Developing inhibitors to selectively target two-component and phosphorelay signal transduction systems of pathogenic microorganisms.

abstract：:Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind...

journal_title：Current medicinal chemistry

authors： López-Rodríguez ML,Ayala D,Benhamú B,Morcillo MJ,Viso A

更新日期：2002-02-01 00:00:00

abstract：:Differentiation therapy of acute promyelocytic leukemia with all-trans retinoic acid represents the most successful pharmacological therapy of acute myeloid leukemia (AML). Numerous studies demonstrate that drugs that inhibit mechanistic target of rapamycin (mTOR) and activate AMP-kinase (AMPK) have beneficial effects...

journal_title：Current medicinal chemistry

authors： Visnjic D,Dembitz V,Lalic H

更新日期：2019-01-01 00:00:00

abstract：:Coumarins are of many different structures. They constitute an important class of pharmacological agents possessing a range of different physiological activities including anti-cancer, anti-oxidant, anti- inflammation, anti-HIV, anti-coagulant, anti-bacterial, analgesic and comparative immune-modulation. Recently, cou...

journal_title：Current medicinal chemistry

authors： Wu L,Wang X,Xu W,Farzaneh F,Xu R

更新日期：2009-01-01 00:00:00

abstract：:Drug resistance is one of the major obstacles limiting the success of cancer chemotherapy. Biological mechanisms contributing to drug resistance may be present de novo and related to inherent features or may be raised after exposure to anticancer drugs. In recent years, both clinical observations and experimental stud...

journal_title：Current medicinal chemistry

authors： Sui M,Zhang H,Fan W

更新日期：2011-01-01 00:00:00

abstract：:The hemostatic system comprises platelet aggregation, coagulation and fibrinolysis also termed primary, secondary and tertiary hemostasis. From the platelet transcriptome 6000 mRNA species and represent receptors, ion channels, signalling molecules, kinases, phosphatases, and structural, metabolic and regulatory prote...

journal_title：Current medicinal chemistry

authors： Stassen JM,Arnout J,Deckmyn H

更新日期：2004-09-01 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：:Anthocyanins are generally considered to be the largest and the most important group of water-soluble pigments in plants. They are widely consumed by humans as natural compounds of vegetables, fruits, and red wine. Anthocyanins as well as other flavonoids show protective qualities against variety of pathologies, inclu...

journal_title：Current medicinal chemistry

authors： Bártíková H,Skálová L,Dršata J,Boušová I

更新日期：2013-01-01 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：: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：:It is well-recognized that the majority of cancer-related deaths is attributed to metastasis, which can arise from virtually any type of tumor. Metastasis is a complex multistep process wherein cancer cells must break away from the primary tumor, intravasate into the circulatory or lymphatic systems, extravasate, prol...

journal_title：Current medicinal chemistry

authors： Wong KM,Song J,Saini V,Wong YH

更新日期：2019-01-01 00:00:00

abstract：:Artificial intelligence methods, in particular, machine learning, has been playing a pivotal role in drug development, from structural design to clinical trial. This approach is harnessing the impact of computer-aided drug discovery thanks to large available data sets for drug candidates and its new and complex manner...

journal_title：Current medicinal chemistry

authors： Musella S,Verna G,Fasano A,Di Micco S

更新日期：2020-11-11 00:00:00

abstract：:Non-alcoholic fatty liver disease is regarded as the hepatic manifestation of metabolic syndrome and is an important and common cause of chronic liver disease with a potential to develop end-stage liver disease. While important advances in the pathophysiology have been achieved using genetically modified and diet-indu...

journal_title：Current medicinal chemistry

authors： Chavez-Tapia NC,Rosso N,Tiribelli C

更新日期：2011-01-01 00:00:00

abstract：:Osteogenic peptides are, or have potential to be, therapies for the treatment of osteoporosis, fracture repair, and repair of loosened bone implants. Human parathyroid hormone has been approved for the treatment of post-menopausal osteoporosis. Constrained analogs of PTH and the parathyroid-hormone related peptide (PT...

journal_title：Current medicinal chemistry

authors： Willick GE,Morley P,Whitfield JF

更新日期：2004-11-01 00:00:00

abstract：:It is well recognised that increased levels of high density lipoprotein (HDL) protect against atherosclerosis and correlate with improved prognosis for vascular disease associated events. While many of the atheroprotective effects of HDL are ascribed to the ability to remove cholesterol from the vasculature through th...

journal_title：Current medicinal chemistry

authors： Murphy AJ,Chin-Dusting JP,Sviridov D,Woollard KJ

更新日期：2009-01-01 00:00:00

abstract：:Endothelial cells (ECs) play a pivotal role in physiological and altered tissue neovascularization. They face multiple morphological, biochemical and functional changes during the different phases of angiogenesis, under the regulation of a great number of proangiogenic and antiangiogenic signals, including soluble and...

journal_title：Current medicinal chemistry

authors： Munaron L,Fiorio Pla A

更新日期：2009-01-01 00:00:00

abstract：:5-Aminoisoquinolin-1-one (5-AIQ) is a water-soluble inhibitor of the poly(ADPribose) polymerases (PARPs), lacking isoform-selectivity. Although of only moderate potency in vitro against PARP-1, it is highly active in many assays in cells and in models in vivo, indicating excellent uptake. Optimisation of the several s...

journal_title：Current medicinal chemistry

authors： Threadgill MD

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Vaccines are very effective medical tools for disease prevention and life span increase. Controversies have raised concern about their safety, from autism to polio vaccine contamination with simian virus 40 (SV-40). Hysteria surrounding vaccine-associated risks has resulted in a declining number of vaccinati...

journal_title：Current medicinal chemistry

authors： Pandolfi F,Franza L,Todi L,Carusi V,Centrone M,Buonomo A,Chini R,Newton EE,Schiavino D,Nucera E

更新日期：2018-01-01 00:00:00

abstract：:Gum resin extracts of Boswellia species have been traditionally applied in folk medicine for centuries to treat various chronic inflammatory diseases, and experimental data from animal models and studies with human subjects confirmed the potential of B. spec extracts for the treatment of not only inflammation but also...

journal_title：Current medicinal chemistry

authors： Poeckel D,Werz O

更新日期：2006-01-01 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 need for innovation in research is leading to an increased use of imaging biomarkers, which have shown to reduce timings and increase productivity, thus saving costs. PET and SPECT neurotransmission imaging has shown usefulness in the discovery and development of drugs for the central nervous system, providing uni...

journal_title：Current medicinal chemistry

authors： Catafau AM,Bullich S

更新日期：2013-01-01 00:00:00

abstract：:Glutamate carboxypeptidase II (GCPII) and its splice variants, paralogs and human homologs represent a family of proteins with diverse tissue distribution, cellular localization and largely unknown function which have been explored only recently. While GCPII itself has been thoroughly studied from different perspectiv...

journal_title：Current medicinal chemistry

authors： Hlouchová K,Navrátil V,Tykvart J,Sácha P,Konvalinka J

更新日期：2012-01-01 00:00:00

abstract：:A BRAF somatic mutation at residue 600 of the BRAF protein (BRAFV600E) is highly prevalent in papillary thyroid carcinomas (PTC). This mutation occurs in approximately 44% (from 29% to 83%) of PTC depending on the different studies. BRAFV600E is almost always found in PTC with a papillary or a mixed follicular/papilla...

journal_title：Current medicinal chemistry

authors： Lassalle S,Hofman V,Ilie M,Butori C,Bozec A,Santini J,Vielh P,Hofman P

更新日期：2010-01-01 00:00:00

abstract：:In healthy individuals, natural and adaptive immune responses are able to control virus entry into the host. In particular, CD8(+)-mediated cytotoxicity, sustained by the intervention of CD4+ cells, represents the major key event leading to virus eradication. On the other hand, viruses are able to evade from host immu...

journal_title：Current medicinal chemistry

authors： Amati L,Passeri ME,Lippolis A,Lio D,Caruso C,Jirillo E,Covelli V

更新日期：2006-01-01 00:00:00

abstract：:Since the discovery of penicillin, natural and synthetic β-lactams have aroused great interest not only as sources of effective antibacterial agents but also as specific inhibitors of proteases responsible for various non-bacterial pathological processes. This interest was reflected in our review published in Current ...

journal_title：Current medicinal chemistry

authors： Veinberg G,Potorocina I,Vorona M

更新日期：2014-01-01 00:00:00

abstract：:Systemic Lupus Erythematosus (SLE) is a chronic and relapsing heterogenous autoimmune disease that primarily affects women of reproductive age. Genetic and environmental risk factors are involved in the pathogenesis of SLE, and susceptibility genes have recently been identified. However, as gene therapy is far from cl...

journal_title：Current medicinal chemistry

authors： Pan Q,Guo Y,Guo L,Liao S,Zhao C,Wang S,Liu HF

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Chronic Liver Disorders (CLD), caused by the lifestyle patterns like alcoholism or by non-alcoholic fatty liver disease or because of virus-mediated hepatitis, affect a large population fraction across the world. CLD progresses into end-stage diseases with a high mortality rate. Liver transplant is the only ...

journal_title：Current medicinal chemistry

authors： Mahmood A,Seetharaman R,Kshatriya P,Patel D,Srivastava AS

更新日期：2020-01-01 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：:The purinergic receptor P2X7 is highly expressed in immune peripheral and central cells suggesting its important role in numerous diseases characterized by inflammatory processes like cancer, or neurodegenerative pathologies in relation with modulation of the immune system. Thereby, antagonization of this receptor may...

journal_title：Current medicinal chemistry

authors： Baudelet D,Lipka E,Millet R,Ghinet A

更新日期：2015-01-01 00:00:00

abstract：:There is evidence that hyperglycemia results in the generation of reactive oxygen species, leading to oxidative stress in various tissues, including vascular system. An important link between oxidative stress, inflammatory response and insulin activity is now well established. The ability of antioxidants to protect ag...

journal_title：Current medicinal chemistry

authors： Nicolle E,Souard F,Faure P,Boumendjel A

更新日期：2011-01-01 00:00:00

abstract：:Hydrogen sulfide (H2S), previously known only as a toxic agent, in the last decades has been recognized as an important endogenous gasotransmitter, playing a key role in the homeostasis of the cardiovascular system. In the last years, the growing evidence about a protective role exhibited by H2S against myocardial isc...

journal_title：Current medicinal chemistry

authors： Citi V,Piragine E,Testai L,Breschi MC,Calderone V,Martelli A

更新日期：2018-01-01 00:00:00