The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development.

abstract：: ...

journal_title：Current medicinal chemistry

authors： Stepnowski P,Paszkiewicz M

更新日期：2019-01-01 00:00:00

abstract：:A dramatical decline in human male reproductive function has been reported for the past 20 years. Many recent epidemiological, clinical and experimental findings suggest that the reproductive dysfunction could result from prenatal and neonatal chemical compound exposure. Even if numerous studies argue for a relationsh...

journal_title：Current medicinal chemistry

authors： Gilleron J,Malassiné A,Carette D,Segretain D,Pointis G

更新日期：2011-01-01 00:00:00

abstract：:This review summarizes our knowledge of biochemical, biological and medical applications and properties of phosphinic acid compounds. Phosphinic acid compounds (phosphinates) are derivatives of phosphinic acid H2P(O)(OH). The major attention of this article is focused on applications of phosphinates of a pseudopeptide...

journal_title：Current medicinal chemistry

authors： Collinsová M,Jirácek J

更新日期：2000-06-01 00:00:00

abstract：:MicroRNAs (miRNAs) translationally repressing their target messenger RNAs due to their gene-regulatory functions play an important but not unexpected role in a tumour development. More surprising are the findings that levels of various miRNAs are well correlated with presence of specific tumours and formation of metas...

journal_title：Current medicinal chemistry

authors： Pekarik V,Gumulec J,Masarik M,Kizek R,Adam V

更新日期：2013-01-01 00:00:00

abstract：:DEAD-box RNA helicase DDX3 is a well-known host factor that inhibits hepatitis B viral proliferation and boosts innate immune responses via TANK-binding kinase 1 (TBK1)/IKKε-mediated and/or interferon (IFN)-β promoter stimulator-1 (IPS-1)-mediated IFN-β induction. Previously, we demonstrated the anti-hepatitis B activ...

journal_title：Current medicinal chemistry

authors： Choi YJ,Kang LJ,Lee SG

更新日期：2014-01-01 00:00:00

abstract：:Protein-based polymers are some of the most promising candidates for a new generation of innovative biomaterials as recent advances in genetic-engineering and biotechnological techniques mean that protein-based biomaterials can be designed and constructed with a higher degree of complexity and accuracy. Moreover, thei...

journal_title：Current medicinal chemistry

authors： Santos M,Serrano-Dúcar S,González-Valdivieso J,Vallejo R,Girotti A,Cuadrado P,Arias FJ

更新日期：2019-01-01 00:00:00

abstract：:Inflammation is a local or systemic tissue reaction caused by external or internal stimuli with the objective to remove the noxa, inhibit its further dissemination and eventually repair damaged tissue. Blood vessels and perivascular connective tissue are important regulators of the inflammatory process. After a short ...

journal_title：Current medicinal chemistry

authors： Wilting J,Becker J,Buttler K,Weich HA

更新日期：2009-01-01 00:00:00

abstract：:Drug resistance is one of the major obstacles limiting the success of cancer chemotherapy. Biological mechanisms contributing to drug resistance may be present de novo and related to inherent features or may be raised after exposure to anticancer drugs. In recent years, both clinical observations and experimental stud...

journal_title：Current medicinal chemistry

authors： Sui M,Zhang H,Fan W

更新日期：2011-01-01 00:00:00

abstract：:The story of antimalarials as antinflammatory drugs dates back several centuries. Chinin, the extract of the Cinchona bark, has been exploited since the 18th century for its antimalarial and antifebrile properties. Later, during the Second World War, the broad use of antimalarials allowed arguing their antirheumatic e...

journal_title：Current medicinal chemistry

authors： Piscianz E,Cuzzoni E,Sharma R,Tesser A,Sapra P,Tommasini A

更新日期：2018-01-01 00:00:00

abstract：:The present article reviews interesting cationic liposomes (cationic transfection lipids) with novel cationic cholesterol derivatives, a new strategy in gene transfection developed by our group and the presently accepted molecular mechanism of gene transfection. Use of confocal laser scanning microscopy and atomic for...

journal_title：Current medicinal chemistry

authors： Nakanishi M

更新日期：2003-07-01 00:00:00

abstract：BACKGROUND:The possibilities of treatment for oncological diseases are growing enormously in the last decades. Unfortunately, these developments have led to the onset of resistances with regards to the new treatments. This is particularly true if we face with the therapeutic field of Tyrosine Kinase Inhibitors (TKIs). ...

journal_title：Current medicinal chemistry

authors： Zanforlin E,Zagotto G,Ribaudo G

更新日期：2019-01-01 00:00:00

abstract：:Tuberculosis (TB) which is caused by the resilient pathogen Mycobacterium tuberculosis (MTB) has re-emerged to become a leading public health problem in the world. The growing number of multi-drug resistant MTB strains and the more recently emerging problem with the extensively drug resistant strains of the pathogen a...

journal_title：Current medicinal chemistry

authors： Viganor L,Skerry C,McCann M,Devereux M

更新日期：2015-01-01 00:00:00

abstract：:This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researc...

journal_title：Current medicinal chemistry

authors： Akhtar MJ,Yar MS,Sharma VK,Khan AA,Ali Z,Haider MDR,Pathak A

更新日期：2020-01-01 00:00:00

abstract：:Glutamate carboxypeptidase II (GCPII) and its splice variants, paralogs and human homologs represent a family of proteins with diverse tissue distribution, cellular localization and largely unknown function which have been explored only recently. While GCPII itself has been thoroughly studied from different perspectiv...

journal_title：Current medicinal chemistry

authors： Hlouchová K,Navrátil V,Tykvart J,Sácha P,Konvalinka J

更新日期：2012-01-01 00:00:00

abstract：:Evidence came out showing that oxidative stress has a pivotal role in development and maintenance of inflammation and aberrant immune responses. Biomarkers of oxidative stress may define the proportion of oxidative damage underlying pathological conditions, and also foresee and monitor the possible efficacy of therape...

journal_title：Current medicinal chemistry

authors： Cristani M,Speciale A,Saija A,Gangemi S,Minciullo PL,Cimino F

更新日期：2016-01-01 00:00:00

abstract：:Deregulation of kinase function has been implicated in several important diseases, including cancer, neurological and metabolic disorders. Because of their key role in causing disease, kinases have become one of the most intensively pursued classes of drug targets. To date, several monoclonal antibodies (mAbs) and sma...

journal_title：Current medicinal chemistry

authors： Cerchia L,de Franciscis V

更新日期：2011-01-01 00:00:00

abstract：:The development of biodegradable nanoparticles is an important tool for the biological transport of chemical compounds. The nanoencapsulation reduces the biopharmaceutical and pharmacokinetic drawbacks of compounds and enhances their biological properties. Naturally occurring polymers such as proteins and polysacchari...

journal_title：Current medicinal chemistry

authors： Lopes VF,Giongo CN,de Almeida Campos L,Abraham WR,Mainardes RM,Khalil NM

更新日期：2020-11-24 00:00:00

abstract：:Breakdown of glucose under physiological conditions gives rise to glucose degradation products (GDPs). GDPs are also formed during heat sterilization of glucose-containing peritoneal dialysis fluids (PD-fluids). In PD-fluids GDPs have been shown in many different in vitro assays to be responsible for adverse effects s...

journal_title：Current medicinal chemistry

authors： Ortiz A,Wieslander A,Linden T,Santamaria B,Sanz A,Justo P,Sanchez-Niño MD,Benito A,Kjellstrand P

更新日期：2006-01-01 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：:Chronic Obstructive Pulmonary Disease (COPD) is a progressive respiratory disorder characterized by irreversible chronic inflammation and airflow obstruction. It affects more than 64 million patients worldwide and it is predicted to become the third cause of death in the industrialized world by 2030. Currently availab...

journal_title：Current medicinal chemistry

authors： Pirozzi F,Ren K,Murabito A,Ghigo A

更新日期：2019-01-01 00:00:00

abstract：:Flavonoids are major dietary constituents of plant-based food found ubiquitously in plant kingdom where they are usually present in substantial amounts. Rutin is a flavonol-type polyphenol which consists of the flavonol quercetin and the disaccharide rutinose. Rutin has been reported to exert diverse biological effect...

journal_title：Current medicinal chemistry

authors： Budzynska B,Faggio C,Kruk-Slomka M,Samec D,Nabavi SF,Sureda A,Devi KP,Nabavi SM

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Despite the historical employment of boron-containing compounds (BCCs) with medicinal purposes, the reported cases of BCC toxicity in humans during the twentieth century were driving us towards an "boron-withdrawal" period. Fortunately, the use of boric acid for specific purposes remains, and the discovery o...

journal_title：Current medicinal chemistry

authors： Soriano-Ursúa MA,Farfán-García ED,Geninatti-Crich S

更新日期：2019-03-27 00:00:00

abstract：:The COVID-19 pandemic has had catastrophic Global effects on financial markets, jobs and peoples' lives. Future prevention/therapy of COVID-19 will rely heavily on vaccine development and attempts to repurpose drugs previously used for other microbial diseases. Little attention, however, has been paid to possible diff...

journal_title：Current medicinal chemistry

authors： Ratcliffe NA,Castro HC,Paixão IC,Mello CB

更新日期：2020-10-27 00:00:00

abstract：:Nowadays, fast and sensitive methods for biomarkers detection exist, but the performance of most of them still rely centralized laboratory testing. The development of small, fast and simple to use medical devices that can help in making diagnosis accurate and with low-invasiveness is now a major challenge for nanotech...

journal_title：Current medicinal chemistry

authors： Bedin C,Crotti S,Tasciotti E,Agostini M

更新日期：2018-01-01 00:00:00

abstract：:The branched-chain fatty acid valproic acid (VPA) is the most commonly used antiepileptic drug for treating generalized epilepsy. Although originally considered to be of low toxicity, VPA has proved to possess considerable teratogenic potential when applied to the pregnant epileptic women. During the last few years, i...

journal_title：Current medicinal chemistry

authors： Blaheta RA,Nau H,Michaelis M,Cinatl J Jr

更新日期：2002-08-01 00:00:00

abstract：:The rising emergence of antibiotic resistance urges the search for new strategies to defeat microorganisms that lead to persistent infections of the host. Tolerant to antibiotics, slowly replicating bacteria often cause latent and persistent infections that are the most challenging for pharmacological treatment. Persi...

journal_title：Current medicinal chemistry

authors： Campanini B,Pieroni M,Raboni S,Bettati S,Benoni R,Pecchini C,Costantino G,Mozzarelli A

更新日期：2015-01-01 00:00:00

abstract：:Drug repositioning, an innovative therapeutic application of an old drug, has received much attention as a particularly costeffective strategy in drug R&D Recent work has indicated that repositioning can be promoted by utilizing a wide range of information sources, including medicinal chemical, target, mechanism, main...

journal_title：Current medicinal chemistry

authors： Arany Á,Bolgár B,Balogh B,Antal P,Mátyus P

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND:During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. However, accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monu...

journal_title：Current medicinal chemistry

authors： O Brien Z,Moghaddam MF

更新日期：2017-01-01 00:00:00

abstract：:Since the beginning of the 20th century, important medicinal progress has led medical doctors to think that the end of devastating epidemics has arrived. In 1930, the discovery of sulfamides and penicillin opened a wide area of applications able to fight against bacterial infections. However, almost all antibiotics we...

journal_title：Current medicinal chemistry

authors： Salzet M

更新日期：2005-01-01 00:00:00

abstract：:Apolipoprotein B -containing lipoproteins include triglyceride-rich lipoproteins (chylomicrons and their remnants, and very low-density lipoproteins and their remnants) and cholesterol-rich low-density lipoprotein particles. Of these, lipoproteins having sizes below 70-80 nm may enter the arterial wall, where they acc...

journal_title：Current medicinal chemistry

authors： Öörni K,Lehti S,Sjövall P,Kovanen PT

更新日期：2019-01-01 00:00:00