Current Status and Future Perspective for Research on Medicinal Plants with Anticancerous Activity and Minimum Cytotoxic Value.
In this study, these medicinal plants were evaluated for dose-dependent cytotoxicological studies via in vitro MTT assay and in vivo tumor models along with some more plants which are reported to have IC50 value in the range of 0.019-0.528 mg/ml. The findings indicate that these plants inhibit tumor growth by their antiproliferative, pro-apoptotic, anti-metastatic and anti-angiogenic molecular targets. They are widely used because of their easy availability, affordable price and having no or sometimes minimal side effects. This review provides a baseline for the discovery of anticancer drugs from medicinal plants having mi...
Source: Current Drug Targets - September 6, 2019 Category: Drugs & Pharmacology Authors: Qamar H, Rehman S, Chauhan DK Tags: Curr Drug Targets Source Type: research

Recent Advances in the Discovery of Novel HSP90 Inhibitors: An Update from 2014.
Abstract HSP90 is a member in the family of heat shock proteins responsible for folding proteins into mature conformations and thus maintaining their biological function in cells. Since it is involved in all hallmarks of cancer, HSP90 has been considered as a promising drug target for cancer therapy. Eighteen HSP90 inhibitors have entered clinical trials, however, none has been approved by FDA. There is still a great need for novel HSP90 inhibitors with strong anticancer activity and good safety profile. In the past several years, many new molecules were identified as HSP90 inhibitors and some of them have shown p...
Source: Current Drug Targets - August 29, 2019 Category: Drugs & Pharmacology Authors: Xiao Y, Liu Y Tags: Curr Drug Targets Source Type: research

Angiotensin Type 1 Receptor Blockers in Heart Failure.
Abstract Homeostasis in the cardiovascular system is maintained by physiological functions of the Renin Angiotensin Aldosterone System (RAAS). In pathophysiological conditions, over activation of RAAS leads to an increase in the concentration of Angiotensin II (AngII) and over activation of Angiotensin Type 1 Receptor (AT1R) resulting in vasoconstriction, sodium retention and change in myocyte growth. In the heart it causes cardiac remodeling which result in left ventricular hypertrophy, dilation and dysfunction which eventually leads to Heart Failure (HF). Inhibition of RAAS using angiotensin converting enzyme in...
Source: Current Drug Targets - August 21, 2019 Category: Drugs & Pharmacology Authors: Singh KD, Karnik SS Tags: Curr Drug Targets Source Type: research

Circulating exosomes and their role in stroke.
Abstract Stroke is an acute neurologic disorder which can be life threatening if left untreated or diagnosed lately. Various detecting techniques including neurologic imaging of brain by computed tomography or magnetic resonance imaging can facilitate diagnosis of stroke. However, according to the recent advances in molecular detection techniques new diagnostic and prognostic has been emerged. Exosomes as an extra cellar particle are one of these markers which can have useful diagnostic, prognostic and even therapeutic impact after stroke. We have previously discussed the role of exosomes in cardiovascular disease...
Source: Current Drug Targets - August 21, 2019 Category: Drugs & Pharmacology Authors: Jafarzadeh-Esfehani R, Soudyab M, Parizadeh SM, Jaripoor ME, Nejad PS, Shariati M, Nabavi AS Tags: Curr Drug Targets Source Type: research

Advances in Current Diabetes Proteomics: From the Perspectives of Label-free Quantification and Biomarker Selection.
CONCLUSION: In summary, this review provides guidelines for researchers who will engage in proteomics biomarker discovery and by properly applying these proteomic computational advances, more reliable therapeutic targets will be found in the field of diabetes mellitus. PMID: 31433754 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - August 21, 2019 Category: Drugs & Pharmacology Authors: Fu J, Luo Y, Mou M, Zhang H, Tang J, Wang Y, Zhu F Tags: Curr Drug Targets Source Type: research

Targeting Cancer Stem Cells Pathways for the Effective Treatment of Cancer.
Abstract Resistance to chemotherapy and relapse are major hurdles for the effective treatment of cancer. Major reason for this is a small sub population of cancer stem cells (CSCs) and its microenvironment. CSCs are critical driving force for several types of cancer such as gastric, colon, breast and many more. Hence, for the complete eradication of cancer, it is necessary to develop therapeutic approaches that can specifically target CSCs. Chemical agents that target different proteins involved in CSC signaling pathways, either as single agent or parallelly targeting two or more proteins have generated promising ...
Source: Current Drug Targets - August 21, 2019 Category: Drugs & Pharmacology Authors: Dwivedi AR, Thakur A, Kumar V, Skvortsova I, Kumar V Tags: Curr Drug Targets Source Type: research

TNF- α and IL-6: the link between immune and bone system.
TNF-α and IL-6: the link between immune and bone system. Curr Drug Targets. 2019 Aug 21;: Authors: Wang T, He C Abstract Osteoimmunology is a new subject which focuses on the communication between the immune and the skeletal systems. Both the immune system and bone communicate with each other. Pro-inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) play important roles in immune responses and bone metabolism. TNF-α and IL-6 enhance macrophage activation and antigen presentation, as well as regulating immunity through different mechanisms. A va...
Source: Current Drug Targets - August 21, 2019 Category: Drugs & Pharmacology Authors: Wang T, He C Tags: Curr Drug Targets Source Type: research

p19INK4d: As a cyclin-dependent kinase inhibitor and more.
Abstract Cyclin-dependent kinase inhibitors (CDKIs ) are important components of cell cycle regulators. CDKI family is composed of INK4 family and CIP/Kip family. p19INK4d belongs to INK4 gene family, and is involved in in a series of normal physiological activities and pathogenesis of diseases. Many factors play regulatory roles in p19INK4d gene expression at the transcriptional and post-transcriptional levels. p19INK4d not only regulates cell cycle, but also play regulatory roles in apoptosis, DNA damage repair, cell differentiation of hematopoietic cells, and cellular senescence. Herein, the regulation network ...
Source: Current Drug Targets - August 9, 2019 Category: Drugs & Pharmacology Authors: Han X, Kuang Y, Chen H, Liu T, Zhang J, Liu J Tags: Curr Drug Targets Source Type: research

Absolute Blood Eosinophil Counts to Guide Inhaled Corticosteroids Therapy among Patients with COPD: Systematic Review and Meta-analysis of Evidence.
CONCLUSION: This study confirms the validity of the recommended absolute blood eosinophil count thresholds for the escalation and de-escalation of ICS among COPD patients. However, this recommendation is for COPD patients with prior exacerbations rather than among newly diagnosed COPD patients as observed in this study. PMID: 31393244 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - August 8, 2019 Category: Drugs & Pharmacology Authors: Oshagbemi OA, Odiba JO, Daniel A, Yunusa I Tags: Curr Drug Targets Source Type: research

Computational and Pharmacogenomics Insights on Hypertension Treatment: Rational Drug Design and Optimization Strategies.
Abstract Alzheimer's disease (AD) is one of the most common forms of dementia and has been a global concern for several years. Due to the multi-factorial nature of the disease, AD has become irreversible, fatal and imposes a tremendous socio-economic burden. Even though experimental medicines suggested moderate benefits, AD still lacks an effective treatment strategy for the management of symptoms or cure. Among various hypothesises that describe the development and progression of AD, the amyloid hypothesis has been a long-term adherent to the AD due to the involvement of various forms of amyloid beta (Aβ) pe...
Source: Current Drug Targets - August 7, 2019 Category: Drugs & Pharmacology Authors: Loganathan L, Gopinath K, Sankaranarayanan VM, Kukreti R, Rajendran K, Lee JK, Muthusamy K Tags: Curr Drug Targets Source Type: research

Nanosized Modification Strategies for Improving the Antitumor Efficacy of MEK Inhibitors.
Abstract The RAS-RAF-MEK-ERK signaling pathway (MAPK signaling) is hyperactivated in more than 30% of human cancers. The crucial roles of mitogen-activated protein kinase kinase (MEK) in tumorigenesis, cell proliferation and apoptosis inhibition, make MEK inhibitors (MEKi) attractive candidates for the targeted therapy of cancer as a result of gain-of-function mutations in RAS or RAF genes. Several highly selective and potent non-ATP-competitive allosteric MEKi have been developed and have led to substantial improvements in clinical outcomes. However, the drug efficacies and response rates are limited due to compl...
Source: Current Drug Targets - August 7, 2019 Category: Drugs & Pharmacology Authors: Li Y, Dong Q, Mei T, Zheng M, Kumar RR, Yu B, Wu C, Zhang H, An F Tags: Curr Drug Targets Source Type: research

Targeting protein kinase inhibitors with Traditional Chinese Medicine.
Abstract Protein kinases play critical roles in control of cell growth, proliferation, migration, survival and angiogenesis etc. through their catalytic activity. In recent years, numerous protein kinase inhibitors have been developed and are being successfully used clinically. Traditional Chinese medicine (TCM ) represent a large class of bioactive substances, and some of them display anticancer activity via inhibiting protein kinases signal pathway. The phosphoinositide 3-kinase, serine/threonine-specific protein kinases, PI3K/AKT/mTOR), p38mitogen-activated protein kinase (MAPK) and extracellular signal-regulat...
Source: Current Drug Targets - August 2, 2019 Category: Drugs & Pharmacology Authors: Zhang Y, Liu M, Wang J, Huang J, Guo M, Zuo L, Xu B, Cao S, Lin X Tags: Curr Drug Targets Source Type: research

Advances in Discovery of PDE10A Inhibitors for CNS-Related Disorders. Part 2: Focus on Schizophrenia.
Abstract Schizophrenia is a debilitating mental disorder with relatively high prevalence (~1%), during which three main groups of symptoms occur: positive manifestations (such as psychotic states), negative symptoms (e.g., a withdrawal from social life), and cognitive impairment. Schizophrenic patients have an excessive release of dopamine in the striatum and an insufficient amounts of this neurotransmitter in the prefrontal cortex. This imbalance is believed to be partially responsible for the occurrence of the three groups of symptoms. Dopamine D2 receptor blockers are the standard treatment of schizophrenia. Ho...
Source: Current Drug Targets - August 1, 2019 Category: Drugs & Pharmacology Authors: Świerczek A, Jankowska A, Chłoń-Rzepa G, Pawłowski M, Wyska E Tags: Curr Drug Targets Source Type: research

Potential Role of Endonuclease Inhibition and Other Targets in the Treatment of Influenza.
CONCLUSION: Due to the possibility of viral mutations and resistance, it is important to have antivirals with different mechanisms available, especially in the case of a new pandemic strain. Several novel antivirals are within various stages of development and may represent new classes of treatments that can reduce symptoms and complications in those patients who may be at higher risk. PMID: 31368872 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - August 1, 2019 Category: Drugs & Pharmacology Authors: Szollosi DE, Bill A Tags: Curr Drug Targets Source Type: research

Potential Drug Targets against Hepatitis B Virus Based on Both Virus and Host Factors.
CONCLUSION: Since HBV is obligate intracellular parasite, and as such it depends on host cellular components and functions to replicate itself. The targeting both virus and host might be a novel therapeutic option for hepatitis B. Accordingly, we analyse the advances in the study of the potential drug targets for anti-HBV infection, focusing on targeting virus genome, on targeting host cellular functions and on targeting virus-host proteins interactions, respectively. Meanwhile, the immune targets against chronic hepatitis B are also emphasized. In short, the review provides a summary of antiviral therapeutic strategies to...
Source: Current Drug Targets - July 29, 2019 Category: Drugs & Pharmacology Authors: Zhang BY, Chai DP, Wu YH, Qiu LP, Zhang YY, Ye ZH, Yu XP Tags: Curr Drug Targets Source Type: research

Leptin and Its Relatives: A potential target for autoimmune diseases.
Abstract Leptin is an adipocyte-derived hormone and product of the obese (ob) gene. The role of leptin as an immunomodulator in inflammatory and immune responses has attracted increasing attention in recent years. Leptin plays an important regulatory role as an immunomodulatory factor in the maintenance of immune function and homeostasis. It mostly affects responses through the immunomodulation of monocytes, dendritic cells, neutrophils, NK cells, dendritic cells, T and B cell development and functions. Leptin is also an important inflammatory regulator, wherein higher levels influence the secretion rates of IL-6,...
Source: Current Drug Targets - July 29, 2019 Category: Drugs & Pharmacology Authors: Han H, Zhou W Tags: Curr Drug Targets Source Type: research

Aptamers in drug design: An emerging weapon to fight a losing battle.
Abstract Implementation of novel and biocompatible polymers in drug design is an emerging and rapidly growing area of research. Even though we have large number of polymer materials for various applications, biocompatibility of these materials remains as a herculean task for researchers. Aptamers provide a vital and efficient solution to this problem. They are usually small (ranging from 20 to 60 pairs of nucleotides) single-strand of RNA or DNA oligonucleotides which are capable of binding to molecules possessing high affinity and other properties like specificity. This review focuses on different aspects of Apta...
Source: Current Drug Targets - July 29, 2019 Category: Drugs & Pharmacology Authors: Jose J, Thomas AM, Mendonsa D, Al-Sanea MM, Sahab Uddin M, Parambi DGT, Charyulu RN, Mathew B Tags: Curr Drug Targets Source Type: research

Recent progress in Gene Therapy and Other Targeted Therapeutic Approaches for Beta Thalassemia.
Abstract Thalassemia syndromes are a group of inherited blood disorders caused by limitation or absence of alpha or beta- globin chain synthesis resulting in ineffective erythropoiesis and chronic hemolytic anemia. According to the clinical fact of thalassemia as recessive autosomal, thalassemia divided into alpha and beta thalassemia. The main complication of beta thalassemia is excessive red blood cells destruction, oxidative stress, extramedullary hematopoiesis pseudotumors, hemosiderosis-induced organ dysfunction, malignancy, polyneuropathy, myopathy, osteoporosis, and leg ulcers. Although, the first obligator...
Source: Current Drug Targets - July 26, 2019 Category: Drugs & Pharmacology Authors: Hamed EM, Meabed MH, Aly UF, Hussein RRS Tags: Curr Drug Targets Source Type: research

A Multi-perspective Review of Dengue Research.
Abstract Dengue fever is a disease which is caused by a family of viruses Flaviviridae which are transmitted by female Aedes mosquitoes. Today, this is an endemic in more than 100 nations in the World Health Organization's African, Americas, Eastern Mediterranean, South-East Asia and Western Pacific locales. The treatment of typical dengue is focused on relieving the symptoms and signs. Carica papaya is a very common plant whose leaf extract is used in the treatment of this disease. Despite extensive research on Dengue, not a single vaccine or anti-viral drug was available until 2016 (partially effective Chimeric ...
Source: Current Drug Targets - July 24, 2019 Category: Drugs & Pharmacology Authors: Sobhia ME, Ghosh K, Singh A, Sul K, Singh M, Kumar R, Sandeep, Merugu S, Donempudi S Tags: Curr Drug Targets Source Type: research

Prevention And Medical Treatment Of Pouchitis In Ulcerative Colitis.
Abstract Approximately 50% of patients who have undergone IPAA surgery for Ulcerative Colitis (UC) develop at least 1 episode of pouchitis. Patients with pouchitis have a wide range of symptoms, endoscopic and histologic features, disease course, and prognosis. To date, there are no universally accepted diagnostic criteria in terms of endoscopy and histology; though, semi-objective assessments to diagnose pouchitis in patients with ileal pouch- anal anastomosis (IPAA) have been proposed using composite scores such as the Pouchitis Triad, Heidelberg Pouchitis Activity Score and Pouchitis Disease Activity Index (PDA...
Source: Current Drug Targets - July 23, 2019 Category: Drugs & Pharmacology Authors: Benlice C, Shen B, Steele SR Tags: Curr Drug Targets Source Type: research

Computational and Experimental Approaches to Design Inhibitors of Amylin Aggregation.
Abstract Aggregates formed by amylin (a neuroendocrine peptide hormone secreted by pancreatic β-cells) are implicated in the pathogenesis of type 2 diabetes mellitus. To understand amylin's aggregation mechanism and discover its inhibitory drugs, we have reviewed experimental and computational studies on amylin structures and inhibitors. We have also reviewed the role of amylin in other conditions including obesity and Alzheimer's disease (AD), since effective therapeutics are still lacking for AD. Our results of text-mining over 3,000 amylin-related PubMed abstracts suggest the combined therapeutic potential...
Source: Current Drug Targets - July 19, 2019 Category: Drugs & Pharmacology Authors: Kumar AP, Lee S, Lukman S Tags: Curr Drug Targets Source Type: research

The solubility-Permeability interplay for solubility-enabling oral formulations.
This article will help in the designing of the optimized formulations having balanced solubility enhancement without affecting the permeability of drug. PMID: 31333138 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - July 17, 2019 Category: Drugs & Pharmacology Authors: Nainwal N, Jawla S, Singh R, Saharan VA Tags: Curr Drug Targets Source Type: research

Engineering of exosomes: Steps towards green production of drug delivery systems.
Abstract Although many drug delivery systems have been developed to achieve excellent drug therapeutic index ,however, most of these systems still have biocompatibility problems as well as they cause environmental pollution. Therefore, exosomes as biological carries are considered as biocompatible, biodegradable and safe to the environment in comparison with synthetic drug delivery systems. Biologically, exosomes are considered as natural cargoes for bioactive material as well as they involved in the transport of cellular signaling and communications. In respect to biological origin of exosomes, they could be prod...
Source: Current Drug Targets - July 14, 2019 Category: Drugs & Pharmacology Authors: Sherif AY, Harisa GI, Alanazi FK, Youssof AME Tags: Curr Drug Targets Source Type: research

Recognition of plasminogen activator inhibitor type 1 as the primary regulator of fibrinolysis.
Abstract The fibrinolytic system is composed of a balance between rates of plasminogen activation and fibrin degradation, both of which are finely regulated by spatio-temporal mechanisms. Three distinct inhibitors of the fibrinolytic system that differently regulate these steps are: plasminogen activator inhibitor type-1 (PAI-1), α2-antiplasmin, and thrombin activatable fibrinolysis inhibitor (TAFI). In this review, we focus on the mechanisms by which PAI-1 governs total fibrinolytic activity to provide its essential role in many hemostatic disorders, including fibrinolytic shutdown after trauma. PAI-1 is a ...
Source: Current Drug Targets - July 14, 2019 Category: Drugs & Pharmacology Authors: Urano T, Suzuki Y, Iwaki T, Sano H, Honkura N, Castellino FJ Tags: Curr Drug Targets Source Type: research

Circulating and tissue microRNAs as biomarkers for ovarian cancer prognosis.
Abstract Ovarian cancer (OC) is one of the most common cancers globally with a high rate of cancer-associated mortality. OC may be classified into epithelial cell neoplasms, germ cell neoplasms and stromal cell neoplasms. The five-year survival in the early and advanced stages of disease is approximately 90% and 15%, respectively. microRNAs are short, single-stranded, non-coding ribonucleic acid (RNA). miRNAs play critical roles in post transcriptionally regulations of gene expression. miRNAs are found in different tissues and body fluids. In carcinogenesis the expression of miRNAs are altered. Recent studies have...
Source: Current Drug Targets - July 7, 2019 Category: Drugs & Pharmacology Authors: Parizadeh SM, Jafarzadeh-Esfehani R, Ghandehari M, Hasanzadeh M, Parizadeh SMR, Hassanian SM, Rezaei-Kalat A, Aghabozorgi AS, Rahimi-Kakhki R, Zargaran B, Ferns GA, Avan A Tags: Curr Drug Targets Source Type: research

Current drug nano-targeting strategies for improvement in the diagnosis and treatment of prevalent pathologies such as cardiovascular and renal diseases.
cha W Abstract Kidneys and cardiovascular system are closely related among them, but in general, the search for new alternatives for treatment and diagnosis of cardiovascular diseases does not take into account this relationship. In this context, nanotechnology offers multiple pharmacological strategies for overcoming many of the most important restrictions of traditional cardiovascular therapies, such as their unspecific pharmacodynamics distribution. In this sense, drug or contrast agent nano-targeting for treatment or diagnosis of atherosclerosis, thrombosis, renal cancer or fibrosis, glomerulonephritis, among ...
Source: Current Drug Targets - July 2, 2019 Category: Drugs & Pharmacology Authors: Giménez VMM, Fuentes LB, Kassuha DE, Manucha W Tags: Curr Drug Targets Source Type: research

Personalized Peptide-based vaccination for treatment of colorectal cancer: rational and progress.
Abstract Colorectal cancer (CRC) is one of the most common cancers globally and is associated with a high rate of morbidity and mortality. A large proportion of patients with early stage CRC who undergo conventional treatments develop local recurrence or distant metastasis and in this group of advanced disease, the survival rate is low. Furthermore there is often a poor response and/or toxicity associated with chemotherapy and chemo-resistance may limit continuing conventional treatment alone. Choosing novel and targeted therapeutic approaches based on clinicopathological and molecular features of tumors in combin...
Source: Current Drug Targets - June 19, 2019 Category: Drugs & Pharmacology Authors: Parizadeh SM, Jafarzadeh-Esfehani R, Ghandehari M, Rezaei-Kalat A, Parizadeh SMR, Javanbakht A, Hassanian SM, Ferns GA, Khazaei M, Avan A Tags: Curr Drug Targets Source Type: research

PI3K/ Akt/ mTOR pathway as a therapeutic target for colorectal cancer: A review of preclinical and clinical evidence.
CONCLUSION: Inhibitors of the PI3K/mTOR pathway has been successful for the treatment of primary and metastatic colorectal cancers, rendering the pathway as a promising clinical cancer therapeutic target. PMID: 31215384 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - June 18, 2019 Category: Drugs & Pharmacology Authors: Narayanankutty A Tags: Curr Drug Targets Source Type: research

Flavonoid-derived privileged scaffolds in anti-Trypanosoma brucei drug discovery.
CONCLUSION: According to in vitro anti-T brucei studies, there is evidence that flavonoids might be lead compounds for the potential treatment of HAT. However, toxicological studies, as well as mechanism of action of the in vitro active flavonoids are needed to support their use as potential leads for the treatment of HAT. PMID: 31215385 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - June 18, 2019 Category: Drugs & Pharmacology Authors: Boniface PK, Elizabeth FI Tags: Curr Drug Targets Source Type: research

Molecular docking study of active diazenyl scaffolds as inhibitors of essential targets towards antimicrobial drug discovery.
CONCLUSION: Hence, these compounds can be developed as novel antibacterial agents as potent DNA topoisomerase inhibitors and antifungal agents as CYP51 inhibitors. PMID: 31215386 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - June 18, 2019 Category: Drugs & Pharmacology Authors: Kaur H, Gahlawat S, Singh J, Narasimhan B Tags: Curr Drug Targets Source Type: research

Plant Derived Natural Alkaloids as New Antimicrobial and Adjuvant Agents in Existing Antimicrobial Therapy.
Abstract Infectious diseases, instigated by pathogenic microorganisms are the cause of numerous health problems in developing countries. Infectious diseases got a place in list of top ten death causes of worldwide. The reason behind that level of severity is antimicrobial resistance. Antimicrobial resistance made the antimicrobial agents useless, that was used in the treatment of infectious diseases. Microbes very smartly achieved the resistance against synthetic and semi-synthetic antimicrobial agents for their survival. So, handling of these infectious diseases becomes very challenging. The resistance developing...
Source: Current Drug Targets - June 18, 2019 Category: Drugs & Pharmacology Authors: Mittal RP, Jaitak V Tags: Curr Drug Targets Source Type: research

Phytochemical information and biological activities of quinolizidine alkaloids in Sophora: A comprehensive review.
Abstract Quinolizidine alkaloids, a main existence form of alkaloid found in the genus Sophora, have been shown to have many pharmacological effects. This review aims to summarize the photochemical reports and biological activities of quinolizidine alkaloids in Sophora. The collected information suggested that a total of 99 quinolizidine alkaloids were isolated and detected from different parts of Sophora plants, represented by lupinine-type, cytisine-type, sparteine-type, matrine-type. However, quality control needs to be monitored because it could provide basic information for the reasonable and efficient use of...
Source: Current Drug Targets - June 18, 2019 Category: Drugs & Pharmacology Authors: Wang H, Xia C, Chen L, Zhao J, Tao W, Zhang X, Wang J, Gao X, Yong J, Duan JA Tags: Curr Drug Targets Source Type: research

High Mobility Group Box-1 (HMGB1): A potential target in therapeutics.
Abstract High mobility group box-1 (HMGB1) mainly belongs to the non-histone DNA-binding protein. It has been studied as a nuclear protein that is present in eukaryotic cells. From the HMG family, HMGB1 protein has been focused particularly for its pivotal role in several pathologies. HMGB-1 is considered as an essential facilitator in diseases such as sepsis, collagen disease, atherosclerosis, cancers, arthritis, acute lung injury, epilepsy, myocardial infarction, and local and systemic inflammation. Modulation of HMGB1 levels in the human body provides a way in the management of these diseases. Various strategie...
Source: Current Drug Targets - June 18, 2019 Category: Drugs & Pharmacology Authors: Vijayakumar EC, Bhatt LK, Prabhavalkar KS Tags: Curr Drug Targets Source Type: research

Advancement of Mechanisms of Coxsackie Virus B3-Induced Myocarditis Pathogenesis and The Potential Therapeutic Targets.
Abstract Viral myocarditis is a cardiac disease caused by Group B Coxsackie virus of Enterovirus genus in the Picorna viridae family. It causes heart failure in children, young and adults. Ten Percent (10%) of acute heart failure and 12% of sudden deaths in young and adults who are less than 40 years is due to this viral myocarditis. If treatment action is not taken earlier, the viral disease can develop into chronic myocarditis and Dilated Cardiomyopathy which lead to congestive heart failure. And these eventually result in a reduced cardiac function which finally brings the victim to death. The only treatment op...
Source: Current Drug Targets - June 18, 2019 Category: Drugs & Pharmacology Authors: Daba TM, Zhao Y, Pan Z Tags: Curr Drug Targets Source Type: research

Bromodomain-Containing Protein 4: A Druggable Target.
Abstract Bromodomain-containing protein 4 (BRD4) belongs to the bromodomain and extra-terminal family. BRD4 inhibitors can regulate acetylated lysine and form protein complexes that initiate transcriptional programs as an epigenetic regulator of histone code. BRD4 is initially considered to be one of the most promising targets for combating malignant tumors. Recently, many studies have shown that BRD4 plays a crucial role in various kinds of diseases, including cancer, coronary heart disease, neurological disorder, and obesity. Currently, several BRD4 inhibitors are undergoing clinical trials. A search for new BRD...
Source: Current Drug Targets - June 18, 2019 Category: Drugs & Pharmacology Authors: Shi Y, Liu J, Zhao Y, Cao J, Li Y, Guo F Tags: Curr Drug Targets Source Type: research

Considering circadian pattern of blood pressure in treatment of hypertension via chronotherapy: A conducive or a maladroit approach.
In this study we analyze the effect of circadian pattern of blood pressure on action of various antihypertensives and investigate the perspective of chronotherapeutics- whether it's a fruitful approach and rationalize its utility in treatment of hypertension. PMID: 31131750 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - May 27, 2019 Category: Drugs & Pharmacology Authors: Das R, Mehta DK Tags: Curr Drug Targets Source Type: research

PPAR γ: Potential therapeutic target for ailments beyond diabetes and its natural agonism.
PPARγ: Potential therapeutic target for ailments beyond diabetes and its natural agonism. Curr Drug Targets. 2019 May 27;: Authors: Shafi S, Gupta P, Khatik GL, Gupta J Abstract The intense research interests have been observed in establishing PPAR gamma as a therapeutic target for diabetes. However, PPARγ is also emerging as an important therapeutic target for varied diseased states other than type2 diabetes like neurodegenerative disorders, cancer, spinal cord injury, asthma, and cardiovascular problems. Furthermore, glistazones, the synthetic thiazolidinediones, also known as insulin se...
Source: Current Drug Targets - May 27, 2019 Category: Drugs & Pharmacology Authors: Shafi S, Gupta P, Khatik GL, Gupta J Tags: Curr Drug Targets Source Type: research

Nanotechnology in Biomedical Applications.
Abstract PMID: 31096893 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - May 19, 2019 Category: Drugs & Pharmacology Authors: Puig T, Ciurana J Tags: Curr Drug Targets Source Type: research

Diversity of bacteria and bacterial products as antibiofilm and antiquorum sensing drugs against pathogenic bacteria.
Abstract The increase in antibiotic resistance in pathogenic bacteria led to development of new therapeutic approaches to inhibit biofilm formation as well as interfering quorum sensing (QS) signaling systems. The QS system is a phenomenon in which pathogenic bacteria produce signaling molecules that are involved in cell to cell communication, production of virulence factors, biofilm maturation, and several other functions. In the natural environment several non-pathogenic bacteria are present as a mixed population along with pathogenic bacteria and they control the behavior of microbial community by producing sec...
Source: Current Drug Targets - April 23, 2019 Category: Drugs & Pharmacology Authors: Khan F, Oloketuyi SF, Kim YM Tags: Curr Drug Targets Source Type: research

Major kinds of drug targets in Chagas disease or American Trypanosomiasis.
Abstract Chagas disease, a parasitic infection commonly named American Trypanosomiasis affects millions of people all over Latin America. Presently, the number of international infected people estimated by the World Health Organization (WHO) amounts to 7 to 8 million and more than 10.000 deaths are assumed to happen yearly. The disease is an emergent disease elsewhere than non-endemic countries of the word due to transmission of etiologic agent, Trypanosoma cruzi by people migration. The best promising targets for trypanocidal drugs may be classified in three main groups: Group I will include main molecular target...
Source: Current Drug Targets - April 23, 2019 Category: Drugs & Pharmacology Authors: Duschak VG Tags: Curr Drug Targets Source Type: research

Silicon Quantum dots: Promising theranostic probes for the future.
Abstract Nanotechnology has emerged as one of the leading research areas involving nanoscale manipulation of atoms and molecules. During the past decade, the growth of nanotechnology has been one of the most important developments taken place in the biomedical field. The new generation nanomaterials like Quantum dots are gaining much importance. Also, there is a growing interest in the development of nano-theranostics platforms in medical diagnostics, biomedical imaging, drug delivery etc. Quantum dots are also known as nanoscale semiconductor crystals, with unique electronic and optical properties. Recently silic...
Source: Current Drug Targets - April 5, 2019 Category: Drugs & Pharmacology Authors: Sivasankarapillai VS, Jose J, Shanavas MS, Marathakam A, Uddin MS, Mathew B Tags: Curr Drug Targets Source Type: research

Toll-like Receptor as a Molecular Link between Metabolic Syndrome and Inflammation: a Review.
Abstract Metabolic syndrome (MetS) involves a cluster of five conditions, i.e. obesity, hyperglycaemia, hypertension, hypertriglyceridemia and low high-density lipoprotein (HDL) cholesterol. All components of MetS share an underlying chronic inflammatory aetiology, manifested by increased levels of pro-inflammatory cytokines. The pathogenic role of inflammation in the development of MetS suggested that toll-like receptor (TLR) activation may trigger MetS. This review summarises the supporting evidence on the interactions between MetS and TLR activation, bridged by the elevation of TLR ligands during MetS. The regu...
Source: Current Drug Targets - April 5, 2019 Category: Drugs & Pharmacology Authors: Wong SK, Chin KY, Ima-Nirwana S Tags: Curr Drug Targets Source Type: research

Current understanding of Group A Streptococcal biofilms.
CONCLUSION: Further study is needed to improve the current understanding of GAS as both a mono-species biofilm, and as a member of a polymicrobial biofilm. Improved modelling of GAS biofilm formation in settings closely mimicking in vivo conditions will ensure biofilms generated in the lab closely reflect those occurring during a clinical infection. PMID: 30947646 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - April 4, 2019 Category: Drugs & Pharmacology Authors: Vyas HKN, Proctor EJ, McArthur J, Gorman J, Sanderson-Smith M Tags: Curr Drug Targets Source Type: research

Anti-TNF and postoperative complications in abdominal CD surgery.
CONCLUSIONS: Among patients treated with preoperative anti-TNF-α therapy, the risk of overall complications and infectious complications may slightly increase after abdominal surgery for CD. Nevertheless, the previous reports reviewed in this study are suffered from limitations. To rigorously evaluate the risk of anti-TNF-α therapy prior to surgery, large prospective studies with standardised criteria for assessing surgical complications and with proper adjustment for confounding variables are warranted. PMID: 30947671 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - April 4, 2019 Category: Drugs & Pharmacology Authors: Yamamoto T, Teixeira FV, Saad-Hossne R, Kotze PG, Danese S Tags: Curr Drug Targets Source Type: research

Targeting p53-MDM2 interaction using small molecule inhibitors and the challenges needed to be addressed.
Abstract MDM2 protein is the core negative regulator of p53 that maintains the cellular levels of p53 at a low level in normal cells. Mutation of the TP53 gene accounts for 50% of all human cancers. In the remaining malignancies with wild-type TP53, p53 function is inhibited through other mechanisms. Recently, synthetic small molecule inhibitors have been developed which target a small hydrophobic pocket on MDM2 to which p53 normally binds. Given that MDM2-p53 antagonists have been undergoing clinical trials for different types of cancer, this review illustrates different aspects of these new cancer targeted thera...
Source: Current Drug Targets - April 2, 2019 Category: Drugs & Pharmacology Authors: Zanjirband M, Rahgozar S Tags: Curr Drug Targets Source Type: research

Anti-tumor drug targets analysis: current insight and future prospect.
Abstract The incidence and mortality of malignant tumors are on the rise, which has become the second leading cause of death in the world. At present, anti-tumor drugs are one of the most common methods for treating cancer. In recent years, with the in-depth study of tumor biology and related disciplines, it has been gradually discovered that the essence of cell carcinogenesis is the infinite proliferation of cells caused by the disorder of cell signal transduction pathways, followed by a major shift in the concept of anti-tumor drugs research and development. The focus of research and development is shifting from...
Source: Current Drug Targets - April 2, 2019 Category: Drugs & Pharmacology Authors: Wang S, Zhou D, Xu Z, Song J, Qian X, Lv X, Luan J Tags: Curr Drug Targets Source Type: research

Anti-TNF and pouch surgery for ulcerative colitis: the ones who blame for more complications?
Abstract Since the approval in 2005 of anti-TNF drugs for the treatment of ulcerative colitis, concerns have been raised about the potential detrimental effect of these agents on postoperative infectious complications related to pouch surgery. Data on this topic are controversial and mostly derived from retrospective underpowered cohort studies largely affected by relevant bias. Three meta-analyses have been published with contradictory results. Moreover, the correlation between serum levels of infliximab at the time of surgery and the occurrence of septic postoperative complication is far to be proven and remains...
Source: Current Drug Targets - March 28, 2019 Category: Drugs & Pharmacology Authors: Bislenghi G, Ferrante M, D'Hoore A Tags: Curr Drug Targets Source Type: research

Vedolizumab in the perioperative management of inflammatory bowel disease.
CONCLUSION: Vedolizumab may be associated with an increased risk of postoperative infectious complications in Crohn's disease, but the literature remains controversial due to difficulty in isolating the effect of the biologic alone in a chronically ill, heterogeneous patient population who are on multiple medications including corticosteroids. PMID: 30914021 [PubMed - as supplied by publisher] (Source: Current Drug Targets)
Source: Current Drug Targets - March 25, 2019 Category: Drugs & Pharmacology Authors: Lightner AL, Loftus EV, McKenna NP, Raffals LE Tags: Curr Drug Targets Source Type: research

The Computational Methods in Drug Targets Discovery.
PMID: 30887916 [PubMed - in process] (Source: Current Drug Targets)
Source: Current Drug Targets - March 20, 2019 Category: Drugs & Pharmacology Authors: Lin H Tags: Curr Drug Targets Source Type: research

The use of naltrexone in dermatology. Current evidence and future directions.
Abstract Naltrexone is a competitive opioid receptor antagonist approved as supportive treatment in alcohol dependence and opioid addiction. In a dose 50-100 mg daily, naltrexone is used off-label in dermatology for the treatment of trichotillomania and different types of pruritus. At a dose as low as 1-5 mg of drug per day, naltrexone demonstrates immunomodulatory action i.e. modulates Toll-like receptors signaling, decreases release of proinflammatory cytokines (tumor necrosis factor, interleukin-6, interleukin-12), inhibits T lymphocyte proliferation, down-regulates the expression of chemokine receptors and adh...
Source: Current Drug Targets - March 18, 2019 Category: Drugs & Pharmacology Authors: Sikora M, Rakowska A, Olszewska M, Rudnicka L Tags: Curr Drug Targets Source Type: research