Aporphines and Parkinson's Disease: Medical Tools for the Future.

abstract：:In this review the conformational studies of natural enkephalins (H-Tyr-Gly-Gly-Phe-Met-OH; the [Met(5)]enkephalin and H-Tyr-Gly-Gly-Phe-Leu-OH; the [Leu(5)]enkephalin), their acyclic and cyclic analogues, including those carried out in our laboratory, performed by experimental and theoretical methods and their combin...

journal_title：Current topics in medicinal chemistry

authors： Malicka J,Czaplewski C,Groth M,Wiczk W,Oldziej S,Lankiewicz L,Ciarkowski J,Liwo A

更新日期：2004-01-01 00:00:00

abstract：:Imidazo[1,2-a]pyridine has been shown to be an important biologically active moiety. This review is a compilation of the scattered output of results of the anticancer activities of the imidazo[1,2-a]pyridine system since 2001, which have been classified as inhibition of CDK, VEGFR, PI3K, EGFR, RGGT etc. along with inh...

journal_title：Current topics in medicinal chemistry

authors： Goel R,Luxami V,Paul K

更新日期：2016-01-01 00:00:00

abstract：:The novel peptide hormone ghrelin has recently been recognized as an important co-regulator of growth hormone secretion and energy homeostasis. The significance of ghrelin for obesity and cachexia as well as in the regulation of growth processes is the subject of ongoing basic research as well as clinical studies. It ...

journal_title：Current topics in medicinal chemistry

authors： Horvath TL,Diano S,Tschöp M

更新日期：2003-01-01 00:00:00

abstract：:RNA interference (RNAi) is an attractive phenomenon for practical use that specifically inhibits gene expression and is carried out by small double-stranded RNAs (dsRNAs) including small interfering RNA (siRNA) or short hairpin RNA (shRNA). In addition, RNAi is of great interest for clinical use to cure refractory dis...

journal_title：Current topics in medicinal chemistry

authors： Okuda T,Kawaguchi Y,Okamoto H

更新日期：2009-01-01 00:00:00

abstract：:Implantable medical devices are increasingly important in the practice of modern medicine. Unfortunately, almost all medical devices suffer to a different extent from adverse reactions, including inflammation, fibrosis, thrombosis and infection. To improve the safety and function of many types of medical implants, a m...

journal_title：Current topics in medicinal chemistry

authors： Thevenot P,Hu W,Tang L

更新日期：2008-01-01 00:00:00

abstract：:In general perturbation methods starts with a known exact solution of a problem and add "small" variation terms in order to approach to a solution for a related problem without known exact solution. Perturbation theory has been widely used in almost all areas of science. Bhor's quantum model, Heisenberg's matrix mecha...

journal_title：Current topics in medicinal chemistry

authors： González-Díaz H,Arrasate S,Gómez-SanJuan A,Sotomayor N,Lete E,Besada-Porto L,Ruso JM

更新日期：2013-01-01 00:00:00

abstract：:Several strategies used in the rational design and synthesis of fluorinated compounds as potential therapeutic agents are reviewed. Applications of fluorine substitution in empirical SAR studies for lead development also are discussed, along with the implications with respect to fluorine target interactions that can b...

journal_title：Current topics in medicinal chemistry

authors： Kirk KL

更新日期：2006-01-01 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：:Drug resistance is the major cause of the failure of cancer chemotherapy, so one of the most important features in developing effective cancer therapeutic strategies is to overcome drug resistance. Quinoline moiety has become one of the most privileged structural motifs in anticancer agent discovery since its derivati...

journal_title：Current topics in medicinal chemistry

authors： Li HT,Zhu X

更新日期：2020-06-18 00:00:00

abstract：:The neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) family of hormones exhibit a wide variety of biological actions on the mammalian gastrointestinal tract through known G-protein coupled receptor pathways. At least four receptor subtypes, denoted as Y(1), Y(2), Y(4) an Y(5), each with specific ...

journal_title：Current topics in medicinal chemistry

authors： Vona-Davis LC,McFadden DW

更新日期：2007-01-01 00:00:00

abstract：:A modified version of the CORAL software (http://www.insilico.eu/coral) allows building up the classification model for the case of the Yes/No data on the anti-sarcoma activity of organic compounds. Three random splits into the sub-training, calibration, and test sets of the data for 3017 compounds were examined. The ...

journal_title：Current topics in medicinal chemistry

authors： Toropov AA,Toropova AP,Benfenati E,Gini G,Leszczynska D,Leszczynski J

更新日期：2012-01-01 00:00:00

abstract：:Estrogens control a wide number of aspects of human physiology and play a key role in multiple diseases, including cancer. Estrogens act by binding to and activating the cognate receptor (ER), however numerous studies have revealed that the G protein-coupled receptor named GPR30/GPER mediates also estrogen signals. As...

journal_title：Current topics in medicinal chemistry

authors： Sinicropi MS,Lappano R,Caruso A,Santolla MF,Pisano A,Rosano C,Capasso A,Panno A,Lancelot JC,Rault S,Saturnino C,Maggiolini M

更新日期：2015-01-01 00:00:00

abstract：:Three distinct chemical classes for the control of gastrointestinal nematodes are available: benzimidazoles, imidazothiazoles, and macrocyclic lactones. The relentless development of drug resistance has severely limited the usefulness of such drugs and the search for a new class of compounds preferably with a differ...

journal_title：Current topics in medicinal chemistry

authors： Lee BH,Clothier MF,Dutton FE,Nelson SJ,Johnson SS,Thompson DP,Geary TG,Whaley HD,Haber CL,Marshall VP,Kornis GI,McNally PL,Ciadella JI,Martin DG,Bowman JW,Baker CA,Coscarelli EM,Alexander-Bowman SJ,Davis JP,Zinser E

更新日期：2002-07-01 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：:Leukocytes and lung structural cells contribute to the pathophysiology of asthma through the production of numerous mediators including serine proteases. Such proteases include mast cell tryptase and chymase; neutrophil elastase, cathepsin G and myeloblastin (proteinase 3); bronchial epithelial cell-derived transmembr...

journal_title：Current topics in medicinal chemistry

authors： Guay C,Laviolette M,Tremblay GM

更新日期：2006-01-01 00:00:00

abstract：BACKGROUND:Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer´s disease (AD), diabetes type II, neurologic disorders, and cancer. The inhibition of GSK-3β isoforms is likely to...

journal_title：Current topics in medicinal chemistry

authors： Francisco CS,Javarini CL,de S Barcelos I,Morais PAB,de Paula H,de S Borges W,Neto ÁC,Lacerda V

更新日期：2020-01-01 00:00:00

abstract：:Chronic hepatitis B virus (HBV) infection affects about 400 million people worldwide. The development of nucleoside analogs that inhibit HBV polymerase provides an important approach for treating HBV infection. The approval of lamivudine, adefovir and entecavir represents a cornerstone of hepatitis B therapy. However,...

journal_title：Current topics in medicinal chemistry

authors： Zhou XX,Littler E

更新日期：2006-01-01 00:00:00

abstract：:Inflammation is a complex phenomenon necessary in human defense mechanisms but also involved in the development of some human diseases. The discovery of cyclooxygenase-2 (COX- 2) improved the pharmacology of nonsteroidal anti-inflammatory drugs (NSAID) giving a clear mechanism for prostaglandin regulation in vivo and ...

journal_title：Current topics in medicinal chemistry

authors： Rayar AM,Lagarde N,Ferroud C,Zagury JF,Montes M,Sylla-Iyarreta Veitia M

更新日期：2017-01-01 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：: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：:Aptamers- short nucleic acid or peptide ligands- attracted considerable attention across various disciplines as target specific therapeutic, delivery vehicle and diagnostic tools. The applicability of aptamers - often termed as 'chemical antibodies' - continues to grow and possess certain edge over the antibody counte...

journal_title：Current topics in medicinal chemistry

authors： Veedu RN

更新日期：2015-01-01 00:00:00

abstract：:Urinary protein biomarkers and metabolomic markers have been leveraged to detect acute Drug Induced Kidney Injury (DIKI) in rats; however, the utility of these indicators to enable early detection of DIKI in canine models has not been well documented. Therefore, we evaluated temporal changes in biomarkers and metaboli...

journal_title：Current topics in medicinal chemistry

authors： Wagoner MP,Yang Y,McDuffie JE,Klapczynski M,Buck W,Cheatham L,Eisinger D,Sace F,Lynch KM,Sonee M,Ma JY,Chen Y,Marshall K,Damour M,Stephen L,Dragan YP,Fikes J,Snook S,Kinter LB

更新日期：2017-01-01 00:00:00

abstract：:Schizophrenia (SZ) is a severe neuropsychiatric disorder. A leading hypothesis is that SZ is a brain dysconnection syndrome, involving abnormal interactions between widespread brain networks. Resting state functional magnetic resonance imaging (R-fMRI) is a powerful tool to explore the dysconnectivity of brain network...

journal_title：Current topics in medicinal chemistry

authors： Yu Q,Allen EA,Sui J,Arbabshirani MR,Pearlson G,Calhoun VD

更新日期：2012-01-01 00:00:00

abstract：:Autoimmune diseases are characterized by the production of autoantibodies directed against specific organs of own organism. Additional common traits of autoimmune diseases are chronic inflammation due to generation of inflammatory mediators, and disorders of redox processes. The pathogenesis of autoimmune diseases is ...

journal_title：Current topics in medicinal chemistry

authors： Tomczynska M,Bijak M,Saluk J

更新日期：2016-01-01 00:00:00

abstract：:Cathepsin S has been of increasing interest as a target of medicinal chemistry efforts given its role in modulating antigen-presentation by major histocompatibility class II (MHC II) molecules as well as its involvement in extracellular proteolytic activities. Inhibition of the cathepsin S enzyme reduces degradation o...

journal_title：Current topics in medicinal chemistry

authors： Wiener JJ,Sun S,Thurmond RL

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：AIM:The aim of this study is to synthesize, characterize and biological evaluation of 3-ethyl 5- methyl2-(2-aminoethoxy)-4-(2-chlorophenyl)-1,4-dihydropyridine-3,5-dicarboxylate derivatives. BACKGROUND:An efficient synthesis of two series of novel carbamate and sulfonamide derivatives of amlodipine, 3-ethyl 5-methyl 2...

journal_title：Current topics in medicinal chemistry

authors： Sudhana SM,Adi PJ

更新日期：2019-01-01 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：: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