Early Hematoma Enlargement in Primary Intracerebral Hemorrhage.
Abstract Early hematoma growth is not uncommon in patients with intracerebral hemorrhage. It is a devastating complication that independently predicts poor outcome. The early hematoma enlargement is usually defined as an absolute increase in hematoma volume of greater than 33% on repeat CT scan. To date, no ideal animal model can mimic the exact pathophysiological process of early hematoma growth. Novel imaging predictors such as CT angiography spot sign and CT blend sign may predict early hematoma growth in patients with intracerebral hemorrhage. Monitoring and modulation of blood pressure may change the poor out...
Source: Current Drug Targets - April 27, 2017 Category: Drugs & Pharmacology Authors: Cao D, Li Q, Fu P, Zhang J, Yang J Tags: Curr Drug Targets Source Type: research

Application of Plasmonic Gold Nanoparticle for Drug Delivery System.
Abstract Various kinds of colloidal nanoparticles (NPs) have been widely developed as a promising theranostic probe in biomedical fields. Particularly, colloidal gold nanoparticle (GNP) have been extensively utilized as theranostic probe for molecular imaging and drug delivery owing to their unique physiochemical properties with excellent biocompatibility. This review will outline the progress along this line and discuss about gold nanoparticle synthesis method for controlled geometry (spherical, rod and cage), surface functionalization (covalent and non-covalent) and associated in vitro/in vivo cytotoxicity as we...
Source: Current Drug Targets - April 27, 2017 Category: Drugs & Pharmacology Authors: Lee JH, Choi JW Tags: Curr Drug Targets Source Type: research

Kratom and Future Treatment for the Opiods Addiction and Chroic Pain: Periculo Beneficium?
Abstract Kratom (Mitragynaspeciosa), a natural existing plant found in South-East Asia, is tradi-tionally used as an herb to help to elevate a person's energy and also to treat numerous medical ailments. Other than the analgesic property, kratom has been used as an agent to overcome opioid withdrawal as it contains natural alkaloids, i.e. mitragynine, 7-hydroxymitragynine, and MGM-9, which has agonist affinity on the opioid receptors, including mu (μ) and kappa (κ). The role of neural reward pathway linked to μ-opioid receptors and both dopaminergic and GABA-ergic interneurons that express μ-opioid ...
Source: Current Drug Targets - April 25, 2017 Category: Drugs & Pharmacology Authors: Ismail I, Wahab S, Sidi H, Das S, Lin LJ, Razali R Tags: Curr Drug Targets Source Type: research

Potential use of modulators of oxidative stress as add-on therapy in patients with anxiety disorders.
Abstract It is known that an increased oxidative stress is present in a wide range of diseases and, given the vulnerability of the central nervous system, its involvement has been in particular investigated in neurological and psychiatric diseases, including anxiety disorders. In this review we analyse the studies that have been conducted on the effects of oxidative stress modulators in anxiety, focusing on their possible clinical use. While preclinical studies have shown a clear anxiolytic-like effect of different oxidative stress modulators, less significant results have been obtained from clinical studies. Afte...
Source: Current Drug Targets - April 25, 2017 Category: Drugs & Pharmacology Authors: Boldrini P, Fusco A, Nicoletti F, Badiani A, Saso L Tags: Curr Drug Targets Source Type: research

The double roles of the prostaglandin E2 EP2 receptor in intracerebral hemorrhage.
Abstract Intracerebral hemorrhage (ICH), a subtype of stroke, brings high morbidity and mortality to human beings. Multiple studies indicate that neuroinflammation, excitotoxicity, oxidative stress, cytotoxicity resulted from the degradation products of blood clot play vital roles in ICH-induced secondary brain injury, which contributes to deterioration of neurological outcome. Prostaglandin E2 (PGE2), a type of prostanoids commonly up-regulated in these progresses, is known to modulate numerous cellular and molecular processes and involve in various diseases, including ICH, cerebral ischemic, Alzheimer's disease ...
Source: Current Drug Targets - April 24, 2017 Category: Drugs & Pharmacology Authors: Luo X, Zhu Q, Zhang J, Huang Q, Xie Z, Cheng Y Tags: Curr Drug Targets Source Type: research

Drug resistance of enzalutamide in CRPC.
Abstract Enzalutamide (MDV3100, XTANDI ) is a second generation androgen receptor inhibitor that is designed for the treatment of castration-resistant prostate cancer (CRPC) and has prolonged survival time. Although Enzalutamide was also associated with such significant benefits, The majority of treated patients, innate or acquired resistance invariably arises, but the mechanisms of mdv3100 resistance have not yet been clearly clarified. Nevertheless, because the better knowledge of the genetic landscape of MDV3100 is under way, resistance to MDV3100 could be basically divided in two distinct pathways, either depe...
Source: Current Drug Targets - April 17, 2017 Category: Drugs & Pharmacology Authors: Chen X, Lu J, Xia L, Li G Tags: Curr Drug Targets Source Type: research

Advances and Challenges in Drug Design of PPAR δ Ligands.
Advances and Challenges in Drug Design of PPARδ Ligands. Curr Drug Targets. 2017 Apr 14;: Authors: Maltarollo VG, Kronenberger T, Windshügel B, Wrenger C, Trossini GHG, Honorio KM Abstract Peroxisome proliferator-activated receptors (PPAR) are nuclear receptors activated by endogenous fatty acids and prostaglandins that are classified into three types: α, γ and δ, which have different functions and tissue distribution. PPAR modulators have been exploited to the treatment of important metabolic diseases, such as type 2 diabetes mellitus and metabolic syndrome, which are con...
Source: Current Drug Targets - April 14, 2017 Category: Drugs & Pharmacology Authors: Maltarollo VG, Kronenberger T, Windshügel B, Wrenger C, Trossini GHG, Honorio KM Tags: Curr Drug Targets Source Type: research

Therapeutic applications of liposomal based drug delivery and drug targeting for immune linked inflammatory maladies: A contemporary view point.
Abstract Immune-based inflammatory diseases are immune related dysregulation in different sites of body, which includes rheumatoid arthritis, multiple sclerosis, inflammatory bowel disease, atherosclerosis, etc. Advancements in molecular research have facilitated investigation of their pathogenesis which is involved with inflammatory cytokines cells and several genes. The available drug therapy provides suboptimal therapeutic effects and higher adverse effects. Emergence of liposomal systems of the drugs meant for the above mentioned disease have gained wider importance due to in their high treatment efficacy by m...
Source: Current Drug Targets - April 14, 2017 Category: Drugs & Pharmacology Authors: Rahman M, Beg S, Verma A, Kazmi I, Patel DK, Anwar F, Kumar V Tags: Curr Drug Targets Source Type: research

Serum HE4 level as a biomarker for prediction of gynecologic cancer recurrence.
Abstract Recurrence is a major determinant of cancer patient survival and is linked to diagnostic time, stage of cancer, drug resistance, metastatic status, and other factors. Recurrence could be a more specific and treatment-relevant factor than survival, a factor potentially affected by some general elements beyond cancer biology. In a clinical setting, accurate and early prediction of recurrence greatly facilitates the optimal treatment of cancer patients. Numerous studies have shown that serum HE4 is a useful biomarker for the management of gynecological cancers. It has been demonstrated that HE4 is able to pr...
Source: Current Drug Targets - April 4, 2017 Category: Drugs & Pharmacology Authors: Li J, Chen H, Curcuru JR, Patel S, Johns TO, Patel D, Qian H, Jiang SW Tags: Curr Drug Targets Source Type: research

Dysregulation of LncRNAs in placenta and pathogenesis of preeclampsia.
This article reviews published data on this subject and provides detailed information on the regulation and function of LncRNAs IGF2/H19, MEG3, SPRY4-IT1, HOTAIR, MALAT1, and FLT1P1 and CEACAMP8 in placental trophoblasts. The potential mechanisms underlying the action of these LncRNAs are also discussed to facilitate a better understanding on the potential role of these LncRNAs for the pathogenesis of preeclampsia. PMID: 28382860 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - April 4, 2017 Category: Drugs & Pharmacology Authors: Song X, Luo X, Gao Q, Wang Y, Gao Q, Long W Tags: Curr Drug Targets Source Type: research

Hematoma Expansion following Intracerebral Hemorrhage: Mechanisms Targeting the Coagulation Cascade and Platelet Activation.
Abstract Hematoma expansion (HE), defined as a greater than 33% increase in intracerebral hemorrhage (ICH) volume within the first 24 hours, results in significant neurological deficits, and enhancement of ICH-induced primary and secondary brain injury. An escalation in the use of oral anticoagulants has led to a surge in the incidences of oral anticoagulation-associated ICH (OAT-ICH), which has been associated with a greater risk for HE and worse functional outcomes following ICH. The oral anticoagulants in use include vitamin K antagonists, and direct thrombin and factor Xa inhibitors. Fibrinolytic agents are al...
Source: Current Drug Targets - March 29, 2017 Category: Drugs & Pharmacology Authors: Burchell SR, Tang J, Zhang JH Tags: Curr Drug Targets Source Type: research

Can we predict disease course with clinical factors?
Abstract The disease phenotype at diagnosis and the disease course of Crohn's disease (CD) and ulcerative colitis (UC) show remarkable heterogeneity across patients. In recent population-based epidemiological and referral cohort studies, the evolution of disease phenotype of CD and UC varied significantly. Most CD and severe UC patients still requires hospitalization or surgery/colectomy during follow-up. A change in the natural history of IBD with improved outcomes in parallel with tailored positioning of aggressive immunomodulator and biological therapy has been suspected according to the recently available lite...
Source: Current Drug Targets - March 28, 2017 Category: Drugs & Pharmacology Authors: Vegh Z, Kurti Z, Golovics PA, Lakatos L Tags: Curr Drug Targets Source Type: research

Natural Polyphenols in the Treatment of Alzheimer's Disease.
Abstract Neurodegenerative disease is an incurable disease which involves the degeneration or death of the nerve cells. Alzheimer's Disease (AD) is a neurodegenerative disease discovered in 1906 by Alois Alzheimer, a German clinical psychiatrist and neuroanatomist. The main pathological hallmarks of this disease are the formation of extracellular amyloid β (Aβ) plaques and intracellular neurofibrillary tangle (NFT). The accumulation of the amyloid protein aggregates in the brain of AD patients leads to oxidative stress and inflammation. Other postulated reasons for the development of this disease are cho...
Source: Current Drug Targets - March 28, 2017 Category: Drugs & Pharmacology Authors: Noratiqah SB, Naina-Mohamed I, Zulfarina MS, Qodriyah HM Tags: Curr Drug Targets Source Type: research

The Application of Nanomaterials in Stem Cell Therapy for some Neurological Diseases.
Abstract Stem cell therapy provides great promising therapeutic benefits for various neurological disorders. Cell transplantation has emerged as cell replacement application for nerve damage. Recently, nanomaterials obtain wide development in various industrial and medical fields, and nanoparticles have been applied to neuro-medical field for tracking and treating nervous system diseases. Combining stem cell with nanotechnology has raised more and more attentions; and it has demonstrated that it has huge effects on clinical diagnosis and therapeutics in multiple central nervous system diseases, meanwhile, improvin...
Source: Current Drug Targets - March 28, 2017 Category: Drugs & Pharmacology Authors: Zhang G, Khan AA, Wu H, Chen L, Gu Y, Gu N Tags: Curr Drug Targets Source Type: research

Oncogenic role of SET/I2PP2A for gynecologic cancers.
Abstract SET (SE translocation, SET) is an evolutionarily conserved gene broadly expressed in various human tissues, especially in the gonadal and neural system. As a multitasking protein, SET is involved in essential cell processes such as histone modification, chromatin remodeling, DNA repair, gene transcription, and androgen synthesis. Recent studies showed that SET is overexpressed in breast cancers, ovary cancers and a variety of other malignancies. The strong correlation between SET expression levels and survival of ovarian cancer patients, and SET-mediated activation of androgen synthesis, strongly indicate...
Source: Current Drug Targets - March 28, 2017 Category: Drugs & Pharmacology Authors: Jiang SW, Xu S, Chen H, Liu J, Duan P Tags: Curr Drug Targets Source Type: research

Therapeutic potential and outlook of alternative medicine for osteoporosis.
Abstract Osteoporosis, a bone disease resulting in loss of bone density and microstructure quality, is often associated with fragility fractures, and the latter imposes a great burden on the patient and society. Although there are several different treatments available for osteoporosis such as hormone replacement therapy, bisphosphonates, Denosumab, and parathyroid hormone some concern has been raised regarding the inherent side effects of their long term use. It would be of great relevance to search for alternative natural compounds, which could complementarily overcome the limitations of the currently available ...
Source: Current Drug Targets - March 21, 2017 Category: Drugs & Pharmacology Authors: Wang T, Liu Q, Tjhioe W, Zhao J, Lu A, Zhang G, Tan R, Zhou M, Xu J, Feng H Tags: Curr Drug Targets Source Type: research

Nanotechnology As Potential Tool for siRNA Delivery in Parkinson's Disease.
D, Leyva-Gómez G, Florán B Abstract The lack of an outright treatment for Parkinson's disease (PD) is a pivotal concern in medicine and has driven the search for novel alternatives for treating the disease. Among the proposed approaches, small interfering RNA (siRNA)-based therapy is attracting significant attention as a potential method for the treatment of PD; however, siRNAs delivery possesses potential drawbacks, such as reduced stability in blood circulation and low capacity for reaching the target site. Therefore, siRNA delivery to the brain is a key issue that remains unsolved to date. In thi...
Source: Current Drug Targets - March 21, 2017 Category: Drugs & Pharmacology Authors: Cortés H, Alcalá-Alcalá S, Ávalos-Fuentes A, Mendoza-Muñoz N, Quintanar-Guerrero D, Leyva-Gómez G, Florán B Tags: Curr Drug Targets Source Type: research

Hypersexuality as a Neuropsychiatric Disorder: The neurobiology and treatment options.
Abstract Hypersexuality refers to abnormally increased or extreme involvement in any sexual activity. It is clinically challenging, presents trans-diagnostically and there is extensive medical literature addressing nosology, pathogenesis and neuropsychiatric aspects. Classification includes deviant behaviours, diagnosable entities related to impulsivity, and obsessional phenomena. Some clinicians view an increase in sexual desire as 'normal' while psychodynamic theorists consider it ego-defensive at times alleviating unconscious anxiety rooted in intrapsychic conflicts. We highlight the hypersexuality as multi-dim...
Source: Current Drug Targets - March 21, 2017 Category: Drugs & Pharmacology Authors: Sidi H, Asiff M, Kumar J, Das S, Hatta NH, Alfonso C Tags: Curr Drug Targets Source Type: research

The Use of Methylphenidate in Cancer Patients: A Review.
CONCLUSION: This review potentially supports the use of methylphenidate for opioid-induced sedation, cognitive decline and fatigue in cancer patients. Further placebo-controlled trials would help in strengthening the evidence for this treatment. PMID: 28322161 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - March 17, 2017 Category: Drugs & Pharmacology Authors: Andrew B, Ng CG, Jaafar NR Tags: Curr Drug Targets Source Type: research

Co-Morbid Erectile Dysfunction (Ed) and Antidepressant Treatment in a Patient - A Management Challenge?
Abstract Across the globe, antidepressants (AD) and phosphodiesterase-5 inhibitors (PDE-5i) are commonly prescribed psychopharmacological agents for patients with co-morbid mental-health problem and sexual dysfunction (SD). The serotonergic and/or noradrenergic ADs, although is an effective agent are not without SD side-effects, especially erectile dysfunction (ED). ED is an inability to achieve, or maintain an erection for satisfactory sexual intercourse during the phases of male's sexual arousal. It is recognized as an important reason why non-adherence to treatment was observed in patients who are on AD. AD int...
Source: Current Drug Targets - March 15, 2017 Category: Drugs & Pharmacology Authors: Zainol M, Sidi H, Kumar J, Das S, Ismail S, Hatta MH, Baharudin N, Ravindran A Tags: Curr Drug Targets Source Type: research

Translational Multimodality Neuroimaging.
Abstract Recently high-resolution, noninvasive, multimodality in-vivo molecular imaging with PET, SPECT, CT and MRI, employing fusion algorithms has revolutionized personalized medicine. However, specific radiopharmaceuticals (RPs) for the accurate diagnosis and effective treatment of progressive neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, drug addiction, and other cognitive impairments still remain in developmental phase. Currently, multimodality fusion neuroimaging is utilized for the determination of: pharmacokinetics and pre-clinical development of radiopharmaceuticals (RPs); i...
Source: Current Drug Targets - March 15, 2017 Category: Drugs & Pharmacology Authors: Sharma SK Tags: Curr Drug Targets Source Type: research

Pharmacological effects of turmeric on learning, memory and expression of muscarinic receptor genes (M1, M3 and M5) in stress-induced mouse model.
CONCLUSIONS: These findings highlight the therapeutic role of turmeric by increasing the expression of M3 and M5 and improving learning and memory. Turmeric can be an effective candidate for treatment of amnesia caused by the stress. PMID: 28302036 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - March 15, 2017 Category: Drugs & Pharmacology Authors: Khalid A, Shakeel R, Justin S, Iqbal G, Shah SA, Zahid S, Ahmed T Tags: Curr Drug Targets Source Type: research

Editorial: Targets for Immunotherapy in Acute Leukemia.
PMID: 28264642 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - March 9, 2017 Category: Drugs & Pharmacology Authors: Hourigan CS Tags: Curr Drug Targets Source Type: research

Editorial: Natural and Synthetic Polyphenols as Emerging Drugs: Design, Delivery Systems and Preclinical & Clinical Therapeutic Approaches.
Editorial: Natural and Synthetic Polyphenols as Emerging Drugs: Design, Delivery Systems and Preclinical & Clinical Therapeutic Approaches. Curr Drug Targets. 2017;18(2):134 Authors: Puig T PMID: 28264643 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - March 9, 2017 Category: Drugs & Pharmacology Authors: Puig T Tags: Curr Drug Targets Source Type: research

Editorial: CML HSCs: Are the True Enemies for the Patient?
PMID: 28264644 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - March 9, 2017 Category: Drugs & Pharmacology Authors: Mancini M Tags: Curr Drug Targets Source Type: research

Editorial: Multi-Target in Computer-Aided Drug Design Studies.
PMID: 28270060 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - March 9, 2017 Category: Drugs & Pharmacology Authors: Scotti L, Scotti MT Tags: Curr Drug Targets Source Type: research

The Hot and Potential Targets of Type 2 Diabetes Mellitus Treatment in Recent Decade.
This article is intended to provide a broad ranging overview of 14 prominent molecule targets currently being pursued for the treatment of diabetes, with regard to their therapeutic rationale, small molecule modulators and application prospects. These targets are roughly divided into four general areas that correlate with insulin secretion, act on the insulin sensitivity, and have an effect on the complications. This article could provides the medicinal chemist interested in discovering novel therapeutic small molecules with a myriad of promising diabetes targets and broader development space for treating T2DM. PMID: ...
Source: Current Drug Targets - March 6, 2017 Category: Drugs & Pharmacology Authors: Shi D, Luo J, Wang L, Xu Q Tags: Curr Drug Targets Source Type: research

Improved Protein Toxin Delivery Based on ATTEMPTS Systems.
Abstract Ribosome-inactivating proteins (RIPs) are wildly found in multiple species of plants, bacteria and fungi. As a special family of protein toxins, RIPs can inhibit protein synthesis and induce cell death via inactivating ribosome in eukaryotic cells. Thus, RIPs have been applied for anti-tumor therapy in the past two decades. However, because of poor cell permeability, nonselective mode of action for tumor cells, poor pharmacokinetic profiles and immunogenicity, their clinical application has been severely constrained. As an effort to overcome these obstacles, tumor-specific monoclonal antibodies (mAb) have...
Source: Current Drug Targets - February 28, 2017 Category: Drugs & Pharmacology Authors: Huang Y, Yang VC, Li F, Shin MC, Wang H, Min KA, Zhang M, Chen Y Tags: Curr Drug Targets Source Type: research

Current Drug Targets in Obesity Pharmacotherapy - A Review.
Abstract Obesity, an impending global pandemic, is not being effectively controlled by current measures such as lifestyle modifications, bariatric surgery or available medications. Its toll on health and economy compels us to look for more effective measures. Fortunately, the advances in biology and molecular technology have been in our favour for delineating new pathways in the pathophysiology of obesity and have led to subsequent development of new drug targets. Development of anti-obesity drugs has often been riddled with problems in the past. Some of the recently approved drugs for pharmacotherapy of obesity h...
Source: Current Drug Targets - February 26, 2017 Category: Drugs & Pharmacology Authors: Bhat SP, Sharma A Tags: Curr Drug Targets Source Type: research

The Neurobiology and Psychiatric Perspective of Vaginismus: Linking the Pharmacological and Psycho-Social Interventions.
Abstract Vaginismus is an involuntary muscle contraction of the outer third of vaginal barrel causing sexual penetration almost impossible. It is generally classified under sexual pain disorder (SPD). In Diagnostic and Statistical Manual, 5th edition, it is classified under the new rubric of Genito-Pelvic Pain/Sexual Penetration Disorder. This fear-avoidance condition poses an ongoing significant challenge to the medical and health professionals due to the very demanding needs in health care despite its unpredictable prognosis. The etiology of vaginismus is complex: through multiple bio-psycho-social processes, in...
Source: Current Drug Targets - February 21, 2017 Category: Drugs & Pharmacology Authors: Kadir ZS, Sidi H, Kumar J, Das S, Midin M, Baharuddin N Tags: Curr Drug Targets Source Type: research

Recent Advances in Protein Tyrosine Phosphatase 1B Targeted Drug Discovery for Type II Diabetes and Obesity.
Abstract Protein tyrosine phosphatase 1B (PTP1B) is an important therapeutic target for type II diabetes and obesity because of its pivotal role as a negative modulator in both insulin and leptin signalling pathways. Consequently, the discovery of PTP1B inhibitors has been the focus of researchers in both academia and pharmaceutical industry over the last two decades. Though, intense pharmaceutical research in this area has resulted in many potent PTP1B inhibitors, a vast majority of them possessed pTyr mimetic group such as phosphonates, carboxylic acids and sulphamic acids, which led to poor PTP1B selectivity an...
Source: Current Drug Targets - February 21, 2017 Category: Drugs & Pharmacology Authors: Maheswari N, Karthikeyan C, Trivedi P, Moorthy NS Tags: Curr Drug Targets Source Type: research

The Phosphodiesterase 5-Inhibitors (PDE-5i) for ERECTILE DYSFUNCTION (ED): A Therapeutic Challenge For Psychiatrists.
Abstract Erectile function (EF) is a prerequisite for satisfactory sexual intercourse (SI) and central to male sexual functioning. Satisfactory SI eventually leads to orgasm - a biopsychophysiological state of euphoria - leading to a sense of bliss, enjoyment and positive mental well being. For a psychiatrist, treating ED is self-propelled to harmonize these pleasurable experiences alongside with encouragement of physical wellness and sensuality. Hence, the role of PDE-5i is pivotal in the context of treating ED constitutes a therapeutic challenge. PDE-5i work via the dopaminergic-oxytocin-nitric oxide pathway by ...
Source: Current Drug Targets - February 14, 2017 Category: Drugs & Pharmacology Authors: Koon CS, Sidi H, Kumar J, Das S, Xi OW, Hatta MH, Alfonso C Tags: Curr Drug Targets Source Type: research

TXNIP in Metabolic Regulation: Physiological Role and Therapeutic Outlook.
Abstract Thioredoxin-interacting protein (TXNIP) also known as thioredoxin binding protein-2 is a ubiquitously expressed protein that interacts and negatively regulates expression and function of Thioredoxin (TXN). Over the last few years TXNIP has attracted considerable attention due to its wide-ranging functions impacting several aspects of energy metabolism. TXNIP acts as an important regulator of glucose and lipid metabolism through pleiotropic actions including regulation of β-cell function, hepatic glucose production, peripheral glucose uptake, adipogenesis, and substrate utilization. Overexpression of ...
Source: Current Drug Targets - January 29, 2017 Category: Drugs & Pharmacology Authors: Alhawiti NM, Almahri S, Aziz MA, Malik SS, Mohammad S Tags: Curr Drug Targets Source Type: research

Cytochrome P450 structure, function and clinical significance: A review.
Abstract The cytochrome P450 (CYP) enzymes are membrane-bound hemoproteins that play a pivotal role in the detoxification of xenobiotics, cellular metabolism and homeostasis. Induction or inhibition of CYP enzymes is a major mechanism that underlies drug-drug interactions. CYP enzymes can be transcriptionally activated by various xenobiotics and endogenous substrates through receptor-dependent mechanisms. CYP enzyme inhibition is a principal mechanism for metabolism-based drug-drug interactions. Many chemotherapeutic drugs can cause drug interactions due to their ability to either inhibit or induce the CYP enzyme ...
Source: Current Drug Targets - January 24, 2017 Category: Drugs & Pharmacology Authors: Palrasu M, Nagini S Tags: Curr Drug Targets Source Type: research

The antioxidant activities of polysaccharides and their derivatives.
Abstract Polysaccharides are a kind of biological macromolecules with immune regulation, anti-tumor, anti-radiation, anti-inflammation, anti-fatigue and anti-aging effects. These effects are related to their antioxidant properties. The action mechanisms of antioxidation and scavenging free radicals for polysaccharides were reviewed. The polysaccharides contain plant polysaccharides, animal polysaccharides and microbial polysaccharides. The recent research progresses and our work on antioxidant properties of polysaccharides and their derivatives were summarized. At last, the existing problems of antioxidant polysac...
Source: Current Drug Targets - January 22, 2017 Category: Drugs & Pharmacology Authors: Mei X, Yi C, Huang G Tags: Curr Drug Targets Source Type: research

B3-Adrenoceptor Control Of Lower Gen ıtourınary Tract Organs And Functıon In Male: An Overvıew.
CONCLUSION: This review discusses the potential roles of β3-AR as new therapeutic targets by evaluating the results of preclinical and clinical studies related to male lower genitourinary tract function. Looking to the future, the potential benefits of β3-AR agonists from experimental and clinical investigations may provide an attractive therapeutic option. PMID: 28117002 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - January 19, 2017 Category: Drugs & Pharmacology Authors: Kaya E, Sikka SC, Oral DY, Ozakca I, Gur S Tags: Curr Drug Targets Source Type: research

Designing isoform-selective inhibitors against Classical HDACs for effective anticancer therapy: Insight and perspectives from in silico.
Abstract Histone deacetylase inhibitors, the small molecules modulating the biological activity of histone deacetylases are emerging as potent chemotherapeutic agents. Despite their considerable therapeutic benefits in disease models, the lack of isoform specificity culminates in debilitating off target effects, raising serious concerns regarding their applicability. This emphasizes the pressing and unmet medical need of designing isoform selective inhibitors for safe and effective anticancer therapy. Keeping these grim facts in view, the current article sheds light on structural basis of off-targeting. Furthermor...
Source: Current Drug Targets - January 11, 2017 Category: Drugs & Pharmacology Authors: Ganai SA Tags: Curr Drug Targets Source Type: research

Can Surgery for Inflammatory Bowel Disease be personalized?
Abstract In the treatment of Inflammatory Bowel Diseases (IBD) despite advances in medical therapies, surgery has maintained a leading role in the management of complications of the disease, as well as in cases of failure of medical therapy. Surgery has become more and more minimally invasive, struggling for a difficult balance between guidelines and personalized treatment tailored on the single patient's need. In the present paper, the authors discuss the possible role for a personalization in debated fields of surgical treatment of Crohn&s disease and ulcerative colitis. PMID: 28068895 [PubMed - as supp...
Source: Current Drug Targets - January 4, 2017 Category: Drugs & Pharmacology Authors: Spinelli A, Marano A, Bacchelli C, Mariani NM, Montorsi M, Kotze PG Tags: Curr Drug Targets Source Type: research

Pro-Inflammation Cytokines: New Potential Therapeutic Targets for Obesity-Related Bone Disorders.
Abstract Obesity was traditionally thought as a positive regulator on the strength of bone. With the in-depth study, obesity is considered as a major risk factor for osteoporosis. Some pro-inflammation cytokines such as tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) are the factors that fat uses to negatively regulate bone metabolism. Obese people and animals show a higher level of serum TNF-α and IL-6, which are produced by macrophages derived from adipose tissue. These pro-inflammation cytokines regulate the proliferation and apoptosis of adipocyte, promote lipolysis, inhibit lipid synt...
Source: Current Drug Targets - January 3, 2017 Category: Drugs & Pharmacology Authors: Wang TT, He CQ, Yu XJ Tags: Curr Drug Targets Source Type: research

The two faces of Interleukin-17A in atherosclerosis Interleukin-17A and atherosclerosis.
Abstract A complex network of different cytokines and chemokines modulate atherosclerosis, a chronic inflammatory disease. Interleukin-17A (IL-17A) is expressed by different leukocyte subsets such as CD4+IL-17+ T cells (Th17), γδ T cells, natural killer cells, natural killer T cells, and neutrophils. IL-17A plays an important role in host defense and is involved in the pathology of different autoimmune and inflammatory diseases. Recent studies demonstrate an association of IL-17A with atherosclerosis. IL-17A seems to have primarily pro-inflammatory effects in atherogenesis, although there are partially...
Source: Current Drug Targets - December 28, 2016 Category: Drugs & Pharmacology Authors: Akhavanpoor M, Akhavanpoor H, Gleissner CA, Wangler S, Doesch AO, Katus HA, Erbel C Tags: Curr Drug Targets Source Type: research

CEBP epigenetic dysregulation as a drug target for the treatment of hematologic and gynecologic malignancies.
Abstract The CCAAT/enhancer binding proteins (C/EBPs) form a family of transcription factors regulating many genes' expression in a variety of cells/tissues/organs at different developmental stages. With their capability of binding to a loosely defined consensus DNA sequence and through extensive protein-protein interactions, C/EBPs modulate diverse functions including cell differentiation, metabolism, and immune response, under both physiological and pathological conditions such as the establishment of hematological lineages, the maintenance of normal reproductive function, and the development of malignant diseas...
Source: Current Drug Targets - December 27, 2016 Category: Drugs & Pharmacology Authors: Sun C, Duan P, Luan C Tags: Curr Drug Targets Source Type: research

Serotonin Selective Reuptake Inhibitors (SSRIs) and Female Sexual Dysfunction (FSD): Hypothesis on Its association and options of treatment.
Abstract Sexual dysfunctions are commonly seen in women on selective serotonin reuptake inhibitors (SSRIs). The complexities of female sexual functioning are reflected through modulation of inter-playing factors like the neuropsychophysiological factors, inter-personal and relationship issue, psychiatric co-morbidities and physical disorder. The incidence of SSRIs-induced FSD is difficult to estimate because of the potentially confounding effects of SSRIs, presence of polypharmacy, marital effect, socio-cultural factors and due to the design and assessment problems in majority of the studies.The exact mechanism of...
Source: Current Drug Targets - December 26, 2016 Category: Drugs & Pharmacology Authors: Rappek NA, Sidi H, Kumar J, Kamarazaman S, Das S, Masiran R, Baharudin N, Hatta M Tags: Curr Drug Targets Source Type: research

A mini review on the chemistry and neuroprotective effects of silymarin.
Abstract The plant milk thistle and silymarin has been traditionally used as a natural remedy for the treatment of various ailments including neurological disorders such Alzheimer's and Parkinson's Disease and cerebral ischemia for over 2000 years. The neuroprotective effects conferred by silymarin include modulation of various antioxidant mechanisms, and several kinases involved in cell signaling pathways, inhibition of the inflammatory response generated during neurodegeneration, neurotropic effects, regulation of neurotransmitters and inhibition of apoptosis. The ease of availability, comparative low cost and s...
Source: Current Drug Targets - December 26, 2016 Category: Drugs & Pharmacology Authors: Devi KP, Malar DS, Braidy N, Nabavi SM, Nabavi SF Tags: Curr Drug Targets Source Type: research

Bone: A Fertile Soil for Cancer Metastasis.
We describe some of the current methodologies used to study bone metastasis, highlighting the limitations of these methods and alternative future strategies to be used to study bone metastasis. While in vivo animal and patient studies may provide the gold standard for studying metastasis, ex vivo models can be used as an alternative to enable more controlled experiments designed to study the late stages of bone metastasis. PMID: 28025941 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - December 25, 2016 Category: Drugs & Pharmacology Authors: Coughlin T, Moreno RR, Mason D, Nystrom L, Boerckel J, Niebur G, Littlepage LE Tags: Curr Drug Targets Source Type: research

Kynurenine system and multiple sclerosis, pathomechanism and drug targets with an emphasis on laquinimod.
, Vécsei L Abstract Multiple sclerosis is a common chronic, disabling autoimmune neurological disease affecting mainly young adults. In its pathomechanism, neurodegenerative and acute inflammatory characteristics are both involved. Disease-modifying therapies aim to reduce relapse-rate and slow down the deterioration in neurological functions. The currently available therapies fail to exert neuroprotective effects and most of them are associated with potentially toxic side-effects, therefore, ongoing research aims to develop novel drug candidates to cover these therapeutic gaps. The kynurenine pathway has b...
Source: Current Drug Targets - December 22, 2016 Category: Drugs & Pharmacology Authors: Majláth Z, Annus Á, Vécsei L Tags: Curr Drug Targets Source Type: research

Review of theoretical models to study natural products with antiprotozoal activity.
do-Prado FJ Abstract There exists many pathogen parasite species with different susceptibility profiles of antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one parasite species. Consequently, predicting the probability with which a drug is active against different species with a single unified model is a goal of major importance. In doing so, we use Markov Chains theory to calculate new multi-target spectral moments to fit a QSAR model that for the first time, can predicta meet-QSAR model for more than 40,000 cases obtained from databases CHEMBL against m...
Source: Current Drug Targets - December 21, 2016 Category: Drugs & Pharmacology Authors: Herrera-Rueda MA, Navarrete-Vázquez G, Aguirre-Crespo F, Maldonado-Velazquez MG, Vergara-Galicia J, Canul HC, García-Mera X, Prado-Prado FJ Tags: Curr Drug Targets Source Type: research

Recent Advances in Transcranial Focused Ultrasound (FUS) Triggered Brain Delivery.
Abstract Successful delivery of therapeutic agents in the brain is very challenging, which makes treatment of various brain disorders very difficult. One of the major causes of this difficulty is the presence of physiological barriers in the brain like blood brain barrier (BBB) and blood cerebro-spinal fluid (CSF) barrier. These barriers are very specific and restrict the entry of water soluble agents and ionized molecule. Only lipid soluble and small molecular size agents are allowed to enter into the brain. But there are several serious brain diseases in which the use of only conventional small molecular mass li...
Source: Current Drug Targets - December 21, 2016 Category: Drugs & Pharmacology Authors: Nainwal N Tags: Curr Drug Targets Source Type: research

Editorial: High Performance Computing in Drug Discovery.
, Merelli I PMID: 27991399 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - December 21, 2016 Category: Drugs & Pharmacology Authors: Pérez-Sánchez H, Gesing S, Merelli I Tags: Curr Drug Targets Source Type: research

Editorial (Thematic Issue: Common Receptor Signalling in Glial & Immune Cells).
Editorial (Thematic Issue: Common Receptor Signalling in Glial & Immune Cells). Curr Drug Targets. 2016;17(16):1828 Authors: Dev KK PMID: 27991401 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - December 21, 2016 Category: Drugs & Pharmacology Authors: Dev KK Tags: Curr Drug Targets Source Type: research

Editorial (Thematic Issue: The Predictive Pathology in the Target Therapy Era).
PMID: 27991404 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - December 21, 2016 Category: Drugs & Pharmacology Authors: Franco R, Cantile M Tags: Curr Drug Targets Source Type: research