Lead optimization of melanin concentrating hormone receptor 1 antagonists with low hERG channel activity.

abstract：:Degenerative diseases are becoming more common with increasing life expectancy of the human population. The 20th century faced a progressive demographic change in the industrialized world, followed by identical trends in population aging in Asia, Africa, and Middle and South America. A significant increase in chronic ...

journal_title：Current topics in medicinal chemistry

authors： Delogu GL,Matos MJ

更新日期：2017-01-01 00:00:00

abstract：:A better understanding of the biology and pathogenesis of hematological malignancies has led to the development of immunotherapeutic and immunoregulatory drugs. Many of these agents have revolutionized the current treatment modalities, while others are under investigation. Rituximab (anti-CD20 antibody) has been estab...

journal_title：Current topics in medicinal chemistry

authors： Pangalis GA,Kyrtsonis MC,Vassilakopoulos TP,Dimopoulou MN,Siakantaris MP,Emmanouilides C,Doufexis D,Sahanas S,Kontopidou FN,Kalpadakis C,Angelopoulou MK,Dimitriadou EM,Kokoris SI,Panayiotidis P

更新日期：2006-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Liu W,Wang X,Zhu H,Duan Y

更新日期：2019-01-01 00:00:00

abstract：:Neuronal nicotinic acetylcholine ion channel receptors (nAChRs) exist as several subtypes and are involved in a variety of functions and disorders of the central nervous system (CNS), such as Alzheimer's and Parkinson's diseases. The lack of reliable information on the 3D structure of nAChRs prompted us to focus effor...

journal_title：Current topics in medicinal chemistry

authors： Nicolotti O,Altomare C,Pellegrini-Calace M,Carotti A

更新日期：2004-01-01 00:00:00

abstract：:This article is a review with 83 references of the application of NMR to the measurement of the dissociation constants of protein-ligand complexes. After briefly discussing some general concepts of molecular stability, the text turns to consider which NMR parameters are reporters of complex formation. The available da...

journal_title：Current topics in medicinal chemistry

authors： Fielding L

更新日期：2003-01-01 00:00:00

abstract：:Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and recept...

journal_title：Current topics in medicinal chemistry

authors： Pereira TM,Franco DP,Vitorio F,Kummerle AE

更新日期：2018-01-01 00:00:00

abstract：:The adenosine A(2A) receptor is a member of the G protein-coupled receptor family and mediates multiple physiological effects of adenosine, both at the central nervous system and at peripheral tissues. Increasing evidence relates the A(2A) receptor with several pathological conditions such as neurodegenerative disorde...

journal_title：Current topics in medicinal chemistry

authors： Clementina M,Giuseppe S

更新日期：2010-01-01 00:00:00

abstract：:Post translational modification (PTM) is one of the critical levels in regulation of gene expression that determines the fate of proteins after translation in eukaryotic cells. Since the detection of PTM sites in proteins is useful for diagnosis and prevention of diseases, numerous web-tool predictors are introduced t...

journal_title：Current topics in medicinal chemistry

authors： Mohabatkar H,Rabiei P,Alamdaran M

更新日期：2017-01-01 00:00:00

abstract：:Iron chelators may be of value as therapeutic agents in the treatment of cancer. They may act by depleting iron, a necessary nutrient, and limiting tumor growth. Alternatively or additionally, they may form redox-active metal complexes that cause oxidative stress via production of reactive oxygen species, damaging cri...

journal_title：Current topics in medicinal chemistry

authors： Buss JL,Greene BT,Turner J,Torti FM,Torti SV

更新日期：2004-01-01 00:00:00

abstract：:Prion diseases or transmissible spongiform encephalopathies (TSEs) are fatal neurodegenerative disorders associated with the conformational conversion of the cellular prion protein, PrP(C), into a pathological form known as prion or PrP(Sc). They can be classified into sporadic, inherited and infectious forms. Spontan...

journal_title：Current topics in medicinal chemistry

authors： Biljan I,Ilc G,Giachin G,Legname G,Plavec J

更新日期：2013-01-01 00:00:00

abstract：:The increase of pathogens being resistant to antibiotics represents a global health problem and therefore it is a pressing need to develop antibiotics with novel mechanisms of action. Host defense peptides, which have direct antimicrobial activity (also termed antimicrobial peptides) or immune modulating activity, are...

journal_title：Current topics in medicinal chemistry

authors： Lohner K

更新日期：2017-01-01 00:00:00

abstract：:Drugs with poor lipid and water solubility are some of the most challenging to formulate in nanocarriers, typically resulting in low encapsulation efficiencies and uncontrolled release profiles. PEGylated nanocapsules (PEG-NC) are known for their amenability to diverse modifications that allow the formation of domains...

journal_title：Current topics in medicinal chemistry

authors： Hervella P,Alonso-Sande M,Ledo F,Lucero ML,Alonso MJ,Garcia-Fuentes M

更新日期：2014-01-01 00:00:00

abstract：:Olefin metathesis has rapidly established itself as an essential tool in the synthetic chemist's armoury. The ease of operation and functional group tolerance that is obtained with the modern generation of catalysts makes the use of metathesis an extremely attractive option when preparing medicinally interesting molec...

journal_title：Current topics in medicinal chemistry

authors： Martin WH,Blechert S

更新日期：2005-01-01 00:00:00

abstract：:The first-ever World Chagas Disease Day, celebrated in April 14, 2020, is a key initiative to raise awareness of the impact of this neglected tropical disease (NTD). This landmark comes along with the first World NTD Day and the new WHO Road Map on NTDs for 2021-2030. ...

journal_title：Current topics in medicinal chemistry

authors： Ferreira LLG,Andricopulo AD

更新日期：2020-01-01 00:00:00

abstract：:Pyrola (Pyrolaceae), also known as Luxiancao/in China, was recorded in Sheng Nong's Herbal Classic listed in top grade. Pyrola herbs were used as medicinal plants for a long history with wide-ranging activities such as nourishing kidney-yang, strengthening muscles and bones, activating blood, stopping bleeding, dispel...

journal_title：Current topics in medicinal chemistry

authors： Yang X,She J,Liu J,Yang T,An G,Chen Q,Fan C,Li S,Liu Q,Qian C,Liu Y,Zhou Y,Zhao J

更新日期：2020-01-01 00:00:00

abstract：:Untargeted metabolomics is a promising approach for reducing the significant attrition rate for discovering and developing drugs in the pharmaceutical industry. This review aims to highlight the practical decision-making value of untargeted metabolomics for the advancement of drug candidates in drug discovery/developm...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Leo GC

更新日期：2017-01-01 00:00:00

abstract：:Since the histamine-3 receptor (H₃R) was cloned in 1999, huge efforts have been made by most of the key players in the pharmaceutical industry as well as in smaller biotech companies to increase the knowledge on this peculiar receptor, with the ultimate goal of bringing new drugs to the market. This review gives a sur...

journal_title：Current topics in medicinal chemistry

authors： Plancher JM

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Biofilm is a critical virulence factor associated with the strains of Candida spp. pathogens as it confers significant resistance to the pathogen against antifungal drugs. METHODS:A systematic review of the literature was undertaken by focusing on natural products, which have been reported to inhibit biofil...

journal_title：Current topics in medicinal chemistry

authors： Singla RK,Dubey AK

更新日期：2019-01-01 00:00:00

abstract：:(18)F-labeled amino acids are an important class of imaging agents for positron emission tomography (PET) that target the increased rates of amino acid transport by many tumor cells. This class of tracers is structurally diverse, and the biological and imaging properties of a given (18)F-labeled amino acid depends lar...

journal_title：Current topics in medicinal chemistry

authors： Huang C,McConathy J

更新日期：2013-01-01 00:00:00

abstract：:Errors in the mitotic process are thought to be one of the principal sources of the genetic instability that hallmarks cancer. Unsurprisingly, many of the proteins that regulate mitosis are aberrantly expressed in tumour cells when compared to their normal counterparts. These may represent a good source of targets for...

journal_title：Current topics in medicinal chemistry

authors： Mortlock AA,Keen NJ,Jung FH,Heron NM,Foote KM,Wilkinson RW,Green S

更新日期：2005-01-01 00:00:00

abstract：:The gradual alignment with all of drug metabolism with all aspects of drug discovery and development has led to a complete realignment of the way the work is conducted. From a background of conducting bespoke in vivo studies much of the work is now in a high throughput screening mode. Large technological advances have...

journal_title：Current topics in medicinal chemistry

authors： Smith DA

更新日期：2011-01-01 00:00:00

abstract：:Integrating physicochemical, drug metabolism, pharmacokinetics, ADME, and toxicity assays into drug discovery in order to reduce the attrition rates in clinical development is reviewed. The review is organized around three main decision points used in discovery including hit generation, lead optimization and final can...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Yan Z,Tang W,Dasgupta M,Hasting B

更新日期：2009-01-01 00:00:00

abstract：:Cardiovascular disease represents an unparalleled proportion of the global burden of disease and will remain the main cause of mortality for the near future. Fortunately, most premature cardiovascular deaths are preventable. Therefore, prevention becomes vital and diet has shown beneficial effects to protect from CVD ...

journal_title：Current topics in medicinal chemistry

authors： Núñez-Córdoba JM,Martínez-González MA

更新日期：2011-01-01 00:00:00

abstract：:Biomarkers in the clinical oncology field can have tremendous therapeutic impact especially if the marker is detected before clinical symptoms. This impact can be extended to the evaluation of clinical oncology treatments allowing evaluation of potential compounds to determine their efficacy in the disease treatment. ...

journal_title：Current topics in medicinal chemistry

authors： Belkowski SM,Polkovitch D,D'Andrea MR

更新日期：2005-01-01 00:00:00

abstract：:Low drug productivity has been a significant problem of the pharmaceutical industry for several decades even though numerous novel technologies were introduced during this period. Currently pharmacologic dogma, "single drug, single target, single disease", is at the root of the lack of drug productivity. From a system...

journal_title：Current topics in medicinal chemistry

authors： Ye H,Wei J,Tang K,Feuers R,Hong H

更新日期：2016-01-01 00:00:00

abstract：:The scaffold protein Axin plays important roles in multiple signaling pathways through mediating the formation of different signaling complexes. Axin is best known for its role as a negative regulator in Wnt/β-catenin pathway. Aberrant activation of the key components in Wnt/β-catenin pathway including Axin has been l...

journal_title：Current topics in medicinal chemistry

authors： Song X,Cai W,Li L

更新日期：2016-01-01 00:00:00

abstract：:In the late 1970s and the early 1980s the initial p38 chemotype, the triaryl imidazoles, was discovered as an off-target effect during the development of cyclooxygenase and 5-lipoxygenase inhibitors long before the identity of the p38 kinase was known. During the last 10 years a number of novel p38 chemotypes were dis...

journal_title：Current topics in medicinal chemistry

authors： Diller DJ,Lin TH,Metzger A

更新日期：2005-01-01 00:00:00

abstract：:The replication cycle of human immunodeficiency virus (HIV) is divided into an early and a late phase. Most of the steps of the cycle have been targeted in antiviral therapy, although the drugs currently available for clinical use are only effective against two replication enzymes of the virus, either against the reve...

journal_title：Current topics in medicinal chemistry

authors： Tözsér J

更新日期：2003-01-01 00:00:00

abstract：:In recent years the development of small organic molecules modulating protein-protein interactions (P-PIs) has drawn major attention in both academic and industrial research. Despite the appreciable progress being made, targeting such extensive interaction areas with comparatively small, drug-like agents has proven to...

journal_title：Current topics in medicinal chemistry

authors： Rechfeld F,Gruber P,Hofmann J,Kirchmair J

更新日期：2011-01-01 00:00:00

abstract：:Artemisinin is isolated from Artemisia annua L. with peroxide-containing sesquiterpene lactone structure. Because of its unique structural characteristics and promising anticancer, antivirus activities, it has recently received increasing attention. The aim of this review is to summarize recent discoveries of artemisi...

journal_title：Current topics in medicinal chemistry

authors： Liu X,Cao J,Huang G,Zhao Q,Shen J

更新日期：2019-01-01 00:00:00