abstract：:Prostacyclin (PGI(2)) is one of the major vascular protectors against thrombosis and vasoconstriction, caused by thromboxane A(2). Understanding the molecular mechanisms of PGI(2) biosynthesis and signaling is crucial to the development of therapeutic approaches to regulate PGI(2) functions. This review provides infor...

journal_title：Current pharmaceutical design

authors： Ruan KH,Dogné JM

更新日期：2006-01-01 00:00:00

abstract：:The hypothesis that the interaction of agouti-related protein (AGRP) and the melanocortin-4 receptor (MC4R) modulates feeding behavior in humans has stimulated the synthesis of conformationally constrained peptides, peptoids and small molecules in efforts to identify novel compounds that can potentially be used in the...

journal_title：Current pharmaceutical design

authors： Wang X,Richards NG

更新日期：2005-01-01 00:00:00

abstract：:The pivotal role of leptin in regulating body weight and energy homeostasis is very well established. More recently, leptin also emerged as an important regulator of T-cell-dependent immunity. Reduced leptin levels, as observed during periods of starvation, correlate with an impaired cellular immune response, whereby ...

journal_title：Current pharmaceutical design

authors： Peelman F,Iserentant H,Eyckerman S,Zabeau L,Tavernier J

更新日期：2005-01-01 00:00:00

abstract：:Severe sepsis leading to shock is the principal cause of death in intensive care units. It is a systemic inflammatory response caused by excessive secretion of pro-inflammatory mediators, such as tumor necrosis factor-alpha (TNFalpha) and reactive oxygen species (ROS), mainly induced by endotoxin (a major component of...

journal_title：Current pharmaceutical design

authors： Victor VM,Rocha M,Esplugues JV,De la Fuente M

更新日期：2005-01-01 00:00:00

abstract：:Opiates lack potent analgesic efficacy in neuropathic pain although it is now generally accepted that the poor effect of these drugs reflects a reduction in their potency. Reduction of morphine antinociceptive potency was postulated to be due to the fact that nerve injury altered the activity of opioid systems or opio...

journal_title：Current pharmaceutical design

authors： Przewlocki R,Przewlocka B

更新日期：2005-01-01 00:00:00

abstract：:Prevention, improved screening, and better treatment regimens have improved cancer incidence and mortality in the last decade. Chemoradiation continues to cause high morbidity in patients undergoing treatment. DNA therapeutics have the potential to modify the genes that cause tumor progression in order to produce a re...

journal_title：Current pharmaceutical design

authors： Coppelli FM,Grandis JR

更新日期：2005-01-01 00:00:00

abstract：:ATP-sensitive K+ channels, termed K(ATP) channels, provide a link between cellular metabolism and membrane electrical activity in a variety of tissues. Channel isoforms have been identified and are targets for compounds that both stimulate and inhibit their activity resulting in membrane hyperpolarization and depolari...

journal_title：Current pharmaceutical design

authors： Bryan J,Crane A,Vila-Carriles WH,Babenko AP,Aguilar-Bryan L

更新日期：2005-01-01 00:00:00

abstract：:Research on Substance P (SP) has, until recently, focused on its role in pain and inflammation. However, a report that NK(1) receptor antagonists have utility in the treatment of depression has stimulated research into the function of SP and the NK(1)receptor in anxiety and depression. The distribution of SP and the N...

journal_title：Current pharmaceutical design

authors： McLean S

更新日期：2005-01-01 00:00:00

abstract：:During the last years, mass spectrometry has revolutionised protein biochemistry and has advanced to a superior tool for the identification and detailed analysis of peptides and proteins. The high throughput allowed by some mass spectrometry platforms has enabled the important step from analysis of individual proteins...

journal_title：Current pharmaceutical design

authors： Pusch W,Kostrzewa M

更新日期：2005-01-01 00:00:00

abstract：:Natural product drugs that target the tubulin/microtubule system remain an important component in the therapeutic arsenal to treat many types of malignancies. Agents such as the taxanes and vinca alkaloids bind to beta-tubulin and disrupt microtubule dynamics by inducing a potent mitotic block and subsequent cell deat...

journal_title：Current pharmaceutical design

authors： Verrills NM,Kavallaris M

更新日期：2005-01-01 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

authors： Coppage KH,Sibai BM

更新日期：2005-01-01 00:00:00

abstract：:In recent years, our understanding of the molecular interaction of collagens with their cognate integrin receptors has remarkably improved. Structural elucidations of both the integrin and the collagenous triple helix have contributed to this achievement. The structures of an entire integrin ectodomain and of an A-dom...

journal_title：Current pharmaceutical design

authors： Eble JA

更新日期：2005-01-01 00:00:00

abstract：:Parkinson's disease (PD) is a movement disorder caused by degeneration of the nigrostriatal dopamine (DA) neurons in the substantia nigra pars compacta and the resultant deficiency in the neurotransmitter DA at the nerve terminals in the striatum. We and other investigators found increased levels of pro-inflammatory c...

journal_title：Current pharmaceutical design

authors： Nagatsu T,Sawada M

更新日期：2005-01-01 00:00:00

abstract：:Angiogenic eye disease is among the most common causes of blindness worldwide. Current treatment approaches are insufficiently effective and partially associated with significant adverse effects. From an investigational view, the eye provides an ideal setting to observe real-time and serial observations of angiogenesi...

journal_title：Current pharmaceutical design

authors： Wegewitz U,Göhring I,Spranger J

更新日期：2005-01-01 00:00:00

abstract：:CHD is one of the most common serious chronic conditions in postmenopausal women and leads to extremely high risk for recurrent myocardial infarction and death. On the basis of the currently available randomized clinical-trial results the role of conventional HRT for treatment and prevention of CHD is rapidly evolving...

journal_title：Current pharmaceutical design

authors： Francucci CM,Camilletti A,Boscaro M

更新日期：2005-01-01 00:00:00

abstract：:The review describes key aspects of the synthesis and biological activities of conjugates of oligonucleotides and their analogues with synthetic peptides, in particular aimed towards gene silencing applications. The common methods of synthesis of oligonucleotide-peptide conjugates (OPCs) and PNA-peptide conjugates (PP...

journal_title：Current pharmaceutical design

authors： Zatsepin TS,Turner JJ,Oretskaya TS,Gait MJ

更新日期：2005-01-01 00:00:00

abstract：:Most heterosexual women want to reduce the risk of acquiring a sexually transmitted infection; many also want to control their fertility. Several chemical agents have been proposed to dramatically slow the spread of HIV infections. Ideally, vaginal microbicides, with or without contraceptive properties, should be safe...

journal_title：Current pharmaceutical design

authors： Gandour RD

更新日期：2005-01-01 00:00:00

abstract：BACKGROUND:Ximelagatran has been approved in Europe for VTE prophylaxis in orthopedic surgery at fixed doses and without laboratory monitoring. Aim of the study was to evaluate safety and efficacy of ximelagatran in a meta-analysis of prophylaxis and/or treatment randomized controlled trials. METHODS:Absolute risk of ...

journal_title：Current pharmaceutical design

authors： Iorio A,Guercini F,Ferrante F,Nenci GG

更新日期：2005-01-01 00:00:00

abstract：:There is extensive evidence that changes in immune system activation accompany the pathological changes of Alzheimer's disease (AD), but a mechanistic understanding of how the immune system actually participates in disease pathogenesis is still largely lacking. Because of the complexity of the immunological response, ...

journal_title：Current pharmaceutical design

authors： Nelson RB

更新日期：2005-01-01 00:00:00

abstract：:Oxidative processes exert a fundamental regulatory function during pregnancy. It depends on the influence of oxygen, nitric oxide, reactive oxygen species and reactive nitrogen species metabolic pathways upon the vascular changes in the maternal organism, as well as on the regulation of uterine and cervical tone throu...

journal_title：Current pharmaceutical design

authors： Biondi C,Pavan B,Lunghi L,Fiorini S,Vesce F

更新日期：2005-01-01 00:00:00

abstract：:Over the last two decades, SPECT (single photon emission computed tomography) and especially PET (positron emission tomography) have proven increasingly effective imaging modalities in the study of human psychopharmacology. Abusing populations can be studied at multiple times after abstinence begins, to give informati...

journal_title：Current pharmaceutical design

authors： Gatley SJ,Volkow ND,Wang GJ,Fowler JS,Logan J,Ding YS,Gerasimov M

更新日期：2005-01-01 00:00:00

abstract：:Cardiac arrhythmias remain a major source of morbidity and mortality in developed countries. Antiarrhythmic drug therapy was traditionally the mainstay of cardiac arrhythmia treatment; however, drug therapy of cardiac arrhythmias has been plagued by incomplete efficacy and by potentially serious adverse reactions, of ...

journal_title：Current pharmaceutical design

authors： Hesketh JC,Herrera D,Zicha S,Nattel S

更新日期：2005-01-01 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

authors： Seftel AD

更新日期：2005-01-01 00:00:00

abstract：:The production of autoreactive antibodies from self-reactive B cells results in the formation of immune complexes that deposit in tissue and fix complement, contributing to the pathogenesis of rheumatoid arthritis (RA). Earlier mouse models emphasize the importance of autoreactive antibodies formed against "self" prot...

journal_title：Current pharmaceutical design

authors： Low JM,Moore TL

更新日期：2005-01-01 00:00:00

abstract：:Lipid markers are well established predictors of vascular disease. The most frequently measured lipid variables are total cholesterol, high density lipoprotein cholesterol, low density lipoprotein cholesterol and triglycerides. In this review we consider the predictive value of these variables and other more specialis...

journal_title：Current pharmaceutical design

authors： Milionis HJ,Daskalopoulou SS,Elisaf M,Mikhailidis DP

更新日期：2005-01-01 00:00:00

abstract：:Agitation is commonly seen in acute schizophrenic patients and core symptoms include a wide range of symptom. It requires rapid and effective treatment approaches in order to protect patient and caregiver from potential injury. Clinician's decision of pharmacological treatment should be individualized to the needs and...

journal_title：Current pharmaceutical design

authors： San L,Arranz B,Escobar R

更新日期：2005-01-01 00:00:00

abstract：:Recent advances in DNA sequencing has made it possible to accurately decipher the entire genetic complement of a probiotic bacterium. Increases in sequencing capabilities have been enhanced through improved computer software that can annotate, or identify, the majority of genes encoded by the sequence. The availabilit...

journal_title：Current pharmaceutical design

authors： Callanan M

更新日期：2005-01-01 00:00:00

abstract：:Hypericin is a naturally occurring substance found in the common St. John's Wort (Hypericum species) and can also be synthesized from the anthraquinone derivative emodin. As the main component of Hypericum perforatum, it has traditionally been used throughout the history of folk medicine. In the last three decades, hy...

journal_title：Current pharmaceutical design

authors： Kubin A,Wierrani F,Burner U,Alth G,Grünberger W

更新日期：2005-01-01 00:00:00

abstract：:Since identifying a transmissible agent responsible for tumorigenesis in chickens, the v-Src oncogene, significant progress has been made in determining the functions of its cellular homologue. c-Src is the product of the SRC gene and has been found both over-expressed and highly activated in a number of human cancers...

journal_title：Current pharmaceutical design

authors： Alper O,Bowden ET

更新日期：2005-01-01 00:00:00

abstract：:The cytokine tumor necrosis factor(alpha) (TNF(alpha)) is associated with a constellation of physiological and behavioral characteristics that follow in response to infection such as fever, fatigue, listlessness, loss of appetite, malaise, and tactile hypersensitivity. These responses are examples of central nervous s...

journal_title：Current pharmaceutical design

authors： Hermann GE,Holmes GM,Rogers RC

更新日期：2005-01-01 00:00:00

abstract：:Following injury, as part of the wound-healing process, cell proliferation occurs mostly to replace damaged cells and to reconstitute the tissue back to normal condition/function. In the spinal cord some of the dividing cells following injury interfere with the repair processes. This interference occurs at the later s...

journal_title：Current pharmaceutical design

authors： Kalderon N

更新日期：2005-01-01 00:00:00

abstract：:Peroxynitrite, the product of the reaction between nitric oxide and superoxide, is spontaneouly formed within most mammalian cells under physiological conditions. Initial work addressing the pathophysiology of peroxynitrite afforded the generally accepted notion that this compound would be the long-term neurotoxic nit...

journal_title：Current pharmaceutical design

authors： Bolanos JP,García-Nogales P,Almeida A

更新日期：2004-01-01 00:00:00

abstract：:Mediation of antinociception via opioid receptors located in the periphery is a viable strategy to produce analgesia without the occurrence of side effects associated with stimulation of opioid receptors located in the central nervous system. Peripheral opioid receptors are particularly important in inflammatory pain ...

journal_title：Current pharmaceutical design

authors： DeHaven-Hudkins DL,Dolle RE

更新日期：2004-01-01 00:00:00

abstract：:The tumor cell growth inhibitory activities (log 1/GI(50)) of 166 anticancer agents studied at the National Cancer Institute (NCI) in vitro anticancer screening program have allowed us to analyze the relative importance of physicochemical parameters in influencing the inhibitory activities. Increased molecular weight,...

journal_title：Current pharmaceutical design

authors： Ren SS,Lien EJ

更新日期：2004-01-01 00:00:00

abstract：:Cumulative scientific evidence gathered over the past ten years has confirmed the role of platelet GP IIb/IIIa inhibitors in reducing ischemic complications of patients undergoing percutaneous coronary intervention (PCI). Recently, mortality data available on more than 20,000 patients enrolled in randomized clinical t...

journal_title：Current pharmaceutical design

authors： Dery JP,Harrington RA,Tcheng JE

更新日期：2004-01-01 00:00:00

abstract：:In recent years, new strategies in cancer therapy have been developed targeting key signaling molecules in the receptor tyrosine kinase signal transduction pathway. In contrast, most therapeutical concepts to manipulate G protein-coupled receptors (GPCR)-mediated disorders are still limited to the use of receptor-spec...

journal_title：Current pharmaceutical design

authors： Liebmann C

更新日期：2004-01-01 00:00:00

abstract：:BMS-378806 is a prototype of a new class of small molecule HIV-1 inhibitors that blocks viral attachment to cells. This compound exhibits potent inhibitory activity against a panel of HIV-1 laboratory and clinical isolates (M- and T-tropic), selective for HIV-1 and inactive against HIV-2, SIV and a panel of other viru...

journal_title：Current pharmaceutical design

authors： Wang HG,Williams RE,Lin PF

更新日期：2004-01-01 00:00:00

abstract：:The diatomic molecule of oxygen contains two uncoupled electrons and can therefore undergo reduction, yielding several different oxygen metabolites, which are collectively called Reactive Oxygen Species or ROS. They are invariably produced in aerobic environments through a variety of mechanisms, which include electron...

journal_title：Current pharmaceutical design

authors： Bergamini CM,Gambetti S,Dondi A,Cervellati C

更新日期：2004-01-01 00:00:00

abstract：:The HIV/AIDS pandemic continues its spread at a rate of over 15,000 new infections every day. Sexual transmission of HIV-1 is the dominant mode of this pandemic spread. For the first time since the disease emerged in the early 1980s, about half the 42 million people now living with HIV/AIDS worldwide are women. Worldw...

journal_title：Current pharmaceutical design

authors： D'Cruz OJ,Uckun FM

更新日期：2004-01-01 00:00:00

abstract：:The development of radioligands to image beta-amyloid (A beta) plaques and neurofibrillary tangles (NFTs) in vivo in the aging human brain is an important and active area of radiopharmaceutical design. When used in combination with positron emission tomography (Pet) or single photon emission computed tomography (spect...

journal_title：Current pharmaceutical design

authors： Mathis CA,Wang Y,Klunk WE

更新日期：2004-01-01 00:00:00