5-Aminoisoquinolin-1-one (5-AIQ), a Water-Soluble Inhibitor of the Poly(ADP-Ribose)Polymerases (PARPs).

abstract：:HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) nowadays represent most promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT). They have a unique antiviral potency, high specificity and low cytotoxicity. However, to a great extent, the efficacy of HIV-1 NNRTIs is compounde...

journal_title：Current medicinal chemistry

authors： Chen X,Zhan P,Li D,De Clercq E,Liu X

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:The therapeutic properties of cannabinoids are well-known since ancient years. Growing evidence exist on endocannabinoid system (ECS) modulation related with human tumorigenesis. OBJECTIVE:Taking into account the substantial role of ECS on immune cell regulation, the present review is aimed to summarize the...

journal_title：Current medicinal chemistry

authors： Giaginis C,Lakiotaki E,Korkolopoulou P,Konstantopoulos K,Patsouris E,Theocharis S

更新日期：2016-01-01 00:00:00

abstract：:Many non-cardiovascular drugs of common clinical use cause, as an unwanted accessory property, the prolongation of the cardiac repolarisation process, due to the block of the HERG (Human Ether-a-go-go Related Gene) potassium channel, responsible for the repolarising I(Kr) current. This delayed cardiac repolarisation p...

journal_title：Current medicinal chemistry

authors： Testai L,Bianucci AM,Massarelli I,Breschi MC,Martinotti E,Calderone V

更新日期：2004-10-01 00:00:00

abstract：:Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharma...

journal_title：Current medicinal chemistry

authors： Álvarez R,Aramburu L,Puebla P,Caballero E,González M,Vicente A,Medarde M,Peláez R

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:Resveratrol, a natural polyphenol product, is used in plant defense from fungal and microbial aggression. It is found naturally, especially in plants such as grapes, peanuts, and berries. It has the highest concentrations in blueberries, mulberries, blackberries, and the skin of red grapes. Resveratrol has v...

journal_title：Current medicinal chemistry

authors： Kumar S,Chang YC,Lai KH,Hwang TL

更新日期：2020-09-17 00:00:00

abstract：:The clinical treatment of multifactorial pathologies (e.g. cancer, Alzheimer's disease, psychiatric disorders), is still a major challenge. Many researches have been published dealing with the design of multiple ligands, able to act at the same time towards several targets relevant for a given pathology. In the presen...

journal_title：Current medicinal chemistry

authors： Costantino L,Barlocco D

更新日期：2012-01-01 00:00:00

abstract：:Chagas disease is an infectious tropical disease included within the group of neglected tropical diseases. Though historically endemic to Latin America, it has lately spread to high-income countries due to human migration. At present, there are only two available drugs, nifurtimox and benznidazole, approved for this t...

journal_title：Current medicinal chemistry

authors： Bellera CL,Alberca LN,Sbaraglini ML,Talevi A

更新日期：2020-01-01 00:00:00

abstract：:A BRAF somatic mutation at residue 600 of the BRAF protein (BRAFV600E) is highly prevalent in papillary thyroid carcinomas (PTC). This mutation occurs in approximately 44% (from 29% to 83%) of PTC depending on the different studies. BRAFV600E is almost always found in PTC with a papillary or a mixed follicular/papilla...

journal_title：Current medicinal chemistry

authors： Lassalle S,Hofman V,Ilie M,Butori C,Bozec A,Santini J,Vielh P,Hofman P

更新日期：2010-01-01 00:00:00

abstract：:Gossypol, a disesquiterpene from cottonseed, exhibits multiple biological properties, including male antifertility activity and anticancer activity. Gossypol also inhibits the growth of numerous parasitic organisms and shows antiviral activity against a number of enveloped viruses, including the AIDS virus. Derivative...

journal_title：Current medicinal chemistry

authors： Vander Jagt DL,Deck LM,Royer RE

更新日期：2000-04-01 00:00:00

abstract：:Polymyxins are polypeptide antibiotics, with a primary effect of membrane damaging due to their selective binding to the lipopolysaccharide of Gram-negative bacteria. Their nephro- and neurotoxic side effects limited their use, however, in the last decade the emergence of multidrug-resistant Gram-negative bacteria led...

journal_title：Current medicinal chemistry

authors： Kadar B,Kocsis B,Nagy K,Szabo D

更新日期：2013-01-01 00:00:00

abstract：:Voltage-gated sodium channels are large transmembrane protein complexes responsible for the propagation and transmission of electrical impulses through nerve, muscle and endocrine cells and cell systems. Dysregulated expression and/or functional changes of ion channel isoforms are found in many associated pathological...

journal_title：Current medicinal chemistry

authors： Jukič M,Kikelj D,Anderluh M

更新日期：2014-01-01 00:00:00

abstract：:For many years clinicians have been searching for "kidney troponin"- a simple diagnostic tool to assess risk of acute kidney injury (AKI). Recently, the rise in the variety of contrast-related procedures (contrast computed tomography [CT], percutaneous coronary intervention [PCI] and angiography) have resulted in incr...

journal_title：Current medicinal chemistry

authors： Zdziechowska M,Gluba-Brzózka A,Franczyk B,Rysz J

更新日期：2020-05-01 00:00:00

abstract：BACKGROUND:Nitric oxide (NO) plays important regulatory roles in a plethora of biological functions and thus holds tremendous potential to be exploited for clinical uses. However, the chemistries in the molecular design of nano-nitric oxide delivery systems is currently lacking. OBJECTIVE:The overarching aim of this r...

journal_title：Current medicinal chemistry

authors： Nguyen KT,Wu Z,Huang T,Tay CY

更新日期：2018-01-01 00:00:00

abstract：:Drug repositioning is an important area of biomedical research. The drug repositioning studies have shifted to computational approaches. Large-scale perturbation databases, such as the Connectivity Map and the Library of Integrated Network-Based Cellular Signatures, contain a number of chemical-induced gene expression...

journal_title：Current medicinal chemistry

authors： Wang F,Lei X,Wu FX

更新日期：2020-01-01 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：:Vitamin D has been known for a long time as a major factor involved in the calcium- phosphate balance and homeostasis, along with parathyroid hormone (PTH). While vitamin D effects on calcium and phosphate are fully known, recent studies attempted to link vitamin D status and cardiovascular diseases. The involvement o...

journal_title：Current medicinal chemistry

authors： Santoro D,Pellicanò V,Cernaro V,Lacava V,Lacquaniti A,Atteritano M,Buemi M

更新日期：2016-01-01 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：:The market, sales and regulatory approval of new human medicines, during the past few years, indicates increasing number and share of new biologics and emergence of new multibillion dollar molecules. The global sale of monoclonal antibodies in 2006 were $20.6 billion. Remicade had annual sales gain of $1 billion durin...

journal_title：Current medicinal chemistry

authors： Maggon K

更新日期：2007-01-01 00:00:00

abstract：:With many advantages over other therapeutic agents such as monoclonal antibodies, aptamers have recently emerged as a novel and powerful class of ligands with excellent potential for diagnostic and therapeutic applications. Typically generated through Systematic Evolution of Ligands by EXponential enrichment (SELEX), ...

journal_title：Current medicinal chemistry

authors： Wang P,Yang Y,Hong H,Zhang Y,Cai W,Fang D

更新日期：2011-01-01 00:00:00

abstract：:Novel molecular genetic approaches, at genome-scale in different species allowed characterizing genes that have undergone recent selection. The interest in this research field is not limited to the natural curiosity about our evolutionary past, but it is also to identify novel susceptibility genes for neuropsychiatic ...

journal_title：Current medicinal chemistry

authors： Moalic JM,Le Strat Y,Lepagnol-Bestel AM,Ramoz N,Loe-Mie Y,Maussion G,Gorwood P,Simonneau M

更新日期：2010-01-01 00:00:00

abstract：:Systemic Lupus Erythematosus (SLE) is a chronic and relapsing heterogenous autoimmune disease that primarily affects women of reproductive age. Genetic and environmental risk factors are involved in the pathogenesis of SLE, and susceptibility genes have recently been identified. However, as gene therapy is far from cl...

journal_title：Current medicinal chemistry

authors： Pan Q,Guo Y,Guo L,Liao S,Zhao C,Wang S,Liu HF

更新日期：2020-01-01 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

abstract：:Universal stress proteins are ubiquitously expressed in bacteria, archaea and plants and other eukaryotes. A general property of USPs is their role in adaptation of bacteria to oxidative stress, high temperature, low pH and/or hypoxia. There is increasing evidence that these proteins facilitate the adaption of bacteri...

journal_title：Current medicinal chemistry

authors： O'Connor A,McClean S

更新日期：2017-11-24 00:00:00

abstract：:Potent enzyme inhibitors have long been recognized as powerful tools for assessing the physiological roles of enzymes and have led to the therapeutic drugs able to modulate their activities in vivo. However, to be valuable tools such inhibitors should be selective so that they do not interfere with other members of th...

journal_title：Current medicinal chemistry

authors： Batra S,Srinivasan T,Rastogi SK,Kundu B

更新日期：2002-02-01 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：:Since the outbreak of SARS (severe acute respiratory syndrome) in November 2002 in Southern China's Guangdong Province, considerable progress has been made in the development of drugs for SARS therapy. The present mini review is focused on the area of computer-aided drug discovery, i.e., the advances achieved mainly f...

journal_title：Current medicinal chemistry

authors： Chou KC,Wei DQ,Du QS,Sirois S,Zhong WZ

更新日期：2006-01-01 00:00:00

abstract：BACKGROUND:Stimuli-responsive carriers are a class of drug delivery systems which can change their physicochemical properties and/or structural conformations in response to specific stimuli. Although passive and active drug targeting has proved to reduce the side effects to normal cells, controlled intracellular drug r...

journal_title：Current medicinal chemistry

authors： Sheng Y,Hu J,Shi J,Lee LJ

更新日期：2019-01-01 00:00:00

abstract：:DNA mutation is a very important step in carcinogenesis and elevated levels of oxidative DNA damage have been monitored in a variety of tumors. The discovery of the role of free radicals in cancer has led to a new medical approach. Minimizing oxidative damage may be a significant advance in the prevention or treatment...

journal_title：Current medicinal chemistry

authors： Tekiner-Gulbas B,Westwell AD,Suzen S

更新日期：2013-01-01 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：:It is well accepted that inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease, is one of high risk factors for colorectal cancer (CRC). This supports the notion that inflammation plays a key role in cancer development. Epidemiologic studies have shown that vitamin D (Vit D) deficiency is ...

journal_title：Current medicinal chemistry

authors： Luan Z,Ma Y,Xin Y,Qian J,Wang H

更新日期：2017-01-01 00:00:00