Dipeptide inhibitors of thermolysin and angiotensin I-converting enzyme.

abstract：BACKGROUND:Zika is a worldwide pandemic dreadful viral transmission through Aedes mosquito vector. It significantly causes fever, joint pain or rash, and conjunctivitis. Pregnant mothers suffering from Zika viral infection may have fetal abnormalities due to severe neurological problems, characterized by microcephaly a...

journal_title：Current topics in medicinal chemistry

authors： Nandi S,Kaur R,Kumar M,Sharma A,Naaz A,Mandal SC

更新日期：2018-01-01 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：:Cytochrome P450 17A1 (CYP17A1; also P450c17and P450sccII) is a critically important enzyme in humans that catalyzes the formation of all endogenous androgens. It is an atypical cytochrome P450 enzyme in that it catalyzes two distinct types of substrate oxidation. Through its hydroxylase activity, it catalyzes the 17α-...

journal_title：Current topics in medicinal chemistry

authors： Porubek D

更新日期：2013-01-01 00:00:00

abstract：:Results of various projects on Mexican Indian ethnobotany and some of the subsequent pharmacological and phytochemical studies are summarised focusing both on chemical-pharmacological as well as anthropological (ethnopharmacological) aspects of our research. We have identified taste and smell properties of medicinal (...

journal_title：Current topics in medicinal chemistry

authors： Heinrich M

更新日期：2003-01-01 00:00:00

abstract：:Asthma, a chronic inflammatory disease of the airways, is a significant burden on our healthcare system. There is high unmet need for treatments directed towards the underlying causes of the disease. The cell surface integrin VLA-4 (very late antigen-4; alpha4beta1; CD49d/CD29) plays an important role in the trafficki...

journal_title：Current topics in medicinal chemistry

authors： Singh J,Adams S,Carter MB,Cuervo H,Lee WC,Lobb RR,Pepinsky RB,Petter R,Scott D

更新日期：2004-01-01 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

abstract：:Low drug productivity has been a significant problem of the pharmaceutical industry for several decades even though numerous novel technologies were introduced during this period. Currently pharmacologic dogma, "single drug, single target, single disease", is at the root of the lack of drug productivity. From a system...

journal_title：Current topics in medicinal chemistry

authors： Ye H,Wei J,Tang K,Feuers R,Hong H

更新日期：2016-01-01 00:00:00

abstract：:Pharmacokinetic limitations affect drug bioavailability determining the loss or the reduction of the pharmacological effects. The Gastro Intestinal tract (GI) and the Blood Brain Barrier (BBB) are the most important restrictive and selective physiological lines of defense of the organism. Although several parameters s...

journal_title：Current topics in medicinal chemistry

authors： Colabufo NA,Berardi F,Contino M,Niso M,Perrone R

更新日期：2009-01-01 00:00:00

abstract：:The dynamics of gene expression are regulated by histone acetylases (HATs) and histone deacetylases (HDACs) that control the acetylation state of lysine side chains of the histone proteins of chromatin. The catalytic activity of these two enzymes remodels chromatin to control gene expression without altering gene sequ...

journal_title：Current topics in medicinal chemistry

authors： Wiech NL,Fisher JF,Helquist P,Wiest O

更新日期：2009-01-01 00:00:00

abstract：:Choline kinase (CK) is a homodimeric enzyme that catalyses the transfer of the ATP γ-phosphate to choline, generating phosphocholine and ADP in the presence of magnesium. Several isoforms of CK are present in humans but only the HsCKα has been associated with cancer and validated as a drug target to treat this disease...

journal_title：Current topics in medicinal chemistry

authors： Serran-Aguilera L,Nuti R,López-Cara LC,Ríos-Marco P,Carrasco MP,Marco C,Entrena A,Macchiarulo A,Hurtado-Guerrero R

更新日期：2014-01-01 00:00:00

abstract：:Although bioactivation is a well-documented process and the role of active metabolites in the drug discovery field has long been recognized, drug metabolites are usually ignored in virtual screening campaigns oriented to drug repositioning. The present article discusses different issues related to overlooking of the a...

journal_title：Current topics in medicinal chemistry

authors： Talevi A

更新日期：2016-01-01 00:00:00

abstract：:Safety and biocompatibility assessment of biomaterials are themes of constant concern as advanced materials enter the market as well as products manufactured by new techniques emerge. Within this context, this review provides an up-to-date approach on current methods for the characterization and safety assessment of b...

journal_title：Current topics in medicinal chemistry

authors： Oliveira JPR,Melendez-Ortiz HI,Bucio E,Alves PT,Lima MIS,Goulart LR,Mathor MB,Varca GHC,Lugao AB

更新日期：2018-01-01 00:00:00

abstract：AIMS:Computational modelling may help us to detect the more important factors governing this process in order to optimize it. BACKGROUND:The generation of hazardous organic waste in teaching and research laboratories poses a big problem that universities have to manage. METHODS:In this work, we report on the experime...

journal_title：Current topics in medicinal chemistry

authors： Montes-Bageneta I,Akesolo U,López S,Merino M,Anakabe E,Arrasate S

更新日期：2020-01-01 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：:PLA2 enzyme catalyses the hydrolysis of cellular phospholipids at the sn-2 position to liberate arachidonic acid and lysophospholipid to generate a family of pro-inflammatory eicosanoids and platelet activating factor. The generation of pro-inflammatory eicosanoids involves a series of free radical intermediates with ...

journal_title：Current topics in medicinal chemistry

authors： Nanda BL,Nataraju A,Rajesh R,Rangappa KS,Shekar MA,Vishwanath BS

更新日期：2007-01-01 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：: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：: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：: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：: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：:An evaluation of existing and proposed Fe chelators, both synthetic and natural products, for the treatment of Fe-overload disease must address a number of issues. There are fundamental parameters that determine the efficacy of a drug: absorption, distribution, metabolism, clearance and toxicity. However, the administ...

journal_title：Current topics in medicinal chemistry

authors： Sharpe PC,Richardson DR,Kalinowski DS,Bernhardt PV

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：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：:Apoptosis is a vital physiological process, which is observed in various biological events. The anti-apoptotic and pro-apoptotic members of Bcl-2 family are the most characterized proteins which are involved in the regulation of apoptotic cell death. The anti-apoptotic proteins such as Bcl-2 and Bcl-xL prevent apoptos...

journal_title：Current topics in medicinal chemistry

authors： Salam AAA,Nayek U,Sunil D

更新日期：2018-01-01 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：: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：: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：: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：: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：BACKGROUND:Chemoinformatics has several applications in the field of drug design, helping to identify new compounds against a range of ailments. Among these are Leishmaniasis, effective treatments for which are currently limited. OBJECTIVE:To construct new indole 2-aminothiophene molecules using computational tools an...

journal_title：Current topics in medicinal chemistry

authors： Félix MB,de Araújo RSA,Barros RPC,de Simone CA,Rodrigues RRL,de Lima Nunes TA,da Franca Rodrigues KA,Junior FJBM,Muratov E,Scotti L,Scotti MT

更新日期：2020-01-01 00:00:00