From recognition to reaction mechanism: an overview on the interactions between HIV-1 protease and its natural targets.
Abstract Current investigations of the human immunodeficiency virus protease (HIV-1 PR) as a druggable target towards the treatment of AIDS require an update to facilitate further development of promising inhibitors with improved inhibitory activities. For the past two decades, up to 100 scholarly reports appeared annually on the inhibition and catalytic mechanism of HIV-1 PR. A fundamental literature review on the prerequisite of HIV-1 PR action leading to the release of infectious virion is absent. Herein, recent advances (both computationally and experimentally) on the recognition mode and reaction mechanism of...
Source: Current Medicinal Chemistry - November 13, 2018 Category: Chemistry Authors: Lawal MM, Sanusi ZK, Govender T, Maguire GEM, Honarparvar B, Kruger HG Tags: Curr Med Chem Source Type: research

Use of hemoglobin for delivering exogenous carbon monoxide in medicinal applications.
Abstract Carbon monoxide (CO), at low concentrations, can have a variety of positive effects on the body including anti-apoptosis, anti-inflammatory, anti-oxidative and anti-proliferative effects. Although CO has great potential for use as a potent medical bioactive gas, for it to exist in the body in stable form, it must be associated with a carrier. Hemoglobin (Hb) represents a promising material for use as a CO carrier because most of the total CO in the body is stored associated with Hb in red blood cells (RBC). Attempts have been made to develop an Hb-based CO carrying system using RBC and Hb-based artificial...
Source: Current Medicinal Chemistry - November 13, 2018 Category: Chemistry Authors: Taguchi K, Maruyama T, Otagiri M Tags: Curr Med Chem Source Type: research

Nanoparticle-Plasma Membrane interactions: thermodynamics, toxicity and cellular response.
a-Saquero A Abstract Nanomaterials have become part of our daily lives, particularly nanoparticles contained in food, water, cosmetics, additives and textiles. Nanoparticles interact with organisms at the cellular level. The cell membrane is the first protective barrier against the potential toxic effect of nanoparticles. This first contact, including the interaction between the cell membranes -and associated proteins- and the nanoparticles is critically reviewed here. Nanoparticles, depending on their toxicity, can cause cellular physiology alterations, such as disruption in cell signaling or changes in gene expr...
Source: Current Medicinal Chemistry - November 11, 2018 Category: Chemistry Authors: Rodríguez-Hernández AG, Vazquez-Duhalt R, Huerta-Saquero A Tags: Curr Med Chem Source Type: research

Isoliquiritigenin (ISL) and its formulations: potential antitumor agents.
Abstract Isoliquiritigenin (2',4',4-trihydroxychalcone, ISL) is one of the most important chalcone compound which mainly derived from licorice root and many other plants. It exhibits a remarkable range of potent biological and pharmacological activities such as antioxidative, antitumor, antiaging, anti-inflammatory, anti-diabetic activities, etc. Numerous research teams have demonstrated that ISL process the ability to antigrowth and proliferation in various cancer cells in vitro and in vivo. Meanwhile, the underlying mechanisms of ISL inhibits cancer cell proliferation have not been well explored. However, the po...
Source: Current Medicinal Chemistry - November 11, 2018 Category: Chemistry Authors: Zhao TT, Gong HB, Zhu HL, Xu YQ, Hu HM Tags: Curr Med Chem Source Type: research

Structural and Bioactive Studies of Halogenated Constituents from Sponges.
Abstract Marine organisms are abundant sources of bioactive natural products. Among metabolites produced by sponges and their associated microbial communities, halogenated natural compounds accounted for an important part due to their potent biological activities. The present review updates and compiles a total of 258 halogenated organic compounds isolated in the past three decades, especially brominated derivatives derived from 31 genera of marine sponges. These compounds can be classified as the following classes: brominated polyunsaturated lipids, nitrogen compounds, brominated tyrosine derivatives and other ha...
Source: Current Medicinal Chemistry - November 11, 2018 Category: Chemistry Authors: Li C, Shi D Tags: Curr Med Chem Source Type: research

Anthocyanins As Modulators of Cell Redox-Dependent Pathways in Non-Communicable Diseases.
This article directly addresses the scientific evidences supporting that ACNs could be useful to protect human population against several NCDs not only acting as antioxidant but through their capability to modulate cell redox-dependent signaling. In particular, ACNs interact with the NF-κB and AP-1 signal transduction pathways, which respond to oxidative signals and mediate a proinflammatory effect, and the Nrf2/ARE pathway and its regulated cytoprotective proteins (GST, NQO, HO-1, etc.), involved in both cellular antioxidant defenses and elimination/inactivation of toxic compounds, so countering the alterations caus...
Source: Current Medicinal Chemistry - November 11, 2018 Category: Chemistry Authors: Speciale A, Saija A, Bashllari R, Molonia MS, Muscara C, Occhiuto C, Cimino F, Cristani M Tags: Curr Med Chem Source Type: research

An Update On The Neurochemistry Of Essential Tremor.
CONCLUSION: The most consistent data regarding neurochemistry of ET are related with the GABAergic and glutamatergic systems, with a lesser contribution of adenosine and dopaminergic and adrenergic systems, while there is not enough evidence of a definite role of other neurotransmitter systems in ET. The improvement of harmaline-induced tremor in rodent models achieved with T-type calcium channel antagonists, cannabinoid 1 receptor, sphingosine-1-phosphate receptor agonists, and gap-junction blockers, suggests a potential role of these structures in the pathogenesis of ET. PMID: 30417772 [PubMed - as supplied by publi...
Source: Current Medicinal Chemistry - November 11, 2018 Category: Chemistry Authors: Jiménez-Jiménez FJ, Alonso-Navarro H, García-Martín E, Agúndez JAG Tags: Curr Med Chem Source Type: research

Pharmaceutical Mixtures: Still A Concern For Human And Environmental Health.
Abstract In the present work, recent data onto the sources, occurrence and fate of human-use pharmaceutical active compounds (PhACs) in the aquatic environment have been reviewed. Since PhACs and their metabolites are usually present as mixtures in the environment at very low concentrations, , a particular emphasis was placed onto the PhACs mixtures, as well as on their short-term and long-term effects against human and environmental health. Moreover, a general overview of the main conventional as well as of the latest trends in wastewaters decontaminant technologies was outlined. Advantages and disadvantages of c...
Source: Current Medicinal Chemistry - November 7, 2018 Category: Chemistry Authors: Simu GM, Atchana J, Soica CM, Coricovac DE, Simu SC, Dehelean CA Tags: Curr Med Chem Source Type: research

Current challenges in the development of vaccines and drugs against emerging vector-borne diseases.
Abstract Vectors are living organisms that transmit infectious diseases from an infected animal to humans or another animal. Biological vectors such as mosquitoes, ticks, and sand flies carry pathogens that multiply within their bodies prior to delivery to a new host. The increased prevalence of vector-borne diseases (VBDs) such as Aedes-borne dengue, Chikungunya (CHIKV), Zika (ZIKV), malaria, tick-borne disease (TBD), and scrub typhus has a huge impact on the health of both humans and livestock worldwide. In particular, zoonotic diseases transmitted by mosquitoes and ticks place a considerable burden on public h...
Source: Current Medicinal Chemistry - November 5, 2018 Category: Chemistry Authors: Kim KS Tags: Curr Med Chem Source Type: research

Development of Pin1 inhibitors and their potential as therapeutic agents.
Abstract The prolyl isomerase Pin1 is a unique enzyme, which isomerizes the cis-trans conformation between pSer/pThr and proline, and thereby regulates the function, stability and/or subcellular distribution of its target proteins. Such regulations by Pin1 are involved in numerous physiological functions as well as the pathogenic mechanisms underlying various diseases. Notably, Pin1 deficiency or inactivation is a potential cause of Alzheimer disease, since Pin1 induces the degradation of Tau. In contrast, Pin1 overexpression is highly correlated with the degree of malignancy of cancers, as Pin1 controls a number ...
Source: Current Medicinal Chemistry - November 5, 2018 Category: Chemistry Authors: Nakatsu Y, Matsunaga Y, Ueda K, Yamamotoya T, Inoue Y, Inoue MK, Mizuno Y, Kushiyama A, Ono H, Fujishiro M, Ito H, Okabe T, Asano T Tags: Curr Med Chem Source Type: research

Manipulation of the immune system for cancer defeat: a focus on the T cell inhibitory checkpoint molecules.
This article aims to review the inhibitory checkpoints, which are known up to now, along with the mechanisms of cancer immunoediting. An outline of the immune checkpoint targeting approaches, also including combined immunotherapies and the existing trials, is also provided. Notwithstanding the great efforts devoted by researchers in the field of biomarkers of response, to date, no validated FDA-approved immunological biomarkers exist for cancer patients. We highlight relevant studies on predictive biomarkers and attempt to discuss the challenges in this field, due to the complex and largely unknown dynamic mechanisms that ...
Source: Current Medicinal Chemistry - November 5, 2018 Category: Chemistry Authors: D'Arrigo P, Tufano M, Rea A, Vigorito V, Novizio N, Russo S, Romano MF, Romano S Tags: Curr Med Chem Source Type: research

Use of anticancer platinum compounds in combination therapies and challenges in drug delivery.
Abstract As one of the leading and most important metal-based drugs, platinum based pharmaceuticals are widely used in the treatment of solid malignancies. However, significant side effects and acquired drug resistance have limited their clinical applications, despite this, platinum has shown strong inhibitory effects for a wide assortment of tumors. Drug delivery systems using emerging technologies such as liposomes, dendrimers, polymers, nanotubes and other nano-compositions, all show promise for the safe delivery of platinum based compounds. Due to the specificity of nano-formulations; unwanted side-effects and...
Source: Current Medicinal Chemistry - November 4, 2018 Category: Chemistry Authors: Xiao X, Oswald JT, Wang T, Zhang W, Li W Tags: Curr Med Chem Source Type: research

Advances in Medicinal Chemistry from Analytical Perspectives.
Abstract PMID: 30378490 [PubMed - in process] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - November 2, 2018 Category: Chemistry Authors: Ozkan SA Tags: Curr Med Chem Source Type: research

Animal venom peptides as a treasure trove for new therapeutics against neurodegenerative disorders.
CONCLUSION: Thus, components of venom hold considerable capacity as drug candidates for the alleviation or reduction of neurodegeneration. This review highlights studies evaluating different animal toxins, especially peptides, as promising therapeutic tools for treatment of different neurodegenerative diseases and disorders. PMID: 30378475 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 31, 2018 Category: Chemistry Authors: Yang X, Wang Y, Wu C, Ling EA Tags: Curr Med Chem Source Type: research

Gold-Based Nanoparticles Systems in Phototherapy - Current Strategies.
CONCLUSION: In this work, we show numerous medically and chemically important development strategies of hybrid types of drugs which can be used in phototherapy. These systems have a high affinity to the tumor cells surface proteins which transport the nanoparticles directly into a cell. The application of functionalized metallic nanoparticles in phototherapy improved photophysical properties, lowered cytotoxicity of common used photosensitizers and facilitated the development of the third generation photosensitizers. Furthermore, this type of nanoparticles could also be used as a cytostatic drug carrier in the chemo or com...
Source: Current Medicinal Chemistry - October 31, 2018 Category: Chemistry Authors: Blaszkiewicz P, Kotkowiak M Tags: Curr Med Chem Source Type: research

Natural compounds therapeutic features in brain disorders by experimental, bioinformatics and cheminformatics methods.
CONCLUSION: Our paper indicates that natural compounds are a real alternative for nervous system therapy and represents a helpful tool for the future papers focused on the study of the natural compounds. PMID: 30378477 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 31, 2018 Category: Chemistry Authors: Avram S, Puia A, Udrea AM, Mihailescu D, Mernea M, Dinischiotu A, Oancea F, Stiens J Tags: Curr Med Chem Source Type: research

Outer Membrane Proteins of Salmonella As Potential Markers of Resistance to Serum, Antibiotics and Biocides.
Abstract Salmonellosis continues to be a significant worldwide health problem. Despite rapid progress in identifying mechanisms of Salmonella virulence and resistance to chemicals, our knowledge of these mechanisms remain limited. Furthermore, it appears that the resistance to antibiotics can be amplified by ubiquitous usage of the disinfectants (biocides), both by industry and by ordinary households. Salmonella, as other Gram-negative bacteria possess outer membrane proteins (OMPs), which participate in maintaining cell integrity, adapting to environment, and interacting with infected host. Moreover, the OMPs may...
Source: Current Medicinal Chemistry - October 31, 2018 Category: Chemistry Authors: Futoma-Koloch B, Bugla-Płoskońska G, Dudek B, Dorotkiewicz-Jach A, Drulis-Kawa Z, Gamian A Tags: Curr Med Chem Source Type: research

Aim for the readers! Bromodomains as new targets against Chagas' disease.
Abstract Bromodomains recognize and bind acetyl-lysine residues present in histone and non-histone proteins in a specific manner. In the last decade they have raised as attractive target for drug discovery because the miss-regulation of human bromodomains was discovered to be involved in the development of a large spectrum of diseases. However, targeting eukaryotic pathogens bromodomains continues to be almost unexplored. We and others have reported the essentiality of diverse bromodomain-containing proteins in protozoa, offering a new opportunity for the development of antiparasitic drugs, especially for Trypanso...
Source: Current Medicinal Chemistry - October 31, 2018 Category: Chemistry Authors: Alonso VL, Tavernelli LE, Pezza A, Cribb P, Ritagliati C, Serra EC Tags: Curr Med Chem Source Type: research

Current Development of Metal Complexes with Diamine Ligands as Potential Anticancer Agents.
CONCLUSION: Metal complexes with diamine ligands are promising candidates for efficient and more selective alternatives to conventional platinum-based chemotherapeutics. Further research is required to reveal the chemico-physical properties and molecular mechanisms underlying their biological activity. PMID: 30378486 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 31, 2018 Category: Chemistry Authors: Misirlic-Dencic ST, Poljarevic J, Isakovic AM, Sabo T, Markovic I, Trajkovic V Tags: Curr Med Chem Source Type: research

Advanced in silico methods for the development of anti-leishmaniasis and anti-trypanosomiasis agents.
We describe recent applications of some important in silico approaches, such as 2D-QSAR, 3D-QSAR, pharmacophore mapping, molecular docking, and so forth, with the aim of understanding the utility of these techniques for the design of novel therapeutic anti-parasitic agents. This review focus on: (a) advanced computational drug design options; (b) diverse methodologies - e.g.: use of machine learning tools, software solutions, and web-platforms; (c) recent applications and advances in the last five years; (d) experimental validations of in silico predictions; and (e) virtual screening tools; as well as (f) rationale or just...
Source: Current Medicinal Chemistry - October 30, 2018 Category: Chemistry Authors: Halder AK, Cordeiro MN Tags: Curr Med Chem Source Type: research

Polyethylenimine-based formulations for delivery of oligonucleotides.
Abstract Polyethylenimine (PEI) is well-known as the non-viral gene delivery vector, especially for the oligonucleotides delivery. However, its clinical applications are significantly limited due to its high cationic charge, low cell recognition, and interaction with the proteins and non-target cells in the biological fluids, resulting in high cytotoxicity, poor stability and low transfection efficiency for oligonucleotides transporting. Many researchers have concluded that the molecular weight (MW) of PEI, degree of branched or linear structure, N/P ratio, buffer capacity, oligonucleotides structure, culture medi...
Source: Current Medicinal Chemistry - October 30, 2018 Category: Chemistry Authors: Hao F, Li Y, Zhu J, Sun J, Marshall B, Lee RJ, Teng L, Yang Z, Xie J Tags: Curr Med Chem Source Type: research

Pharmacological Management of Chronic Obstructive Lung Disease (COPD). Evidence from a Real-World Perspective.
CONCLUSION: Comprehensive assessment of COPD management requires strategies able to evaluate efficacy and usefulness in a real-world population, that take into account the interaction between experience and academic training, research, adherence to guidelines and judgments in order to plan the appropriate and optimum use of available strategies. PMID: 30378484 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 30, 2018 Category: Chemistry Authors: Kisialiou A, Prinzi G, Lamonaca P, Cardaci V, Fini M, Bonassi S, Russo P Tags: Curr Med Chem Source Type: research

Linseed essential oil - Source of Lipids as Active Ingredients for Pharmaceuticals and Nutraceuticals.
Abstract Linseed - also known as flaxseed -, is known for its beneficial effects on animal health attributed to its composition, comprising omega-6 (linoleic) and omega-3 (α-linolenic) fatty acids, various dietary fibers and lignans, which have health benefits in reducing the risk of cancer and cardiovascular diseases, lowering the levels of LDL-cholesterol and relaxing the smooth muscle cells in arteries increasing the blood flow. Essential fatty acids from flax participate in several metabolic processes of the cell, not only as structuring components of the cell membrane, but also as storage lipids. Flax i...
Source: Current Medicinal Chemistry - October 30, 2018 Category: Chemistry Authors: Campos J, Severino P, Ferreira C, Zielinska A, Santini A, Souto S, Souto EB Tags: Curr Med Chem Source Type: research

Rho-kinase (ROCK) Inhibitors- A Neuroprotective Therapeutic Paradigm with a Focus on Ocular Utility.
CONCLUSION: Based on the results of high-throughput screening, several Rho kinase inhibitors have been designed and developed comprising of diverse scaffolds exhibiting Rho kinase inhibitory activity from micromolar to subnanomolar ranges. This diversity in the scaffolds with inhibitory potential against the kinase and their SAR development will be intricated in the present review. Ripasudil is the only Rho kinase inhibitor marketed to date for the treatment of glaucoma. Another ROCK inhibitor AR-13324 has recently passed the clinical trials whereas AMA0076, K115, PG324, Y39983 and RKI-983 are still under trials. In view o...
Source: Current Medicinal Chemistry - October 30, 2018 Category: Chemistry Authors: Abbhi V, Piplani P Tags: Curr Med Chem Source Type: research

Computational approaches for the design of mosquito repellent chemicals.
CONCLUSION: Results reviewed in this article show that both QSAR and pharmacophore based methods can be used in the design of novel repellents. PMID: 30378480 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 29, 2018 Category: Chemistry Authors: Basak SC, Bhattacharjee AK Tags: Curr Med Chem Source Type: research

The Mycobacterial HBHA Protein: a Promising Biomarker for Tuberculosis.
Abstract A major goal in tuberculosis (TB) research is the identification, among the subjects infected with Mycobacterium tuberculosis (Mtb), of those with active TB, or at higher risk of developing active disease, from the latently infected subjects. The classical heterogeneity of Mtb infection and TB disease is a major obstacle toward the identification of reliable biomarkers that can stratify Mtb infected subjects based on disease risk. The heparin-binding haemagglutinin (HBHA) is a mycobacterial surface antigen that is implicated in tuberculosis (TB) pathogenesis. The host immune response against HBHA varies d...
Source: Current Medicinal Chemistry - October 29, 2018 Category: Chemistry Authors: Maio F, Squeglia F, Goletti D, Delogu G Tags: Curr Med Chem Source Type: research

New Targets for Treating Chronic Pain and Inflammation.
Abstract PMID: 30352549 [PubMed - in process] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 27, 2018 Category: Chemistry Authors: Guida F, Luongo L, Di Cesare Mannelli L Tags: Curr Med Chem Source Type: research

From Levinthal's Paradox to the Effects of Cell Environmental Perturbation on Protein Folding.
CONCLUSION: This paper concludes that the cellular environment could directly intervene in protein folding. The long-term interactions of the cellular environment and sequence evolution may enable proteins to fold efficiently. Therefore, to correctly understand the folding mechanism of proteins, the effect of the cellular environment on protein folding should be considered. PMID: 30332937 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 17, 2018 Category: Chemistry Authors: Zeng J, Huang Z Tags: Curr Med Chem Source Type: research

Proteomic and Glycomic Markers to Differentiate Lung Adenocarcinoma from COPD.
nky E Abstract Lung adenocarcinoma is one of the leading causes of mortality among cancer patients worldwide and chronic obstructive pulmonary disease (COPD) is also high in death statistics. In addition, patients with chronic obstructive pulmonary disease (COPD) have high risk for developing primary lung cancer. Prevention, risk estimation and a non-invasive diagnostics are essential to decrease COPD and lung cancer mortality. Therefore, better and more accurate molecular diagnostic markers (biomarkers) are needed for the early differential diagnosis of these lung diseases to help clinicians making better therape...
Source: Current Medicinal Chemistry - October 17, 2018 Category: Chemistry Authors: Szabo M, Hajba L, Kuhn R, Guttman A, Csánky E Tags: Curr Med Chem Source Type: research

The ERM complex: a new player involved in diabetes-induced vascular leakage.
In conclusion, ERMs play an essential role in endothelium homeostasis and can be envisaged as a new therapeutic molecular target for preventing or arresting diabetes-induced vascular leakage. PMID: 30332939 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 16, 2018 Category: Chemistry Authors: Simo-Servat O, Hernández C, Simó R Tags: Curr Med Chem Source Type: research

Recent Progress in Histone Deacetylase Inhibitors as Anticancer Agents.
Abstract Histone deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis, and cell cycle arrest in cancer cells. Recently, their use has been clinically validated in cancer patients resulting in the approval by the FDA of four HDAC inhibitors, vorinostat, romidepsin, belinostat and panobinostat, used for the treatment of cutaneous/peripheral T-cell lymphoma and multiple myeloma. Many more HDAC inhibitors are in different stages of clinical development for the treatment of hematological malignancie...
Source: Current Medicinal Chemistry - October 16, 2018 Category: Chemistry Authors: Cappellacci L, Perinelli DR, Maggi F, Grifantini M, Petrelli R Tags: Curr Med Chem Source Type: research

Small Peptides as Modulators of Serine Proteases.
Abstract Serine proteases play critical roles in many physiological and pathological processes, and are proven diagnostic and therapeutic targets in a number of clinical indications. Suppression of the aberrant proteolytic activities of these proteases has been clinically used for the treatments of relevant diseases. Poly-peptides with 10-20 residues are of great interests as medicinal modulators of serine proteases, because these peptides combined the characteristics of both small molecule drugs and macromolecular drugs. In this review, we summarized the recent development of peptide-based inhibitors against seri...
Source: Current Medicinal Chemistry - October 16, 2018 Category: Chemistry Authors: Xu P, Huang M Tags: Curr Med Chem Source Type: research

Perioperative Heart-Brain Axis Protection in Obese Surgical Patients: the Nutrigenomic Approach.
Abstract The number of obese patients undergoing cardiac and non cardiac surgery is rapidly increasing because they are more prone to concomitant diseases, such as diabetes, thrombosis, sleep-disordered breathing, cardiovascular and cerebrovascular diseases. Even if guidelines are already available to manage anesthesia and surgery of obese patients, the assessment of the perioperative morbidity and mortality from heart and brain disorders in morbidly obese surgical patients will be challenging in the next years. The present review will recapitulate the new mechanisms underlying the heart-brain axis vulnerability d...
Source: Current Medicinal Chemistry - October 15, 2018 Category: Chemistry Authors: Agrimi J, Baroni C, Anakor E, Lionetti V Tags: Curr Med Chem Source Type: research

Stimuli-responsive drug delivery nanocarriers in the treatment of breast cancer.
Abstract Stimuli-responsive drug-delivery nanocarriers (DDNs) have been increasingly reported in the literature as an alternative for breast cancer therapy. Stimuli-responsive DDNs are developed with materials that present a drastic change in response to intrinsic/chemical stimuli (pH, redox and enzyme) and extrinsic/physical stimuli (ultrasound, light, magnetic field and electric current). In addition, they can be developed using different strategies, such as functionalization with signaling molecules, leading to several advantages, such as (a) improved pharmaceutical properties of liposoluble drugs, (b) selectiv...
Source: Current Medicinal Chemistry - October 9, 2018 Category: Chemistry Authors: Oshiro-Junior JA, Alves RC, Hanck-Silva G, Sato MR, Rodero C, Eloy JO, Chorilli M Tags: Curr Med Chem Source Type: research

Sam domains in multiple diseases.
CONCLUSION: Considering the many roles of the Sam domain into a significant variety of diseases, more efforts and novel drug discovery campaigns need to be engaged to find out small molecules and/or peptides targeting Sam domains. Such compounds may represent the pillars on which to build novel therapeutic strategies to cure different pathologies. PMID: 30306850 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 9, 2018 Category: Chemistry Authors: Vincenzi M, Mercurio FA, Leone M Tags: Curr Med Chem Source Type: research

Recent Advances and Challenges of the Drugs Acting on Monoamine Transporters.
CONCLUSION: The reported new compounds act on hMATs as well as the structures of the transporters complexed with diverse ligands by either experiment or computational modeling have shed light on the poly-pharmacology, multimodal and allosteric regulation of the drugs to transporters. All of the studies will greatly promote the structure-based drug design (SBDD) of structurally novel scaffolds with high activity and selectivity for hMATs. PMID: 30306851 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 9, 2018 Category: Chemistry Authors: Xue W, Fu T, Zheng G, Tu G, Zhang Y, Yang F, Tao L, Yao L, Zhu F Tags: Curr Med Chem Source Type: research

The glycogen synthase kinase-3 in the regulation of ion channels and cellular carriers.
Abstract Glycogen synthase kinase-3 (GSK-3) is a highly evolutionarily conserved and ubiquitously expressed serine/threonine kinase, an enzyme protein profoundly specific for glycogen synthase (GS). GSK-3 is involved in various cellular functions and physiological processes, including cell proliferation, differentiation, motility, and survival as well as glycogen metabolism, protein synthesis, and apoptosis. There are two isoforms of human GSK-3 (named GSK-3α and GSK-3β) encoded by two distinct genes. Recently, GSK-3β has been reported to function as a powerful regulator of various transport proces...
Source: Current Medicinal Chemistry - October 9, 2018 Category: Chemistry Authors: Sopjani M, Millaku L, Nebija D, Emini M, Dermaku-Sopjani M Tags: Curr Med Chem Source Type: research

NADPH producing enzymes as promising drug targets for Chagas Disease.
Abstract Reduced nicotinamide adenine dinucleotide phosphate (NADPH) is a cofactor used in different anabolic reactions, such as lipid and nucleic acid synthesis, and for oxidative stress defense. NADPH is essential for parasite growth and viability. In trypanosomatid parasites, NADPH is supplied by the oxidative branch of the pentose phosphate pathway and by enzymes associated with the citric acid cycle. The present article will review recent achievements that suggest glucose-6-phosphate dehydrogenase and the cytosolic isoform of the malic enzyme as promising drug targets for the discovery of new drugs against Tr...
Source: Current Medicinal Chemistry - October 9, 2018 Category: Chemistry Authors: Cordeiro A Tags: Curr Med Chem Source Type: research

Structural and molecular tear film changes in glaucoma.
Abstract The tear film (TF) is a trilaminar and dynamic fluid covering the entire ocular surface (OS), consisting of a mucus, aqueous, and lipid layer deeply interacting between them. Because of its structure and functions, TF plays a pivotal role in the preservation of the OS integrity and the quality of vision. Medical therapy for glaucoma is recognized to profoundly disturb the OS homeostasis by altering all components of the ocular surface unit, including TF. The presence of preservatives, the number of daily eye drops instillations, and the duration of therapy are the main contributors to TF changes. From the...
Source: Current Medicinal Chemistry - October 9, 2018 Category: Chemistry Authors: Mastropasqua R, Agnifili L, Mastropasqua L Tags: Curr Med Chem Source Type: research

Peripheral Immunity, Immunoaging and Neuroinflammation in Parkinson's Disease.
Abstract Parkinson's disease (PD) is the second most common neurodegenerative disorder among elderly population, and it is depicted by the degeneration of dopaminergic neurons in the midbrain which is progressive. Up to the present time, the precise cause remains ill-defined and the mechanism of neurons death indeterminate. It is typically considered as a disease of central nervous system (CNS). Nevertheless, numerous evidences have been accumulated in several past years testifying undoubtedly about the principal role of neuroinflammation in progression of PD. Neuroinflammation is associated with presence of activ...
Source: Current Medicinal Chemistry - October 9, 2018 Category: Chemistry Authors: Natasa K, Franca M, Cosentino M Tags: Curr Med Chem Source Type: research

Goniothalamin-Related Styryl Lactones. Isolation, Synthesis, Biological Activity and Mode of Action.
Abstract This review covers the chemistry and biological aspects of goniothalamin-related styryl lactones isolated from natural sources. This family of secondary metabolites has been reported to display diverse uses in folk medicine, but only a limited number of these compounds have been throughly investigated regarding their biological profile. Herein, we cover the goniothalamin-related styryl lactones having a C6-C3-C4 framework which appeared in the literature for the first time in the period 2000-2017, and the reports on the synthesis, biological activity and mechanism of action which were published from 2007-...
Source: Current Medicinal Chemistry - October 9, 2018 Category: Chemistry Authors: Pilli RA, de Toledo IA, Meirelles MA, Grigolo TA Tags: Curr Med Chem Source Type: research

Role of Fatty Acid Binding Protein 4 (FABP4) in Kidney Disease.
Abstract Accumulating evidences indicated that obesity and metabolic syndrome were independent risk factors for the development and progression of kidney diseases. Apart from inflammation, lipotoxicity, and hemodynamic factors, adipokines have been proposed to play crucial roles in the relationship between kidney diseases and metabolic disorders. As one of key adipokines, fatty acid binding protein 4 (FABP4), which is mainly expressed in adipocytes and macrophages, has recently been shown to be associated with renal dysfunction and kidney damage. Both clinical and experimental studies have proposed circulating FAB...
Source: Current Medicinal Chemistry - October 8, 2018 Category: Chemistry Authors: Shi M, Ma L, Fu PI Tags: Curr Med Chem Source Type: research

Cubilin, the intrinsic factor-vitamin B12 receptor in development and disease.
Abstract Gp280/Intrinsic factor-vitamin B12 receptor/Cubilin (CUBN) is a large endocytic receptor serving multiple functions in vitamin B12 homeostasis, renal reabsorption of protein or toxic substances including albumin, vitamin D-binding protein or cadmium.Cubilin is a peripheral membrane protein consisting of 8 epidermal growth factor (EGF)-like repeats and 27 CUB (defined as Complement C1r/C1s, Uegf, BMP1) domains. This structurally unique protein interacts with at least two molecular partners, amnionless (AMN) and Lrp2/Megalin. AMN is involved in appropriate plasma membrane transport of Cubilin whereas Lrp2 i...
Source: Current Medicinal Chemistry - October 8, 2018 Category: Chemistry Authors: Kozyraki R, Cases O Tags: Curr Med Chem Source Type: research

Antimicrobial Capacity of Plant Polyphenols against Gram-positive Bacteria: a Comprehensive Review.
CONCLUSION: Plant polyphenols mean a promising source of antibacterial agents, either alone or in combination with existing antibiotics, for the development of new antibiotic therapies. PMID: 30295182 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 8, 2018 Category: Chemistry Authors: Alvarez-Martinez FJ, Barrajon-Catalan E, Encinar JA, Rodriguez-Diaz JC, Micol V Tags: Curr Med Chem Source Type: research

Aptamer Based Targeted Drug Delivery Systems: Current Potential and Challenges.
Abstract Aptamers are single-stranded DNA or RNA with 20-100 nucleotides in length that can specifically bind to target molecules via formed three-dimensional structures. These innovative targeting molecules have attracted an increasing interest in biomedical field. Compared to traditional protein antibodies, aptamers have several advantages, such as small size, high binding affinity, specificity, good biocompatibility, high stability and low immunogenicity, which all contribute to their wide application in biomedical field. Aptamers can bind to the receptors on the cell membrane and mediate themselves or conjugat...
Source: Current Medicinal Chemistry - October 8, 2018 Category: Chemistry Authors: He F, Wen N, Xiao D, Yan J, Xiong H, Cai S, Liu Z, Liu Y Tags: Curr Med Chem Source Type: research

Phenylboronic acid-polymers for biomedical applications.
CONCLUSION: The presence of PBA in polymer chain can render it with diverse functions/relativities without changing their intrinsic properties. In this review, we discuss the development of PBA polymers with diverse functions and their biomedical applications with a specific focus on the dynamic nature of boronate ester groups.  . PMID: 30295184 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 8, 2018 Category: Chemistry Authors: Ryu JH, Lee GJ, Shih YV, Kim TI, Varghese S Tags: Curr Med Chem Source Type: research

Metabolomics of exhaled breath condensate by nuclear magnetic resonance spectroscopy and mass spectrometry: a methodological approach.
Abstract Respiratory diseases present a very high prevalence in the general population, with an increase in morbidity, mortality and health-care expenses worldwide. They are complex and heterogeneous pathologies that may present different pathological facets in different subjects, often with personal evolution. Therefore, there is a need to identify patients with similar characteristics, prognosis or treatment, defining the so-called phenotype, but also to mark specific differences within each phenotype, defining the endotypes. Biomarkers are very useful to study respiratory phenotypes and endotypes. Metabolomics,...
Source: Current Medicinal Chemistry - October 8, 2018 Category: Chemistry Authors: Maniscalco M, Cutignano A, Paris D, Melck DJ, Molino A, Fuschillo S, Motta A Tags: Curr Med Chem Source Type: research

Graphene and Graphene Oxide Applications for SERS Sensing and Imaging.
Abstract Surface Enhanced Raman Spectroscopy (SERS) has long history as ultrasensitive platform for the detection of biological species from small aromatic molecules to complex biological systems as circulating tumor cells. Thanks to unique properties of graphene, the range of SERS applications has largely expanded. Graphene is efficient fluorescence quencher improving quality of Raman spectra. It contributes also to the SERS enhancement factor through the chemical mechanism. In turn, the chemical flexibility of reduced graphene oxide (RGO) enables tunable adsorption of molecules or cells on SERS active surfaces. ...
Source: Current Medicinal Chemistry - October 4, 2018 Category: Chemistry Authors: Jablonska A, Jaworska A, Kasztelan M, Berbec S, Palys B Tags: Curr Med Chem Source Type: research

Systematic review on anti-diabetic properties of chalcones.
Abstract The use of anti-diabetic drugs has been increasing worldwide and the evolution of therapeutics has been enormous. Still, the currently available anti-diabetic drugs do not present the desired efficacy and are generally associated with serious adverse side effects. Thus, entirely new interventions, addressing the underlying etiopathogenesis of type 2 diabetes mellitus, are required. Chalcones, secondary metabolites of terrestrial plants and precursors of the flavonoids biosynthesis, have been used for a long time in the traditional medicine due to their wide-range of biological activities, from which the a...
Source: Current Medicinal Chemistry - October 1, 2018 Category: Chemistry Authors: Rocha S, Ribeiro D, Fernandes E, Freitas M Tags: Curr Med Chem Source Type: research

Bio-polymer Substrates in Buccal Drug Delivery: Current Status and Future Trend.
CONCLUSION: The findings of this perspective paper proposed the potential use of cellulose derivatives, the typical kind of biopolymers, in the buccal drug delivery system for promoting the bioavailability of the macromolecular drugs. Nanocellulose (NC) in particular was proposed as an innovative bio-binder/carrier for the controlled-release of drugs. PMID: 30277141 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - October 1, 2018 Category: Chemistry Authors: Sun B, Wang W, He Z, Zhang M, Kong F, Sain M Tags: Curr Med Chem Source Type: research