abstract：:The emergence of bacterial strains with resistance to currently marketed antibacterial agents has spurred interest in the discovery of new antibacterial agents with novel modes of action. One set of potential novel targets are the family of bacterial aminoacyltRNA synthetases (AaRS). Aminoacyl-tRNA synthetases are the...

journal_title：Current medicinal chemistry

authors： Lv PC,Zhu HL

更新日期：2012-01-01 00:00:00

abstract：:In situ hybridization (ISH) is a type of hybridization that uses a labeled complementary DNA or RNA strand to localize a specific DNA or RNA sequence on a chromosome or section of tissue (in-situ) fixed on a slide. Flourescence in-situ hybridization (FISH) technique facilitates the localization of genes to different c...

journal_title：Current medicinal chemistry

authors： Jehan Z,Uddin S,Al-Kuraya KS

更新日期：2012-01-01 00:00:00

abstract：:Lipoxygenases (LOXs) are non-heme iron containing dioxygenases involved in the oxygenation of polyunsaturated fatty acids (PUFAs) such as arachidonic acid (AA). Depending on the position of insertion of oxygen, LOXs are classified into 5-, 8-, 9-, 12- and 15-LOX. Among these, 5-LOX is the most predominant isoform asso...

journal_title：Current medicinal chemistry

authors： Aparoy P,Reddy KK,Reddanna P

更新日期：2012-01-01 00:00:00

abstract：:This research evaluated the effect of multiple-wave lasertherapy on the healing process of surgical wounds based on in vitro models denominated stem-dermal equivalents. These human skin models were obtained from a co-culture of dermal cells and bone marrow mesenchymal stem cells. The experimental tests were carried ou...

journal_title：Current medicinal chemistry

authors： Primo FL,de Paula LB,de Siqueira-Moura MP,Tedesco AC

更新日期：2012-01-01 00:00:00

abstract：:The bi-aryl urea multi-kinase inhibitor Sorafenib (BAY 43-9006, Nexavar) was initially approved for the treatment of unresectable hepatocellular carcinoma and advanced renal cell carcinoma. Eleven years after its first description in PubMed, the therapeutic potential of Sorafenib has been evaluated in an increasing nu...

journal_title：Current medicinal chemistry

authors： Zauli G,Voltan R,Tisato V,Secchiero P

更新日期：2012-01-01 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：:The bryostatins, powerful protein kinase C (PKC) agonists, are a family of complex macrolactone natural products. They are originally isolated from the marine bryozoan Bugula neritina. So far tweenty bryostatins have been obtained naturally and exhibit a remarkable range of biological activities, including antineoplas...

journal_title：Current medicinal chemistry

authors： Ruan BF,Zhu HL

更新日期：2012-01-01 00:00:00

abstract：:Physalia physalis is a marine cnidarian from which high molecular weight toxins with hemolytic and neurotoxic effects have been isolated. In the present work, two novel toxins, PpV9.4 and PpV19.3 were purified from P. physalis by bioactive guideline isolation. It involved two steps of column chromatography, gel filtra...

journal_title：Current medicinal chemistry

authors： Diaz-Garcia CM,Fuentes-Silva D,Sanchez-Soto C,Domínguez-Pérez D,García-Delgado N,Varela C,Mendoza-Hernández G,Rodriguez-Romero A,Castaneda O,Hiriart M

更新日期：2012-01-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs) are essential for the degradation and turnover of components of the extracellular matrix (ECM) and, when pathologically elevated, mediate connective tissue loss (including bone destruction) in various inflammatory and other diseases. Tetracyclines (TCs) are known inhibitors of mammalia...

journal_title：Current medicinal chemistry

authors： Zhang Y,Gu Y,Lee HM,Hambardjieva E,Vranková K,Golub LM,Johnson F

更新日期：2012-01-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) comprise a large protein family of transmembrane receptors involved in many physiological processes. They are engaged in various transduction processes of extracellular signals into intracellular responses. Due to their involvement in numerous diseases they represent an important ph...

journal_title：Current medicinal chemistry

authors： Jakobs D,Sorkalla T,Häberlein H

更新日期：2012-01-01 00:00:00

abstract：:Glutamate carboxypeptidase II (GCPII) is a membrane-bound binuclear zinc metallopeptidase with the highest expression levels found in the nervous and prostatic tissue. Throughout the nervous system, glia-bound GCPII is intimately involved in the neuron-neuron and neuron-glia signaling via the hydrolysis of N-acetylasp...

journal_title：Current medicinal chemistry

authors： Bařinka C,Rojas C,Slusher B,Pomper M

更新日期：2012-01-01 00:00:00

abstract：:The existence of functional NT/dopamine interactions in the central nervous system has been extensively documented. Among others, a possible molecular mechanism underlying the NT-induced modulation of dopamine release is a direct antagonistic NTS(1)/D(2) receptor interaction. More recently, neurochemical experiments a...

journal_title：Current medicinal chemistry

authors： Tanganelli S,Antonelli T,Tomasini MC,Beggiato S,Fuxe K,Ferraro L

更新日期：2012-01-01 00:00:00

abstract：:Sufficient organ blood flow of healthy newborn babies is maintained by relatively low systemic blood pressure. Premature infants are at an increased risk of systemic hypotension, often but not obviously, resulting in hypoperfusion of the cerebral, renal and intestinal vascular beds. Maintaining a stable blood pressure...

journal_title：Current medicinal chemistry

authors： Toth-Heyn P,Cataldi L

更新日期：2012-01-01 00:00:00

abstract：:Since its discovery in 1995 adiponectin has garnered considerable interest from the academic, clinical and biotech communities due to its proposed salutary anti-inflammatory, anti-diabetic, anti-atherogenic and cardioprotective properties. As a result our appreciation of adiponectin's structure and the importance of p...

journal_title：Current medicinal chemistry

authors： Hickman IJ,Whitehead JP

更新日期：2012-01-01 00:00:00

abstract：:Despite advances in cancer treatment, a large number of patients eventually develop metastatic disease that is generally incurable. Systemic chemotherapy remains the standard treatment for these patients. Several chemotherapeutic combinations have proven effective in the management of cancer. Paradoxically, although t...

journal_title：Current medicinal chemistry

authors： Prados J,Alvarez PJ,Melguizo C,Rodriguez-Serrano F,Carrillo E,Boulaiz H,Vélez C,Marchal JA,Caba O,Ortiz R,Rama A,Aranega A

更新日期：2012-01-01 00:00:00

abstract：:Dose-limiting toxicity to healthy tissues is among the major hurdles in anticancer treatment along with intrinsic or acquired multi-drug resistance. Development of small molecule inhibitors (SMI) specific for antiapoptotic Bcl-2 proteins is a novel approach in a way that these antagonists are aimed to interfere with s...

journal_title：Current medicinal chemistry

authors： Bodur C,Basaga H

更新日期：2012-01-01 00:00:00

abstract：:On December 23rd, 1971, President Richard Nixon signed the National Cancer Act and invested more than $ 100 million "to launch an intensive campaign to find a cure for cancer". Today, despite these considerable efforts, cancer still remains a very aggressive silent killer all over the world. Moreover, over the last de...

journal_title：Current medicinal chemistry

authors： Orlikova B,Diederich M

更新日期：2012-01-01 00:00:00

abstract：:To date, many scientific attempts have been directed towards the development of experimental models for the identification of neuronal mechanisms evoking cardiovascular and hemodynamic dysfunctions. The spontaneously hypertensive rat (SHR), a genetic model of essential hypertension, has become a valuable rodent for th...

journal_title：Current medicinal chemistry

authors： Giusi G,Alò R,Avolio E,Zizza M,Facciolo RM,Talani G,Biggio G,Sanna E,Canonaco M

更新日期：2012-01-01 00:00:00

abstract：:The resin of Pistacia lentiscus (L.) var. chia (Duham), an evergreen shrub belonging to the family Anacardiaceae and uniquely cultivated in southern Chios, is known as mastic. It has been used for more than 2500 years in traditional Greek medicine for treating several diseases such as gastralgia and peptic ulcers, whi...

journal_title：Current medicinal chemistry

authors： Paraschos S,Mitakou S,Skaltsounis AL

更新日期：2012-01-01 00:00:00

abstract：:Patients with peripheral arterial disease (PAD) suffer from increased cardiovascular morbidity and mortality. The ankle brachial index has been widely used as an easy tool to identify and stratify patients with PAD, however its predictive value remains limited. Higher levels of inflammatory and prothrombotic biomarker...

journal_title：Current medicinal chemistry

authors： Charakida M,Masi S,Tousoulis D

更新日期：2012-01-01 00:00:00

abstract：:Ca(2+) is a highly versatile intracellular second messenger in the central nervous system, and regulates many complicated cellular processes, including excitation, plasticity and apoptosis. Influx of Ca(2+) from the extracellular fluid is required for sustained elevation of the cytosolic Ca(2+) concentration and full ...

journal_title：Current medicinal chemistry

authors： Yagami T,Kohma H,Yamamoto Y

更新日期：2012-01-01 00:00:00

abstract：:Drug-loaded nanoparticles have shown great potential in the study of carriers for disease-targeting drug delivery. Drug-loaded nanoparticles are excellent in keeping the drug in the systemic circulation for a prolonged period of time, introducing targeting molecules to improve targeting efficiency and to reduce side e...

journal_title：Current medicinal chemistry

authors： Tu Q,Zhang Y,Liu R,Wang JC,Li L,Nie N,Liu A,Wang L,Liu W,Ren L,Wang X,Wang J

更新日期：2012-01-01 00:00:00

abstract：:Naturally occurring nonanolides (synonym decanolides) are a large family of secondary metabolites with an interesting 10- membered macrolide subunit. Metabolites of the nonanolide family have been found to have various biological activities, including cytotoxic, phytotoxic, antimalarial, antifungal, antibacterial, and...

journal_title：Current medicinal chemistry

authors： Sun P,Lu S,Ree TV,Krohn K,Li L,Zhang W

更新日期：2012-01-01 00:00:00

abstract：:Cocaine is one of the most used psychomotor stimulants all over the world. On this basis, the interest for the pharmacological activity and the pharmacodynamic and pharmacokinetic aspects of this drug is very prominent in both clinical and forensic toxicological environments. The review presents and discusses 65 scien...

journal_title：Current medicinal chemistry

authors： Bortolotti F,Gottardo R,Pascali J,Tagliaro F

更新日期：2012-01-01 00:00:00

abstract：:AG490 is a tyrphostin originally described as a Janus Activated Kinase (JAK) 2 inhibitor. AG490 also inhibits epidermal growth factor receptor (EGFR) and guanylyl cyclases (GC). More recently, AG490 was associated with oxidative stress protection in experimental acute kidney injury models. We now show that AG490 is al...

journal_title：Current medicinal chemistry

authors： Fernández-Sánchez R,Berzal S,Sánchez-Niño MD,Neria F,Gonçalves S,Calabia O,Tejedor A,Calzada MJ,Caramelo C,Deudero JJ,Ortiz A

更新日期：2012-01-01 00:00:00

abstract：:Sulfonyl group-containing compounds constitute an important class of therapeutical agents in medicinal chemistry presumably because of the tense chemical structure and functionality of the sulfonyl, which could not only form hydrogen bonding interactions with active site residues of biological targets but also, as inc...

journal_title：Current medicinal chemistry

authors： Chen X,Hussain S,Parveen S,Zhang S,Yang Y,Zhu C

更新日期：2012-01-01 00:00:00

abstract：:Dipeptidyl peptidase 4 (DPP-4), a substrate-specific serine protease, has been validated as a promising drug target for the treatment of type 2 diabetes. DPP-4 inhibitors significantly lowered blood glucose levels in patients with type 2 diabetes without common body weight gain, hypoglycemia and gastrointestinal distu...

journal_title：Current medicinal chemistry

authors： Liu Y,Hu Y,Liu T

更新日期：2012-01-01 00:00:00

abstract：:Despite the protective role of diets rich in fruit plant polyphenols against some cancers and chronic degenerative and inflammatory diseases, insufficient emphasis has been placed on oral health. Numerous studies have aimed to ascertain the role of polyphenols in the prevention and treatment of oral diseases; however,...

journal_title：Current medicinal chemistry

authors： Varoni EM,Lodi G,Sardella A,Carrassi A,Iriti M

更新日期：2012-01-01 00:00:00

abstract：:Frontotemporal Lobar Degeneration (FTLD) is characterized by behavioral changes, executive dysfunctions, and language impairment, sustained by different neuropathological patterns. The collective efforts of clinical, pathological and genetic studies have recently opened new insights into the underpinnings of pathologi...

journal_title：Current medicinal chemistry

authors： Bigni B,Premi E,Pilotto A,Padovani A,Borroni B

更新日期：2012-01-01 00:00:00

abstract：:G protein coupled receptors (GPCRs) are a large eukaryotic protein family of transmembrane receptors that react to a signal coming from the extracellular environment to generate an intracellular response through the activation of a signal transduction pathway mediated by a heterotrimeric G protein. Their diversity, di...

journal_title：Current medicinal chemistry

authors： Vanni S,Rothlisberger U

更新日期：2012-01-01 00:00:00

abstract：:Recent advances in endoscopic techniques such as capsule endoscopy have revealed that aspirin and other nonsteroidal antiinflammatory drugs (NSAIDs) often cause mucosal lesions not only in the upper gastrointestinal tract, but also in the small intestine in humans. Gastric and duodenal lesions caused by NSAIDs can be ...

journal_title：Current medicinal chemistry

authors： Satoh H,Takeuchi K

更新日期：2012-01-01 00:00:00

abstract：:The study of iron chelators as anti-tumor agents is still in its infancy. Iron is important for cellular proliferation and this is demonstrated by observations that iron-depletion results in cell cycle arrest and also apoptosis. In addition, many iron chelators are known to inhibit ribonucleotide reductase, the iron-c...

journal_title：Current medicinal chemistry

authors： Yu Y,Gutierrez E,Kovacevic Z,Saletta F,Obeidy P,Suryo Rahmanto Y,Richardson DR

更新日期：2012-01-01 00:00:00

abstract：:Protein tyrosine phosphatases (PTPs) are crucial regulators for numerous biological processes in nature. The dysfunction and overexpression of many PTP members have been demonstrated to cause fatal human diseases such as cancers, diabetes, obesity, neurodegenerative diseases and autoimmune disorders. In the past decad...

journal_title：Current medicinal chemistry

authors： He XP,Xie J,Tang Y,Li J,Chen GR

更新日期：2012-01-01 00:00:00

abstract：:Hereditary amyloidogenic transthyretin (TTR) (ATTR) amyloidosis is an autosomal dominant form of fatal hereditary amyloidosis. Owing to progress in biochemical and molecular genetic analyses, this disease is now believed to occur worldwide. As of today, reports of about 120 different points of single or double mutatio...

journal_title：Current medicinal chemistry

authors： Ando Y,Ueda M

更新日期：2012-01-01 00:00:00

abstract：:Specific noncovalent interactions that are indicative of attractive, directional intermolecular forces have always been of key interest to medicinal chemists in their search for the "glue" that holds drugs and their targets together. With the rapid increase in the number of solved biomolecular structures as well as th...

journal_title：Current medicinal chemistry

authors： Zhou P,Huang J,Tian F

更新日期：2012-01-01 00:00:00

abstract：:Cellular interactions among platelets, leukocytes and endothelial cells are considered as a major cause of inflammation and atherosclerosis in many diseases. Via exposed surface receptors and released soluble substances, activated platelets play a crucial role in the initiation of inflammatory processes, resulting in ...

journal_title：Current medicinal chemistry

authors： Nagy B Jr,Miszti-Blasius K,Kerenyi A,Clemetson KJ,Kappelmayer J

更新日期：2012-01-01 00:00:00

abstract：:K(V)10.1 has recently become generally accepted as a promising cancer target, as it is ectopically expressed in the majority of solid tumors. Due to its cell-surface accessibility, K(V)10.1 has a strong potential for tumor treatment and diagnosis. Given that its mode of action is likely independent of conventional can...

journal_title：Current medicinal chemistry

authors： Pardo LA,Gómez-Varela D,Major F,Sansuk K,Leurs R,Downie BR,Tietze LF,Stühmer W

更新日期：2012-01-01 00:00:00

abstract：:Mast cells are best known as central effector cells in IgE-mediated type I allergic diseases including asthma and hay fever. An increasing amount of evidence, however, has demonstrated that mast cells are sentinel cells playing a critical role in host defense against invading microbes. Mast cells are located immediate...

journal_title：Current medicinal chemistry

authors： Matsuguchi T

更新日期：2012-01-01 00:00:00

abstract：:The calcium ion is quite possibly the single most pervasive signaling molecule used by living organisms for the purpose of communicating internal and external states. It differs from other messengers in that it is neither created nor destroyed, but just moved around inside and outside the cell via transporters, pumps ...

journal_title：Current medicinal chemistry

authors： Hofer AM

更新日期：2012-01-01 00:00:00

abstract：:The evidence seems to be growing in favor of the stem cell theory of cancer with the emergence of studies demonstrating the parallel mechanisms of self renewing pathways in stem cells and particular subsets of cancer cells. The finding of leukemia stem cells and subsequently breast cancer stem cells (BCSC) further sup...

journal_title：Current medicinal chemistry

authors： Nahas GR,Patel SA,Bliss SA,Rameshwar P

更新日期：2012-01-01 00:00:00