Enhancement of chemotherapeutic efficacy by small molecule inhibition of NF-kappaB and checkpoint kinases.

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：:Epigenetics is a field of biological sciences focused on the study of reversible, heritable changes in gene function not due to modifications of the genomic sequence. These changes are the result of a complex cross-talk between several molecular mechanisms, that is in turn orchestrated by genetic and environmental fac...

journal_title：Current medicinal chemistry

authors： De Riso G,Cocozza S

更新日期：2020-11-17 00:00:00

abstract：:Receptor-binding peptides have attracted an enormous interest in targeting molecules for the development of tumour specific radiopharmaceutical compounds. The overexpression of many receptors on human tumour makes such peptide-ligands attractive agents for diagnostic imaging and therapy of cancers. The use of solid-ph...

journal_title：Current medicinal chemistry

authors： Bolzati C,Refosco F,Marchiani A,Ruzza P

更新日期：2010-01-01 00:00:00

abstract：:Patients with homozygous familial hypercholesterolemia (HoFH) represent the most severe patients within the spectrum of dyslipidemias. Untreated Low-Density Lipoprotein Cholesterol (LDL-C) levels in these patients are usually in the range 500 to 1200 mg/dL. Moreover, these patients exhibit a scarce responsiveness or e...

journal_title：Current medicinal chemistry

authors： Stefanutti C,Morozzi C,Di Giacomo S

更新日期：2012-01-01 00:00:00

abstract：:Inflammation is an initial response of the body to a harmful stimuli and it is achieved by the increased movement of leukocytes (especially granulocytes) from blood into injured tissues. It is required for healing wounds and infections. Despite their indispensable role in microbial killing, the inflammation reactions ...

journal_title：Current medicinal chemistry

authors： Soubhye J,Aldib I,Delporte C,Prévost M,Dufrasne F,Antwerpen PV

更新日期：2016-01-01 00:00:00

abstract：:About 2.3% of the world's population is infected with hepatitis C virus (HCV) and patients have a high risk of developing liver cirrhosis and its complications. Current therapeutic strategies are based on a combination of pegylatedinterferon, ribavirin and (only for patients with genotype 1 infection) a protease inhib...

journal_title：Current medicinal chemistry

authors： Gentile I,Borgia F,Buonomo AR,Zappulo E,Castaldo G,Borgia G

更新日期：2014-01-01 00:00:00

abstract：:Irinotecan, a camptothecin analogue, is a prodrug which requires bioactivation to form the active metabolite SN-38. SN-38 acts as a DNA topoisomerase I poison. Irinotecan has been widely used in the treatment of metastatic colorectal cancer, small cell lung cancer and several other solid tumors. However, large inter-p...

journal_title：Current medicinal chemistry

authors： Ma MK,McLeod HL

更新日期：2003-01-01 00:00:00

abstract：BACKGROUND:Chronic, degenerative diseases are often characterized by inflammation and aberrant angiogenesis. For these pathologies, including rheumatoid arthritis, cardiovascular and autoimmune diseases, cancer, diabetes, and obesity, current therapies have limited efficacy. OBJECTIVES:The validation of novel (chemo)p...

journal_title：Current medicinal chemistry

authors： Albini A,Bassani B,Baci D,Dallaglio K,Gallazzi M,Corradino P,Bruno A,Noonan DM

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：:The expansion of fluorescent techniques for studying the ligand-receptor interaction resulted in a burst of the novel fluorescent ligands development. The discovery of the ligand, that is of high affinity to the receptor and whose localization could be easily visualized, even on the single cell level, gave the researc...

journal_title：Current medicinal chemistry

authors： Kuder K,Kieć-Kononowicz K

更新日期：2008-01-01 00:00:00

abstract：BACKGROUND:Leukotrienes (LTs) constitute a bioactive group of polyunsaturated fatty acid (PUFA) metabolites molded by the enzymatic activity of lipoxygenase (LO) and have a pivotal role in inflammation and allergy. Evidence is accumulating both by in vitro cell culture experiments and animal tumor model studies in supp...

journal_title：Current medicinal chemistry

authors： Mahboubi-Rabbani M,Zarghi A

更新日期：2019-12-09 00:00:00

abstract：:In recent years several mutations and sequence polymorphisms of the glucocorticoid receptor gene have been described. The majority of mutations have been found in patients with a rare endocrinological abnormality, the glucocorticoid resistance syndrome. In addition, some sequence polymorphisms have been considered to ...

journal_title：Current medicinal chemistry

authors： Likó I,Igaz P,Patócs A,Tóth S,Pázmány T,Tóth M,Rácz K

更新日期：2004-12-01 00:00:00

abstract：:Mitochondria are cytoplasmic double-membraned organelles that are involved in a myriad of key cellular regulatory processes. The loss of mitochondrial function is related to the pathogenesis of several human diseases. Over the last decades, an increasing number of studies have shown that dietary polyphenols can regula...

journal_title：Current medicinal chemistry

authors： Teixeira J,Chavarria D,Borges F,Wojtczak L,Wieckowski MR,Karkucinska-Wieckowska A,Oliveira PJ

更新日期：2019-01-01 00:00:00

abstract：:The polystyrene-based 2-chlorotrityl resin was originally used in the synthesis of peptides using an Fmoc-amino acid/carboxyl-linked protocol. While traditionally employed to prepare a number of biologically active peptides, the resin has received increasing attention as a support for the synthesis of pseudopeptide an...

journal_title：Current medicinal chemistry

authors： Hoekstra WJ

更新日期：2001-05-01 00:00:00

abstract：:Statins are inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate-limiting enzyme of cholesterol synthesis. In recent years, statins have become the major choice of treatment for hypercholesterolemia. Emerging evidence from both animal and human studies indicates that mechanisms i...

journal_title：Current medicinal chemistry

authors： Luo JD,Chen AF

更新日期：2003-08-01 00:00:00

abstract：:The Src family consists of eight non-receptor protein tyrosine kinases characterised by a common structure. Based on their amino acid sequence, Src family kinases are grouped into two subfamilies, which are also characterised by different tissue specificity. Src kinases are involved in signal transduction pathways tri...

journal_title：Current medicinal chemistry

authors： Benati D,Baldari CT

更新日期：2008-01-01 00:00:00

abstract：:ATP binding cassette (ABC) transporters are involved in drug absorption, distribution and elimination. They also mediate multidrug resistance in cancer cells. Isoflavones, such as genistein (GNT), belong to a class of naturally-occurring compounds found at high concentrations in commonly consumed soya based-foods and ...

journal_title：Current medicinal chemistry

authors： Rigalli JP,Ciriaci N,Mottino AD,Catania VA,Ruiz ML

更新日期：2016-01-01 00:00:00

abstract：:Nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF) belong to the protein family of neurotrophins. They both display profound neuromodulatory functions and are essentially involved in the survival and homeostatic maintenance of central and peripheral neurons during development and adulthood. Moreove...

journal_title：Current medicinal chemistry

authors： Schulte-Herbrüggen O,Braun A,Rochlitzer S,Jockers-Scherübl MC,Hellweg R

更新日期：2007-01-01 00:00:00

abstract：:The term Lewy body diseases (LBDs) refers to a subset of neurodegenerative disorders that share the accumulation of the so-called Lewy bodies (LB) including: Parkinson's disease (PD), dementia with Lewy bodies (DLB), and PD later characterized by the occurrence of dementia (PDD). Moreover, multiple system atrophy (MSA...

journal_title：Current medicinal chemistry

authors： Bauckneht M,Arnaldi D,Nobili F,Aarsland D,Morbelli S

更新日期：2018-01-01 00:00:00

abstract：:Mycobacterium tuberculosis (Mtb), the main aetiological agent of tuberculosis (TB) in humans, is estimated to cause nearly two million deaths every year. Despite their huge therapeutic value, existing antitubercular drugs have several shortcomings, such as for instance the insurgence of drug resistance, which is mostl...

journal_title：Current medicinal chemistry

authors： Fanzani L,Porta F,Meneghetti F,Villa S,Gelain A,Lucarelli AP,Parisini E

更新日期：2015-01-01 00:00:00

abstract：:The reductive conversion of ribonucleotides to deoxyribonucleotides by ribonucleotide reductase (RR) is a crucial and rate-controlling step in the pathway leading to the biosynthesis of DNA, since deoxyribonucleotides are present in extremely low levels in mammalian cells. Mammalian ribonucleotide reductase (RR) is co...

journal_title：Current medicinal chemistry

authors： Li J,Zheng LM,King I,Doyle TW,Chen SH

更新日期：2001-02-01 00:00:00

abstract：:Similarly to a series of chronic diseases, essential arterial hypertension (HTN) may be manifested during childhood as a blood pressure (BP) reading which repeatedly rises above the 95(th) percentile of population-specific standards. Since BP tends to track along the same percentiles throughout life, children with hig...

journal_title：Current medicinal chemistry

authors： Bassareo PP,Bassareo V,Iacovidou N,Mercuro G

更新日期：2014-01-01 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：BACKGROUND:Pollutants are diverse chemical entities, including gases such as ozone and particulate matter PM. PM contains toxic chemicals such as polycyclic aromatic hydrocarbons (PAHs). Some PAHs can induce strong oxidative stress under UVA exposure. Pollution aggravates some skin diseases such as atopy or eczema, but...

journal_title：Current medicinal chemistry

authors： Marrot L

更新日期：2018-01-01 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

abstract：:Histone deacetylase inhibitors have generated significant interest as anti-cancer agents due to their ability to cause growth arrest, terminal differentiation and/ or apoptosis in carcinoma cells. Abbott entered this area after the serendipitous discovery of the biaryl hydroxamate A-161906 in a TGF beta mimetic screen...

journal_title：Current medicinal chemistry

authors： Curtin M,Glaser K

更新日期：2003-11-01 00:00:00

abstract：:Diabetic patients have a two- to four-fold increased risk for the development of microvascular (renal, neuronal and retinal) and macrovascular complications. Unfortunately, these complications may develop in both Type 1 and Type 2 diabetic patients even with careful glycaemic, blood pressure and lipid control. With th...

journal_title：Current medicinal chemistry

authors： Soro-Paavonen A,Forbes JM

更新日期：2006-01-01 00:00:00

abstract：:Alzheimer's disease (AD) is a highly complex and rapidly progressive neurodegenerative disorder characterized by the systemic collapse of cognitive function and formation of dense amyloid plaques and neurofibrillary tangles. AD pathology is derived from the cholinergic, amyloid and tau hypotheses, respectively. Curren...

journal_title：Current medicinal chemistry

authors： Mohamed T,Rao PP

更新日期：2011-01-01 00:00:00

abstract：:In the hit to lead process, a drug candidate is selected from a set of potential leads by screening its binding with potential targets. This review focuses on the lead identification assays that employ a bio-chemical or bio-physical test to detect molecular recognition events between proteins and small molecules in a ...

journal_title：Current medicinal chemistry

authors： Bergese P,Cretich M,Oldani C,Oliviero G,Di Carlo G,Depero LE,Chiari M

更新日期：2008-01-01 00:00:00

abstract：:Developing suitable medicines for genetic diseases requires a detailed understanding of not only the pathways that cause the disease, but also the identification of the genetic components involved in disease manifestation. This article focuses on the complexities associated with ocular ciliopathies - a class of debili...

journal_title：Current medicinal chemistry

authors： Shivanna M,Anand M,Chakrabarti S,Khanna H

更新日期：2019-01-01 00:00:00