Biochemical and structural investigations on kynurenine aminotransferase II: an example of conformation-driven species-specific inhibition?

abstract：BACKGROUND:Candida species are the important etiologic agents for candidiasis, the most prevalent cause of opportunistic fungal infections. Candida invasion results in mucosal to systemic infections through immune dysfunction and helps in further invasion and proliferation at several sites in the host. The host defence...

journal_title：Current topics in medicinal chemistry

authors： Wadhwa R,Pandey P,Gupta G,Aggarwal T,Kumar N,Mehta M,Satija S,Gulati M,Madan JR,Dureja H,Balusamy SR,Perumalsamy H,Maurya PK,Collet T,Tambuwala MM,Hansbro PM,Chellappan DK,Dua K

更新日期：2019-01-01 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：:Olefin metathesis has rapidly established itself as an essential tool in the synthetic chemist's armoury. The ease of operation and functional group tolerance that is obtained with the modern generation of catalysts makes the use of metathesis an extremely attractive option when preparing medicinally interesting molec...

journal_title：Current topics in medicinal chemistry

authors： Martin WH,Blechert S

更新日期：2005-01-01 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：: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：:In this review the preclinical medicinal chemistry, biochemistry and clinical results achieved in the treatment of prostatic disease with dutasteride, a dual inhibitor of type 1 and type 2,5alpha-reductase are described. During the discovery phase, dutasteride was optimized to inhibit both forms of human 5 alpha-reduc...

journal_title：Current topics in medicinal chemistry

authors： Frye SV

更新日期：2006-01-01 00:00:00

abstract：:Rhodiola as one of traditional medicines has been used for clinical treatments due to its strong antioxidant properties. Phytochemical analysis revealed the presence of flavonoids, phenylpropanoids, phenylethanol/benzyl alcohol derivatives, cyanogenic glycosides and terpenoids. The bioactive compounds had been demonst...

journal_title：Current topics in medicinal chemistry

authors： Li Y,Wu J,Shi R,Li N,Xu Z,Sun M

更新日期：2017-01-01 00:00:00

abstract：:Prion diseases or transmissible spongiform encephalopathies (TSEs) are fatal neurodegenerative disorders associated with the conformational conversion of the cellular prion protein, PrP(C), into a pathological form known as prion or PrP(Sc). They can be classified into sporadic, inherited and infectious forms. Spontan...

journal_title：Current topics in medicinal chemistry

authors： Biljan I,Ilc G,Giachin G,Legname G,Plavec J

更新日期：2013-01-01 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：:Autophagy is an important basic metabolic mechanism by engulfing and degrading the unnecessary or dysfunctional cellular components within double-membered autolysosomes to maintain cellular homeostasis. Autophagy has sparkled great interest for its complicated functions in different stages of cancer, and is regarded a...

journal_title：Current topics in medicinal chemistry

authors： Li S,Wang L,Hu Y,Sheng R

更新日期：2015-01-01 00:00:00

abstract：:The genetics of Alzheimer's disease (AD) implies that restoring non-pathological levels or ratios of different amyloid-beta (Abeta) peptide species in the brain could prevent the onset or delay the progression of this neurodegenerative disease. In particular, a selective reduction of the longer Abeta(1-42) peptide whi...

journal_title：Current topics in medicinal chemistry

authors： Beher D

更新日期：2008-01-01 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：:An intensive research effort during the last 25 years has generated an impressive number of alkaloids isolated from marine ascidians, which remain unique among marine invertebrates in that they overwhelmingly produce this kind of metabolites. The present review is focused on some major groups of ascidians' bioactive a...

journal_title：Current topics in medicinal chemistry

authors： Menna M

更新日期：2014-01-01 00:00:00

abstract：:A better understanding of the biology and pathogenesis of hematological malignancies has led to the development of immunotherapeutic and immunoregulatory drugs. Many of these agents have revolutionized the current treatment modalities, while others are under investigation. Rituximab (anti-CD20 antibody) has been estab...

journal_title：Current topics in medicinal chemistry

authors： Pangalis GA,Kyrtsonis MC,Vassilakopoulos TP,Dimopoulou MN,Siakantaris MP,Emmanouilides C,Doufexis D,Sahanas S,Kontopidou FN,Kalpadakis C,Angelopoulou MK,Dimitriadou EM,Kokoris SI,Panayiotidis P

更新日期：2006-01-01 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：:The adenosine A(2A) receptor is a member of the G protein-coupled receptor family and mediates multiple physiological effects of adenosine, both at the central nervous system and at peripheral tissues. Increasing evidence relates the A(2A) receptor with several pathological conditions such as neurodegenerative disorde...

journal_title：Current topics in medicinal chemistry

authors： Clementina M,Giuseppe S

更新日期：2010-01-01 00:00:00

abstract：:R115777 (R)-6-amino[(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone is a potent and selective inhibitor of farnesyl protein transferase with significant antitumor effects in vivo subsequent to oral administration in mice. Taking its roots into Janssen's ketoconazole and...

journal_title：Current topics in medicinal chemistry

authors： Venet M,End D,Angibaud P

更新日期：2003-01-01 00:00:00

abstract：:A substantial number of antimicrobial agents target some activity of the bacterial ribosome for inhibition. Mechanistic studies and recent structural investigations of the ribosome have identified the binding sites and presumed mechanism of inhibitory activity for some compounds. A second target for many of these anti...

journal_title：Current topics in medicinal chemistry

authors： Champney WS

更新日期：2003-01-01 00:00:00

abstract：:The treatment and prevention of atrial fibrillation (AF) remains a significant unmet medical need. Existing therapies that maintain or restore sinus rhythm (rhythm control) have deleterious effects on the ventricle. A major goal for finding new AF therapies is the identification of repolarization mechanisms that are p...

journal_title：Current topics in medicinal chemistry

authors： Bilodeau MT,Trotter BW

更新日期：2009-01-01 00:00:00

abstract：:Tanshinones are a class of bioactive compounds present in the Chinese herbal medicine Danshen (Salvia miltiorrhiza Bunge), containing among others, abietane diterpene quinone scaffolds. Chemical synthesis and biological activity studies of natural and unnatural tanshinone derivatives have been reviewed in this article...

journal_title：Current topics in medicinal chemistry

authors： Huang H,Song C,Chang J

更新日期：2020-01-01 00:00:00

abstract：AIMS:The need to find new antimicrobial agents to cope with this phenomenon increases. BACKGROUND:Infection diseases are illness caused by different microorganisms, such as bacteria, among those caused by resistant bacteria are associated with greater morbidity, mortality and cost of the treatment than those caused by...

journal_title：Current topics in medicinal chemistry

authors： Nocedo-Mena D,Garza-González E,González-Ferrara M,Del Rayo Camacho-Corona M

更新日期：2020-01-01 00:00:00

abstract：:This review highlights the biological importance of many polysubstituted nitro-prolines and -pyrrolidines. Their preparation using asymmetric 1,3-dipolar cycloadditions of azomethine ylides with nitroalkenes using diastereoselective and enantioselective strategies is described remarking the scope and main features of ...

journal_title：Current topics in medicinal chemistry

authors： Nejera C,Sansano JM

更新日期：2014-01-01 00:00:00

abstract：:In recent years the development of small organic molecules modulating protein-protein interactions (P-PIs) has drawn major attention in both academic and industrial research. Despite the appreciable progress being made, targeting such extensive interaction areas with comparatively small, drug-like agents has proven to...

journal_title：Current topics in medicinal chemistry

authors： Rechfeld F,Gruber P,Hofmann J,Kirchmair J

更新日期：2011-01-01 00:00:00

abstract：:Firefly shows bioluminescence by "luciferin-luciferase" (L-L) reaction using luciferin, luciferase, ATP and O2. The chemical photon generation by an enzymatic reaction is widely utilized for analytical methods including biological imaging in the life science fields. To expand photondetecting analyses with firefly biol...

journal_title：Current topics in medicinal chemistry

authors： Hirano T

更新日期：2016-01-01 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：:The human tuberculosis (TB) is primarily caused by Mycobacterium tuberculosis (Mtb) that inhabits inside and amidst immune cells of the host with adapted physiology to regulate interdependent cellular functions with intact pathogenic potential. The complexity of this disease is attributed to various factors such as th...

journal_title：Current topics in medicinal chemistry

authors： Borah P,Deb PK,Venugopala KN,Al-Shar'i NA,Singh V,Deka S,Srivastava A,Tiwari V,Mailavaram RP

更新日期：2020-12-11 00:00:00

abstract：:Computational toxicity modeling can have significant impact in the drug discovery process, especially when utilized as a sentinel filter for common drug safety liabilities, such as mutagenicity, carcinogenicity and teratogenicity. This review will focus on the strengths and limitations of the current computational mod...

journal_title：Current topics in medicinal chemistry

authors： Pearl GM,Livingston-Carr S,Durham SK

更新日期：2001-09-01 00:00:00

abstract：:The first proteolytic step in the processing of amyloid precursor protein (APP) to amyloid-beta (Abeta) in the brain is performed by beta-site APP cleaving enzyme (BACE1). This enzyme is a membrane bound aspartic protease with high homology of the catalytic domain to renin and pepsin and of yet unknown physiologic fun...

journal_title：Current topics in medicinal chemistry

authors： Roggo S

更新日期：2002-04-01 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：:Nicotinic acid adenine dinucleotide phosphate (NAADP) is the most potent Ca²⁺ mobilizing endogenous compound known to date. Although its Ca²⁺ releasing activity has been demonstrated in many cell types and in response to different extracellular stimuli, several aspects of NAADP signaling are unclear. This overview foc...

journal_title：Current topics in medicinal chemistry

authors： Guse AH,Ernst IM,Fliegert R

更新日期：2013-01-01 00:00:00