Abstract：
:The increase of pathogens being resistant to antibiotics represents a global health problem and therefore it is a pressing need to develop antibiotics with novel mechanisms of action. Host defense peptides, which have direct antimicrobial activity (also termed antimicrobial peptides) or immune modulating activity, are valuable template structures for the development of such compounds. Antimicrobial peptides exhibit remarkably different structures as well as biological activity profiles with multiple targets. A large fraction of these peptides interfere physically with the cell membrane of bacteria (focus of this review), but can also translocate into the cytosol, where they interact with nucleic acids, ribosomes and proteins. Several potential interaction sites have to be considered on the route of the peptides from the environment to the cytoplasmic membrane. Translocation of peptides through the cell wall may not be impaired by the thick but relatively porous peptidoglycan layer. However, interaction with lipopolysaccharides of the outer membrane of Gram-negative bacteria and (lipo)teichoic acids of Gram-positive bacteria may reduce the effective concentration at the cytoplasmic membrane, where supposedly the killing event takes place. On a molecular level several mechanisms are discussed, which are important for the rational design of improved antimicrobial compounds: toroidal pore formation, carpet model (coverage of membrane surface by peptides), interfacial activity, void formation, clustering of lipids and effects of membrane curvature. In summary, many of these models just represent special cases that can be interrelated to each other and depend on both the nature of lipids and peptides.
journal_name
Curr Top Med Chemjournal_title
Current topics in medicinal chemistryauthors
Lohner Ksubject
Has Abstractpub_date
2017-01-01 00:00:00pages
508-519issue
5eissn
1568-0266issn
1873-4294pii
CTMC-EPUB-77046journal_volume
17pub_type
杂志文章,评审abstract：:A major strategy used in drug design is the inhibition of enzyme activity. The ability to accurately measure the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half is extremely important in ranking compounds. Since the concept of the half maximal inhibitory c...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802612800672844
更新日期：2012-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026619666190122144217
更新日期：2019-01-01 00:00:00
abstract：:Cyclic peptide scaffolds are key components of signal transduction pathways in both prokaryotic and eukaryotic organisms since they act as chemical messengers that activate or inhibit specific cognate receptors. In prokaryotic organisms these peptides are utilized in non-essential pathways, such as quorum sensing, tha...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026618666180518090705
更新日期：2018-01-01 00:00:00
abstract：:The IkappaB kinases (IKKs) are essential components of the signaling pathway by which the NF-kappaB p50/RelA transcription factor is activated in response to pro-inflammatory stimuli such as lipopolysaccharide (LPS) and tumor necrosis factor (TNFalpha). NF-kappaB signaling results in the expression of numerous genes i...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802609789007336
更新日期：2009-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026613666131213155813
更新日期：2014-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026614666141203142926
更新日期：2014-01-01 00:00:00
abstract：:The pharmacophore modeling in modern drug research has been applied for both bioactivity profiling and early stage of risk assessment of potential side effects and toxicity due to interactions of drug candidates with antitargets namely P-glycoprotein, hERG, cytochrome P450 and pregnane X-receptor. In this article, an ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026611313090004
更新日期：2013-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026043387520
更新日期：2004-01-01 00:00:00
abstract：:The connection of microbial biosynthetic gene clusters to the small molecule metabolites they encode is central to the discovery and characterization of new metabolic pathways with ecological and pharmacological potential. With increasing microbial genome sequence information being deposited into publicly available da...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026616666151012111046
更新日期：2016-01-01 00:00:00
abstract：:This review reports the recent advances in chlorotoxin (CTX)-targeted nanoparticles (NPs) for imaging and therapy of glioma. CTX has been identified as a targeting ligand to specifically bind to glioma. Through different conjugation approaches, CTX can be conjugated onto iron oxide NPs, quantum dots, and rare-earth up...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026615666150330110822
更新日期：2015-01-01 00:00:00
abstract：:Notwithstanding the functional role that the aggregates of some amyloidogenic proteins can play in different organisms, protein aggregation plays a pivotal role in the pathogenesis of a large number of human diseases. One of such diseases is Alzheimer's disease (AD), where the overproduction and aggregation of the β-a...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/15680266113139990139
更新日期：2013-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/156802611795589610
更新日期：2011-01-01 00:00:00
abstract：:Lipoic acid (LA) is an antioxidant able to produce its effects in aqueous or lipophilic environments. Lipoate is the conjugate base of lipoic acid, and the most prevalent form of LA under physiological conditions. It presents a highly negative reduction potential, increases the expression of antioxidant enzymes and pa...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026615666150114161358
更新日期：2015-01-01 00:00:00
abstract：:Ischemic heart disease and cerebrovascular disease are the leading causes of death in the world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due to our improved understanding of the underlying pathology of these diseases, and a number of technological advances in tools for drug di...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026013395380
更新日期：2001-06-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026023392986
更新日期：2002-11-01 00:00:00
abstract：:For successful drug discovery it is important to understand the fundamentals of the underlying causes and consequences of the diseases for which the drug is being developed. One such physiological process in eukaryotic cells is protein phosphorylation, which is the main post-translational modification of proteins resp...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026617666170531113233
更新日期：2017-01-01 00:00:00
abstract：:Metabolic syndrome (MS) is a modern medical condition characterized by central obesity, hyperglycaemia, hypercholesterolemia and hypertension. The beneficial effects of mushrooms in lowering the symptoms of MS were known from both traditional and conventional medicine. Edible mushrooms, their extracts, polysaccharide ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/15680266113136660196
更新日期：2013-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/156802607780487623
更新日期：2007-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026033392570
更新日期：2003-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/156802611797470349
更新日期：2011-01-01 00:00:00
abstract：:Autoimmune diseases are characterized by the production of autoantibodies directed against specific organs of own organism. Additional common traits of autoimmune diseases are chronic inflammation due to generation of inflammatory mediators, and disorders of redox processes. The pathogenesis of autoimmune diseases is ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026616666160216152324
更新日期：2016-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026616666160927155515
更新日期：2017-01-01 00:00:00
abstract：:Ipilimumab, a fully human monoclonal antibody that binds to CTLA-4 (cytotoxic T lymphocyte-associated antigen 4), is the new hope in the treatment of patients with advanced melanoma. Anti-CTLA-4 antibodies enhance T cell responses in vitro and in vivo and activate proliferation of tumour-specific T cells. The blockade...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802612798919231
更新日期：2012-01-01 00:00:00
abstract：:Non-selective NSAIDs enhance the risk of serious ulcer complications (bleeding, perforation, obstruction), hospitalization and death about 3-10-fold. The gastrointestinal side effects of NSAIDs have a considerable economical burden, since they are responsible for 5-10 billion dollars in hospitalization charges and los...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026054201703
更新日期：2005-01-01 00:00:00
abstract：:Traditionally the role of sexual steroid hormones was focused primarily on reproductive organs: the breast, female reproductive tract (uterus, mammary gland, and ovary), and male reproductive tract (testes, epididymis and prostate), however our current understanding of tissue-specific effects of sex steroids has eluci...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802611796117540
更新日期：2011-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026618666181029144653
更新日期：2018-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026054750254
更新日期：2005-01-01 00:00:00
abstract：:Cells rely on several transition metals to regulate a wide range of metabolic and signaling functions. The diversity and efficiency of their physiological functions are derived from atomic properties that are specific to transition metals, most notably an incomplete inner valence subshell. These properties impart upon...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026013394796
更新日期：2001-12-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026617666170707130032
更新日期：2017-01-01 00:00:00
abstract：:In general perturbation methods starts with a known exact solution of a problem and add "small" variation terms in order to approach to a solution for a related problem without known exact solution. Perturbation theory has been widely used in almost all areas of science. Bhor's quantum model, Heisenberg's matrix mecha...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026611313140011
更新日期：2013-01-01 00:00:00
