Progress towards the development of anti-inflammatory inhibitors of IKKbeta.

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：:This review discusses the state of the art, challenges and perspectives in recent applications of electrochemistry in the life sciences. It deals mainly with the elucidation of molecular mechanisms of drug action, drug design and development, involving electron transfer, pharmaco-electrochemistry (the combination of e...

journal_title：Current topics in medicinal chemistry

authors： de Paiva YG,da Rocha Ferreira F,Silva TL,Labbe E,Buriez O,Amatore C,Fonseca Goulart MO

更新日期：2015-01-01 00:00:00

abstract：:In the last decade, we have been developing some gold(III) derivatives showing interesting antitumor properties and reduced systemic and renal toxicity, compared to the clinically-established reference drug cisplatin. Starting from the rationale at the base of our investigations, this review has been divided into two ...

journal_title：Current topics in medicinal chemistry

authors： Nardon C,Fregona D

更新日期：2016-01-01 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：:Ropivacaine, the S-(-)-enantiomer of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinecarboxamide is a new long-acting local anesthetic. This review demonstrates that it is effective in brachial plexus anesthesia. It is at least as efficient as bupivacaine in terms of quality, duration of analgesia, anesthesia, and motor b...

journal_title：Current topics in medicinal chemistry

authors： Singelyn FJ

更新日期：2001-08-01 00:00:00

abstract：:Efflux pumps of the Resistance Nodulation Division (RND) superfamily play a major role in the intrinsic and acquired resistance of Gram-negative pathogens to antibiotics. Moreover, they are largely responsible for multi-drug resistance (MDR) phenomena in these bacteria. The last decade has seen a sharp increase in the...

journal_title：Current topics in medicinal chemistry

authors： Ruggerone P,Murakami S,Pos KM,Vargiu AV

更新日期：2013-01-01 00:00:00

abstract：:Many efforts are currently being made to connect small molecules to target proteins by extracting pharmacological data from bibliographic sources and storing them in annotated chemical libraries. Here, small molecules are further connected to biological pathways, with particular focus to pathways involving members of ...

journal_title：Current topics in medicinal chemistry

authors： Hettne K,Cases M,Boyer S,Mestres J

更新日期：2007-01-01 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 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：:Over the past decades, a tremendous rise in invasive fungal infection diseases attributed to the yeast Candida albicans in immunocompromised individuals poses a seriously challenging issue. Another concern is the emergence of multi-drug resistant pathogens to the existing medicines due to their overuse and misuse. It ...

journal_title：Current topics in medicinal chemistry

authors： Tratrat C

更新日期：2020-01-01 00:00:00

abstract：:Cancer is a multifactorial disease including interactions of complex genetic and environmental factors. Clinical efficacy of anticancer chemotherapies is hampered by various factors including multidrug resistance (MDR). There is a strong need to discover more potent novel cancer drugs to kill cancer cells selectively....

journal_title：Current topics in medicinal chemistry

authors： Kucuksayan E,Ozben T

更新日期：2017-01-01 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：:Alzheimer's disease (AD) is a multifactorial complex disease. The pathogenesis of AD is very complicated, and involves the β-amyloid (Aβ) cascade, tau hyperphosphorylation, neuroinflammation, oxidative stress, mitochondrial dysfunction, reduced levels of neurotrophic factors, and damage and loss of synapses as well as...

journal_title：Current topics in medicinal chemistry

authors： Li L,Zhang L,Yang CC

更新日期：2016-01-01 00:00:00

abstract：:The ryanodine receptor (RyR) is the major calcium (Ca(2+)) release channel in the sarcoplasmic reticulum (SR) of skeletal and cardiac muscle and is required for excitation-contraction (EC) coupling. The 565 kDa RyR protein forms a tetrameric channel that is part of a macromolecular signaling complex that also includes...

journal_title：Current topics in medicinal chemistry

authors： Lehnart SE,Huang F,Marx SO,Marks AR

更新日期：2003-01-01 00:00:00

abstract：:Thiosemicarbazones (TSCNs) constitute a broad family of compounds (R1R2C=N-NH-C(S)- NR3R4), particularly attractive because many of them display some biological activity against a wide range of microorganisms and cancer cells. Their activity can be related to their electronic and structural properties, which offer a r...

journal_title：Current topics in medicinal chemistry

authors： Matesanz AI,Herrero JM,Quiroga AG

更新日期：2021-01-01 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：:Malaria, caused by protozoa of the genus Plasmodium, remains one of the most dreadful infectious diseases worldwide killing more than 1 million people per year. The emergence of multidrug-resistant parasites highly demands a steadfast and continuous search not only for new targets but also for new anti-infectives addr...

journal_title：Current topics in medicinal chemistry

authors： Wegscheid-Gerlach C,Gerber HD,Diederich WE

更新日期：2010-01-01 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：:Transition metal complexes with terpyridine ligands have attracted a widespread interest with respect to biomedical applications: [(tpy)PtCl]Cl and [(tpy)RuCl(3)] are potent anti-tumor agents with activities comparable to those of cisplatin and carboplatin. The Ru(II) complexes feature a high potential as reactive pro...

journal_title：Current topics in medicinal chemistry

authors： Winter A,Gottschaldt M,Newkome GR,Schubert US

更新日期：2012-01-01 00:00:00

abstract：:Dipeptidyl peptidase-IV (DPP-IV) (EC 3.4.14.5) is а member of the broad class of hydrolytic enzymes which is responsible for degradation of the incretin peptide hormones regulating blood glucose levels. In this article we review the literature on natural and synthetic DPP-IV inhibitors, focusing their chemical structu...

journal_title：Current topics in medicinal chemistry

authors： Smelcerovic A,Miljkovic F,Kolarevic A,Lazarevic J,Djordjevic A,Kocic G,Anderluh M

更新日期：2015-01-01 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：:HIV-1 integrase (IN) plays an important role in the life cycle of HIV and is responsible for integration of the virus into the human genome. We present computational approaches used to design novel HIV-1 IN inhibitors. We created an IN inhibitor database by collecting experimental data from the literature. We develope...

journal_title：Current topics in medicinal chemistry

authors： Guasch L,Zakharov AV,Tarasova OA,Poroikov VV,Liao C,Nicklaus MC

更新日期：2016-01-01 00:00:00

abstract：:L-DOPA is a di-hydroxy-phenyl, catecholamine precursor, amino acid, initially considered as an inert compound and now the key stone for the treatment of Parkinson's disease (PD) and some hereditary dystonias. L-DOPA, when administered to mammals, is rapidly metabolized to dopamine and 3-OM-DOPA, and its half-life in p...

journal_title：Current topics in medicinal chemistry

authors： Mena MA,Casarejos MJ,Solano RM,de Yébenes JG

更新日期：2009-01-01 00:00:00

abstract：:Over activation of the NMDA receptor complex has been implicated in a number of neurological conditions. The use of NMDA antagonists as therapeutic agents has been limited by serious cognitive and motor side effects. Significant efforts have been reported in the development of NR2B subtype-selective antagonists, which...

journal_title：Current topics in medicinal chemistry

authors： Layton ME,Kelly MJ 3rd,Rodzinak KJ

更新日期：2006-01-01 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：BACKGROUND:Nowadays, malaria is still one of the most important and lethal diseases worldwide, causing 445,000 deaths in a year. Due to the actual treatment resistance, there is an emergency to find new drugs. OBJECTIVE:The aim of this work was to find potential inhibitors of phosphoglycerate mutase 1 from P. falcipar...

journal_title：Current topics in medicinal chemistry

authors： Ríos-Soto L,Avitia-Domínguez C,Sierra-Campos E,Valdez-Solana M,Cisneros-Martínez J,Palacio-Gastellum MG,Téllez-Valencia A

更新日期：2018-01-01 00:00:00

abstract：:Neural activity utilizes energy resources and requires replenishment of metabolites through vascular dilation. During wake, cortical neurons usually have depolarized membrane potentials and exhibit frequent spontaneous action potentials, requiring an increased metabolic delivery to activated tissue and causing blood v...

journal_title：Current topics in medicinal chemistry

authors： Schei JL,Rector DM

更新日期：2011-01-01 00:00:00

abstract：AIMS:A series of 8-methoxy ciprofloxacin- hydrazone/acylhydrazone hybrids were evaluated for their activity against a panel of cancer cell lines including HepG2 liver cancer cells, MCF-7, doxorubicin- resistant MCF-7 (MCF-7/DOX) breast cancer cells, DU-145 and multidrug-resistant DU145 (MDR DU-145) prostate cancer cell...

journal_title：Current topics in medicinal chemistry

authors： Wang LP,Xu Z,Deng GY,Xu SL

更新日期：2020-01-01 00:00:00

abstract：:Multi-drug resistant bacteria are appearing at an alarming rate and impose significant burdens on healthcare systems worldwide. Cationic peptides have shown great promise as broad spectrum antimicrobial agents with a demonstrated ability to kill resistant bacteria, however, issues such as protease susceptibility and t...

journal_title：Current topics in medicinal chemistry

authors： Hadley EB,Hancock RE

更新日期：2010-01-01 00:00:00

abstract：:Homologation is a concept introduced by Gerhard in 1853 to describe a homologous series in organic chemistry. Since then, the concept has been adapted and used in medicinal chemistry as one of the most important strategies for molecular modification. The homologation types, their influence on physico-chemical properti...

journal_title：Current topics in medicinal chemistry

authors： Lima LM,Alves MA,do Amaral DN

更新日期：2019-01-01 00:00:00