abstract：:Vascular disorders, resulting from endothelial cell dysfunction, may be caused by various stimuli, including infectious pathogens, cytotoxic reagents, and pathophysiological mechanisms mediated by immune responses. Endothelial cell dysfunction characterized by apoptosis and abnormal immune activation is, at least in p...

journal_title：Current pharmaceutical design

authors： Lin YS,Lin CF,Lei HY,Liu HS,Yeh TM,Chen SH,Liu CC

更新日期：2004-01-01 00:00:00

abstract：:Parkinson's disease (PD) is a common neurodegenerative disorder characterized by cardinal features of tremor, bradykinesia, rigidity and postural instability. In addition to the motor symptoms patients experience cognitive decline eventually resulting in severe disability. Pathologically PD is characterized by neurode...

journal_title：Current pharmaceutical design

authors： Thomas M,Le WD

更新日期：2004-01-01 00:00:00

abstract：:A wide range of peptides and polypeptides can be appended to either the N- or C-terminus of G protein-coupled receptors without disrupting substantially ligand binding and signal transduction. Following fusion of fluorescent proteins, reporter gene constructs or G protein alpha subunits to the C-terminal tail of a rec...

journal_title：Current pharmaceutical design

authors： Milligan G,Feng GJ,Ward RJ,Sartania N,Ramsay D,McLean AJ,Carrillo JJ

更新日期：2004-01-01 00:00:00

abstract：:The introduction of highly active anti-retroviral therapy (HAART) for Human Immunodeficiency Virus (HIV) infection has significantly improved the life expectancy of HIV positive patients. Hepatitis C virus (HCV) co-infection is common in HIV infected patients and is now a significant cause of morbidity and mortality. ...

journal_title：Current pharmaceutical design

authors： Fabris P,Barnes E,Tositti G,Giordani MT,Grasso A,De Lalla F

更新日期：2004-01-01 00:00:00

abstract：:Membrane disrupting lytic peptides are abundant in nature and serve insects, invertebrates, vertebrates and humans as defense molecules. Initially, these peptides attracted attention as antimicrobial agents; later, the sensitivity of tumor cells to lytic peptides was discovered. In the last decade intensive research h...

journal_title：Current pharmaceutical design

authors： Leuschner C,Hansel W

更新日期：2004-01-01 00:00:00

abstract：:Macrolides have broad antibacterial spectrum and proven efficacy in the management of respiratory tract infections. Over the past decade there has been progressive interest in these agents for their potential role as tissue modifying, anti-inflammatory agents. Increasingly, the effect of macrolides on numerous cell ty...

journal_title：Current pharmaceutical design

authors： Martinez FJ,Simon RH

更新日期：2004-01-01 00:00:00

abstract：:The antimicrobial agents used in the treatment of mycobacterial infections have remained largely unchanged for several decades. Primary treatment of tuberculosis relies on four drugs, isoniazid, a rifamycin, pyrazinamide, and ethambutol (or streptomycin), and generally results in >95% cure in uncomplicated tuberculosi...

journal_title：Current pharmaceutical design

authors： Jacobs MR

更新日期：2004-01-01 00:00:00

abstract：:Prostaglandin (PG) D(2), the major cyclooxygenase metabolite generated from immunologically stimulated mast cells, is thought to contribute to the pathogenesis of allergic diseases due to its various inflammatory effects. However, the lack of PGD(2) (DP) receptor antagonists has limited the study of its essential role...

journal_title：Current pharmaceutical design

authors： Mitsumori S

更新日期：2004-01-01 00:00:00

abstract：:Diabetic retinopathy remains the most common microvascular complication suffered by diabetic patients and is the leading cause of registerable blindness in the working population of developed countries. The clinicopathological lesions of diabetic retinopathy have been well characterised and although a multitude of pat...

journal_title：Current pharmaceutical design

authors： Stitt AW,Frizzell N,Thorpe SR

更新日期：2004-01-01 00:00:00

abstract：:Propofol (2, 6-diisopropylphenol) is a potent intravenous hypnotic agent which is widely used for the induction and maintenance of anesthesia and for sedation in the intensive care unit. Propofol is an oil at room temperature and insoluble in aqueous solution. Present formulations consists of 1% or 2% (w/v) propofol, ...

journal_title：Current pharmaceutical design

authors： Marik PE

更新日期：2004-01-01 00:00:00

abstract：:Rotaviruses are an important cause of human morbidity and mortality, representing the primary pathogens responsible for acute dehydrating diarrhea in children under the age of 3. The infectious rotavirus particle is made up of three concentric layers of protein, and contains a genome consisting of eleven segments of d...

journal_title：Current pharmaceutical design

authors： Patton JT,Vasquez-Del Carpio R,Spencer E

更新日期：2004-01-01 00:00:00

abstract：:The CCN family of growth factors is composed of six structurally related proteins including the cysteine-rich 61 (Cyr61), connective tissue growth factor (CTGF), nephroblastoma overexpressed (NOV), Wnt-1 induced secreted protein-1 (WISP-1), WISP-2 and WISP-3. Each family member consists of four conserved cysteine rich...

journal_title：Current pharmaceutical design

authors： Desnoyers L

更新日期：2004-01-01 00:00:00

abstract：:Despite the significant progresses made in antiretroviral therapy, current drugs still cannot cure or prevent HIV infection. And all drugs continue to select for drug-resistant HIV strains. Consequently, new antiretroviral drugs are constantly being developed. To ensure safety, these drugs are usually designed to inhi...

journal_title：Current pharmaceutical design

authors： Provencher VM,Coccaro E,Lacasse JJ,Schang LM

更新日期：2004-01-01 00:00:00

abstract：:Microdialysis is a technique for sampling the chemistry of the interstitial fluid of tissues and organs in animal and man. It is minimally invasive and simple to perform in a clinical setting. Although microdialysis samples essentially all small molecular substances present in the interstitial fluid the use of microdi...

journal_title：Current pharmaceutical design

authors： Ungerstedt U,Rostami E

更新日期：2004-01-01 00:00:00

abstract：:Approximately half of patients with schizophrenia have a lifetime diagnosis of substance abuse disorders. These dual diagnosis patients are more likely to have poorer outcomes, including more severe psychiatric symptoms with increased hospitalizations, higher utilization of services and frequent homelessness. Assessme...

journal_title：Current pharmaceutical design

authors： Tsuang J,Fong TW

更新日期：2004-01-01 00:00:00

abstract：:Nuclear medicine offers powerful noninvasive techniques for visualization of infectious and inflammatory disorders using whole body imaging enabling the determination of both localization and number of inflammatory foci. A wide variety of approaches depicting the different stages of the inflammatory response have been...

journal_title：Current pharmaceutical design

authors： Bleeker-Rovers CP,Boerman OC,Rennen HJ,Corstens FH,Oyen WJ

更新日期：2004-01-01 00:00:00

abstract：:Glucocorticoids are the first line medication used in the therapy of many severe inflammatory disorders. They exert their activity through binding to the glucocorticoid receptor, a ligand-dependent transcription factor, and result in either activation or repression of a large set of glucocorticoid responsive genes. Th...

journal_title：Current pharmaceutical design

authors： Schulz M,Eggert M

更新日期：2004-01-01 00:00:00

abstract：:Phytoestrogens are plant-derived compounds with estrogen-like activities. Certain foods such as soy-derived products are known to have high levels of phytoestrogens, and about 25% of commercial infant formulas used in the United States are soy-based. One of the most important phytoestrogens is the isoflavone genistein...

journal_title：Current pharmaceutical design

authors： You L

更新日期：2004-01-01 00:00:00

abstract：:Mechanical loading provides an anabolic stimulus for bone. More importantly, the mechanosensing apparatus in bone directs osteogenesis to where it is most needed for improving bone strength. The biological processes involved in bone mechanotransduction are poorly understood and further investigation of the molecular m...

journal_title：Current pharmaceutical design

authors： Turner CH,Robling AG

更新日期：2004-01-01 00:00:00

abstract：:Human arylamine N-acetyltransferases 1 and 2 (NAT1 and NAT2) are polymorphic phase II xenobiotic-metabolising enzymes (XME) that acetylate arylamine compounds. They therefore play an important role in the detoxication and/or metabolic activation of certain therapeutic drugs, occupational chemicals and carcinogens. Alt...

journal_title：Current pharmaceutical design

authors： Rodrigues-Lima F,Dupret JM

更新日期：2004-01-01 00:00:00

abstract：:Virtual screening, especially the structure-based virtual screening, has emerged as a reliable, cost-effective and time-saving technique for the discovery of lead compounds. Here, the basic ideas and computational tools for virtual screening have been briefly introduced, and emphasis is placed on aspects of recent dev...

journal_title：Current pharmaceutical design

authors： Hou T,Xu X

更新日期：2004-01-01 00:00:00

abstract：:Various growth factors such as the platelet derived growth factor (PDGF), insulin-like growth factor (IGF), epidermal growth factor (EGF), fibroblast growth factor (FGF), and vascular endothelial growth factor (VEGF) transduce their mitogenic signals through the activation of tyrosine kinase receptors (RTKs). Since en...

journal_title：Current pharmaceutical design

authors： Gouni-Berthold I,Sachinidis A

更新日期：2004-01-01 00:00:00

abstract：:DAP12 is a novel immunoreceptor tyrosine-based activation motifs (ITAM)-bearing transmembrane adapter molecule. This molecule, together with its partner receptor complex molecules including the killer cell activating receptors (KARs), myeloid DAP12 associating lectin-1 (MDL-1), triggering receptor expressed on myeloid...

journal_title：Current pharmaceutical design

authors： Aoki N,Kimura S,Xing Z

更新日期：2003-01-01 00:00:00

abstract：:Myocarditis is a disease whose pathogenesis is not completely understood and whose prevalence is likely underestimated. Individuals afflicted with this condition may be treated with agents that relieve symptoms arising from inflammation and concurrent cellular damage. One class of drugs commonly used in the treatment ...

journal_title：Current pharmaceutical design

authors： Godsel LM,Leon JS,Engman DM

更新日期：2003-01-01 00:00:00

abstract：:Angiogenesis, the development of new capillaries form pre-existing vessels, requires the coordinate activation of endothelial cells, which migrate and proliferate in response to growth factors to form functional vessels. Therapeutic angiogenesis is proposed to restore tissue integrity and function following damage and...

journal_title：Current pharmaceutical design

authors： Morbidelli L,Donnini S,Ziche M

更新日期：2003-01-01 00:00:00

abstract：:Pituitary adenylate cyclase-activating polypeptide (PACAP) is a novel member of the secretin/glucagon/vasoactive intestinal peptide (VIP) superfamily. In vertebrates, including avians, it occurs in two forms: PACAP(38) and PACAP(27). PACAP structure is well conserved during evolution, being identical in mammals, and s...

journal_title：Current pharmaceutical design

authors： Nowak JZ,Zawilska JB

更新日期：2003-01-01 00:00:00

abstract：:Although the cause of Crohn's disease remains unknown considerable progress has been made in recent years to unravel the pathogenesis of the inflammatory processes seen in chronic idiopathic inflammatory bowel diseases (IBD). Th-1 lymphocytes seem to orchestrate the inflammation through the production of pro-inflammat...

journal_title：Current pharmaceutical design

authors： D'Haens G

更新日期：2003-01-01 00:00:00

abstract：:Macrophages are professional scavengers of apoptotic and necrotic cells, and hence constantly take up self antigens. Paradoxically, macrophages are also professional antigen-presenting cells, which would seem to invite autoimmune disorders. Moreover, macrophages are effector cells in the tissue-destruction phase of au...

journal_title：Current pharmaceutical design

authors： Munn DH,Mellor AL

更新日期：2003-01-01 00:00:00

abstract：:In recent years, the simple paradigm of adipose tissue as merely a fat store is rapidly evolving into a complex paradigm of this tissue as multipotential secretory organ, partitioned into a few large depots, including visceral and subcutaneous location, and many small depots, associated with a variety of organs in the...

journal_title：Current pharmaceutical design

authors： Chaldakov GN,Stankulov IS,Hristova M,Ghenev PI

更新日期：2003-01-01 00:00:00

abstract：:This review summarizes some of the published attempts to incorporate protein and NMR structures in the design of new antibiotics that specifically target Cell Wall biosynthesis. Most of the steps involved in peptidglycan synthesis have been investigated as potential strategies against cell wall inhibition. Structural ...

journal_title：Current pharmaceutical design

authors： Katz AH,Caufield CE

更新日期：2003-01-01 00:00:00

abstract：:Leptin has been shown to have a wide repertoire of peripheral effects, some of which are mediated through the central nervous system and others that are induced through a direct action on target tissues. There is now evidence showing that leptin exerts some of its metabolic effects acting directly on peripheral tissue...

journal_title：Current pharmaceutical design

authors： Veniant MM,LeBel CP

更新日期：2003-01-01 00:00:00

abstract：:A review of the Electron-Conformational (EC) method of pharmacophore (Pha) identification and quantitative bioactivity prediction in drug design and toxicology is presented, which includes the latest advances and improvements of the method as a whole and details of its realization with illustration of results. In the ...

journal_title：Current pharmaceutical design

authors： Bersuker IB

更新日期：2003-01-01 00:00:00

abstract：:Several lines of evidence support a mutual relationship between the nervous system and the immune system. Therefore, it is not surprising that some neuropsychiatric disorders are also characterized by immune abnormalities. In patients with phobic disorders and in patients with migraine without aura some common immune ...

journal_title：Current pharmaceutical design

authors： Covelli V,Pellegrino NM,Jirillo E

更新日期：2003-01-01 00:00:00

abstract：:Immune complexes are major pathogenic factors contributing to tissue injury in a number of autoimmune diseases. Immune complexes consist of autoantibodies to self-antigens, which initiate an inflammatory response through binding to immunoglobulin Fc receptors (FcRs) or via complement components. The significance of Fc...

journal_title：Current pharmaceutical design

authors： Kleinau S

更新日期：2003-01-01 00:00:00

abstract：:In order to develop an effective pharmacological treatment for obesity, an endogenous factor that promotes a positive energy balance by increasing appetite and decreasing fat oxidation could represent the drug target scientists have been looking for. The recently discovered gastric endocrine agent ghrelin, which appea...

journal_title：Current pharmaceutical design

authors： Horvath TL,Castañeda T,Tang-Christensen M,Pagotto U,Tschöp MH

更新日期：2003-01-01 00:00:00

abstract：:Management of hypertension has evolved steadily through 25 years of major clinical trials results modifying both the definition of hypertension and clinical management strategies. Trials experience in heart failure is much less extensive given the far smaller therapeutic market and traditionally often followed on the ...

journal_title：Current pharmaceutical design

authors： MacFadyen RJ,Lip GY,Davis R

更新日期：2003-01-01 00:00:00

abstract：:Opioid peptides showing selectivity for delta receptor have been isolated from enzymatic digests of plant proteins. Five peptides were derived from wheat gluten, and named gluten exorphins A5, A4, B5, B4 and C. Two opioid peptides were also released from spinach ribulose-bisphosphate-carboxylase/oxygenase (Rubisco), a...

journal_title：Current pharmaceutical design

authors： Yoshikawa M,Takahashi M,Yang S

更新日期：2003-01-01 00:00:00

abstract：:Although the pathogenesis of inflammatory bowel disease (IBD) remains elusive, it appears that there is chronic activation of the immune and inflammatory cascade in genetically susceptible individuals. Current disease management guidelines have therefore focused on the use of anti-inflammatory agents, aminosalicylates...

journal_title：Current pharmaceutical design

authors： Ogata H,Hibi T

更新日期：2003-01-01 00:00:00

abstract：:Cyclooxygenase-1 (COX-1) derived eicosanoids promote gastroprotective mucosal defenses and induce platelet aggregation. By sparing COX-1, COX-2 specific inhibitors provide effective anti-inflammatory and analgesic activity while substantially reducing the risk of peptic ulcer disease and GI bleeding compared to dual C...

journal_title：Current pharmaceutical design

authors： Scheiman JM

更新日期：2003-01-01 00:00:00

abstract：:Improvements in the radiotherapeutic management of solid tumors through the concurrent use of gene therapy is a realistic possibility. Of the broad array of candidate genes that have been evaluated, those encoding prodrug-activating enzymes are particularly appealing since they directly complement ongoing clinical che...

journal_title：Current pharmaceutical design

authors： Patterson AV,Saunders MP,Greco O

更新日期：2003-01-01 00:00:00