Abstract:
:More and more evidences are still accumulating rapidly on the G-protein-coupled-receptors (GPCRs) dimerization/oligomerization. Such common feature of GPCRs has called extensive attention to both pharmacologists and medicinal chemists for illustration of the pharmacological functions and therapeutic utilities of such receptor complex. Although there is still no clear explanation for the receptor dimerization/oligomerization, a large number of multivalent ligands (MLs) have been designed to target the receptor-dimers/oligomers. Such MLs have gained much acceptance in exploring the receptor complex of dopaminergic, adrenergic, serotoninergic, and opioidic receptor systems, due to the relatively broader experience in recognizing the receptor-dimerization. More and more MLs have also been designed to face GPCR-related very complex neurodegenerative diseases, such as Parkinson's disease (PD), Alzheimer's disease (AD) and schizophrenia, which are not effectively treated by traditional highly selective drugs. Herein, some of the most recent developments in this field, as well as some typical examples of MLs, are highlighted, with a particular focus on GPCRs.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Liu Z,Zhang J,Zhang Adoi
10.2174/138161209787315639subject
Has Abstractpub_date
2009-01-01 00:00:00pages
682-718issue
6eissn
1381-6128issn
1873-4286journal_volume
15pub_type
杂志文章,评审abstract::Nonalcoholic fatty liver disease (NAFLD) is one of the most prevalent causes of hepatic dysfunction and is highly correlated with components of the metabolic syndrome such as obesity, insulin resistance and type 2 diabetes. Among others, nutritional factors, physical inactivity, genetic variants and visceral obesity h...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210791208938
更新日期:2010-06-01 00:00:00
abstract::Cardiac ischemia, followed by reperfusion, often results in the development of cardiac contractile dysfunction that limits the recovery prognosis of patients. The current goal of pharmacological therapy in the course of ischemic heart disease is to improve the oxygen supply/demand ratio for the heart. Cardiac contract...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990556
更新日期:2014-01-01 00:00:00
abstract::The large conduit arteries of the thorax and abdomen are elastic while those in the arms and legs are muscular. Alterations in wall properties of elastic arteries occur over time and are usually permanent in nature; acute changes can, however, occur is response to a change in transmural pressure. Chronic alterations i...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209787354258
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:The integrin family receptors stimulate the cellular proliferation and migration through the focal adhesion pathway by the activation of PTK2, VASP and TSP1 proteins. The purpose of this study was to investigate the integrin-ligated motifs through the activation of focal adhesion pathway. METHODS:A chimeric...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200311125325
更新日期:2020-01-01 00:00:00
abstract::Over the last 15 years, the use of various biological therapies has largely improved the way we manage patients with Inflammatory Bowel Diseases (IBDs). Blockade of cytokine synthesis and/or activity is at the forefront of this new era with the success of inhibitors of tumor necrosis factor (TNF)-α. These therapies ar...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210794079164
更新日期:2010-01-01 00:00:00
abstract:BACKGROUND:There is an increasing interest from the pharmaceutical and food industry in natural antioxidant and bioactive compounds derived from plants as substitutes for synthetic compounds. The genus Allium is one of the largest genera, with more than 900 species, including important cultivated and wild species, havi...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200203145851
更新日期:2020-01-01 00:00:00
abstract::The prevalence of fungal infections of skin has increased rapidly, affecting approximately 40 million people across the globe. A wide variety of antifungal drugs has been utilized in the effective management of numerous dermatological infections. Topical treatment of fungal infections has proved to be quite advantageo...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150428150456
更新日期:2015-01-01 00:00:00
abstract::There is a plausible role for cytokines, brain-derived neurotrophic factor (BDNF), and their interaction in major depressive disorder's (MDD) etiology. This review includes (i) briefly defining cytokines, (ii) a discussion of theories for why they may affect brain function, (iii) cross-sectional associations between c...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161212803523680
更新日期:2012-01-01 00:00:00
abstract::New biopharmaceutical molecules, potentially able to provide more personalized and effective treatments, are being identified through the advent of advanced synthetic biology strategies, sophisticated chemical synthesis approaches, and new analytical methods to assess biological potency. However, translation of many o...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666151216151420
更新日期:2016-01-01 00:00:00
abstract::Commonly, the angiogenic growth factors signify healing. However, gastrointestinal ulceration is still poorly understood particularly with respect to a general pharmacological/pathophysiological role of various angiogenic growth factors implemented in growth factors wound healing concept. Thereby, we focused on the st...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612824666180712110447
更新日期:2018-01-01 00:00:00
abstract::Histone deacetylases (HDACs), which act on acetylated histones and/or other non-histone protein substrates, represent validated epigenetic targets for the treatment of cancer and other human diseases. The inhibition of HDAC activity was shown to induce cell cycle arrest, differentiation, apoptosis as well as a decreas...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666141110164604
更新日期:2015-01-01 00:00:00
abstract::The common mechanism of action of aspirin and the chemically unrelated non-steroidal anti-inflammatory drugs (NSAIDs) is the inhibition of prostaglandin (PG) production due to interference with the enzymatic activity of cyclooxygenase (COX). These agents have long been used as effective treatments for arthritis. The r...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612003398753
更新日期:2000-11-01 00:00:00
abstract::Reduced levels of high-density lipoprotein cholesterol (HDL) are associated with a substantially increased risk of coronary disease and cardiovascular events. Furthermore, numerous studies have suggested that HDL may exert several potentially important antiatherosclerotic and endothelial-protective effects. In particu...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210791051013
更新日期:2010-05-01 00:00:00
abstract::Agomelatine markedly differs from other classes of antidepressant drugs: its primary molecular targets in vivo are the melatonin MT(1) and MT(2) receptors, where it acts as a potent agonist, and the 5-HT(2C) receptors, where it exerts clear-cut antagonist properties. Agomelatine across a wide range of clinical trials ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209788168056
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:Fragile X syndrome (FXS) is the most common form of monogenic hereditary cognitive impairment, including intellectual disability, autism, hyperactivity, and epilepsy. METHODS:This article reviews the literature pertaining to the role of synaptic dysfunction in FXS. RESULTS:In FXS, synaptic dysfunction alte...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666191102165206
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:The objective of this study was to apply Quality by Design (QbD) principles on process parameter optimization for the development of hybrid delivery system (combination of (SLNs) and In-situ gelling system) for hydrophilic drug Moxifloxacin Hydrochloride (MOX) to achieve its controlled delivery, which otherw...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612824666180403115106
更新日期:2018-01-01 00:00:00
abstract::Recent advances in the fabrication, characterization and application of micro- and nano-particles that possess a non-uniform internal structure are reviewed. The particle structures include core-shell particles, particles with multiple cores or a multi-layered structure, porous particles with both regular and random p...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612811319350007
更新日期:2013-01-01 00:00:00
abstract::Diabetic patients are considered as high risk for development of atherosclerotic disease. Cholesterol treatment is of paramount importance in order to optimise cardiovascular outcomes in this subset of patients. Although statins are regarded as the mainstay of treatment, these may not be tolerated or as efficacious as...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200617170252
更新日期:2020-06-17 00:00:00
abstract::Lowering low density lipoprotein (LDL) - cholesterol is one of the key issues in modern preventive cardiology by which we are able to interact with the natural course of atherosclerosis. Diet and healthy life style are mandatory for the treatment of CAD high risk patients. Numerous lipid lowering trials confirmed the ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211795428849
更新日期:2011-01-01 00:00:00
abstract::Inhibition of fatty acid oxidation is well recognized as a potentially effective mechanism for controlling glycemia in non-insulin-dependent diabetes mellitus (NIDDM). However, a direct targeting of inhibition of the intramitochondrial beta-oxidation pathway or an indirect modulation of fatty acid oxidation by inhibit...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:
更新日期:1998-02-01 00:00:00
abstract::Runx2/Cbfa/AML3 is a member of the runt homology domain family of transcription factors, essential for osteoblast differentiation and bone formation. Defining the molecular mechanisms by which Runx2 can function as a master regulatory gene for activating the program of osteoblastogenesis has provided novel insights fo...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612033453659
更新日期:2003-01-01 00:00:00
abstract::Since ancient times the operation of the brain has elicited more than usual interest. Data mining of the human genome is revealing that many CNS abnormalities have a genetic component. As yet this information can not be used directly to cure or ameliorate specific CNS disorders although this is regarded as having grea...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612023394250
更新日期:2002-01-01 00:00:00
abstract::Introduction of flow cytometric technique to the research on basophil activation has led to significant achievements in allergy diagnosis in vitro. Most of the studies employing the flow cytometry used CD63 as a marker of basophil activation and only some of them used CD203c. Recently discovered basophil activation ma...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211798357890
更新日期:2011-11-01 00:00:00
abstract::Type 2 diabetes is associated with substantially increased cardiovascular mortality. The need to reduce the progression of atherosclerosis alongside lowering blood glucose levels is now well established. Ideally, pharmaceutical treatment should address both of these needs. This review summarises current evidence of th...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209789057995
更新日期:2009-01-01 00:00:00
abstract::Hypertension is the most common medical disorder during pregnancy. Approximately 70 percent of women diagnosed with hypertension during pregnancy will have gestational hypertension-preeclampsia. The term gestational hypertension-preeclampsia is used to describe a wide spectrum of patients who may have only mild elevat...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612053381864
更新日期:2005-01-01 00:00:00
abstract::Atrial fibrillation (AF) is the most common sustained rhythm disturbance, increasing prevalence with age, in particular in patients with cardiovascular disease. On the other hand, a subset of patients with AF being <60 years old and no evidence of underlying cardiovascular disease, and laboratory tests including thyro...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666140825142206
更新日期:2015-01-01 00:00:00
abstract::Erectile function is determined by tight regulation of relaxation or contraction of corpus cavernosal smooth muscle, which is the result of a long and complex chain of molecular events. Control of erectile function resides in signaling pathways of the central and peripheral nervous system, as well as intracellular eve...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161205774913426
更新日期:2005-01-01 00:00:00
abstract::Metabolic syndrome (MetS) which is caused by poor dietary habits and sedentary behavior is a serious global health problem. MetS is a cluster of risk factors, represented by central obesity, hyperglycemia, dyslipidemia, and hypertension. In the 21st century, MetS and associated comorbidities, including obesity, diabet...
journal_title:Current pharmaceutical design
pub_type: 社论
doi:10.2174/138161282639201110165712
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:Human brain is amongst the most complex organs in human body, and delivery of therapeutic agents across the brain is a tedious task. Existence of blood brain barrier (BBB) protects the brain from invasion of undesirable substances; therefore it hinders the transport of various drugs used for the treatment of...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200417141600
更新日期:2020-01-01 00:00:00
abstract::Human embryonic stem cells (hESCs) and induced pluripotent stem cells (hiPSCs) can self-renew indefinitely, while maintaining the capacity to differentiate into useful somatic cell types, including cardiomyocytes. As such, these stem cell types represent an essentially inexhaustible source of committed human cardiomyo...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209788923804
更新日期:2009-01-01 00:00:00