Protective mechanism of lignans from Phyllanthus amarus against galactosamine/ lipopolysaccharide-induced hepatitis: an in-vivo and in-silico studies.

abstract：:One of the major events occurring at biological interfaces is the specific recognition of bioactive ligands by their receptor proteins. The elucidation of interacting partners is an immediate entrance into the discovery of medicinal leads. The method of photoaffinity labeling enables the direct probing of target prote...

journal_title：Current topics in medicinal chemistry

authors： Hatanaka Y,Sadakane Y

更新日期：2002-03-01 00:00:00

abstract：:Protein kinases (Ser/Thr and Tyr) play a key role in signal transduction pathways. It has been shown that deregulation of the Cdk activity is linked to cell proliferation and cancer. Inhibition of cyclin-dependent kinases (Cdks) is an important target for potential new anti-cancer drugs. Following the discovery of Olo...

journal_title：Current topics in medicinal chemistry

authors： Haesslein JL,Jullian N

更新日期：2002-09-01 00:00:00

abstract：:Psychiatric diagnosis has long been perceived as more of an art than a science since its foundations lie within the observation, and the self-report of the patients themselves and objective diagnostic biomarkers are lacking. Furthermore, the diagnostic tools in use not only stray away from the conventional medical fra...

journal_title：Current topics in medicinal chemistry

authors： Todeva-Radneva A,Paunova R,Kandilarova S,St Stoyanov D

更新日期：2020-01-01 00:00:00

abstract：:Cancer research has progressed leaps and bounds over the years. This review is a brief overview of the cancer research, milestone achievements and therapeutic studies on it over the one hundred ten years which would give us an insight into how far we have come to understand and combat this fatal disease leading to mil...

journal_title：Current topics in medicinal chemistry

authors： Shastri S,Chatterjee B,Thakur SS

更新日期：2019-01-01 00:00:00

abstract：:Our understanding of glutamatergic transmission in the central nervous system has been greatly expanded with the discovery and investigation of the metabotropic glutamate receptor family. Complementing the ionotropic glutamate-gated ion channels, these G-protein coupled receptors play critical roles in neuronal and gl...

journal_title：Current topics in medicinal chemistry

authors： Niswender CM,Jones CK,Conn PJ

更新日期：2005-01-01 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：:The chemical versatility of the indole nucleus still inspires the pharmaceutical research to develop innovative suitable indole based drugs. The present work is an overview of the use and application of indole molecule based derivatives, as possible treatment in the main Oxidative Stress related diseases, such as card...

journal_title：Current topics in medicinal chemistry

authors： Aiello F,Valacchi G

更新日期：2014-01-01 00:00:00

abstract：:Research over the years has gradually and sequentially highlighted contributory role of hypothalamic- based kisspeptin-signaling axis as a major positive modulator of the neuroendocrinological reproductive axis in mammals. However, a series of landmark studies provided convincing evidence of role of this signaling in ...

journal_title：Current topics in medicinal chemistry

authors： Jabeen S,Qureshi MZ,Javed Z,Iqbal MJ,Ismail M,Farooqi AA

更新日期：2016-01-01 00:00:00

abstract：:Antiplatelets represent a diverse group of agents that share the ability to reduce platelet activity through a variety of mechanisms. Antithrombotic agents are effective in the secondary prevention of ischemic strokes. Most strokes are caused by a sudden blockage of an artery in the brain (called an ischaemic stroke) ...

journal_title：Current topics in medicinal chemistry

authors： Pinto A,Di Raimondo D,Tuttolomondo A,Di Sciacca R,Arnao V,La Placa S,Milio G,Miceli S,Licata G

更新日期：2009-01-01 00:00:00

abstract：:This chapter describes the life cycle, general morphology and ultrastructure of the larval and adult stages of Taenia solium, a parasitic flatworm of humans found in underdeveloped countries. Experimental results describing the role of proteins and glycoproteins in the host-parasite relationship, as well as the variou...

journal_title：Current topics in medicinal chemistry

authors： Willms K

更新日期：2008-01-01 00:00:00

abstract：:There are several significant setbacks including limited bioavailability, high clearance, and further current therapies require higher and frequent dosing to gain desired therapeutic effects. Nanomedicines have been widely investigated for rheumatoid arthritis (RA). Though, higher doses also increase the incidence of ...

journal_title：Current topics in medicinal chemistry

authors： Rahman M,Sharma G,Thakur K,Anwar F,Katare OP,Goni VG,Kumar V,Zamzami MA,Akhter S

更新日期：2017-01-01 00:00:00

abstract：:The design of syringeable cyclodextrin (CD) gels is a developing area in the drug delivery and tissue engineering fields, since they offer the possibility of being administered with minimally invasive maneuvers to form depots that can remain for prolonged time in the implantation site. Two different supramolecular sys...

journal_title：Current topics in medicinal chemistry

authors： Simões SM,Veiga F,Torres-Labandeira JJ,Ribeiro AC,Concheiro A,Alvarez-Lorenzo C

更新日期：2014-01-01 00:00:00

abstract：:Hepatitis C virus (HCV) is a major cause of acute hepatitis and chronic liver disease, including cirrhosis and hepatocellular carcinoma (HCC). No vaccine is currently available to prevent hepatitis C, and the current standard of care (SOC) - pegylated interferon-α (PEG-IFN-α) in combination with ribavirin (RBV) - is o...

journal_title：Current topics in medicinal chemistry

authors： Avolio S,Summa V

更新日期：2010-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Scotti MT,Muratov EN,González-Díaz H

更新日期：2019-01-01 00:00:00

abstract：:Two general aspects which need to be considered for the successful application of dendrimers for biomedical purposes are their availability at an acceptable cost and their suitability as regards their pharmacodynamic and pharmacokinetic properties. These two aspects are covered in this review. In the first part, synth...

journal_title：Current topics in medicinal chemistry

authors： Villalonga-Barber C,Micha-Screttas M,Steele BR,Georgopoulos A,Demetzos C

更新日期：2008-01-01 00:00:00

abstract：:Among the many important physiological functions of the activated vitamin D receptor (VDR) is the signaling of monocytic differentiation, first demonstrated by conversion of malignant myeloid leukemia cells to nonproliferating cells with mature monocyte/macrophage appearance. However, the understanding of how 1, 25-di...

journal_title：Current topics in medicinal chemistry

authors： Studzinski GP,Garay E,Patel R,Zhang J,Wang X

更新日期：2006-01-01 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

abstract：:For effective tumour imaging by magnetic resonance imaging (MRI) there is a clear need to develop organ, tissue and cell specific contrast agents that can selectively bind to tumour biomarkers. The versatility of a range of bioconjugation techniques and facile coupling chemistries has facilitated the synthesis of MRI ...

journal_title：Current topics in medicinal chemistry

authors： Kamaly N,Miller AD,Bell JD

更新日期：2010-01-01 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：BACKGROUND:The high sequence and structural homology among the hsp90 paralogs - Hsp90α, Hsp90β, Grp94, and Trap-1 - has made the development of paralog-specific inhibitors a challenging proposition. OBJECTIVE:This review surveys the state of developments in structural analysis, compound screening, and structure-based ...

journal_title：Current topics in medicinal chemistry

authors： Gewirth DT

更新日期：2016-01-01 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：:The first-ever World Chagas Disease Day, celebrated in April 14, 2020, is a key initiative to raise awareness of the impact of this neglected tropical disease (NTD). This landmark comes along with the first World NTD Day and the new WHO Road Map on NTDs for 2021-2030. ...

journal_title：Current topics in medicinal chemistry

authors： Ferreira LLG,Andricopulo AD

更新日期：2020-01-01 00:00:00

abstract：:Penile erection is a complex physiologic event resulting from the interactions of the nervous system on a highly specialized vascular organ. Activation of central nervous system melanocortinergic (MC) receptors with either endogenous or synthetic melanotropic ligands may initiate and/or facilitate spontaneous penile e...

journal_title：Current topics in medicinal chemistry

authors： King SH,Mayorov AV,Balse-Srinivasan P,Hruby VJ,Vanderah TW,Wessells H

更新日期：2007-01-01 00:00:00

abstract：:The vesicular acetylcholine transporter (VAChT) is a glycoprotein responsible for the accumulation of acetylcholine into pre-synaptic vesicules of cholinergic neurons. Cholinergic innervation has been shown to be decreased at the earlier stages of Alzheimer's disease (AD). Thus, the expression of VAChT has been correl...

journal_title：Current topics in medicinal chemistry

authors： Giboureau N,Som IM,Boucher-Arnold A,Guilloteau D,Kassiou M

更新日期：2010-01-01 00:00:00

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：:Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are hydrolytic enzymes which degrade the endogenous cannabinoids (endocannabinoids) N-arachidonoylethanolamine (anandamide, AEA) and 2-arachidonoylglycerol (2-AG), respectively. Endocannabinoids are an important class of lipid messenger molecules that ar...

journal_title：Current topics in medicinal chemistry

authors： Minkkilä A,Saario S,Nevalainen T

更新日期：2010-01-01 00:00:00

abstract：:There exists a huge attrition rate of molecules in clinical trials. It was expected that high-throughput screening and combinatorial chemistry would make the task of producing drugs easier. However, the efforts of the past decade have not been an unvarnished success. As a result, a lot of experimental and computationa...

journal_title：Current topics in medicinal chemistry

authors： Ajay

更新日期：2002-12-01 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：: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 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