abstract：:Anticancer drugs are often nonselective antiproliferative agents (cytotoxins) that preferentially kill dividing cells by attacking their DNA at some level. The lack of selectivity results in significant toxicity to noncancerous proliferating cells. These toxicities along with drug resistance exhibited by the solid tum...

journal_title：Current medicinal chemistry

authors： Singh Y,Palombo M,Sinko PJ

更新日期：2008-01-01 00:00:00

abstract：:Over the last decade there has been significant progress in understanding the molecular basis of disease processes. At the same time the technological advances in the area of genomics and the efforts in proteomics research have increased the possibility of discovering many proteins with defined therapeutic functions. ...

journal_title：Current medicinal chemistry

authors： Platis D,Labrou NE

更新日期：2008-01-01 00:00:00

abstract：:The fibrinolytic system includes a broad spectrum of proteolytic enzymes with physiological and pathophysiological functions in several processes, such as haemostatic balance, tissue remodeling, tumor invasion, angiogenesis and reproduction. The main enzyme of the plasminogen activator system is plasmin, which is resp...

journal_title：Current medicinal chemistry

authors： Zorio E,Gilabert-Estellés J,España F,Ramón LA,Cosín R,Estellés A

更新日期：2008-01-01 00:00:00

abstract：:In the hit to lead process, a drug candidate is selected from a set of potential leads by screening its binding with potential targets. This review focuses on the lead identification assays that employ a bio-chemical or bio-physical test to detect molecular recognition events between proteins and small molecules in a ...

journal_title：Current medicinal chemistry

authors： Bergese P,Cretich M,Oldani C,Oliviero G,Di Carlo G,Depero LE,Chiari M

更新日期：2008-01-01 00:00:00

abstract：:The Src family consists of eight non-receptor protein tyrosine kinases characterised by a common structure. Based on their amino acid sequence, Src family kinases are grouped into two subfamilies, which are also characterised by different tissue specificity. Src kinases are involved in signal transduction pathways tri...

journal_title：Current medicinal chemistry

authors： Benati D,Baldari CT

更新日期：2008-01-01 00:00:00

abstract：:Recent advances have identified the podocyte as a key target in glomerular injury. The podocyte is a highly specialized cell which is responsible for the glomerular permselectivity for proteins in the kidney. Podocyte injury or loss leads to proteinuria. Apoptosis has been shown to contribute to renal cell loss, inclu...

journal_title：Current medicinal chemistry

authors： Moreno JA,Sanchez-Niño MD,Sanz AB,Lassila M,Holthofer H,Blanco-Colio LM,Egido J,Ruiz-Ortega M,Ortiz A

更新日期：2008-01-01 00:00:00

abstract：:Proteomics has unraveled important questions in the biology of cardiovascular disease and holds even greater promise for the development of novel diagnostic and prognostic biomarkers. This approach may establish early detection strategies, and monitor responses to therapies. Technological advances (most notably blue n...

journal_title：Current medicinal chemistry

authors： Balestrieri ML,Giovane A,Mancini FP,Napoli C

更新日期：2008-01-01 00:00:00

abstract：:Nicotinamide adenine dinucleotide (NAD), generally considered a key component involved in redox reactions, has been found to participate in an increasingly diverse range of cellular processes, including signal transduction, DNA repair, and post-translational protein modifications. In recent years, medicinal chemists h...

journal_title：Current medicinal chemistry

authors： Chen L,Petrelli R,Felczak K,Gao G,Bonnac L,Yu JS,Bennett EM,Pankiewicz KW

更新日期：2008-01-01 00:00:00

abstract：:Factor Xa (fXa) is a critical serine protease situated at the confluence of the intrinsic and extrinsic pathways of the blood coagulation cascade. FXa catalyses the conversion of prothrombin to thrombin via the prothrombinase complex. Its singular role in thrombin generation, coupled with its potentiating effects on c...

journal_title：Current medicinal chemistry

authors： Guertin KR,Choi YM

更新日期：2007-01-01 00:00:00

abstract：:Coeliac disease is a multifactorial disease characterized by a dysregulated immune response to ingested wheat gluten and related cereal proteins. With an incidence of about 1% of the general population, it is considered the most common food intolerance disorder. The mainstay of coeliac disease treatment is strict life...

journal_title：Current medicinal chemistry

authors： Esposito C,Caputo I,Troncone R

更新日期：2007-01-01 00:00:00

abstract：:Several lines of defense maintain the surface integrity of the delicate airway epithelium which is regularly subjected to severe trauma. These defense mechanisms include protection by the mucus layer, rapid repair by restitution (cell migration) and regeneration via proliferation and differentiation. Luminal surveilla...

journal_title：Current medicinal chemistry

authors： Hoffmann W

更新日期：2007-01-01 00:00:00

abstract：:Nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF) belong to the protein family of neurotrophins. They both display profound neuromodulatory functions and are essentially involved in the survival and homeostatic maintenance of central and peripheral neurons during development and adulthood. Moreove...

journal_title：Current medicinal chemistry

authors： Schulte-Herbrüggen O,Braun A,Rochlitzer S,Jockers-Scherübl MC,Hellweg R

更新日期：2007-01-01 00:00:00

abstract：:N-BP, rapamycin and its derivatives have been originally developed respectively as anti-resorptive and anti-fungal agents. In fact, in vitro and in vivo experiments demonstrated that these compounds are multi-functional molecules exerting their effects on tumour cell growth and bone remodelling. The major challenge in...

journal_title：Current medicinal chemistry

authors： Ory B,Moriceau G,Redini F,Heymann D

更新日期：2007-01-01 00:00:00

abstract：:The ionotropic P2X7 receptor (P2X7R) has become the focus of intense research interest for a number of reasons: i) it is a cation selective ion channel that is modulated by extracellular ATP. Upon stimulation by high concentrations of ATP it generates a non-selective membrane pore which is permeable to hydrophilic mol...

journal_title：Current medicinal chemistry

authors： Gunosewoyo H,Coster MJ,Kassiou M

更新日期：2007-01-01 00:00:00

abstract：:A challenging question in biology is how cells control their shape and volume. The relative abundance of organelles can be radically modified to comply with a new task, an example being the massive development of the endoplasmic reticulum (ER) in Ig-secreting plasma cells. The ER is the site where secretory proteins a...

journal_title：Current medicinal chemistry

authors： Otsu M,Sitia R

更新日期：2007-01-01 00:00:00

abstract：:The cation-independent mannose 6-phosphate receptor is a multifunctional protein which binds at the cell surface to two distinct classes of ligands, the mannose 6-phosphate (M6P) bearing proteins and IGF-II. Its major function is to bind and transport M6P-enzymes to lysosomes, but it can also modulate the activity of ...

journal_title：Current medicinal chemistry

authors： Gary-Bobo M,Nirdé P,Jeanjean A,Morère A,Garcia M

更新日期：2007-01-01 00:00:00

abstract：:Mast cells are potent effectors playing a key role in IgE-associated hypersensitivity reactions, allergic disorders, inflammation and protective immune responses. Mast cell development in vivo occurs mainly in non-hematopoietic microenvironments and increased mast cell numbers can be seen in various inflammatory disea...

journal_title：Current medicinal chemistry

authors： Hu ZQ,Zhao WH,Shimamura T

更新日期：2007-01-01 00:00:00

abstract：:gammadelta T lymphocytes are involved in the defence from viral and mycobacterial infections; however they are also responsible for autoimmune reactions. Herein, we discuss the characteristics of these cells, focusing on the mechanism(s) underlying extravasation and tissue localization. We show that Vdelta1 and Vdelta...

journal_title：Current medicinal chemistry

authors： Poggi A,Catellani S,Fenoglio D,Borsellino G,Battistini L,Zocchi MR

更新日期：2007-01-01 00:00:00

abstract：:The introduction of highly active antiretroviral therapy (HAART) in 1996 dramatically changed the course of HIV infection. This therapy involves the use of at least three agents from two distinct classes of antivirals: a protease inhibitor (PI) in combination with two nucleoside/nucleotide reverse transcriptase inhibi...

journal_title：Current medicinal chemistry

authors： Mastrolorenzo A,Rusconi S,Scozzafava A,Barbaro G,Supuran CT

更新日期：2007-01-01 00:00:00

abstract：:Stress or heat shock proteins (Hsps) Hsp90, Hsp70 and Hsp27 are chaperones that assist the proteins in their folding, stability, assembly into multi-protein complexes and transport across cellular membranes. The expression of some of them is highly induced in response to a wide variety of physiological and environment...

journal_title：Current medicinal chemistry

authors： Didelot C,Lanneau D,Brunet M,Joly AL,De Thonel A,Chiosis G,Garrido C

更新日期：2007-01-01 00:00:00

abstract：:Aberrant signaling caused by mutations in the RAS-RAF-MEK-ERK pathway and its upstream activators critically contributes to human tumor development. Strategies, which aim at inhibiting hyperactive signaling molecules, appear conceptually straight forward, but their translation into clinical practice has been hampered ...

journal_title：Current medicinal chemistry

authors： Zebisch A,Czernilofsky AP,Keri G,Smigelskaite J,Sill H,Troppmair J

更新日期：2007-01-01 00:00:00

abstract：:Ageing is an aggravating factor leading to alterations in the biotransformation of drugs, and therefore their therapeutic efficacy and safety. In this review we discuss the influence of ageing on drug metabolizing enzymes in male Wistar rats. We report that drug metabolizing enzymes can be affected by ageing either by...

journal_title：Current medicinal chemistry

authors： Wauthier V,Verbeeck RK,Calderon PB

更新日期：2007-01-01 00:00:00

abstract：:Enteroviruses are members of picornavirus family which causes diverse and severe diseases in humans and animals. Clinical manifestations of enterovirus infections include fever, hand, foot, and mouth disease, and herpangina. Enteroviruses also cause potentially severe and life-threatening infections such as meningitis...

journal_title：Current medicinal chemistry

authors： Li C,Wang H,Shih SR,Chen TC,Li ML

更新日期：2007-01-01 00:00:00

abstract：:The market, sales and regulatory approval of new human medicines, during the past few years, indicates increasing number and share of new biologics and emergence of new multibillion dollar molecules. The global sale of monoclonal antibodies in 2006 were $20.6 billion. Remicade had annual sales gain of $1 billion durin...

journal_title：Current medicinal chemistry

authors： Maggon K

更新日期：2007-01-01 00:00:00

abstract：:The maximum therapeutic potentials of pharmacologically active molecules are generally not attained due to their non specific delivery. Ligands associated with drug or delivery system through which it is delivered provide navigation and direction to the carrier system(s) so as to reach and release bioactive(s) at the ...

journal_title：Current medicinal chemistry

authors： Rai S,Paliwal R,Vaidya B,Gupta PN,Mahor S,Khatri K,Goyal AK,Rawat A,Vyas SP

更新日期：2007-01-01 00:00:00

abstract：:The chemokine receptor, CXCR4, is a GPCR that transduces signals of its endogenous ligand, CXCL12 (stromal cell-derived factor-1, SDF-1). The CXCL12-CXCR4 system plays an important role in the migration of progenitors during embryologic development of the cardiovascular, hemopoietic, central nervous systems, etc. This...

journal_title：Current medicinal chemistry

authors： Tamamura H,Tsutsumi H,Masuno H,Fujii N

更新日期：2007-01-01 00:00:00

abstract：:The lung is a unique organ in terms of its direct exposure to high levels of oxygen and reactive compounds. Several parenchymal lung diseases (e.g. emphysema associated with smoking and a number of fibrotic lung disorders) have been proposed to be due to the exposure of the lung to exogenous irritants leading to local...

journal_title：Current medicinal chemistry

authors： Kinnula VL,Vuorinen K,Ilumets H,Rytilä P,Myllärniemi M

更新日期：2007-01-01 00:00:00

abstract：:The blood-brain barrier (BBB) impedes the influx of intravascular compounds from the blood to the brain. The elements composing the BBB are endothelial cells, pericytes and the end-feet of astrocytes. Among them, the endothelial cell barrier line is the most critical for preventing toxic substances from entering the b...

journal_title：Current medicinal chemistry

authors： Ueno M

更新日期：2007-01-01 00:00:00

abstract：:Homocysteine is a thiol aminoacid synthesized during the metabolism of methionine. Increased plasma levels of homocysteine can be the result of mutations in the enzymes responsible for homocysteine metabolism, particularly cystathionine-beta synthase (CBS) and 5,10-methylenetetrahydrofolate reductase (MTHFR). Addition...

journal_title：Current medicinal chemistry

authors： Pezzini A,Del Zotto E,Padovani A

更新日期：2007-01-01 00:00:00

abstract：:The role of cell adhesion molecules (CAMs), such as intercellular cell adhesion molecule-1 (ICAM-1), vascular endothelial cell adhesion molecule-1 (VCAM-1), E-selectin, and P-selectin, has been studied extensively in the process of inflammation. These molecules are responsible for recruiting leukocytes onto the vascul...

journal_title：Current medicinal chemistry

authors： Kobayashi H,Boelte KC,Lin PC

更新日期：2007-01-01 00:00:00

abstract：:Apoptosis or programmed cell death is a cellular mechanism used to regulate cell number and eliminate damaged or mutated cells. Many chemotherapeutic agents and ionizing radiation induce not only apoptotic signaling pathways, but also survival responses such as DNA damage responses and cell cycle arrest, which allow f...

journal_title：Current medicinal chemistry

authors： Sharma V,Hupp CD,Tepe JJ

更新日期：2007-01-01 00:00:00

abstract：:Diabetes mellitus (DM) is a significant healthcare concern worldwide that affects more than 165 million individuals leading to cardiovascular disease, nephropathy, retinopathy, and widespread disease of both the peripheral and central nervous systems. The incidence of undiagnosed diabetes, impaired glucose tolerance, ...

journal_title：Current medicinal chemistry

authors： Maiese K,Chong ZZ,Shang YC

更新日期：2007-01-01 00:00:00

abstract：:Molecular hybridization is a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hybrid compound with improved affinity and efficacy, when compared to the parent drugs. Additionally, this strategy can result in compounds pres...

journal_title：Current medicinal chemistry

authors： Viegas-Junior C,Danuello A,da Silva Bolzani V,Barreiro EJ,Fraga CA

更新日期：2007-01-01 00:00:00

abstract：:Leukoaraiosis (LA), one of the most frequent causes of cognitive disturbances, is presumed to involve vascular demyelinization and cerebral small-vessel diseases. Although it has been suggested that the development of LA is associated with cerebral circulatory disturbances, the pathomechanism of this circulatory probl...

journal_title：Current medicinal chemistry

authors： Szolnoki Z

更新日期：2007-01-01 00:00:00

abstract：:Coumarins, also referred as benzopyran-2-ones, and their corresponding nitrogen counterpart, 1-azacoumarins also referred to as carbostyrils, are a family of nature-occurring lactones and lactams respectively. The plant extracts containing coumarin-related heterocycles, which were employed as herbal remedies in early ...

journal_title：Current medicinal chemistry

authors： Kulkarni MV,Kulkarni GM,Lin CH,Sun CM

更新日期：2006-01-01 00:00:00

abstract：:Acyclic nucleoside analogues bearing phosphonomethoxy residues in the side chain (ANP) attract much attention due to a very beneficial combination of biological properties. Intensive work of organic chemists during the last two decades resulted in a large panel of new compounds that were evaluated as potential antivir...

journal_title：Current medicinal chemistry

authors： Khandazhinskaya A,Yasko M,Shirokova E

更新日期：2006-01-01 00:00:00

abstract：:It is now widely accepted that airway inflammation is the key factor underlying the pathogenesis of asthma. Inhaled corticosteroids remain the most important anti-inflammatory treatment for asthma. However, they are rather non-specific in their actions and their use raises concerns over side effects and compliance iss...

journal_title：Current medicinal chemistry

authors： Walsh GM

更新日期：2006-01-01 00:00:00

abstract：:Transglutaminases (TGases) are enzymes which catalyze the cross linking of a glutaminyl residue of a protein/peptide substrate to a lysyl residue of a protein/peptide co-substrate with the formation of an N-gamma-(epsilon-L-glutamyl)-L-lysine [GGEL] cross link (isopeptidic bond) and the concomitant release of ammonia....

journal_title：Current medicinal chemistry

authors： Martin A,Romito G,Pepe I,De Vivo G,Merola MR,Limatola A,Gentile V

更新日期：2006-01-01 00:00:00

abstract：:Currently available therapeutic options for non-insulin-dependent diabetes mellitus, such as dietary modification, oral hypoglycemics, and insulin, have limitations of their own. Many natural products and herbal medicines have been recommended for the treatment of diabetes. The present paper reviews medicinal plants t...

journal_title：Current medicinal chemistry

authors： Jung M,Park M,Lee HC,Kang YH,Kang ES,Kim SK

更新日期：2006-01-01 00:00:00

abstract：:Symmetry plays a crucial role in a variety of biological processes. For instance, many protein receptors, upon activation, dimerize to its active form and subsequently produce its biological action. Hence, there is a renewal of curiosity for the synthesis of dimeric molecules (or bivalent ligands) capable, not only to...

journal_title：Current medicinal chemistry

authors： Bérubé G

更新日期：2006-01-01 00:00:00