Managing the liabilities arising from structural alerts: a safe philosophy for medicinal chemists.

abstract：:First described by Alois Alzheimer in 1907, Alzheimer's disease (AD) is the most common dementia type, affecting approximately 20 million people worldwide. As the population is getting older, AD is a growing health problem. AD is currently treated by symptomatic drugs, the acetylcholinesterase inhibitors, based on the...

journal_title：Current medicinal chemistry

authors： Francotte P,Graindorge E,Boverie S,de Tullio P,Pirotte B

更新日期：2004-07-01 00:00:00

abstract：:Nowadays, the use of synthetic carriers as biochemical reagents and immunogens is entering a new phase. The multimeric nature of these constructs, the unambiguous composition and the ease, reliability and versatility of their production, make this type of carriers well-suited to various biotechnological and biochemica...

journal_title：Current medicinal chemistry

authors： Alexopoulos Ch,Sakarellos-Daitsiotis M,Sakarellos C

更新日期：2005-01-01 00:00:00

abstract：:Fibroblast growth factor receptor-4 (FGFR4) is a tyrosine kinase with a range of important physiological functions. However, it is also frequently mutated in various cancers and is now generating significant interest as a potential therapeutic target. Unfortunately, biochemical characterization of its role in disease,...

journal_title：Current medicinal chemistry

authors： Ho HK,Németh G,Ng YR,Pang E,Szántai-Kis C,Zsákai L,Breza N,Greff Z,Horváth Z,Pató J,Szabadkai I,Szokol B,Baska F,Őrfî L,Ullrich A,Kéri G,Chua BT

更新日期：2013-01-01 00:00:00

abstract：:Hydrogen sulfide (H2S), previously known only as a toxic agent, in the last decades has been recognized as an important endogenous gasotransmitter, playing a key role in the homeostasis of the cardiovascular system. In the last years, the growing evidence about a protective role exhibited by H2S against myocardial isc...

journal_title：Current medicinal chemistry

authors： Citi V,Piragine E,Testai L,Breschi MC,Calderone V,Martelli A

更新日期：2018-01-01 00:00:00

abstract：:Nature as a source of inspiration has been shown to have a great beneficial impact on the development of new computational methodologies. In this scenario, analyses of the interactions between a protein target and a ligand can be simulated by biologically inspired algorithms (BIAs). These algorithms mimic biological s...

journal_title：Current medicinal chemistry

authors： Heberlé G,de Azevedo WF Jr

更新日期：2011-01-01 00:00:00

abstract：:Poly(aminoester) dendrimers are expected to hold great promise as biodegradable nanocarriers for drug delivery due to their advantageous properties allowing their biodegradability, potentially lower toxicity and possibility of diverse chemical conjugations. The synthetic strategies for constructing such dendrimers inc...

journal_title：Current medicinal chemistry

authors： Wang Y,Quelever G,Peng L

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:Fungi play an important role in terrestrial ecosystems interacting positively or negatively with plants. These interactions are complex and the outcomes are different depending on the fungal lifestyles, saprotrophic, mutualistic or pathogenic. Furthermore, fungi are well known for producing secondary metabol...

journal_title：Current medicinal chemistry

authors： Masi M,Maddau L,Linaldeddu BT,Scanu B,Evidente A,Cimmino A

更新日期：2018-01-01 00:00:00

abstract：:Natural products from symbiotic or commensal associations between marine invertebrate and microbial organisms show exceptional promise as pharmaceuticals in many therapeutic areas. An economic and sustainable global market supply due to difficulty of synthesis is cited as the main obstacle for exploitation of these ot...

journal_title：Current medicinal chemistry

authors： Dunlap WC,Jaspars M,Hranueli D,Battershill CN,Perić-Concha N,Zucko J,Wright SH,Long PF

更新日期：2006-01-01 00:00:00

abstract：:The maximum therapeutic potentials of pharmacologically active molecules are generally not attained due to their non specific delivery. Ligands associated with drug or delivery system through which it is delivered provide navigation and direction to the carrier system(s) so as to reach and release bioactive(s) at the ...

journal_title：Current medicinal chemistry

authors： Rai S,Paliwal R,Vaidya B,Gupta PN,Mahor S,Khatri K,Goyal AK,Rawat A,Vyas SP

更新日期：2007-01-01 00:00:00

abstract：:Two-component signal transduction systems and their expanded variants known as phosphorelays are integral elements of the virulence and antimicrobial resistance responses of a wide range of pathogenic bacteria and fungi and also regulate essential functions. As a consequence, two-component systems and phosphorelays ar...

journal_title：Current medicinal chemistry

authors： Stephenson K,Hoch JA

更新日期：2004-03-01 00:00:00

abstract：:Differentiation therapy of acute promyelocytic leukemia with all-trans retinoic acid represents the most successful pharmacological therapy of acute myeloid leukemia (AML). Numerous studies demonstrate that drugs that inhibit mechanistic target of rapamycin (mTOR) and activate AMP-kinase (AMPK) have beneficial effects...

journal_title：Current medicinal chemistry

authors： Visnjic D,Dembitz V,Lalic H

更新日期：2019-01-01 00:00:00

abstract：:Staphylococcus aureus is a notorious pathogenic bacterium causing a wide range of diseases from soft-tissue contamination, to more serious and deep-seated infections. This species is highlighted by its ability to express several kinds of virulence factors and to acquire genes related to drug resistance. Target this nu...

journal_title：Current medicinal chemistry

authors： Diniz RC,Soares LW,Nascimento da Silva LC

更新日期：2018-01-01 00:00:00

abstract：:Sarcomas are tumours of mesenchymal origin, which can arise in bone or soft tissues. They are rare but frequently quite aggressive and with a poor outcome. New approaches are needed to characterise these tumours and their resistance mechanisms to current therapies, responsible for tumour recurrence and treatment failu...

journal_title：Current medicinal chemistry

authors： Heredia-Soto V,Redondo A,Kreilinger JJP,Martínez-Marín V,Berjón A,Mendiola M

更新日期：2020-01-01 00:00:00

abstract：:Reprogramming technologies have been developed to revert somatic differentiated cells into pluripotent stem cells that can be differentiated into different lineages potentially useful in stem cell therapy. Reprogramming methods have been progressively refined to increase their efficiency, to obtain a cell population s...

journal_title：Current medicinal chemistry

authors： Tafani M,Perrone GA,Pucci B,Russo A,Bizzarri M,Mechanick JI,Carpi A,Russo MA

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Numerous studies have demonstrated that halogenated agents elicit myocardial conditioning effects when adminis-tered perioperatively in cardiac surgery. Recent evidence has been published of the benefits of maintaining exposure to halogenated agents during the early postoperative period. The enzymatic mechan...

journal_title：Current medicinal chemistry

authors： Guerrero Orriach JL,Escalona Belmonte JJ,Ramirez Aliaga M,Ramirez Fernandez A,Rodriguez Capitan MJ,Quesada Muñoz G,Raigón Ponferrada A,Alcaide Torres J,Santiago-Fernandez C,Matute Gonzalez E,Rubio Navarro M,Bautista R,Gómez Maldo

更新日期：2020-10-01 00:00:00

abstract：:The biological relevance of sulfur containing carbohydrates is gaining substantial attention. Thus the new developments, especially in the synthetic and medicinal chemistry of thio-sugars are critically important for carbohydrate drug design. New studies of biological processes including biosynthetic reactions and enz...

journal_title：Current medicinal chemistry

authors： Witczak ZJ

更新日期：1999-02-01 00:00:00

abstract：:Andrographolide, the main bioactive component separated from Andrographis paniculata in 1951, have been scrutinized with modern drug discovery approach for anti-inflammatory properties since 1984. Identifying new uses for existing drugs can be facilitated by evidence linking them to known or yet undiscovered drug targ...

journal_title：Current medicinal chemistry

authors： Ren X,Xu W,Sun J,Dong B,Awala H,Wang L

更新日期：2020-08-10 00:00:00

abstract：:Anticancer drugs are often nonselective antiproliferative agents (cytotoxins) that preferentially kill dividing cells by attacking their DNA at some level. The lack of selectivity results in significant toxicity to noncancerous proliferating cells. These toxicities along with drug resistance exhibited by the solid tum...

journal_title：Current medicinal chemistry

authors： Singh Y,Palombo M,Sinko PJ

更新日期：2008-01-01 00:00:00

abstract：:Agents modulating apoptosis are of extraordinary promise for the treatment of several states of disease including cancer, AIDS, neurodegenerative and ischemic diseases. In this review a brief summary of cellular pathways relevant to programmed cell death first is given and potential therapeutic targets therein are emp...

journal_title：Current medicinal chemistry

authors： Deigner HP,Kinscherf R

更新日期：1999-05-01 00:00:00

abstract：:Numerous compounds with a benzothiazole scaffold that have been described in the literature show promising activities against several Gram-positive and Gramnegative bacteria, and also against Mycobacterium tuberculosis. Benzothiazole-based antibacterial compounds bind to different biological targets in bacterial cells...

journal_title：Current medicinal chemistry

authors： Gjorgjieva M,Tomašič T,Kikelj D,Mašič LP

更新日期：2018-01-01 00:00:00

abstract：:Atrial fibrillation represents a major clinical, social and economical matter, and its importance is expected to increase even more in the near future. The progressive ageing of population is associated with an inevitable rising in incidence and prevalence of this rhythm disorder, which limits functional capability, f...

journal_title：Current medicinal chemistry

authors： Lombardi F,Terranova P

更新日期：2006-01-01 00:00:00

abstract：:Coumarins, also referred as benzopyran-2-ones, and their corresponding nitrogen counterpart, 1-azacoumarins also referred to as carbostyrils, are a family of nature-occurring lactones and lactams respectively. The plant extracts containing coumarin-related heterocycles, which were employed as herbal remedies in early ...

journal_title：Current medicinal chemistry

authors： Kulkarni MV,Kulkarni GM,Lin CH,Sun CM

更新日期：2006-01-01 00:00:00

abstract：:Analytical chemists have increasingly turned their attention to drug discovery and drug analysis and to solve fundamental questions of biological significance in physiology and genetics. New technologies have been developed, and a variety of instruments have been redesigned for biomedical applications. The development...

journal_title：Current medicinal chemistry

authors： Hanai T

更新日期：2005-01-01 00:00:00

abstract：:The peroxisome proliferator-activated receptor (PPAR) family of nuclear receptors, a set of three receptor sub-types encoded by distinct genes, function as lipid sensors to regulate a broad range of genes in many metabolically active tissues. Synthetic PPAR agonists have exhibited therapeutic benefits in treating diab...

journal_title：Current medicinal chemistry

authors： Shearer BG,Hoekstra WJ

更新日期：2003-02-01 00:00:00

abstract：:Fourier-transform infrared (FT-IR) based mapping and imaging is a fast emerging technology which is being increasingly applied to investigate tissues in the high-throughput mode. The high resolution close to the cellular level, the possibility to determine the bio-distribution of molecules of interest (proteins, pepti...

journal_title：Current medicinal chemistry

authors： Petter CH,Heigl N,Rainer M,Bakry R,Pallua J,Bonn GK,Huck CW

更新日期：2009-01-01 00:00:00

abstract：:Whilst knowledge of basic biology, diagnosis and prognosis of glioblastoma (GB - WHO grade IV) are steadily improving, advancements of therapy are discouragingly slow, with the only significant novelty during last ten years represented by introduction of temozolomide in chemotherapy. In order to analyze the current st...

journal_title：Current medicinal chemistry

authors： Frosina G

更新日期：2015-01-01 00:00:00

abstract：:Epidemiological studies demonstrated that even in the absence of other risk factors (e.g. diabetes, hypertension, hyperhomocysteinemia, hypercholesterolemia), advanced age itself significantly increases cardiovascular morbidity by enhancing vascular oxidative stress and inflammation. Because the population in the West...

journal_title：Current medicinal chemistry

authors： Labinskyy N,Csiszar A,Veress G,Stef G,Pacher P,Oroszi G,Wu J,Ungvari Z

更新日期：2006-01-01 00:00:00

abstract：:Raltegravir, the only drug targeting the integration step in HIV-1 life cycle, makes β-ketoenol integrase (IN) strand transfer inhibitor (STI) gain a definitive place in the treatment of HIV-1 infection. However, the emergence of viral strains resistant to β-ketoenol STI demands a continued effort toward the discovery...

journal_title：Current medicinal chemistry

authors： Yu S,Zhao G

更新日期：2012-01-01 00:00:00

abstract：:In the long human tradition honey has been used not only as a nutrient but also as a medicine. Its composition is rather variable and depends on the floral source and on external factors, such as seasonal, environmental conditions and processing. In this review, specific attention is focused on absorption, metabolism,...

journal_title：Current medicinal chemistry

authors： Alvarez-Suarez JM,Giampieri F,Battino M

更新日期：2013-01-01 00:00:00

abstract：:Resistance to quinolones and fluoroquinolones has been increasingly reported among human and veterinary isolates during the last three decades related to their wide clinical use. Until recently, the mechanisms of resistance to quinolones in Enterobacteriaceae were believed to be only chromosome-encoded, i.e. related t...

journal_title：Current medicinal chemistry

authors： Cattoir V,Nordmann P

更新日期：2009-01-01 00:00:00