Dimeric and hybrid anti-Alzheimer drug candidates.

abstract：:Semicarbazide-sensitive amine-oxidase (SSAO) is present in various human tissues and in plasma. Oxidative deamination of short-chain aliphatic amines is catalyzed by this enzyme to afford the corresponding aldehydes, ammonia and hydrogen peroxide. Methylamine and aminoacetone have been recognized to be physiological s...

journal_title：Current medicinal chemistry

authors： Mátyus P,Dajka-Halász B,Földi A,Haider N,Barlocco D,Magyar K

更新日期：2004-05-01 00:00:00

abstract：:Snake venoms are natural sources of biologically active molecules that are able to act selectively and specifically on different cellular targets, modulating physiological functions. Thus, these mixtures, composed mainly of proteins and peptides, provide ample and challenging opportunities and a diversified molecular ...

journal_title：Current medicinal chemistry

authors： Almeida JR,Resende LM,Watanabe RK,Carregari VC,Huancahuire-Vega S,da S Caldeira CA,Coutinho-Neto A,Soares AM,Vale N,de C Gomes PA,Marangoni S,de A Calderon L,Da Silva SL

更新日期：2017-01-01 00:00:00

abstract：:Receptor-binding peptides have attracted an enormous interest in targeting molecules for the development of tumour specific radiopharmaceutical compounds. The overexpression of many receptors on human tumour makes such peptide-ligands attractive agents for diagnostic imaging and therapy of cancers. The use of solid-ph...

journal_title：Current medicinal chemistry

authors： Bolzati C,Refosco F,Marchiani A,Ruzza P

更新日期：2010-01-01 00:00:00

abstract：:Neurodegenerative disorders (NDDs) like Alzheimer's disease, Parkinson's disease and Huntington's disease are a heterogeneous group of disorders with the progressive and severe loss of neurons. There are no full proof cures for these diseases, and only medicines are available that can alleviate some of the symptoms. D...

journal_title：Current medicinal chemistry

authors： Volcho KP,Laev SS,Ashraf GM,Aliev G,Salakhutdinov NF

更新日期：2018-01-01 00:00:00

abstract：:Fulvestrant is a novel endocrine therapy for breast cancer, with a unique structure and mode of action. It binds competitively to the oestrogen receptor (ER), with high affinity, and downregulates ER by functional blockade and increased turnover. Fulvestrant has reached the clinic via extensive pre-clinical and clinic...

journal_title：Current medicinal chemistry

authors： Johnston SJ,Cheung KL

更新日期：2010-01-01 00:00:00

abstract：:Amyotrophic Lateral Sclerosis (ALS) is a fatal neurodegenerative disease characterized by progressive degeneration of motor neurons which brings to muscular atrophy, paralysis and death in 3-5 years from starting symptoms. In about 10% of cases ALS is familiar and in a relevant percent of these cases, mutations of the...

journal_title：Current medicinal chemistry

authors： Contestabile A

更新日期：2011-01-01 00:00:00

abstract：:Dendritic cells (DCs) play a central role in the establishment of tolerance/immunity, because they activate naïve T cells (TCs). Therefore, the pharmacological modulation of DCs has become a major field of interest in immunology. A large body of literature has arisen from the studies of DC biology during immunosuppres...

journal_title：Current medicinal chemistry

authors： Schlichting CL,Schareck WD,Nickel T,Weis M

更新日期：2005-01-01 00:00:00

abstract：:Fabry disease (FD) is an X-linked glycosphingolipid storage disorder caused by deficient activity of the lysosomal enzyme alpha-galactosidase A. This leads to a progressive accumulation of globotriaosylceramide (Gb3) in the lysosomes of different cells and tissues, causing principally ventricular hypertrophy, renal fa...

journal_title：Current medicinal chemistry

authors： Caballero L,Climent V,Hernández-Romero D,Quintanilla MA,de la Morena G,Marín F

更新日期：2010-01-01 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：:Recent advances in endoscopic techniques such as capsule endoscopy have revealed that aspirin and other nonsteroidal antiinflammatory drugs (NSAIDs) often cause mucosal lesions not only in the upper gastrointestinal tract, but also in the small intestine in humans. Gastric and duodenal lesions caused by NSAIDs can be ...

journal_title：Current medicinal chemistry

authors： Satoh H,Takeuchi K

更新日期：2012-01-01 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：:Mycobacterium tuberculosis (Mtb), the main aetiological agent of tuberculosis (TB) in humans, is estimated to cause nearly two million deaths every year. Despite their huge therapeutic value, existing antitubercular drugs have several shortcomings, such as for instance the insurgence of drug resistance, which is mostl...

journal_title：Current medicinal chemistry

authors： Fanzani L,Porta F,Meneghetti F,Villa S,Gelain A,Lucarelli AP,Parisini E

更新日期：2015-01-01 00:00:00

abstract：:Among naturally occurring isoflavones, soy isoflavones are an important class with various biological activities. Due to their phytoestrogenic structure, their effects on the brain are profound thus making the neurobiological effects of these compounds an active area of research. One such compound is daidzein, which h...

journal_title：Current medicinal chemistry

authors： Ahmed T,Javed S,Tariq A,Budzyńska B,D'Onofrio G,Daglia M,Nabavi SF,Nabavi SM

更新日期：2017-01-01 00:00:00

abstract：BACKGROUND:Steroid hormones belong to a group of low-molecular weight compounds which are responsible for maintenance of various body functions, thus, their accurate assessment is crucial for evaluation of biosynthetic defects. The development of reliable methods allowing disease diagnosis is essential to improve early...

journal_title：Current medicinal chemistry

authors： Kotłowska A,Szefer P

更新日期：2019-01-01 00:00:00

abstract：:HupA is a potent, reversible AChEI, which crosses the blood-brain barrier smoothly, and shows high specificity for AChE with a prolonged biological half-life. It has been approved as the drug for the treatment of AD in China, and marketed in USA as a dietary supplement. HupA has been the subject of investigations by a...

journal_title：Current medicinal chemistry

authors： Jiang H,Luo X,Bai D

更新日期：2003-11-01 00:00:00

abstract：:The inhibition of protein degradation through the ubiquitin-proteasome pathway is a recently developed approach to cancer treatment which extends the range of cellular targets for chemotherapy. This therapeutic strategy is very interesting since the proteasomes carry out the regulated degradation of unnecessary or dam...

journal_title：Current medicinal chemistry

authors： Gilardini A,Marmiroli P,Cavaletti G

更新日期：2008-01-01 00:00:00

abstract：:Tumor necrosis factor (TNF) is a cytokine with well known anticancer properties and is being utilized as anticancer agent for the treatment of patients with locally advanced solid tumors. However, TNF role in cancer biology is debated. In fact, in spite of the wealth of evidence supporting its antitumor activity, the ...

journal_title：Current medicinal chemistry

authors： Bertazza L,Mocellin S

更新日期：2010-01-01 00:00:00

abstract：:Heme is an essential molecule with contradictory biological functions. In hemoproteins such as hemoglobin and cytochromes protein-bound heme is a prosthetic group serving physiological functions as a transporter for oxygen and electrons. On the other hand free heme can have deleterious effects by generating reactive o...

journal_title：Current medicinal chemistry

authors： Wijayanti N,Katz N,Immenschuh S

更新日期：2004-04-01 00:00:00

abstract：:Hypoxia in tumor cells is characterized by a lack of oxygen resulting from reduced blood supply to the surrounding tissue, and is a common characteristic of solid tumors as a consequence of rapid cell growth. Hypoxia in tumors is a predictor of both resistance to chemotherapy and of a metastatic/aggressive form of can...

journal_title：Current medicinal chemistry

authors： Liang D,Miller GH,Tranmer GK

更新日期：2015-01-01 00:00:00

abstract：:Xanthones (dibenzo-γ-pyrones) constitutes an important class of oxygenated heterocycles and occur as secondary metabolites in plants and microorganisms. They are known for various biological activities such as antioxidant, monoamine oxidase inhibitor, antihypertensive, hepatoprotective, antithrombotic, antifungal and ...

journal_title：Current medicinal chemistry

authors： Panda SS,Chand M,Sakhuja R,Jain SC

更新日期：2013-01-01 00:00:00

abstract：:Multitarget-directed ligands (MTDLs), an emerging and appealing drug discovery strategy, utilizing a single chemical entity to inhibit multitargets, was confirmed to be effective in reducing the likelihood of drug resistance, diminishing problems of dosing complexity, drug-drug interactions and toxicities, as well as ...

journal_title：Current medicinal chemistry

authors： Zhan P,Liu X

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND:Cholesterol efflux as a key event in reverse cholesterol transport (RCT) is considered now as both diagnostic tool and a promising target for the treatment of atherosclerosis. Radioactive in vitro cholesterol efflux assay (CEA) is the gold standard for determination of efflux at cellular level. Fluorescent t...

journal_title：Current medicinal chemistry

authors： Litvinov DY,Savushkin EV,Garaeva EA,Dergunov AD

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:The evolutionarily conserved Hedgehog (Hh) signaling cascade is one of the key mediators of embryonic development of many metazoans. This pathway has been extensively targeted by small molecule inhibitors as its misregulation leads to various malignancies and developmental disorders. Thus, blocking this path...

journal_title：Current medicinal chemistry

authors： Khatra H,Bose C,Sinha S

更新日期：2017-01-01 00:00:00

abstract：:The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient non-steroidal anti-inflammatory drugs with reduced side effects compared to standard NSAIDs. This review will focus on the structural features needed to achieve COX-2 selectivity. Five struc...

journal_title：Current medicinal chemistry

authors： Dannhardt G,Laufer S

更新日期：2000-11-01 00:00:00

abstract：:Insulin dependent diabetes mellitus (Type 1 diabetes, T1D) is a chronic autoimmune disorder characterized by the destruction of insulin-producing pancreatic beta cells by proinflammatory autoreactive T cells. In the past, several therapeutic approaches have been exploited by immunologists aiming to regulate the autoim...

journal_title：Current medicinal chemistry

authors： Fierabracci A

更新日期：2011-01-01 00:00:00

abstract：:Epidemiological studies demonstrated that even in the absence of other risk factors (e.g. diabetes, hypertension, hyperhomocysteinemia, hypercholesterolemia), advanced age itself significantly increases cardiovascular morbidity by enhancing vascular oxidative stress and inflammation. Because the population in the West...

journal_title：Current medicinal chemistry

authors： Labinskyy N,Csiszar A,Veress G,Stef G,Pacher P,Oroszi G,Wu J,Ungvari Z

更新日期：2006-01-01 00:00:00

abstract：:Photodynamic therapy (PDT) involves the administration of a photosensitizer (PS) followed by illumination with visible light, leading to generation of reactive oxygen species. The mechanisms of resistance to PDT ascribed to the PS may be shared with the general mechanisms of drug resistance, and are related to altered...

journal_title：Current medicinal chemistry

authors： Casas A,Di Venosa G,Hasan T,Al Batlle

更新日期：2011-01-01 00:00:00

abstract：:Resistance to quinolones and fluoroquinolones has been increasingly reported among human and veterinary isolates during the last three decades related to their wide clinical use. Until recently, the mechanisms of resistance to quinolones in Enterobacteriaceae were believed to be only chromosome-encoded, i.e. related t...

journal_title：Current medicinal chemistry

authors： Cattoir V,Nordmann P

更新日期：2009-01-01 00:00:00

abstract：:HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) nowadays represent most promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT). They have a unique antiviral potency, high specificity and low cytotoxicity. However, to a great extent, the efficacy of HIV-1 NNRTIs is compounde...

journal_title：Current medicinal chemistry

authors： Chen X,Zhan P,Li D,De Clercq E,Liu X

更新日期：2011-01-01 00:00:00

abstract：:The hyaluronidases (HAases) are a group of less extensively studied glycosidases distributed throughout the animal kingdom and are popularly known as 'spreading factors'. In recent years, HAases received much attention due to their ability to abruptly alter the hyaluronic acid (HA) homeostasis. HAases preferentially d...

journal_title：Current medicinal chemistry

authors： Girish KS,Kemparaju K,Nagaraju S,Vishwanath BS

更新日期：2009-01-01 00:00:00