Achievements in Cancer Research and its Therapeutics in Hundred Years.

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 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：:Glucuronidation has been recognized as an important clearance mechanism in humans. Therefore, knowledge about the contribution of glucuronidation to clearance of drug candidates is of great value in early drug development. In this article, we discuss the recent progress made to predict in vivo glucuronidation paramete...

journal_title：Current topics in medicinal chemistry

authors： Wu B,Dong D,Hu M,Zhang S

更新日期：2013-01-01 00:00:00

abstract：:Release of somatostatin into the circulation from the activated TRPV1-expressing nociceptors revealed by antidromic stimulation of dorsal roots in the rat pinpointed to a novel potential drug target on these nociceptors. The review summarizes the functional, biochemical and pharmacological evidence for a novel somatos...

journal_title：Current topics in medicinal chemistry

authors： Szolcsányi J,Pintér E,Helyes Z,Petho G

更新日期：2011-01-01 00:00:00

abstract：:Modulation of the androgen receptor has the potential to be an effective treatment for hypogonadism, andropause, and associated conditions such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and sexual dysfunction. Side effects associated with classical anabolic steroid treatments have driven the quest for...

journal_title：Current topics in medicinal chemistry

authors： Cadilla R,Turnbull P

更新日期：2006-01-01 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：:Trichomoniasis, one of the most common non-viral sexually transmitted infections worldwide, is caused by the parasite Trichomonas vaginalis. The pathogen colonizes the human urogenital tract, and the infection is associated with complications such as adverse pregnancy outcomes, cervical cancer, and an increase in HIV ...

journal_title：Current topics in medicinal chemistry

authors： Ferla M,Tasca T

更新日期：2021-01-01 00:00:00

abstract：:Structure-activity relationships of a 4-aminoquinoline MCH-1R antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4- and 6-positions of the original HTS hit. Improvements to the original screening lead were made by addition of lipophilic groups at the 2-position and biphenyl, cyc...

journal_title：Current topics in medicinal chemistry

authors： DeVita RJ

更新日期：2007-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Yu Y

更新日期：2019-01-01 00:00:00

abstract：:Kynurenic acid (KYNA), one of the metabolites belonging to the kynurenine pathway, has been described as an important neuroprotective compound, its unbalancing being associated with several pathological conditions. In human brain, the majority of KYNA production is sustained by kynurenine aminotransferase II (KAT II)....

journal_title：Current topics in medicinal chemistry

authors： Casazza V,Rossi F,Rizzi M

更新日期：2011-01-01 00:00:00

abstract：:The replication cycle of human immunodeficiency virus (HIV) is divided into an early and a late phase. Most of the steps of the cycle have been targeted in antiviral therapy, although the drugs currently available for clinical use are only effective against two replication enzymes of the virus, either against the reve...

journal_title：Current topics in medicinal chemistry

authors： Tözsér J

更新日期：2003-01-01 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：: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

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：:Over the last decade, a number of computational methods have been developed, which attempt to evaluate the thermodynamic properties of individual water molecules at the solute-solvent interface, in order to assess contributions to protein-ligand binding. In some cases, these tools tell us what we already know, e.g. th...

journal_title：Current topics in medicinal chemistry

authors： Graves AP,Wall ID,Edge CM,Woolven JM,Cui G,Le Gall A,Hong X,Raha K,Manas ES

更新日期：2017-01-01 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：INTRODUCTION:Anxiety disorders manifest in women more than in men by almost twofold. This narrative review aims to summarize the sex-related biological factors, which underpin anxiety, focusing on the interactions of sex and tryptophan/serotonin with anxiety. METHODS:A literature search was conducted using Google Scho...

journal_title：Current topics in medicinal chemistry

authors： Songtachalert T,Roomruangwong C,Carvalho AF,Bourin M,Maes M

更新日期：2018-01-01 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：:In recent years, relationship between free radicals and oxidative stress with aging, cancer, atherosclerosis, neurodegenerative disorders, diabetes, and inflammatory diseases became increasingly clear. Confirming the role of oxidants in numerous pathological conditions such as cancer, the antioxidants developed as the...

journal_title：Current topics in medicinal chemistry

authors： Karaaslan C,Suzen S

更新日期：2015-01-01 00:00:00

abstract：:Artemisinin is isolated from Artemisia annua L. with peroxide-containing sesquiterpene lactone structure. Because of its unique structural characteristics and promising anticancer, antivirus activities, it has recently received increasing attention. The aim of this review is to summarize recent discoveries of artemisi...

journal_title：Current topics in medicinal chemistry

authors： Liu X,Cao J,Huang G,Zhao Q,Shen J

更新日期：2019-01-01 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：:Seizures are one of the most common neurological disorders in clinical medicine. Triggering mechanisms by which seizures form remain unclear, but are related to a rapid change in ionic composition, including an increase of intracellular potassium concentration and pH shifts within the brain. pH buffering of extra- and...

journal_title：Current topics in medicinal chemistry

authors： Thiry A,Dogné JM,Supuran CT,Masereel B

更新日期：2007-01-01 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：: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：:This is a general review of currently available antimalarial drugs, these compounds are gathered according with its chemical structure and the biological targets. A great number of these new antimalarial agents are now moving actively in the pipeline from basic science to clinical studies. ...

journal_title：Current topics in medicinal chemistry

authors： Domínguez JN

更新日期：2002-11-01 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：:Bacterial infections constitute an always growing health problem worldwide. The resistance to antibiotics of an increasing number of bacterial pathogens necessitates a permanent search for new molecules with different mechanisms of action. Histidine biosynthesis is an ancient pathway found in bacteria, archaebacteria,...

journal_title：Current topics in medicinal chemistry

authors： Monti SM,De Simone G,D'Ambrosio K

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Neuraminidase inhibitors (NAIs) are the only class of antivirals in clinical use against influenza virus approved worldwide. However, approximately 1-3% of circulating strains present resistance mutations to oseltamivir (OST), the most used NAI. Therefore, it is important to catalogue new molecules to inhibi...

journal_title：Current topics in medicinal chemistry

authors： de Freitas CS,Rocha MEN,Sacramento CQ,Marttorelli A,Ferreira AC,Rocha N,de Oliveira AC,de Oliveira Gomes AM,Dos Santos PS,da Silva EO,da Costa JP,de Lima Moreira D,Bozza PT,Silva JL,Barroso SPC,Souza TML

更新日期：2020-01-01 00:00:00

abstract：:This review describes the role of nuclear receptors in the regulation of genes involved in cholesterol transport and synthetic modulators of these receptors. Increasing the efflux of cholesterol from peripheral cells, such as lipid-laden macrophages, through a process called reverse cholesterol transport (RCT) require...

journal_title：Current topics in medicinal chemistry

authors： Pelton PD,Patel M,Demarest KT

更新日期：2005-01-01 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