Connecting small molecules to nuclear receptor pathways.

abstract：:Ascidians (tunicates; sea squirts) are marine animals which provide a source of diverse, bioactive natural products, and a model for toxicity screenings. Compounds isolated from ascidians comprise an approved anti-tumor drug and many others are potent drug leads. Furthermore, the use of invertebrate embryos for toxico...

journal_title：Current topics in medicinal chemistry

authors： Dumollard R,Gazo I,Gomes IDL,Besnardeau L,McDougall A

更新日期：2017-01-01 00:00:00

abstract：:As master regulators of lipid metabolism the peroxisome proliferator activated receptor (PPAR) family controls a wide variety of cellular processes, and thus it is not surprising that a large effort has focussed on discovering agents to pharmacologically modulate activity of these receptors. Early generation PPAR liga...

journal_title：Current topics in medicinal chemistry

authors： Etgen GJ,Mantlo N

更新日期：2003-01-01 00:00:00

abstract：:Phyllanthus amarus is a medicinal herb used in traditional Indian medicine for liver disorders. Several researches also show that it acts primarily in the liver, but the molecules were unidentified for liver protective activity. This study was to determine whether the lignans isolated from P. amarus attenuates the D-g...

journal_title：Current topics in medicinal chemistry

authors： Bawankule DU,Trivedi P,Pal A,Shanker K,Singh M,Sharma P,Khan F,Maurya AK,Verma RK,Gupta MM

更新日期：2014-01-01 00:00:00

abstract：:Natural quinoline alkaloid camptothecin (CPT) is used for the treatment of colon, lung, breast and ovarian cancers still facing challenges due to low solubility in aqueous and biological fluids. Its lactone form easily converts into a toxic carboxylic form at slightly basic pH, typical in blood and tissue fluid has ra...

journal_title：Current topics in medicinal chemistry

authors： Mishra D,Yadav V,Khare P,Jyotshna,Das MR,Meena A,Shanker K

更新日期：2016-01-01 00:00:00

abstract：:Increasing evidence has shown that chemokine receptors may form functional dimers with unique pharmacological profiles. A common practice to characterize such G protein-coupled receptor dimerization processes is to apply bivalent ligands as chemical probes which can interact with both receptors simultaneously. Current...

journal_title：Current topics in medicinal chemistry

authors： Arnatt CK,Zhang Y

更新日期：2014-01-01 00:00:00

abstract：:Nanotechnology is revolutionizing the development of different branches of science. The investigation of nanomaterials in the battle against cancer is not an exception. The main goal of this contribution is to bring an overview about the types of organic and inorganic nanomaterials that are under investigation for its...

journal_title：Current topics in medicinal chemistry

authors： Sanchez-Dominguez CN,Gallardo-Blanco HL,Rodriguez-Rodriguez AA,Vela-Gonzalez AV,Sanchez-Dominguez M

更新日期：2014-03-01 00:00:00

abstract：:There are several significant setbacks including limited bioavailability, high clearance, and further current therapies require higher and frequent dosing to gain desired therapeutic effects. Nanomedicines have been widely investigated for rheumatoid arthritis (RA). Though, higher doses also increase the incidence of ...

journal_title：Current topics in medicinal chemistry

authors： Rahman M,Sharma G,Thakur K,Anwar F,Katare OP,Goni VG,Kumar V,Zamzami MA,Akhter S

更新日期：2017-01-01 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：: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：:The treatment and prevention of atrial fibrillation (AF) remains a significant unmet medical need. Existing therapies that maintain or restore sinus rhythm (rhythm control) have deleterious effects on the ventricle. A major goal for finding new AF therapies is the identification of repolarization mechanisms that are p...

journal_title：Current topics in medicinal chemistry

authors： Bilodeau MT,Trotter BW

更新日期：2009-01-01 00:00:00

abstract：:Recent advances in synthesis of functional poly-ε-caprolactone (PCL) and its self-assembly behavior, as well as application in drug delivery have been reviewed. Three strategies including end group functionalization, postpolymerization modification and new monomer preparation have been summarized to show possibilities...

journal_title：Current topics in medicinal chemistry

authors： Xiao Y,Yuan M,Zhang J,Yan J,Lang M

更新日期：2014-01-01 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：:Autophagy is an important basic metabolic mechanism by engulfing and degrading the unnecessary or dysfunctional cellular components within double-membered autolysosomes to maintain cellular homeostasis. Autophagy has sparkled great interest for its complicated functions in different stages of cancer, and is regarded a...

journal_title：Current topics in medicinal chemistry

authors： Li S,Wang L,Hu Y,Sheng R

更新日期：2015-01-01 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：:Parkinson's disease is a motor dysfunction that has been widely studied but many of the reports on commercial drugs for the treatment of this disease have afforded some undesirable side effects that generate an extensive and unviable treatment by economic costs and due to the bioavailability of the assayed compounds. ...

journal_title：Current topics in medicinal chemistry

authors： Fazel Nabavi S,Uriarte E,Rastrelli L,Modak B,Sobarzo-Sánchez E

更新日期：2016-01-01 00:00:00

abstract：:The Human Genome Project and the explosion of high-throughput data have transformed the areas of molecular and personalized medicine, which are producing a wide range of studies and experimental results and providing new insights for developing medical applications. Research in many interdisciplinary fields is resulti...

journal_title：Current topics in medicinal chemistry

authors： de la Iglesia D,García-Remesal M,de la Calle G,Kulikowski C,Sanz F,Maojo V

更新日期：2013-01-01 00:00:00

abstract：:An intensive research effort during the last 25 years has generated an impressive number of alkaloids isolated from marine ascidians, which remain unique among marine invertebrates in that they overwhelmingly produce this kind of metabolites. The present review is focused on some major groups of ascidians' bioactive a...

journal_title：Current topics in medicinal chemistry

authors： Menna M

更新日期：2014-01-01 00:00:00

abstract：:Aurora kinases are a group of serine/threonine kinases responsible for the regulation of mitosis. In recent years, with the increase in Aurora kinase-related research, the important role of Aurora kinases in tumorigenesis has been gradually recognized. Aurora kinases have been regarded as a new target for cancer thera...

journal_title：Current topics in medicinal chemistry

authors： Qi G,Liu J,Mi S,Tsunematsu T,Jin S,Shao W,Liu T,Ishimaru N,Tang B,Kudo Y

更新日期：2018-01-01 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：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：:The genetics of Alzheimer's disease (AD) implies that restoring non-pathological levels or ratios of different amyloid-beta (Abeta) peptide species in the brain could prevent the onset or delay the progression of this neurodegenerative disease. In particular, a selective reduction of the longer Abeta(1-42) peptide whi...

journal_title：Current topics in medicinal chemistry

authors： Beher D

更新日期：2008-01-01 00:00:00

abstract：:Cells rely on several transition metals to regulate a wide range of metabolic and signaling functions. The diversity and efficiency of their physiological functions are derived from atomic properties that are specific to transition metals, most notably an incomplete inner valence subshell. These properties impart upon...

journal_title：Current topics in medicinal chemistry

authors： Hamai D,Bondy SC,Becaria A,Campbell A

更新日期：2001-12-01 00:00:00

abstract：:The design of syringeable cyclodextrin (CD) gels is a developing area in the drug delivery and tissue engineering fields, since they offer the possibility of being administered with minimally invasive maneuvers to form depots that can remain for prolonged time in the implantation site. Two different supramolecular sys...

journal_title：Current topics in medicinal chemistry

authors： Simões SM,Veiga F,Torres-Labandeira JJ,Ribeiro AC,Concheiro A,Alvarez-Lorenzo C

更新日期：2014-01-01 00:00:00

abstract：:Histone deacetylase (HDAC) inhibitors constitute a novel and growing class of anticancer agents that function by altering intracellular patterns of histone acetylation, the so-called epigenetic "histone code," thereby producing changes in cell cycle arrest, differentiation, and/or apoptosis in tumor cells. This overvi...

journal_title：Current topics in medicinal chemistry

authors： Moradei O,Vaisburg A,Martell RE

更新日期：2008-01-01 00:00:00

abstract：:This article reviews recent molecular dynamics simulations of the Alzheimer's amyloid-β protein, the primary component of the amyloid plaques found in the brain of Alzheimer's patients. Different simulation techniques, and their application to the study of monomeric, oligomeric, and fibrillar species is discussed. Thi...

journal_title：Current topics in medicinal chemistry

authors： Shea JE,Urbanc B

更新日期：2012-01-01 00:00:00

abstract：:The task of rationally designing vaccines that can effectively impact on the survival of cancer patients remains challenging. Monoclonal antibodies and T cell receptors have proven to be viable templates for the application of pharmacophore design principles to develop antigens and immunogens as these immune system mo...

journal_title：Current topics in medicinal chemistry

authors： Pashov A,Perry M,Dyar M,Chow M,Kieber-Emmons T

更新日期：2005-01-01 00:00:00

abstract：:As the first stable tachysterol analogs, 14-epi-19-nortachysterol and its 2-substituted derivatives were synthesized using the Stille coupling reaction between the A-ring precursor (three vinylstannanes) and the CD-ring vinyl trifrate. Among them, the 2-methylidene group was hydrogenated with Wilkinson's catalyst regi...

journal_title：Current topics in medicinal chemistry

authors： Sawada D,Kittaka A

更新日期：2014-01-01 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：INTRODUCTION:Fabaceae are a rich source of protease inhibitors. METHODS:A proteinaceous protease inhibitor of 25 KDa designated as Macrotyloma uniflorum protease inhibitor (MUPI) was isolated from seeds of Macrotyloma uniflorum and purified to homogeneity by ammonium sulphate precipitation, DEAE Sepharose column and C...

journal_title：Current topics in medicinal chemistry

authors： Mohan M,Elyas KK

更新日期：2018-01-01 00:00:00

abstract：:Millions of deaths each year are attributed to malaria worldwide. Transmitted through the bite of an Anopheles mosquito, infection and subsequent death from the Plasmodium species, most notably P. falciparum, can readily spread through a susceptible population. A malaria vaccine does not exist and resistance to virtua...

journal_title：Current topics in medicinal chemistry

authors： Zhang VM,Chavchich M,Waters NC

更新日期：2012-01-01 00:00:00