. The antitumor property of triptolide has made it become a promising anti-cancer drug. However, the widespread use of triptolide in the clinical practice is greatly limited for its multi-organ toxicity and narrow therapeutic window. All the toxic characteristics of triptolide are associated with the pharmacokinetics especially its distribution and accumulation in the target organ. The article presents a comprehensive review of the prec...
Source: Current Drug Metabolism - August 16, 2018 Category: Drugs & Pharmacology Authors: Song W, Liu M, Wu J, Zhai H, Chen Y, Peng Z Tags: Curr Drug Metab Source Type: research

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, reality or dream in managing patients with cardiovascular disease.
Abstract Statins have been a major keystone in the management of patients with atherosclerotic cardiovascular disease. The benefits of inhibiting HMG CoA reductase, via statins, were translated into reduction in LDL-c (cholesterol) with proportionate decrease in cardiovascular events in response to the magnitude of LDL-c reduction. Despite major advances in pharmacological treatments, including the use of high-dose statins, there are urgent need to further reduce future cardiovascular risk. This is in particularly important since 1 out of 5 high-risk atherosclerotic patients who achieve low LDL-c return with a sec...
Source: Current Drug Metabolism - August 16, 2018 Category: Drugs & Pharmacology Authors: Alkhalil M Tags: Curr Drug Metab Source Type: research

Chinese Herbal Medicine Hepatotoxicity: The Evaluation and Recognization Based on Large-scale Evidence Ddatabase.
Abstract This review summarizes the current research status of hepatotoxicity and points out that drug induced liver injury (DILI) remains an important scientific problem that urgently needs to be solved. Due to the special nature of Chinese Herbal medicine and the complexity of its clinical use, it is difficult to identify and evaluate its toxicity and resulting herb induced liver injury (HILI). At the same time, due to a lack of specific indicators, the direct and indirect long-term effects of Chinese Herbal Medicine on the liver are also difficult to be clinically determined. At present, the Roussel Uclaf Causa...
Source: Current Drug Metabolism - August 13, 2018 Category: Drugs & Pharmacology Authors: Liu Z, He X, Wang L, Zhang Y, Hai Y, Gao R Tags: Curr Drug Metab Source Type: research

Understanding and Preventing Adverse Effects of Tacrolimus Metabolization in Transplant Patients.
PMID: 30081785 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - August 6, 2018 Category: Drugs & Pharmacology Authors: Frohlich E Tags: Curr Drug Metab Source Type: research

Xenobiotic conjugation with dicarboxylic acids.
Abstract Although it is believed widely that the various routes of xenobiotic metabolism are now all known and effectively understood, occasionally there emerges a metabolite that signals a novel biotransformation pathway, especially where the xenobiotic may in some way interact with the myriad processes of intermediary metabolism. There are a few reports in the literature where saturated short-chain dicarboxylic acids have been exploited as conjugating agents and these unusual xenobiotic metabolites subsequently excreted intact in the urine. Examples of this as yet relatively rare Phase II reaction occurring in m...
Source: Current Drug Metabolism - August 3, 2018 Category: Drugs & Pharmacology Authors: Mitchell SC, Steventon GB Tags: Curr Drug Metab Source Type: research

Drug-drug interactions of angiotensin converting enzyme inhibitors mediated by metabolizing enzymes and transporters.
CONCLUSION: Inhibition of metabolizing enzymes and transporter system can markedly alter the concentrations of ACE inhibitors. The genetic polymorphisms in the enzymes in some of the specific isoforms seem to explain the inter-individual differences in ACE inhibitors metabolism, and also the inter-individual variation in the pharmacokinetics of ACE inhibitors may be caused by changes in transporter function. Understanding the knowledge of how ACE inhibitors are metabolized and transported is important in predicting and managing DDIs. The data on the roles of drug metabolizing enzymes and transporters in the DDIs of ACE inh...
Source: Current Drug Metabolism - July 30, 2018 Category: Drugs & Pharmacology Authors: Sun P, Liu K Tags: Curr Drug Metab Source Type: research

Interdisciplinary Research Efforts to Advance Neuropsychopharmacology and Mental Health.
PMID: 30039756 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 26, 2018 Category: Drugs & Pharmacology Authors: Scola G Tags: Curr Drug Metab Source Type: research

Essential Oils: Extraction techniques, Pharmaceutical and Therapeutic potential - A review.
CONCLUSION: This manuscript reviewed the major research studies in the field and discussed several research findings on the chemical composition of essential oils, methods of oil extraction, and application of these oils in pharmaceutical and therapeutic fields. These essential oils can be used as anticancer, antimicrobial, antiviral, and as skin permeation enhancer agents. PMID: 30039757 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 23, 2018 Category: Drugs & Pharmacology Authors: Aziz ZAA, Ahmad A, Setapar SHM, Karakucuk A, Azim MM, Lokhat D, Kamal MA, Ashraf GM Tags: Curr Drug Metab Source Type: research

Genetic determinants of vitamin D-related disorders; focus on vitamin D receptor.
Abstract The endocrine system of vitamin D is involved in an extensive variety of biological processes such as bone metabolism, regulation of cell proliferation and differentiation and modulation of the immune response. The active form of vitamin D, 25-hydroxyvitamin D, binds to vitamin D receptor (VDR) controlling the synthesis of many different proteins. Although numerous studies reported polymorphism in the VDR gene, the impact of the polymorphic alleles on VDR protein function remains unknown. BsmI, ApaI, and TaqI are the three adjacent single nucleotide polymorphisms in intron 8/exon nine at the 3' end of the...
Source: Current Drug Metabolism - July 23, 2018 Category: Drugs & Pharmacology Authors: Abouzid M, Karazniewicz-Lada M, Glowka F Tags: Curr Drug Metab Source Type: research

Drug-Induced Nephrotoxicity and Drug Metabolism in Renal Failure.
PMID: 30009693 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 17, 2018 Category: Drugs & Pharmacology Authors: Huang J Tags: Curr Drug Metab Source Type: research

Thiazide Therapy in Chronic Kidney Disease: Renal and Extra Renal Targets.
Abstract Thiazides are the most commonly used medications for the treatment of mild and moderate hypertension. Despite their recognized effect, the mechanism by which thiazides reduce systemic blood pressure remains uncertain. The prevailing belief is that thiazides reduce blood pressure primarily via enhancement of salt excretion consequent to the inhibition of the Na-Cl cotransporter (NCC) in the distal convoluted tubules (DCT). However, recent reports point to a reduction in peripheral vascular resistance as a major mechanism of anti-hypertensive effect of thiazides. It is plausible that both mechanisms, renal ...
Source: Current Drug Metabolism - July 1, 2018 Category: Drugs & Pharmacology Authors: Pourafshar N, Alshahrani S, Karimi A, Soleimani M Tags: Curr Drug Metab Source Type: research

Optimization of Drugs Pharmacotherapy during Pregnancy Using Physiologically Based Pharmacokinetic Models - An Update.
CONCLUSION: More work is needed to fill the gaps in knowledge needed to more accurately and mechanistically simulate simultaneous exposure of the pregnant mother and her fetus/ embryo to drugs using pregnancy physiologically-based pharmacokinetic modeling approach. PMID: 29962340 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - July 1, 2018 Category: Drugs & Pharmacology Authors: Idkaidek N, Alsmadi MM Tags: Curr Drug Metab Source Type: research

Relevance of breast cancer resistance protein to brain distribution and central acting drugs: a pharmacokinetic perspective.
CONCLUSIONS: The clinical significance of BCRP in the disposition of drugs is currently undeniable. PMID: 29956624 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - June 29, 2018 Category: Drugs & Pharmacology Authors: Goncalves J, Bicker J, Alves G, Fortuna A, Falcao A Tags: Curr Drug Metab Source Type: research

Metabolism of Peptide Drugs and Strategies to Improve their Metabolic Stability.
Abstract Peptides are used increasingly as therapeutics and biomarkers because of the development of peptide synthesis technologies. Although peptides are associated with a variety of advantages that include high pharmaceutical activity and low toxicity, the therapeutic use of peptides is limited because of their poor metabolic stability in vivo. The main cause of this instability is that peptides are readily degraded by peptidases distributed widely in the body. This review summarizes peptidases present in the gastrointestinal tract, blood, liver, kidney, nasal cavity and placental barrier, and provides an overvi...
Source: Current Drug Metabolism - June 28, 2018 Category: Drugs & Pharmacology Authors: Yao JF, Yang H, Zhao YZ, Xue M Tags: Curr Drug Metab Source Type: research

Current Designs of Polymer Blends in Solid Dispersions for Improving Drug Bioavailability.
Abstract Ternary solid dispersions have been demonstrated to be an effective strategy in the improvement of drug absorption and bioavailability. The applications of the combination of hydrophilic polymers with the potential of hydrophobic polymer incorporation at moderate concentrations have been discussed in recent publications. In this paper, the general review of this specific type of solid dispersion will be provided with comprehensive understanding of polymer blends of either hydrophilic or hydrophobic polymers. A detailed description of miscible polymers has been developed in recent studies. In addition to d...
Source: Current Drug Metabolism - June 28, 2018 Category: Drugs & Pharmacology Authors: Tran PH, Duan W, Lee BJ, Tran TT Tags: Curr Drug Metab Source Type: research

Total sleep duration and risk of type 2 diabetes: Evidence based on clinical and epidemiological studies.
Abstract Increasing incidences of type 2 diabetes makes it necessary to have a better understanding of the risk factors for its prediction. Taking a note of resilience in risk factors, dynamics of the emerging factors other than traditional ones are showing a great interest in recent years which imprints a significant contribution in the occurrence of diabetes. Of different factors, sleep duration was acknowledged as a most common risk factor for dyslipidemia, obesity, hypertension, metabolic syndrome and diabetes. Adhering to the state of information available, the review highlights the underlying mechanisms towa...
Source: Current Drug Metabolism - June 28, 2018 Category: Drugs & Pharmacology Authors: Yadav D, Cho KH Tags: Curr Drug Metab Source Type: research

The Pharmacogenomics of Asthma beyond its Endotypes.
Abstract Asthma is a heterogeneous disease that consists of different phenotypes and endotypes, driven by different mechanistic pathways. An increasing number of genetic loci and single-nucleotide polymorphisms have been associated with therapeutic responses to asthma drugs. The purpose of this review is to focus on certain susceptibility genes, gene variants and typical therapeutic drugs of the glucocorticoid, leukotriene, histamine, and β2-adrenergic receptor pathways related to asthma. Pharmacogenomics can help us better understand the genetic basis of drug responses and better define new therapeutic targe...
Source: Current Drug Metabolism - June 28, 2018 Category: Drugs & Pharmacology Authors: Meng S, Chen S, Tao A Tags: Curr Drug Metab Source Type: research

Pharmacological and Therapeutic potential of Nitidine, a plant alkaloid.
Abstract Nitidine is a bioactive plant benzophenanthridine alkaloid isolated from the root of Zanthoxylum nitidum. Since its discovery in 1959, literature revealed marked anticancer, neuroprotective, antimalarial, anti-HIV, analgesic, anti-inflammatory, antifungal activities. MOE (molecular operating environment) ligand based pharmacophores features of nitidine showed that it has got multiple bioactive functional sites that implicating its sensitivity towards several receptors protein and therefore could be a useful lead compound. Despite having an outstanding therapeutic potential, it is not subjected to clinical...
Source: Current Drug Metabolism - June 28, 2018 Category: Drugs & Pharmacology Authors: Khan H, Hadda TB, Touzani R, Kamal MA Tags: Curr Drug Metab Source Type: research

Genetic Polymorphism on the Pharmacokinetics and Pharmacodynamics of Platelet-derived Growth Factor Receptor (PDGFR) Kinase Inhibitors.
This article also provides an overview of: (1) general information on PDGFR kinase inhibitors; (2) pharmacokinetic parameters of PDGFR kinase inhibitors; (3) metabolic enzymes and transporters of PDGFR kinase inhibitors; (4) main drug interactions of PDGFR kinase inhibitors; (5) adverse events of PDGFR kinase inhibitors; and (6) genetic polymorphism on pharmacokinetics and pharmacodynamics of PDGFR kinase inhibitors. PMID: 29956623 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - June 28, 2018 Category: Drugs & Pharmacology Authors: Qian Y, Yu L, Zhang XH, Yuan-Zi QY, Zhao P, Sun LN, Wang YQ Tags: Curr Drug Metab Source Type: research

The Role of E-cadherin in Helicobacter pylori-Related Gastric Diseases.
Abstract Helicobacter pylori (H. pylori)-related gastric diseases are a series of gastric mucosal disorders associated with H. pylori infection, including chronic gastritis, gastric ulcer and gastric cancer (GC) etc. The formation of GC is widely believed to be a multistep process, evolving from gastritis and gastric ulcer. Thus, to explore the mechanisms of gastric mucosa from benign to malignant pathological evolution process is the crux of prevention and treatment of GC. As an important adhesion molecule of epithelial cells, E-cadherin plays a key role in the development of gastric diseases. In this review, we ...
Source: Current Drug Metabolism - June 24, 2018 Category: Drugs & Pharmacology Authors: Zhang Y, Dai Y, Li R, Gao Y, Hu L Tags: Curr Drug Metab Source Type: research

Role of Osmolytes and their Transporter Systems in Pathogen Survival and Pathogenicity.
Abstract Pathogenic microbes routinely keep encountering different types of stress in their environment such as high osmolarity, high temperature, pH fluctuations in host gut etc. They tend to acquire certain small molecular weight molecules, termed osmolytes, so as to handle these challenges and survive despite them. These organic osmolytes even at higher concentrations are quite compatible with most of their ongoing intracellular processes. These osmolytes include some which are self-synthesized by the microorganisms, while majority of them are imbibed from the external environment via osmolyte transporters. In ...
Source: Current Drug Metabolism - June 24, 2018 Category: Drugs & Pharmacology Authors: Rahaman S, Archana A, Azam M, Minakshi R Tags: Curr Drug Metab Source Type: research

Recent advances in gold nanoformulations for cancer therapy.
Abstract Nanotechnology based diagnostic and therapeutic approaches have attracted great interest in oncology over the last few years. Especially gold (Au)-based nanoformulations have gained a lot of attention in cancer detection, therapy and monitoring of outcome. The current report provides a summary of methods how to prepare different types of synthetic gold nanoformulations and their potential applications in boosting photothermal and photodynamic tumor therapies and in radiosensitization. PMID: 29886825 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - June 10, 2018 Category: Drugs & Pharmacology Authors: Shevtsov M, Zhou Y, Khachatryan W, Multhoff G, Gao H Tags: Curr Drug Metab Source Type: research

The Therapeutic Role of Xenobiotic Nuclear Receptors against Metabolic Syndrome.
Abstract Xenobiotic nuclear receptors (XNRs) are nuclear receptors that characterized by coordinately regulating the expression of genes encoding drug-metabolizing enzymes and transporters to essentially eliminate and detoxify xenobiotics and endobiotics from the body, including the peroxisome proliferator-activated receptor (PPAR), the farnesoid X receptor (FXR), the liver X receptor (LXR), the pregnane X receptor (PXR) and the constitutive androstane receptor (CAR). Heretofore, increasing evidences have suggested that these five XNRs are not only involved in the regulation of xeno-/endo-biotics detoxication but ...
Source: Current Drug Metabolism - June 10, 2018 Category: Drugs & Pharmacology Authors: Pu S, Wu X, Yang X, Zhang Y, Dai Y, Zhang Y, Wu X, Liu Y, Cui X, Jin H, Cao J, Li R, Cai J, Cao Q, Hu L, Gao Y Tags: Curr Drug Metab Source Type: research

Amino acid metabolism in dairy cows and their regulation in milk synthesis.
Abstract Reducing dietary crude protein (CP) and supplementing with certain amino acids (AAs) has been known as a potential solution to improve nitrogen (N) efficiency in dairy production. Thus understanding how AAs are utilized in various sites along the gut is critical. AA flow from the intestine to portal-drained viscera (PDV) and liver then to the mammary gland was elaborated in this article. Recoveries in individual AA in PDV and liver seem to share similar AA pattern with input: output ratio in mammary gland, which subdivides essential AA (EAA) into two groups, lysine (Lys) and branched-chain AA (BCAA) in gr...
Source: Current Drug Metabolism - June 10, 2018 Category: Drugs & Pharmacology Authors: Wang F, Shi H, Wang S, Wang Y, Cao Z, Li S Tags: Curr Drug Metab Source Type: research

Hypoxia plays a key role in the pharmacokinetic changes of drugs at high altitude.
Abstract Hypoxia can alter the pharmacokinetic (PK) characteristics of drugs, thereby affecting drug absorption, distribution, metabolism, and excretion. Environmental characteristics at high altitude include but are not limited to hypobaric hypoxia, low temperature, high solar radiation, and arid climate, all of which can adversely affect normal bodily functions. Recent studies have indicated that hypoxia may play a key role in the PK changes of drugs at high altitude. Here we reported the effects of hypoxia on drug metabolism at high altitude, elaborated on the metabolic characteristics of some drugs and the act...
Source: Current Drug Metabolism - May 28, 2018 Category: Drugs & Pharmacology Authors: Zhou X, Nian Y, Qiao Y, Yang M, Xin Y, Li X Tags: Curr Drug Metab Source Type: research

Failure of Chemotherapy in Hepatocellular Carcinoma Due to Impaired and Dysregulated Primary Liver Drug Metabolizing Enzymes and Drug Transport Proteins: What to Do?
CONCLUSION: The future of HCC treatment should emphasize the understanding of resistance mechanisms and the finding of novel, safe, and efficacious therapeutic strategies, which will surely benefit patients affected by advanced HCC. PMID: 29807513 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 28, 2018 Category: Drugs & Pharmacology Authors: Ul Islam S, Ahmed MB, Shehzad A, Ul-Islam M, Lee YS Tags: Curr Drug Metab Source Type: research

A Review on the Expression and Metabolic Features of Orphan Human Cytochrome P450 2S1 (CYP2S1).
CONCLUSION: Molecular-based investigations should be performed to better understand the regulation mechanism of CYP2S1 in various cells and tissues. It is pivotal to establish optimum expression and incubation systems in vitro to elucidate the substrate specificity of CYP2S1 and characterise the genetic consequences of variant CYP2S1 in vitro. PMID: 29804525 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 27, 2018 Category: Drugs & Pharmacology Authors: Yan P, Eng OC, Yu CJ Tags: Curr Drug Metab Source Type: research

Editorial: Integrative Approach to Manage Neurological Disorders.
PMID: 29788866 [PubMed - in process] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 25, 2018 Category: Drugs & Pharmacology Authors: Zargaran A Tags: Curr Drug Metab Source Type: research

Impact of Drug Metabolism/Pharmacokinetics and Their Relevance upon Taxus-based Drug Development.
Abstract Drug metabolism and pharmacokinetic (DMPK) studies of Taxus natural products, their semi-synthetic derivatives and analogs are indispensable in the optimization of lead compounds and clinical therapy. These studies can lead to development of new drug entities with improved absorption, distribution, metabolism, excretion and toxicity (ADME/T) profiles. To date, there have been no comprehensive reviews of the DMPK features of Taxus derived medicinal compounds.Natural and semi-synthetic taxanes may cause and could be affected by drug-drug interaction (DDI). Hence ADME/T studies of various taxane-containing f...
Source: Current Drug Metabolism - May 22, 2018 Category: Drugs & Pharmacology Authors: Hao DC, Ge GB, Wang P, Yang L Tags: Curr Drug Metab Source Type: research

Models of Drug Induced Liver Injury (DILI) - Current Issues and Future Perspectives.
Abstract Drug-induced liver injury (DILI) is an important cause of acute liver failure cases in the United States, and remains a common cause of withdrawal of drugs in both preclinical and clinical phases. In this article, we review the existing knowledge of appropriate models to study DILI in vitro and in vivo with special focus on hepatic cell models, variations of 3D co-cultures, animal models, databases and predictive modeling and translational biomarkers developed to understand the mechanisms and pathophysiology of DILI. Besides descriptions of current applications of existing modeling systems, associated adv...
Source: Current Drug Metabolism - May 22, 2018 Category: Drugs & Pharmacology Authors: Kuna L, Bozic I, Kizivat T, Bojanic K, Mrso M, Kralj E, Smolic R, Wu GY, Smolic M Tags: Curr Drug Metab Source Type: research

Progress of Oral Insulin and Related Drug Delivery Systems and their Pharmacokinetics.
CONCLUSION: This review summarized recent advances in oral insulin and the pharmacokinetic profile of the suitable delivery system, providing valuable reference material for future research. PMID: 29788884 [PubMed - as supplied by publisher] (Source: Current Drug Metabolism)
Source: Current Drug Metabolism - May 22, 2018 Category: Drugs & Pharmacology Authors: Chen J, Liu R, Liu C, Jin X, Zhang Q, Wang J, Zhao F, Wang Z, Qiu H, Li Y, Yi X Tags: Curr Drug Metab Source Type: research