G Protein Coupled Receptors And Structure-Based Advances.

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：:The emergence of new DNA sequencing technologies has allowed an exponential growth of genomic and transcriptomic data that ultimately yielded important results to several areas such as medicine and biology. This continuous technological progress presents several advantages and caveats that have to be considered for ea...

journal_title：Current topics in medicinal chemistry

authors： Sanchez-Flores A,Abreu-Goodger C

更新日期：2014-01-01 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：:Non-selective NSAIDs enhance the risk of serious ulcer complications (bleeding, perforation, obstruction), hospitalization and death about 3-10-fold. The gastrointestinal side effects of NSAIDs have a considerable economical burden, since they are responsible for 5-10 billion dollars in hospitalization charges and los...

journal_title：Current topics in medicinal chemistry

authors： Lehmann FS,Beglinger C

更新日期：2005-01-01 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：:Much attention has focused on the development of protein kinases as drug targets to treat a variety of human diseases including diabetes, cancer, hypertension and arthritis. To date, Gleevec is one example of a drug targeting protein that has successfully treated human cancer. Several other protein kinase inhibitors a...

journal_title：Current topics in medicinal chemistry

authors： Haystead TA

更新日期：2006-01-01 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：: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：:Parkinson's disease (PD) is one of the most prevalent and severe neurodegenerative disease affecting more than 6.1 million people globally. It is characterized by age-related progressive deterioration of neurological functions caused by neuronal damage or neuronal death. During PD, the dopamineproducing cells in the s...

journal_title：Current topics in medicinal chemistry

authors： Kumar B,Pandey M,Fayaz F,Izneid TA,Pottoo FH,Manchanda S,Sharma A,Sahoo PK

更新日期：2020-01-01 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：:The introduction of biochemical biomarkers in the evaluation of patients with cardiovascular disease has led to practice-changing advancements in the way these patients are diagnosed and managed. Measurements of cardiac troponins or brain-type natriuretic peptide (BNP) and its precursor, N-terminal brain-type natriure...

journal_title：Current topics in medicinal chemistry

authors： Giannopoulos G,Deftereos S,Panagopoulou V,Kossyvakis C,Kaoukis A,Bouras G,Pyrgakis V,Cleman MW

更新日期：2013-01-01 00:00:00

abstract：:The development of computational tools for the prediction of passive transport is reviewed with particular reference to four diverse approaches: the rule-of-5, polar surface area, Volsurf and Abraham's General Solvation Equation. To illustrate the current state of the art, several examples of the application of in sil...

journal_title：Current topics in medicinal chemistry

authors： Clark DE,Grootenhuis PD

更新日期：2003-01-01 00:00:00

abstract：:Emergence of drug-resistant viral strains is one of the major milestones and the main cause for the failure of antiretroviral therapy. Combination of different anti-HIV agents has become the standard clinical practice to keep the viral load at low or even undetectable levels and to prevent emergence of virus-drug resi...

journal_title：Current topics in medicinal chemistry

authors： Camarasa MJ,San-Félix A,Velázquez S,Pérez-Pérez MJ,Gago F,Balzarini J

更新日期：2004-01-01 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：:A series of novel derivatives of 1,3-oxazolidin-2-one 12a-12n has been synthesized starting from 4-nitro-(L)- phenylalanine by involving five-step reaction sequence. All the compounds were screened for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacill...

journal_title：Current topics in medicinal chemistry

authors： Chandna N,Kapoor JK,Goyal V,Aggarwal NK,Kumari KM,Vijjulatha M

更新日期：2013-08-01 00:00:00

abstract：:Cancer cells alter their metabolism to support the uninterrupted supply of biosynthetic molecules required for continuous proliferation. Glucose metabolism is frequently reprogrammed in several tumors in addition to fatty acid, amino acid and glutamine metabolism. Pyruvate Dehydrogenase Kinase (PDK) is a gatekeeper en...

journal_title：Current topics in medicinal chemistry

authors： Sradhanjali S,Reddy MM

更新日期：2018-01-01 00:00:00

abstract：:The tyrosinase enzyme (EC 1.14.18.1) is an oxidoreductase inside the general enzyme classification and is involved in the oxidation and reduction process in the epidermis. These chemical reactions that the enzyme catalyzes are of principal importance in the melanogenesis process. This process of melanogenesis is relat...

journal_title：Current topics in medicinal chemistry

authors： Casanola-Martin GM,Le-Thi-Thu H,Marrero-Ponce Y,Castillo-Garit JA,Torrens F,Rescigno A,Abad C,Khan MT

更新日期：2014-01-01 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：:Protein-RNA interactions play crucial roles in numerous biological processes. However, detecting the interactions and binding sites between protein and RNA by traditional experiments is still time consuming and labor costing. Thus, it is of importance to develop bioinformatics methods for predicting protein-RNA intera...

journal_title：Current topics in medicinal chemistry

authors： Liu ZP,Chen L

更新日期：2016-01-01 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：: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 neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally α-amino acids with one or more stereogenic centers due to st...

journal_title：Current topics in medicinal chemistry

authors： Vogensen SB,Greenwood JR,Bunch L,Clausen RP

更新日期：2011-01-01 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：:Twenty-five years ago the first small molecule inhibitors of Hsp90 were identified. In the intervening years there has been dramatic progress in basic scientific understanding of the Hsp90 chaperone machinery and in the role of Hsp90 in malignancy. The first-in-class Hsp90 inhibitor 17-AAG entered into Phase I clinica...

journal_title：Current topics in medicinal chemistry

authors： Kim YS,Alarcon SV,Lee S,Lee MJ,Giaccone G,Neckers L,Trepel JB

更新日期：2009-01-01 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：:The conventional way of characterizing a disease consists of correlating clinical symptoms with pathological findings. Although this approach for many years has assisted clinicians in establishing syndromic patterns for pathophenotypes, it has major limitations as it does not consider preclinical disease states and is...

journal_title：Current topics in medicinal chemistry

authors： Rai S,Raj U,Varadwaj PK

更新日期：2018-01-01 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：:Telomeres are structurally nucleoprotein complexes at termini of linear chromosomes and essential to chromosome stability/integrity. In normal human cells, telomere length erodes progressively with each round of cell divisions, which serves as an important barrier to uncontrolled proliferation and malignant transforma...

journal_title：Current topics in medicinal chemistry

authors： Yuan X,Dai M,Xu D

更新日期：2020-01-01 00:00:00

abstract：:Melatonin was found to be a potent free radical scavenger in 1993. Since then over 800 publications have directly or indirectly confirmed this observation. Melatonin scavenges a variety of reactive oxygen and nitrogen species including hydroxyl radical, hydrogen peroxide, singlet oxygen, nitric oxide and peroxynitrite...

journal_title：Current topics in medicinal chemistry

authors： Tan DX,Reiter RJ,Manchester LC,Yan MT,El-Sawi M,Sainz RM,Mayo JC,Kohen R,Allegra M,Hardeland R

更新日期：2002-02-01 00:00:00

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