Chemistry of tumour targeted T1 based MRI contrast agents.

abstract：:Dementia is an increasing health problem in older aged populations worldwide. Age-related changes in the brain can be observed decades before the first symptoms of cognitive decline appear. Cognitive impairment has chronic inflammatory components, which can be enhanced by systemic immune activation. There exist mutual...

journal_title：Current topics in medicinal chemistry

authors： Leblhuber F,Steiner K,Geisler S,Fuchs D,Gostner JM

更新日期：2020-01-01 00:00:00

abstract：:The recognition that malfunction of the microtubule (MT) associated protein tau is likely to play a defining role in the onset and/or progression of a number of neurodegenerative diseases, including Alzheimer's disease, has resulted in the initiation of drug discovery programs that target this protein. Tau is an endog...

journal_title：Current topics in medicinal chemistry

authors： Ballatore C,Brunden KR,Trojanowski JQ,Lee VM,Smith AB 3rd,Huryn DM

更新日期：2011-01-01 00:00:00

abstract：:This review covers recent progress in the discovery of selective glucocorticoid receptor (GR) antagonists. Potential therapeutic applications of selective GR antagonists are described including the pharmacological rationale and, in some cases, clinical evidence that underlies these proposed uses. Disease areas that ar...

journal_title：Current topics in medicinal chemistry

authors： Clark RD

更新日期：2008-01-01 00:00:00

abstract：:The connection of microbial biosynthetic gene clusters to the small molecule metabolites they encode is central to the discovery and characterization of new metabolic pathways with ecological and pharmacological potential. With increasing microbial genome sequence information being deposited into publicly available da...

journal_title：Current topics in medicinal chemistry

authors： Trautman EP,Crawford JM

更新日期：2016-01-01 00:00:00

abstract：:Organic nitrates, such as nitroglycerin, have been used in clinical practice for more than one century for the treatment of angina, even before the identification of Nitric Oxide (NO) as the so-called Endothelium Derived Relaxing Factor (EDRF). Recently, multiple functions of this molecule in biology and pathophysiolo...

journal_title：Current topics in medicinal chemistry

authors： Bolla M,Almirante N,Benedini F

更新日期：2005-01-01 00:00:00

abstract：:Computational toxicity modeling can have significant impact in the drug discovery process, especially when utilized as a sentinel filter for common drug safety liabilities, such as mutagenicity, carcinogenicity and teratogenicity. This review will focus on the strengths and limitations of the current computational mod...

journal_title：Current topics in medicinal chemistry

authors： Pearl GM,Livingston-Carr S,Durham SK

更新日期：2001-09-01 00:00:00

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：:Liver cancer is the fifth (6.3% of all cancers i.e., 548,000 cases/year) and ninth (2.8% of all cancers i.e., 244,000 cases/year) most prevalent cancer worldwide in men and women, respectively. Although multiple choices of therapies are offered for Hepatocellular Carcinoma (HCC) like liver resection or transplant, rad...

journal_title：Current topics in medicinal chemistry

authors： Kumar S,Fayaz F,Pottoo FH,Bajaj S,Manchanda S,Bansal H

更新日期：2020-01-01 00:00:00

abstract：:Human multidrug resistance protein (MRP/ABCC) family contains 9 members (MRP1-9) which transport a structurally diverse array of anticancer and antimicrobial drugs and several important endogenous substances including prostaglandins (PGs) and leukotrienes (LTs) with different substrate specificity. MRP1-5 can collecti...

journal_title：Current topics in medicinal chemistry

authors： Yang AK,Zhou ZW,Wei MQ,Liu JP,Zhou SF

更新日期：2010-01-01 00:00:00

abstract：:The structure-activity relationships of azetidine-based DPP IV inhibitors will be discussed in detail in the following review. The azetidine-based DPP IV inhibitors can be divided into three main subtypes, the 2-cyanoazetidines, 3-fluoroazetidines and 2-ketoazetidines. These subtypes have been explored and structure-a...

journal_title：Current topics in medicinal chemistry

authors： Ferraris D,Belyakov S,Li W,Oliver E,Ko YS,Calvin D,Lautar S,Thomas B,Rojas C

更新日期：2007-01-01 00:00:00

abstract：:Glycopeptide antibiotics are complex natural products biosynthesized by several actinomycete genera. They inhibit bacterial growth by interfering with cell wall biosynthesis. Glycopeptide antibiotics consist of a heptapeptide skeleton highly modified through cross-links of the aromatic moieties. In addition, they are ...

journal_title：Current topics in medicinal chemistry

authors： Donadio S,Sosio M

更新日期：2008-01-01 00:00:00

abstract：:The dopamine transporter (DAT) is a target for the development of pharmacotherapies for a number of central disorders including Parkinson's disease, Alzheimer's disease, schizophrenia, Tourette's syndrome, Lesch-Nyhan disease, attention deficit hyperactivity disorder (ADHD), obesity, depression, and stimulant abuse as...

journal_title：Current topics in medicinal chemistry

authors： Runyon SP,Carroll FI

更新日期：2006-01-01 00:00:00

abstract：:One year after its first outbreak reported in China, coronavirus disease 2019 (COVID-19) pandemic is still sweeping the World causing serious infections and claiming more fatalities. COVID-19 is caused by the novel corona virus SARS-CoV-2, which belongs to the genus Betacoronavirus (β-CoVs) which is of greatest clinic...

journal_title：Current topics in medicinal chemistry

authors： Sabbah DA,Hajjo R,Bardaweel SK,Zhong HA

更新日期：2021-01-18 00:00:00

abstract：:In 2010, the National Institutes of Health (NIH) established the Therapeutics for Rare and Neglected Diseases (TRND) program within the National Center for Advancing Translational Sciences (NCATS), which was created to stimulate drug discovery and development for rare and neglected tropical diseases through a collabor...

journal_title：Current topics in medicinal chemistry

authors： Ottinger EA,Kao ML,Carrillo-Carrasco N,Yanjanin N,Shankar RK,Janssen M,Brewster M,Scott I,Xu X,Cradock J,Terse P,Dehdashti SJ,Marugan J,Zheng W,Portilla L,Hubbs A,Pavan WJ,Heiss J,Vite CH,Walkley SU,Ory DS,Silbe

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：:Pyridine and pyridine-fused ring systems are ubiquitous in medicinal research and demonstrate such diverse pharmacological benefits as anticonvulsant therapies, treatment for fungal and bacterial infections as well as chemotherapy agents. For example, imidazo[1,2-a]pyridines have exhibited a broad range of activity as...

journal_title：Current topics in medicinal chemistry

authors： Kishbaugh TL

更新日期：2016-01-01 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：:Histone deacetylases (HDACs) have recently emerged as key elements in epigenetic control of gene expression. Due to the implication of HDACs in a variety of diseases ranging from cancer to neurodegenerative disorder, HDAC inhibitors have received increased attention in recent years. Over the last few decades, a myriad...

journal_title：Current topics in medicinal chemistry

authors： Kim B,Hong J

更新日期：2015-01-01 00:00:00

abstract：:A proper balance between oxidants and antioxidants is necessary in maintaining health and longevity. Alterations in this balance may result in oxidative stress causing functional disorders and diseases. Oxidative stress is considered to play a vital role in the pathogenesis of diabetes and its complications. Flavanone...

journal_title：Current topics in medicinal chemistry

authors： Sharma M,Akhtar N,Sambhav K,Shete G,Bansal AK,Sharma SS

更新日期：2015-01-01 00:00:00

abstract：:In this paper we applied the "macromolecular docking" procedure to perform molecular modeling with the aim of screening transcription factor sequences for possible interaction to the HIV-1 TAR-RNA, employing the software Hex version 4.2. The molecular modeling data were compared with electrophoretic mobility shift ass...

journal_title：Current topics in medicinal chemistry

authors： Khan MT,Mischiati C,Ather A,Ohyama T,Dedachi K,Borgatti M,Kurita N,Gambari R

更新日期：2012-01-01 00:00:00

abstract：:The IkappaB kinases (IKKs) are essential components of the signaling pathway by which the NF-kappaB p50/RelA transcription factor is activated in response to pro-inflammatory stimuli such as lipopolysaccharide (LPS) and tumor necrosis factor (TNFalpha). NF-kappaB signaling results in the expression of numerous genes i...

journal_title：Current topics in medicinal chemistry

authors： Bamborough P,Callahan JF,Christopher JA,Kerns JK,Liddle J,Miller DD,Morse MA,Rumsey WL,Williamson R

更新日期：2009-01-01 00:00:00

abstract：:A major strategy used in drug design is the inhibition of enzyme activity. The ability to accurately measure the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half is extremely important in ranking compounds. Since the concept of the half maximal inhibitory c...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Yan Z,Lang W,Masucci JA

更新日期：2012-01-01 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：:This review mainly covers last five year literature on CCK1R agonists and antagonists. These CCK1R ligands have been found following the two usual and complementary strategies for drug discovery: rational design based on structure activity relationships on the CCK-7 and CCK-4 peptide sequences of the endogenous ligand...

journal_title：Current topics in medicinal chemistry

authors： García-López MT,González-Muñiz R,Martín-Martínez M,Herranz R

更新日期：2007-01-01 00:00:00

abstract：:There are currently (July, 2002) six protease inhibitors approved for the treatment of HIV infection, each of which can be classified as peptidomimetic in structure. These agents, when used in combination with other antiretroviral agents, produce a sustained decrease in viral load, often to levels below the limits of ...

journal_title：Current topics in medicinal chemistry

authors： Randolph JT,DeGoey DA

更新日期：2004-01-01 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：:Gene therapy has a strong potential in neuroscience by suppressing or replacing abnormalities in genetic materials. The employment of nano-gene carrier for neurological disorders is comparatively young and restricted since the aim to effectively deliver therapeutic agents into the central nervous system (CNS) commonly...

journal_title：Current topics in medicinal chemistry

authors： Khanh TMT,Wei D,Tran PHL,Tran TTD

更新日期：2017-01-01 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：:Four compounds (isoquercitrin, myricetin-3-O-glucoside, catechin and gallocatechin) were isolated from lyophilized aqueous extract of Schizolobium parahyba leaves by chromatography on Sephadex LH-20, followed by semipreparative HPLC using a C-18 column, and identified by 1H and 13C NMR. The compounds were then, tested...

journal_title：Current topics in medicinal chemistry

authors： F Vale LH,Mendes MM,Fernandes RS,Costa TR,S Hage-Melim LI,A Sousa M,Hamaguchi A,Homsi-Brandeburgo MI,Franca SC,Silva CH,Pereira PS,Soares AM,Rodrigues VM

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Chemoinformatics has several applications in the field of drug design, helping to identify new compounds against a range of ailments. Among these are Leishmaniasis, effective treatments for which are currently limited. OBJECTIVE:To construct new indole 2-aminothiophene molecules using computational tools an...

journal_title：Current topics in medicinal chemistry

authors： Félix MB,de Araújo RSA,Barros RPC,de Simone CA,Rodrigues RRL,de Lima Nunes TA,da Franca Rodrigues KA,Junior FJBM,Muratov E,Scotti L,Scotti MT

更新日期：2020-01-01 00:00:00