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The delicate balance between the good and the bad IL-1 proinflammatory effects in endometriosis.
CONCLUSIONS: This observation clearly suggested a significant inadequacy in the specific regulatory mechanisms of IL-1 activity at the peritoneal cavity level. The imbalance between all studied cytokines in endometriosis may escalate peritoneal inflammation and, in consequence, develop endometriosis. PMID: 29332562 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Sikora J, Ferrero S, Mielczarek-Palacz A, Kondera-Anasz Z Tags: Curr Med Chem Source Type: research

Multi-Target Directed Drugs as a Modern Approach for Drug Design Towards Alzheimer's Disease: an update.
Abstract Alzheimer's disease (AD) is a progressive multifactorial neurodegenerative disorder. Currently, no effective treatment is available and this is due to multiple factors involved in pathophysiology and severity of AD. A recent approach for the rational design of new drug candidates, also called multitarget-directed ligands (MTDL) strategy, has been used to develop a variety of hybrid compounds capable to act simultaneously in diverse biological targets. The discovery of drug molecules capable of targeting multiple factors involved in AD pathogenesis would greatly facilitate in improving therapeutic strategi...
Source: Current Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: de Freitas Silva M, Dias KST, Gontijo VS, Ortiz CJC, Viega C Tags: Curr Med Chem Source Type: research

Mesenchymal Stem Cell Therapy in Intracerebral Haemorrhagic Stroke.
CONCLUSION: Further studies have to be implemented in order to achieve standardized methods of MSCs isolation, characterization and administration to improve ICH treatments with MSCs or MSC-derived products. PMID: 29332564 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Bedini G, Bersano A, Zanier ER, Pischiutta F, Parati EA Tags: Curr Med Chem Source Type: research

Beyond the "lock and key" paradigm: targeting lipid rafts to induce the selective apoptosis of cancer cells.
Beyond the "lock and key" paradigm: targeting lipid rafts to induce the selective apoptosis of cancer cells. Curr Med Chem. 2018 Jan 10;: Authors: Alves ACS, Dias RA, Kagami LP, das Neves GM, Torres FC, Eifler-Lima VL, Carvalho I, de Miranda Silva C, Kawano DF Abstract For more than 40 years, the fluid mosaic model of cellular membranes have supported our vision of an inert lipid bilayer containing membrane protein receptors that are randomly hit by extracellular molecules to trigger intracellular signaling events. However, the notion that compartmentalized cholesterol- and sphingomyelin-ric...
Source: Current Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Alves ACS, Dias RA, Kagami LP, das Neves GM, Torres FC, Eifler-Lima VL, Carvalho I, de Miranda Silva C, Kawano DF Tags: Curr Med Chem Source Type: research

Stimuli responsive nanoparticles for controlled anti-cancer drug release.
Abstract Conventional drugs used for cancer chemotherapy have severe toxic side effects and show individually varied therapeutic responses. The convergence of nanotechnology, biology, material science and pharmacy offers a perspective strategy for cancer chemotherapy. Nanoparticles loaded with anti-cancer drug have been designed to overcome the limitations associated with conventional drugs, several nanomedicines have been approved by FDA and shown good performances in clinical practice. However, the therapeutic efficacies cannot be enhanced. Take into this account, stimuli responsive nanoparticles present the abi...
Source: Current Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Tang Q, Yu B, Gao L, Cong H, Song N, Lu C Tags: Curr Med Chem Source Type: research

Nociceptin /Orphanin FQ Peptide (NOP) receptor Modulators: an Update in Structure-Activity Relationships.
Abstract Nociceptin /Orphanin FQ Peptide" receptor (NOPr) is a G-protein-coupled receptor with the nociceptin/orphanin FQ peptide (N/OFQ) as endogenous agonist. It is expressed in the nervous system as well as in some non-neural tissues. Its activation has pronociceptive effect at the supraspinal level, whereas at the spinal level it produces nociceptive effects at low doses and antinociceptive effects at higher doses. NOPr is also involved in mood and blood pressure regulation, immunoregulation, airway constriction, feeding, urination, bowel motility, learning and memory. Selective NOPr agonists have been te...
Source: Current Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Mustazza C, Pieretti S, Marzoli F Tags: Curr Med Chem Source Type: research

FGF-21 as a potential biomarker for mitochondrial diseases.
Abstract The diagnosis of mitochondrial diseases is still challenging due to clinical and genetical heterogeneity. The development of advanced technologies including Whole-Exome-Sequencing (WES) and Whole-Genome-Sequencing (WGS) have led to improvements in genetic diagnosis. However, a reliable biomarker in serum could enhance and ease the diagnosis and indeed reduce the need for muscle biopsy. Several studies suggest Fibroblast growth factor 21 (FGF-21) as a biomarker for diagnosis in mitochondrial disorders. It is known, that in patients with mitochondrial disorders, the expression of FGF-21 gets elevated in an ...
Source: Current Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Scholle LM, Lehmann D, Deschauer M, Kraya T, Zierz S Tags: Curr Med Chem Source Type: research

Cancer Treatment with Liposomes Based Drugs and Genes Co-delivery Systems.
This article provides a brief review on the liposomes based co-delivery systems to overcome cancer resistance by the synergistic effects of drugs and genes. Particularly, the synergistic effects of combinatorial anti-cancer drugs and genes in various cancer models employing multifunctional liposomes based co-delivery systems have been discussed. This review also gives new insights into the challenges of liposomes based co-delivery systems in the field of cancer therapy, by which we hope to provide some suggestions on the development of liposomes based co-delivery systems. PMID: 29332569 [PubMed - as supplied by publis...
Source: Current Medicinal Chemistry - January 10, 2018 Category: Chemistry Authors: Zhang C, Zhang S, Zhi D, Cui J Tags: Curr Med Chem Source Type: research

Novel Biological Therapies in Severe Asthma: Targeting the Right Trait.
Abstract Asthma is a heterogeneous disease characterized by chronic airway inflammation that results in a wide spectrum of clinical manifestations. Patients with severe asthma represent a substantial share of consumption of healthcare resources and hospitalization. Moreover, these patients are at risk of increased morbidity and mortality. Recently, several phenotypes and endotypes of asthma have been identified. The identification of specific subtypes of asthma is fundamental for optimizing the clinical benefit of novel treatments. Although in most patients the disease can be controlled by some combination of phar...
Source: Current Medicinal Chemistry - January 9, 2018 Category: Chemistry Authors: Varricchi G, Marone G, Spadaro G, Russo M, Granata F, Genovese A, Marone G Tags: Curr Med Chem Source Type: research

Nano-scale gene delivery systems; current technology, obstacles, and future directions.
In conclusion, we hope that by bringing the far reaching multidisciplinary nature of nano-gene delivery to light, new targeted nanotechnology-bases strategies are developed to overcome the major challenges covered in this review. PMID: 29308734 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - January 7, 2018 Category: Chemistry Authors: Garcia-Guerra A, Dunwell TL, Trigueros S Tags: Curr Med Chem Source Type: research

Unfolding Cardiac Amyloidosis - From Pathophysiology to Cure.
Abstract Deposition of amyloidogenic proteins leading to the formation of amyloid fibrils in the myocardium cause cardiac amyloidosis. Although any form of systemic amyloidosis can affect the heart, light-chain (AL) or transthyretin amyloidosis (ATTR) account for the majority of diagnosed cardiac amyloid deposition. The extent of cardiac disease independently predicts mortality. The reversal or arrest of adverse cardiac remodeling is the target of current therapies, as cardiac-related mortality worsens prognosis in patients where the underlying systemic amyloidosis was successfully treated. Here, we provide a cond...
Source: Current Medicinal Chemistry - January 4, 2018 Category: Chemistry Authors: Ablasser K, Verheyen N, Glantschnig T, Agnetti G, Rainer PP Tags: Curr Med Chem Source Type: research

Is There A Role For Lifestyle Interventions In Obsessive-Compulsive And Related Disorders?
l M Abstract Many of the currently available treatments for obsessive-compulsive and related disorders (OCRDs) such as pharmacotherapy augmentation strategies, partial hospitalization programs, deep brain stimulation, and neurosurgery are efficacious for individuals suffering from more severe forms of these conditions. Unfortunately, the application of these treatments in milder forms of illness and subclinical samples, which affect a substantial portion of the population, is not justifiable by their costs (e.g. cognitive-behavioral therapy) and/or potential for side effects (serotonin-reuptake inhibitors associat...
Source: Current Medicinal Chemistry - January 4, 2018 Category: Chemistry Authors: Fontenelle LF, Quintas JN, Yücel M Tags: Curr Med Chem Source Type: research

Prenylated Coumarins of the Genus Citrus: an Overview of the 2006-2016 Literature Data.
Abstract O-Prenyl coumarins (3,3-dimethylallyl, geranyl-, farnesyl- and related biosynthetic derivatives) represent a class of rarely occurring natural products. In the last two decades such secondary metabolites have been found to possess promising and effective pharmacological properties, mainly in terms of anti-cancer and anti-inflammatory properties. To date about 160 oxyprenylated coumarins have been extracted from plants, fungi, and bacteria. The genus Citrus have been demonstrated to be among the richest source of the title products. The aim of this comprehensive review is to make a survey of the in so far ...
Source: Current Medicinal Chemistry - January 4, 2018 Category: Chemistry Authors: Genovese S, Taddeo VA, Epifano F, Fiorito S Tags: Curr Med Chem Source Type: research

Generation of Reactive Oxygen Species by Photosensitizers and their Modes of Action on Proteins.
We describe three targeting paradigms for achieving this objective. The first involves the use of a photosensitizer with a high affinity for its target protein; in this case, the photosensitizer is methylene blue for acetylcholinesterase. The second paradigm involves the use of the hydrophobic photosensitizer hypericin, which has the capacity to interact selectively with partially unfolded forms of proteins, including nascent species in rapidly dividing or virus-infected and cancer cells, acting preferentially at membrane interfaces. In this case, partially unfolded molten globule species of acetylcholinesterase serve as t...
Source: Current Medicinal Chemistry - January 4, 2018 Category: Chemistry Authors: Bilkis I, Silman I, Weiner L Tags: Curr Med Chem Source Type: research

Common aspects influencing the translocation of SERS to Biomedicine.
We present the advantages and limitations of this technique relevant for bioanalysis in vitro and in vivo and how this technique goes beyond the state of the art of traditional analytical, labelling and healthcare diagnosis technologies. PMID: 29303073 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - January 4, 2018 Category: Chemistry Authors: Gil PR, Tsouts D, Xiao C, An W, Sanles-Sobrido M, Cabo A Tags: Curr Med Chem Source Type: research

Olfactory loss and dysfunction in ciliopathies: Molecular mechanisms and potential therapies.
Abstract Ciliopathies are a class of inherited pleiotropic genetic disorders in which alterations in cilia assembly, maintenance, and/or function exhibit penetrance in the multiple organ systems. Olfactory dysfunction is one such clinical manifestation that has been shown in both patients and model organisms. Existing therapies for ciliopathies are limited to the treatment or management of symptoms. The last decade has seen an increase in potential curative therapeutic options including small molecules and biologics. Recent work in multiciliated olfactory sensory neurons has demonstrated the capacity of targeted g...
Source: Current Medicinal Chemistry - January 4, 2018 Category: Chemistry Authors: Uytingco CR, Green WW, Martens JR Tags: Curr Med Chem Source Type: research

ABC transporters: Regulation and association with multidrug resistance in hepatocellular carcinoma and colorectal carcinoma.
Abstract For most cancers, the treatment of choice is still being chemotherapy despite of its severe adverse effects, systemic toxicity and limited efficacy due to the development of multidrug resistance (MDR). MDR leads to chemotherapy failure generally associated with a decrease in drug concentration inside cancer cells, frequently due to an overexpression of ABC transporters such as P-glycoprotein (P-gp/MDR1/ABCB1), multidrug resistance-associated proteins (MRPs/ABCCs), and breast cancer resistance protein (BCRP/ABCG2) that limit the efficacy of chemotherapeutic drugs. The aim of this review is to compile infor...
Source: Current Medicinal Chemistry - January 4, 2018 Category: Chemistry Authors: Mancini MPC, Rigalli JP, Cere LI, Semeniuk M, Catania VA, Ruiz ML Tags: Curr Med Chem Source Type: research

Imparting pharmaceutical applications to the surface of fabrics for wound and skin care by ultrasonic waves.
We present coatings from inorganic, organic and biochemical nanoparticles (NPs) on surfaces that impart the ability to kill bacteria, avoid biofilm formation and speed up the recovery of wounds. In all three cases, sonochemistry is used for immobilizing the nanoparticles on the surfaces. The Introduction broadly covers the progress of nanotechnology in the fields of wound and skin care. The first section of this review outlines the mechanism of the ultrasound-assisted deposition of nanoparticles on textiles. The coating can be performed by an in-situ process in which the nanoparticles are formed and subsequently thrown ont...
Source: Current Medicinal Chemistry - December 29, 2017 Category: Chemistry Authors: Gedanken A, Perkas N, Perelshtein I, Lipovsky A Tags: Curr Med Chem Source Type: research

Inorganic Nanoparticles for Cancer Therapy: a Transition from Lab to Clinic.
Abstract Inorganic nanoparticles (NPs) including those derived from metals (e.g., gold, silver), semiconductors (e.g., quantum dots), carbon dots, carbon nanotubes, or oxides (e.g., iron oxide), have been deeply investigated recently for diagnostic and therapeutic purposes in oncology. Compared to organic nanomaterials, inorganic NPs have advanced advantages and unique characteristics for better imaging and drug delivery. Still, only a limited number of inorganic NPs are translated into clinical practice. In this review, we discuss the progression of inorganic NPs for cancer therapy and imaging, focusing our atten...
Source: Current Medicinal Chemistry - December 29, 2017 Category: Chemistry Authors: Bayda S, Hadla M, Palazzolo S, Corona G, Toffoli G, Rizzolio F Tags: Curr Med Chem Source Type: research

MRP4/ABCC4 as a new therapeutic target: meta-analysis to determine cAMP binding sites as a tool for drug design.
Abstract MRP4 transports multiple endogenous and exogenous substances and is critical not only for detoxification but also in the homeostasis of several signaling molecules. Its dysregulation has been reported in numerous pathological disorders, thus MRP4 appears as an attractive therapeutic target. However, the efficacy of MRP4 inhibitors is still controversial. The design of specific pharmacological agents with the ability to selectively modulate the activity of this transporter or modify its affinity to certain substrates represents a challenge in current medicine and chemical biology. The first step in the lon...
Source: Current Medicinal Chemistry - December 29, 2017 Category: Chemistry Authors: Yaneff A, Sahores A, Gomez N, Carozzo A, Shayo C, Davio C Tags: Curr Med Chem Source Type: research

The interplay between G-quadruplex and Transcription.
Abstract G4 DNA is a non-canonical DNA structure consisting of a stacked array of G-quartets held together by base pairing between guanine bases. The formation of G4 DNA requires a cluster of guanine-runs within a strand of DNA. Even though the chemistry of this remarkable DNA structure has been under investigation for decades, evidence supporting the biological relevance of G4 DNA has only begun to emerge and point to very important and conserved biological functions. This review will specifically focus on the interplay between transcription and G4 DNA and discuss two alternative but interconnected perspectives. ...
Source: Current Medicinal Chemistry - December 29, 2017 Category: Chemistry Authors: Kim N Tags: Curr Med Chem Source Type: research

Neuroprotective effects of flavonoid compounds on neuronal death associated to Alzheimer`s disease.
Abstract Alzheimer's disease is an increasing neurodegenerative pathology related to age in many societies. Some aspects of the disease are related to the loss of neuronal cells derived by the formation of extracellular neuritic plaques and the appearance of intracellular neurofibrillary tangles, altogether generate a inflammatory and oxidative status. The accumulation of amyloids in cells induces the activation of the apoptotic cascade which implies capases activation. Alzheimer's disease is treated with acetylcholine esterase inhibitors, although their effects are still far away to reduce or eliminate the proble...
Source: Current Medicinal Chemistry - December 25, 2017 Category: Chemistry Authors: Sureda A, Xavier C, Tejada S Tags: Curr Med Chem Source Type: research

Role of Redox Homeostasis and Inflammation in the Pathogenesis of Pulmonary Arterial Hypertension.
k P Abstract This review addresses pulmonary arterial hypertension (PAH), an incurable disease, which determines high morbidity and mortality. Definition of the disease, its characteristics, classification, and epidemiology are discussed. A difficulty in the diagnosis of PAH due to the lack of symptoms specificity is highlighted. Echocardiographic analysis and electrocardiogram of patients help in the diagnosis and in the follow up of the disease. Nevertheless, right ventricle (RV) catheterization constitutes the gold standard for diagnosing PAH. Oxidative stress and inflammation, in an interactive manner, play a ...
Source: Current Medicinal Chemistry - December 25, 2017 Category: Chemistry Authors: Bello-Klein A, Mancardi D, da Rosa Araujo AS, Schenkel PC, de Lima Seolin BG, Türck P Tags: Curr Med Chem Source Type: research

Looking for new antifungal drugs from flavonoids: impact of the genetic diversity of Candida albicans on the in-vitro response.
Abstract In an era in which antimicrobial resistance is increasing at an alarming pace, it's very important to find new antimicrobial agents effective against pathogenic microrganisms resistant to traditional treatments. Among the notable breakthroughs in the past years of research in natural-drug discovery there is the identification and testing of flavonoids, a group of plant-derived substances capable of promoting many beneficial effects on humans. These compounds show different biological activities such as inhibition of neuroinflammation and tumor growth as well as antidepressant, antiarthritic, anti-hypercho...
Source: Current Medicinal Chemistry - December 25, 2017 Category: Chemistry Authors: Felice MR, Giuffre L, El Aamri L, Hafidi M, Criseo G, Romeo O, Scordino F Tags: Curr Med Chem Source Type: research

A systematic review of evidence-based treatment strategies for obsessive-compulsive disorder resistant to first-line pharmacotherapy.
CONCLUSION: Treatment-resistant OCD remains a significant challenge to psychiatrists. To date, the most effective strategy is the addition of antipsychotics (aripiprazole and risperidone) to SRIs; another effective strategy is CBT addition to medications. Other strategies, such as the switch to another first-line treatment or the switch to intravenous administration are promising but need further confirmation in double-blind studies. The addition of medications other than antipsychotics remains to be studied, as several negative studies exist and positive ones need confirmation (only 1 positive study). PMID: 29278206 ...
Source: Current Medicinal Chemistry - December 22, 2017 Category: Chemistry Authors: Albert U, Marazziti D, Di Salvo G, Solia F, Rosso G, Maina G Tags: Curr Med Chem Source Type: research

Omecamtiv mecarbil: a myosin motor activator agent with promising clinical performance and new in vitro results.
Abstract Clinical treatment of heart failure is still suffering from limited efficacy and unfavorable side effects. The recently developed group of agents, the myosin motor activators, act directly on cardiac myosin resulting in an increased force generation and prolongation of contraction. The lead molecule, omecamtiv mecarbil is now in human phase 3. In addition to the promising clinical data published so far, there are new in vitro results indicating that the effect of omecamtiv mecarbil on contractility is rate-dependent. Furthermore, omecamtiv mecarbil was shown to activate cardiac ryanodine receptors, an eff...
Source: Current Medicinal Chemistry - December 22, 2017 Category: Chemistry Authors: Nanasi P, Komaromi I, Gaburjakova M, Almassy J Tags: Curr Med Chem Source Type: research

Plant-Made Antibodies: Properties and Therapeutic Applications.
Abstract A cost-effective plant platform for therapeutic monoclonal antibody production is both flexible and scalable. In addition, plant-made antibodies (PMAbs) could be advantageous compared to those produced in animal cells due to the absence of a risk of contamination from nucleic acids or proteins of animal origin. In this review, the various platforms of PMAbs production are described, and the widely used transient expression system based on Agrobacterium-mediated delivery of genetic material into plant cells is discussed in detail. Plants produce less complex and diverse Asn-attached glycans compared to ani...
Source: Current Medicinal Chemistry - December 11, 2017 Category: Chemistry Authors: Komarova TRV, Sheshukova EV, Dorokhov YL Tags: Curr Med Chem Source Type: research

Uterine function: from normal to Polycystic Ovarian Syndrome alterations.
CONCLUSIONS: Women with PCOS display a dysregulation of the Hypothalamic-Pituitary-Ovarian axis, which alters the steroid pathway. In addition, the deficiency in the withdrawal of estrogen and progesterone in the endometrium results in abnormal endometrial cellular proliferation. The imbalance in adipose tissue observed in PCOS patients reinforces the increases in circulating hormones. The present review describes the role of hormones, metabolites, cytokines, adhesion molecules and the insulin/glucose pathway related to the uterine endometrium in women with PCOS and their role in implantation failure and development of end...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Ferreira SR, Motta AB Tags: Curr Med Chem Source Type: research

Role of matrix metalloproteinases in degenerative kidney disorders.
Abstract Matrix metalloproteinases (MMPs) are members of calcium dependent-zinc containing endopeptidases that play a pivotal role in extracellular matrix (ECM) remodeling. MMPs are also known to cleave non-matrix proteins, including cell surface receptors, TNF-α, angiotensin-II, growth factors, (especially transforming growth factor-β1, ΤGF-β1) plasminogen, endothelin and other bioactive molecules. The tissue inhibitors of metalloproteinases (TIMPs) inhibit the activity of MMPs and decrease ECM degradation. Various patho-physiological conditions have been linked with the imbalance of ECM synth...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Narula S, Tandon C, Tandon S Tags: Curr Med Chem Source Type: research

Preventive and Therapeutic potentials of Anthocyanins in diabetes and associated complications.
Abstract Diet is an essential factor affecting the development of and risk for diabetes mellitus. In search of preventative and therapeutic strategies, it is to be considering the potential role of certain foods and their bioactive compounds to prevent the pathogenesis associated with metabolic diseases. Human consumption of anthocyanins is among the highest of all flavonoids. Epidemiological studies have suggested that the consumption of anthocyanins lowers the risk of diabetes and diabetic complications. Anthocyanins are important natural bioactive pigments responsible for red to blue colour of fruits, leaves, s...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Putta S, Yarla NS, Kumar EK, Lakkappa DB, Kamal MA, Scotti L, Scotti MT, Ashraf GM, Barreto GE, Rao BSB, Kumari DS, Reddy GV, Tarasov VV, Imandi SB, Aliev G Tags: Curr Med Chem Source Type: research

Potential drug targets in the pentose phosphate pathway of trypanosomatids.
Abstract The trypanosomatids, Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp, are causative agents of important human diseases such African sleeping sickness, Chagas' disease and Leishmaniasis, respectively. The high impact of these diseases on human health and economy worldwide, the unsatisfactory available chemotherapeutic options and the absence of human effective vaccines, strongly justifies the search for new drugs. The pentose phosphate pathway has been proposed to be a viable strategy to defeat several infectious diseases, including those from trypanosomatids, as it includes an oxidative branch, i...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Loureiro I, Faria J, Santarem N, Smith TK, Tavares J, Cordeiro-da-Silva A Tags: Curr Med Chem Source Type: research

New insights into adipokines as potential biomarkers for type-2 diabetes mellitus.
In conclusion, further studies are needed to clarify the pathophysiological significance and clinical value of these biological factors as potential biomarkers in type-2 diabetes and related dysfunctions. PMID: 29210636 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Catalina MO, Redondo PC, Cantonero-Chamorro C, Granados MP, Sanchez-Collado J, Albarran L, Lopez J Tags: Curr Med Chem Source Type: research

Metallopharmaceuticals in Therapy - a New Horizon for Scientific Research.
Abstract Coordination chemistry offers much scope for the design of novel and therapeutic agents, including metallopharmaceuticals. The widespread use of metal complexes as effective pharmaceuticals, e.g. cancer therapeutic, anti-inflammatory, antidiabetic drugs or antimicrobial and diagnostic agents, demonstrates that the cytotoxicity of metal ions can be finely controlled via the appropriate choice of ligands. The successful targeting of radioisotopes again depends on the ligand design and metal oxidation state. The complexes of platinum, ruthenium, cobalt, copper and other d-block metal ions have been used in m...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Chylewska A, Biedulska M, Sumczynski P, Makowski M Tags: Curr Med Chem Source Type: research

Medical applications of collagen and collagen-based materials.
Abstract Collagen and collagen-based materials have been successfully used in medicine for over 50 years. The number of scientific articles about the role of collagen in the construction of scaffolds for tissue engineering has risen precipitously in recent years. The review contains materials about historic and modern applications of collagen in medicine such as soluble collagen injections, solid constructs reconstructed from solution, and decellularized collagen matrices. The analysis of published data proves the efficacy of collagen material in the treatment of chronic wounds, burns, venous and diabetic ulcers, ...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Shekhter AB, Fayzullin AL, Vukolova MN, Rudenko TG, Osipycheva VD, Litvitsky PF Tags: Curr Med Chem Source Type: research

Guanylate cyclase C: a current hot target, from physiology to pathology.
Abstract Guanylate cyclase C (GC-C) receptor is a transmembrane receptor, predominantly expressed in intestinal epithelial cells, that plays a main role in homeostasis and function of the digestive tract. The endogenous ligands for this receptor are the paracrine hormones uroguanylin and guanylin. The heat-stable enterotoxin, produced by enterotoxigenic bacteria, is also a natural ligand of this receptor. Upon ligand binding, GC-C receptors increase the second messenger cyclic guanosine monophosphate (cGMP) levels, regulating a variety of key cell-type specific processes such as chloride and bicarbonate secretion ...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Uranga JA, Castro M, Abalo R Tags: Curr Med Chem Source Type: research

Fine-tuning of microRNAs in type 2 diabetes mellitus.
Abstract Type 2 diabetes mellitus is a metabolic disease widely spread across industrialized countries. Sedentary lifestyle and unhealthy alimentary habits lead to obesity, boosting both glucose and fatty acid in the bloodstream and eventually, insulin resistance, pancreas inflammation and faulty insulin production or secretion, all of them very well-defined hallmarks of type 2 diabetes mellitus. miRNAs, are small sequences of non-coding RNA that may regulate several processes within the cells, fine-tuning protein expression, with an unexpected and subtle precision and in time-frames ranging from minutes to days. ...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Rosado JA, Diez-Bello R, Salido GM, Salido GM Tags: Curr Med Chem Source Type: research

Dynamic Localization of Hepatocellular Transporters: Role in Biliary Excretion and Impairment in Cholestasis.
Abstract Bile flow generation is driven by the vectorial transfer of osmotically active compounds from sinusoidal blood into a confined space, the bile canaliculus. Hence, localization of hepatocellular transporters relevant to bile formation is crucial for bile secretion. Hepatocellular transporters are localized either in the plasma membrane or in recycling endosomes, from where they can be relocated to the plasma membrane on demand, or endocytosed when the demand decreases. The balance between endocytic internalization/exocytic targeting to/from this recycling compartment is therefore the main determinant of th...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Roma MG, Barosso IR, Miszczuk GS, Crocenzi FA, Pozzi EJS Tags: Curr Med Chem Source Type: research

Antidiabetics: Structural Diversity of Molecules with a Common Aim.
CONCLUSION: As diabetes becomes a more common disease, interest in new pharmacological targets is on the rise. PMID: 29210642 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Popovic-Dordevic JB, Jevtic II, Stanojkovic TP Tags: Curr Med Chem Source Type: research

Adipokines and Myokines: A Pivotal Role in Metabolic and Cardiovascular Disorders.
Abstract Obesity induces an imbalance in the expression and secretion of several cytokines, which contributes to the development of metabolic and cardiovascular disorders. On the contrary, skeletal muscle is known to have a role in reversing the detrimental impact of obesity. It has been established that adipose tissue acts as an endocrine organ that secretes proinflammatory and anti-inflammatory adipokines. Similarly, skeletal muscle produces secretory molecules, called myokines, from contracting muscle fibers. Myokines were recently recognized as beneficial modulators of obesity, metabolic syndrome, and type 2 d...
Source: Current Medicinal Chemistry - December 5, 2017 Category: Chemistry Authors: Chung HS, Choi KM Tags: Curr Med Chem Source Type: research

Recent evidence on the role of dietary PUFAs in cancer development and prevention.
Abstract During the last decades a great bulk of scientific information has been accumulated about the metabolic effects of polyunsaturated fatty acids (PUFAs) that can impact human health. In particular, a growing body of evidence from in vitro, animal, and clinical studies supporting the use of n-3 PUFAs in cancer prevention has been collected. Furthermore, a considerable effort has recently been done to evaluate the hypothesis that n-3 PUFAs might improve the efficiency of currently used anticancer drugs. The role of n-6 PUFAs, in contrast, needs to be better assessed. A high dietary intake of n-6 PUFAs has bee...
Source: Current Medicinal Chemistry - December 4, 2017 Category: Chemistry Authors: D'Archivio M, Scazzocchio B, Vari R, Santangelo C, Giovannini C, Masella R Tags: Curr Med Chem Source Type: research

Carboxylesterase inhibitors: an update.
Abstract Mammalian carboxylesterases are key serine hydrolases that catalyze the hydrolysis of a wide variety of ester compounds into the corresponding carboxylic acids and alcohols. In human, two major carboxylesterases, CES1 and CES2, have been identified and well-studied over the past decade. CES1 inhibitors have potential applications in the treatment of hypertriglyceridaemia, obesity and type 2 diabetes, owing to that this enzyme plays prominent role in the metabolism of cholesteryl esters. CES2 plays crucial roles in the metabolic activation of many prodrugs including anticancer agents capecitabine and CPT-1...
Source: Current Medicinal Chemistry - December 4, 2017 Category: Chemistry Authors: Zou LW, Jin Q, Wang DD, Qian QK, Hao DC, Ge GB, Yang L Tags: Curr Med Chem Source Type: research

New treatments for allergy: Advances in peptide immunotherapy.
CONCLUSION: Experimental models and clinical trials have demonstrated the usefulness of SPIRE treatment to cure these diseases, opening a new era in allergen therapeutics. PMID: 29205109 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 30, 2017 Category: Chemistry Authors: Calzada D, Baos S, Cremades L, Cardaba BO Tags: Curr Med Chem Source Type: research

In Silico Prediction of P-glycoprotein Binding: Insights from Molecular Docking Studies.
Abstract The P-glycoprotein is an efflux transporter that expels substances out of the cells and has an important impact in the pharmacokinetic and pharmacodynamic properties of drugs. The study of the interactions between ligands and the P-glycoprotein has implications in the design of Central Nervous System drugs and their transport across the blood-brain barrier. Moreover, since the P-glycoprotein is overexpressed in some types of cancers, the protein is responsible for expelling the drug therapies from the cells, and hence, for drug resistance. In this review we describe different P-glycoprotein binding sites ...
Source: Current Medicinal Chemistry - November 29, 2017 Category: Chemistry Authors: Vilar S, Sobarzo-Sanchez E, Uriarte E Tags: Curr Med Chem Source Type: research

Metals and Parkinson's disease: Mechanisms and biochemical processes.
ter J Abstract Genetic background accounts for only 5 to 10% of the reported cases of Parkinson's disease (PD), while the remaining cases are of unknown etiology. It is believed that environmental factors may be involved in the causality of a large proportion of PD cases. Several PD genes are activated by xenobiotic exposure, and a link between pesticide exposure and PD has been demonstrated. Many epidemiological studies have shown an association between PD and exposure to metals such as mercury, lead, manganese, copper, iron, aluminum, bismuth, thallium, and zinc. This review explores the biological effects, the ...
Source: Current Medicinal Chemistry - November 29, 2017 Category: Chemistry Authors: Bjørklund G, Stejskal V, Urbina MA, Dadar M, Chirumbolo S, Mutter J Tags: Curr Med Chem Source Type: research

Journey of 2'-deoxy-2'-fluoro-5-methyl-1- β-D-arabinofuranosyluracil (FMAU): from Antiviral Drug to PET Imaging Agent.
CONCLUSION: While FMAU was not successful as an antiviral agent, 18F-FMAU is a suitable radiotracer for early detection of cancer and assessment of response to therapy by PET. The process of clinical grade 18F-FMAU production requires further improvement. 18F-FMAU has high potential for clinical application, but further extensive studies are needed to establish this tracer in diagnosis of various cancers and assessment of their response to therapy. PMID: 29189119 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 29, 2017 Category: Chemistry Authors: Alauddin MM Tags: Curr Med Chem Source Type: research

Critical Role of IL-8 Targeting in Gliomas.
CONCLUSION: Several promising approaches that target directly or indirectly IL-8 effects in gliomas are currently in progress while more-in-depth studies are needed to validate its biomarker role and elucidate the underlying molecular mechanisms. PMID: 29189120 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 29, 2017 Category: Chemistry Authors: Kosmopoulos M, Christofides A, Drekolias D, Zavras PD, Gargalionis AN, Piperi C Tags: Curr Med Chem Source Type: research

The Development of Biologically Important Spirooxindoles as New Antimicrobial Agents.
Abstract Spirooxindoles are privileged scaffolds because of their prevalence in numerous biologically validated natural alkaloids and pharmaceutically relevant molecules. In last decades, a large number of structurally novel spirooxindoles have been synthesized mainly based on the ylide intermediates generated in situ and further assessed for their bioactivities. While the antimicrobial activity against different types of bacteria is relatively less studied, mainly centering on primary antimicrobial assessment, some of these compounds have showed interesting antimicrobial activity, comparable to that of antibiotic...
Source: Current Medicinal Chemistry - November 29, 2017 Category: Chemistry Authors: Yang YT, Zhu JF, Liao G, Xu HJ, Yu B Tags: Curr Med Chem Source Type: research

Synthetic polymer-based electrospun fibers: biofunctionalization strategies and recent advances in tissue engineering, drug delivery and diagnostics Vincent Pertici.
CONCLUSION: Owing to flexibility and robustness of ES process as well as advances in conjugation and polymer/material engineering, high degree of control over biofunctionalization can now be achieved, to fit as best as possible the requirements of the targeted application. The performances reached up to now augur well for the future of such class of materials. PMID: 29189122 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 29, 2017 Category: Chemistry Authors: Pertici V, Martrou G, Gigmes D, Trimaille T Tags: Curr Med Chem Source Type: research

Anti-Aging Drugs - Prospect of Longer Life?
CONCLUSION: There is a call for more longitudinal clinical trials, which would prove the efficacy of the promising anti-aging drugs candidates in humans. PMID: 29189123 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 29, 2017 Category: Chemistry Authors: Klimova B, Novotny M, Kuca K Tags: Curr Med Chem Source Type: research

Overview on Anticancer Drug Design and Development.
Abstract Many impediments of current anti-cancer therapies have urged scientists to discover new agents. As a result of growing spectrums of new targets and strategies and recent biological and biotechnological progresses, many anti-cancer agents such as monoclonal antibodies, small molecule tyrosine kinase inhibitors and epigenetic drugs have been reached to clinical trials. Addition to the traditional targets (mitosis, DNA synthesis, repairing systems, tumor growth, apoptosis, tumor vasculature and cell signaling mechanisms), other targets such as proteasome, heat shock proteins (HSPs), and epigenetics (HDACs, H...
Source: Current Medicinal Chemistry - November 29, 2017 Category: Chemistry Authors: Olgen S Tags: Curr Med Chem Source Type: research