The glioblastoma problem: targeting by combined medicinal chemistry approaches.

abstract：:Cancer is the world's second leading cause of death after heart diseases, and involves abnormal cell growth at a primary site and the potential to spread to other parts of the body. Tumors are highly heterogeneous and consist of subgroups of cells with distinct characteristics. Of these, the cancer stem cells (CSC) ni...

journal_title：Current medicinal chemistry

authors： Vizetto-Duarte C,Branco PC,Custódio L

更新日期：2020-03-20 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：:Protein-ligand docking is currently an important tool in drug discovery efforts and an active area of research that has been the subject of important developments over the last decade. These are well portrayed in the rising number of available protein-ligand docking software programs, increasing level of sophisticatio...

journal_title：Current medicinal chemistry

authors： Sousa SF,Ribeiro AJ,Coimbra JT,Neves RP,Martins SA,Moorthy NS,Fernandes PA,Ramos MJ

更新日期：2013-01-01 00:00:00

abstract：:Type 2 diabetes mellitus (DM) is a public health burden and its co-existence with hypertension is long established in the context of the metabolic syndrome. Both DM and hypertension are major risk factors, for end-stage renal disease, cardiovascular events and mortality. Strict blood pressure (BP) control in diabetics...

journal_title：Current medicinal chemistry

authors： Loutradis C,Papadopoulou E,Angeloudi E,Karagiannis A,Sarafidis P

更新日期：2020-01-01 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：:The hyaluronidases (HAases) are a group of less extensively studied glycosidases distributed throughout the animal kingdom and are popularly known as 'spreading factors'. In recent years, HAases received much attention due to their ability to abruptly alter the hyaluronic acid (HA) homeostasis. HAases preferentially d...

journal_title：Current medicinal chemistry

authors： Girish KS,Kemparaju K,Nagaraju S,Vishwanath BS

更新日期：2009-01-01 00:00:00

abstract：:Cardiotrophin-1 (CT-1), a member of the interleukin (IL)-6 family, is reported to exhibit a plethora of pleiotropic effects in the heart such as cytoprotective, pro-proliferative and pro-fibrotic ones. An extensive research has been devoted on proliferative and profibrotic effects of CT-1 on the heart. Thus the presen...

journal_title：Current medicinal chemistry

authors： García-Cenador MB,Lopez-Novoa JM,Díez J,García-Criado FJ

更新日期：2013-01-01 00:00:00

abstract：:Among the strategies that can lead to the discovery of new drugs, the identification and use of privileged structures, molecular fragments that are able to interact with more than one target, gained particular attention, in an attempt to find new drugs in a shorter time with respect to other strategies. These structur...

journal_title：Current medicinal chemistry

authors： Costantino L,Barlocco D

更新日期：2006-01-01 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：:Preterm labour is a major cause of perinatal mortality and morbidity. However, during the past 40 years of clinical studies and despite the use of multiple therapeutic agents, the rate of preterm birth has not drastically declined. In 1991, it was estimated that in the US approximately 116,000 women admitted with acut...

journal_title：Current medicinal chemistry

authors： Schwarz MK,Page P

更新日期：2003-08-01 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：BACKGROUND:Cholesterol efflux as a key event in reverse cholesterol transport (RCT) is considered now as both diagnostic tool and a promising target for the treatment of atherosclerosis. Radioactive in vitro cholesterol efflux assay (CEA) is the gold standard for determination of efflux at cellular level. Fluorescent t...

journal_title：Current medicinal chemistry

authors： Litvinov DY,Savushkin EV,Garaeva EA,Dergunov AD

更新日期：2016-01-01 00:00:00

abstract：:High-resolution nuclear magnetic resonance (NMR) spectroscopy is a universal analytical tool. It can provide detailed information on chemical shifts, J coupling constants, multiplet patterns, and relative peak areas. It plays an important role in the fields of chemistry, biology, medicine, and pharmacy. A highly homog...

journal_title：Current medicinal chemistry

authors： Lin Y,Zeng Q,Lin L,Chen Z

更新日期：2019-01-01 00:00:00

abstract：:Mast cells are potent effectors playing a key role in IgE-associated hypersensitivity reactions, allergic disorders, inflammation and protective immune responses. Mast cell development in vivo occurs mainly in non-hematopoietic microenvironments and increased mast cell numbers can be seen in various inflammatory disea...

journal_title：Current medicinal chemistry

authors： Hu ZQ,Zhao WH,Shimamura T

更新日期：2007-01-01 00:00:00

abstract：:Bioactivation of xenobiotics can, in certain circumstances, result in the formation of reactive electrophilic species. These reactive metabolites may covalently modify proteins and macromolecules and it has been suggested that protein modification is a key initial step in provoking idiosyncratic adverse drug reactions...

journal_title：Current medicinal chemistry

authors： Edwards PJ,Sturino C

更新日期：2011-01-01 00:00:00

abstract：:In the course of studying human mucin MUC1, the attitude towards this molecule has been changing time and again. Initially, the list of presumable functions of MUC1 was restricted to protecting and lubricating epithelium. To date, it is assumed to play an important role in cell signaling as well as in all stages of on...

journal_title：Current medicinal chemistry

authors： Syrkina MS,Vassetzky YS,Rubtsov MA

更新日期：2019-01-01 00:00:00

abstract：:Gene expression, both tissue specific or inducible, is controlled at the level of transcription by various transcription factors interacting with specific sequences of DNA. Anticancer drugs and other potential therapeutic agents alter interactions of regulatory proteins with DNA by a variety of different mechanisms. T...

journal_title：Current medicinal chemistry

authors： Gniazdowski M,Denny WA,Nelson SM,Czyz M

更新日期：2003-06-01 00:00:00

abstract：BACKGROUND:Chronic Liver Disorders (CLD), caused by the lifestyle patterns like alcoholism or by non-alcoholic fatty liver disease or because of virus-mediated hepatitis, affect a large population fraction across the world. CLD progresses into end-stage diseases with a high mortality rate. Liver transplant is the only ...

journal_title：Current medicinal chemistry

authors： Mahmood A,Seetharaman R,Kshatriya P,Patel D,Srivastava AS

更新日期：2020-01-01 00:00:00

abstract：:Although the renin-angiotensin system (RAS) is already an old acquaintance, there are often exciting discoveries that improve our knowledge of it and open new therapeutic possibilities. Moreover, well-established drugs, such as angiotensin-converting enzyme inhibitors (ACEI), angiotensin receptor blockers (ARB), or be...

journal_title：Current medicinal chemistry

authors： Ramírez-Sánchez M,Prieto I,Wangensteen R,Banegas I,Segarra AB,Villarejo AB,Vives F,Cobo J,de Gasparo M

更新日期：2013-01-01 00:00:00

abstract：:Endothelium plays an essential role in human homeostasis by regulating arterial blood pressure, distributing nutrients and hormones as well as providing a smooth surface that modulates coagulation, fibrinolysis and inflammation. Endothelial dysfunction is present in Diabetes Mellitus (DM) and contributes to the develo...

journal_title：Current medicinal chemistry

authors： Tentolouris A,Eleftheriadou I,Tzeravini E,Tsilingiris D,Paschou SA,Siasos G,Tentolouris N

更新日期：2020-01-01 00:00:00

abstract：:Trypanosomatids are a group of flagellated unicellular eukaryotes, causing serious human diseases including Chagas disease (Trypanosoma cruzi), sleeping sickness (Trypanosoma brucei spp.) and Leishmaniasis (Leishmania spp.). The second messenger cAMP is involved in numerous and fundamental processes in these parasites...

journal_title：Current medicinal chemistry

authors： Schoijet AC,Sternlieb T,Alonso GD

更新日期：2019-01-01 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：BACKGROUND:Cancer metabolic reprogramming rekindles enthusiasm for the research of metabolic regulation in cancer drug resistance. A growing number of metabolic modifiers combined with cancer drugs obtain the expected efficacy in in vitro or in vivo studies, also in clinical trial studies, indicating a good potential o...

journal_title：Current medicinal chemistry

authors： Tan W,Zhong Z,Wang S,Liu H,Yu H,Tan R,Hu X,Pan T,Wang Y

更新日期：2017-11-17 00:00:00

abstract：:In healthy individuals, natural and adaptive immune responses are able to control virus entry into the host. In particular, CD8(+)-mediated cytotoxicity, sustained by the intervention of CD4+ cells, represents the major key event leading to virus eradication. On the other hand, viruses are able to evade from host immu...

journal_title：Current medicinal chemistry

authors： Amati L,Passeri ME,Lippolis A,Lio D,Caruso C,Jirillo E,Covelli V

更新日期：2006-01-01 00:00:00

abstract：:The use of anti-diabetic drugs has been increasing worldwide and the evolution of therapeutics has been enormous. Still, the currently available anti-diabetic drugs do not present the desired efficacy and are generally associated with serious adverse effects. Thus, entirely new interventions, addressing the underlying...

journal_title：Current medicinal chemistry

authors： Rocha S,Ribeiro D,Fernandes E,Freitas M

更新日期：2020-01-01 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：: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：:Photodynamic therapy (PDT) is a novel medical technique involving three key components: light, a photosensitizer molecule and molecular oxygen, which are essential to achieve the therapeutic effect. There has been great interest in the use of PDT in the treatment of many cancers and skin disorders. Upon irradiation wi...

journal_title：Current medicinal chemistry

authors： Skupin-Mrugalska P,Sobotta L,Kucinska M,Murias M,Mielcarek J,Düzgüneş N

更新日期：2014-01-01 00:00:00

abstract：:5-Aminoisoquinolin-1-one (5-AIQ) is a water-soluble inhibitor of the poly(ADPribose) polymerases (PARPs), lacking isoform-selectivity. Although of only moderate potency in vitro against PARP-1, it is highly active in many assays in cells and in models in vivo, indicating excellent uptake. Optimisation of the several s...

journal_title：Current medicinal chemistry

authors： Threadgill MD

更新日期：2015-01-01 00:00:00

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