Development of low molecular weight CXCR4 antagonists by exploratory structural tuning of cyclic tetra- and pentapeptide-scaffolds towards the treatment of HIV infection, cancer metastasis and rheumatoid arthritis.

abstract：:Diabetes mellitus (DM) is characterized by hyperglycemia, resulting from defects in insulin secretion, insulin action or both. There are several factors such as hyperlipidemia and oxidative stress (OS), namely the production of reactive oxygen/nitrogen species (ROS/RNS), that actively contribute to the development and...

journal_title：Current medicinal chemistry

authors： Sousa A,Ribeiro D,Fernandes E,Freitas M

更新日期：2020-05-24 00:00:00

abstract：:Diabetic nephropathy (DN) is a major complication of diabetes and the leading cause of end-stage renal disease (ESRD). Approximately, one third of diabetic patients develop diabetic nephropathy. As diabetes and its associated metabolic diseases are becoming epidemic, DN is emerging as a major health threat to humans. ...

journal_title：Current medicinal chemistry

authors： Lin X,Tao L,Tang D

更新日期：2013-01-01 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：BACKGROUND:Serotonin reuptake inhibitors (SRIs) and cognitive-behavioral psychotherapy (CBT) are first-line treatments for obsessive-compulsive disorder (OCD). Since response is often inadequate, in recent years researchers investigated whether combining CBT and SRIs, either ab initio or sequentially, results in a grea...

journal_title：Current medicinal chemistry

authors： Albert U,Di Salvo G,Solia F,Rosso G,Maina G

更新日期：2018-01-01 00:00:00

abstract：:Cardiovascular pathologies in the French are not prevalent despite high dietary saturated fat consumption. This is commonly referred to as the "French Paradox" attributing its anti-lipidemic effects to moderate consumption of red wine. Resveratrol, a phytoalexin found in red wine, is currently the focus of intense res...

journal_title：Current medicinal chemistry

authors： Raval AP,Lin HW,Dave KR,Defazio RA,Della Morte D,Kim EJ,Perez-Pinzon MA

更新日期：2008-01-01 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：:Breast cancer is an example of a solid tumour which is well treated in the early stages of disease by surgical excision, but once metastatic spread has occurred, medical therapies (chemotherapy and radiotherapy) are highly toxic, expensive and palliative. It is known that certain tumours exhibit specific patterns of m...

journal_title：Current medicinal chemistry

authors： Dowsland MH,Harvey JR,Lennard TW,Kirby JA,Ali S

更新日期：2003-04-01 00:00:00

abstract：OBJECTIVES:Post-exercise cardiac troponin T (cTnT) release has been widely reported in adult athletes but limited data is available for adolescents. The aim of this study was to determine the incidence and magnitude of cTnT appearance in a large group of adolescent runners, and to determine any association between cTnT...

journal_title：Current medicinal chemistry

authors： Nie J,George KP,Tong TK,Gaze D,Tian Y,Lin H,Shi Q

更新日期：2011-01-01 00:00:00

abstract：:Anticancer drugs are often nonselective antiproliferative agents (cytotoxins) that preferentially kill dividing cells by attacking their DNA at some level. The lack of selectivity results in significant toxicity to noncancerous proliferating cells. These toxicities along with drug resistance exhibited by the solid tum...

journal_title：Current medicinal chemistry

authors： Singh Y,Palombo M,Sinko PJ

更新日期：2008-01-01 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：:Akuammiline alkaloids are a family of monoterpene indole alkaloids of renewed medicinal interest. These bases act as ligands for a heterogeneous group of molecular targets and, consequently, display a wide variety of pharmacological activities. For example, pseudoakuammigine (2) exhibits opioid activity in vivo, echit...

journal_title：Current medicinal chemistry

authors： Ramírez A,García-Rubio S

更新日期：2003-09-01 00:00:00

abstract：BACKGROUND:N-acetyl-cysteine (NAC) has shown widespread utility in different psychiatric disorders, including a beneficial role in schizophrenic patients. Although the replenishment of glutathione and the antioxidant activity of NAC have been suggested as the mechanisms that improve such a wide range of disorders, none...

journal_title：Current medicinal chemistry

authors： Martínez-Banaclocha M

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Patients with diabetes mellitus have an increased risk of mortality due to cardiovascular complications. Supplementation with specific sulphur-containing amino acids is rapidly emerging as a possible therapeutic adjuvant for diabetes and associated cardiovascular complications. OBSERVATIONS:It is well-known...

journal_title：Current medicinal chemistry

authors： Tappia PS,Adameova A,Dhalla NS

更新日期：2018-01-30 00:00:00

abstract：:The focus of this review is the cellular internalisation mechanism of nanostructured systems (NSs) and their endosomal escape for targeted drug delivery. Endocytosis is a cellular process of internalisation of different molecules and foreign microorganisms. It is currently being studied for drug delivery through nanos...

journal_title：Current medicinal chemistry

authors： Voltan AR,Alarcon KM,Fusco-Almeida AM,Soares CP,Mendes-Giannini MJS,Chorilli M

更新日期：2017-01-01 00:00:00

abstract：:Pyoverdine is the generic name given to a vast family of fluorescent green-yellowish pigments produced by Pseudomonas species. Pseudomonas aeruginosa is an opportunistic pathogen, particularly infecting humans with compromised natural defenses. These infections result in significantly higher morbidity, longer hospital...

journal_title：Current medicinal chemistry

authors： Cézard C,Farvacques N,Sonnet P

更新日期：2015-01-01 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：:The role of MRI in the armory of diagnostic modalities for the medicine of the forthcoming years largely depends on how chemistry will provide advanced tools to meet the medical needs. This review aims at outlining the most innovative approaches that have been undertaken in the recent history of MRI contrast agents fo...

journal_title：Current medicinal chemistry

authors： Terreno E,Dastrù W,Delli Castelli D,Gianolio E,Geninatti Crich S,Longo D,Aime S

更新日期：2010-01-01 00:00:00

abstract：:Bicarbonate (HCO₃⁻) membrane transport systems are crucial players in the physiology of several tissues. The molecular basis of HCO₃⁻ membrane transport is of major physiological relevance since this ion is involved in the establishment of intracellular and extracellular ionic composition, osmolariy and pH. The membra...

journal_title：Current medicinal chemistry

authors： Bernardino RL,Jesus TT,Martins AD,Sousa M,Barros A,Cavaco JE,Socorro S,Alves MG,Oliveira PF

更新日期：2013-01-01 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：:Although it has become acceptable that neuroretinal cells are also affected in diabetes, vascular lesions continue to be considered as the hallmarks of diabetic retinopathy. Animal models are essential for the understanding and treatment of human diabetic retinopathy, and the mouse is intensively used as a model becau...

journal_title：Current medicinal chemistry

authors： Ramos D,Carretero A,Navarro M,Mendes-Jorge L,Nacher V,Rodriguez-Baeza A,Ruberte J

更新日期：2013-01-01 00:00:00

abstract：:Acyclic nucleoside analogues bearing phosphonomethoxy residues in the side chain (ANP) attract much attention due to a very beneficial combination of biological properties. Intensive work of organic chemists during the last two decades resulted in a large panel of new compounds that were evaluated as potential antivir...

journal_title：Current medicinal chemistry

authors： Khandazhinskaya A,Yasko M,Shirokova E

更新日期：2006-01-01 00:00:00

abstract：:Glucagon-like peptide-1 (GLP-1) is an insulinotropic hormone secreted from endocrine cells in the gut mucosa in response to meal ingestion. It is an important incretin hormone; mice with a null mutation in the GLP-1 receptor gene develop glucose intolerance. In addition, it inhibits gastrointestinal secretion and moti...

journal_title：Current medicinal chemistry

authors： Holst JJ

更新日期：1999-11-01 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：: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：BACKGROUND:Numerous studies have reported sex and gender differences in the prevalence and treatment of cardiovascular diseases. However, sex differences in the therapy of hypertension have not been completely examined. OBJECTIVE:To estimate the gender-specific dissimilarity in outcomes among patients following antihy...

journal_title：Current medicinal chemistry

authors： Giorgini P,Sahebkar A,Stamerra CA,Raparelli V,Petrarca M,Grassi D,Ferri C,Di Giosia P

更新日期：2017-01-01 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：:Protein p53 is a key player in mitochondrial mediated apoptotic cell death and excess p53 activity has been implicated in many disease states such athrosclerosis, diabetes, osteoarthritis, Alzheimer's disease, Parkinson's disease, Huntington's disease, AIDS, P. falciparum and S. typhimurium infections. Thus, chemical ...

journal_title：Current medicinal chemistry

authors： Nayak SK,Panesar PS,Kumar H

更新日期：2009-01-01 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：:For many years the spotlight in drug discovery has been on a relatively small number of validated therapeutic target classes, such as G-protein coupled receptors and enzymes such as protein kinases, with well characterized enzymatic and cellular activities. However, with recent progress in genomics and proteomics, pro...

journal_title：Current medicinal chemistry

authors： De Giorgi M,Voisin-Chiret AS,Rault S

更新日期：2013-01-01 00:00:00

abstract：:Kinetoplastid and apicomplexan parasites comprise a group of protozoans responsible for human diseases, with a serious impact on human health and the socioeconomic growth of developing countries. Chemotherapy is the main option to control these pathogenic organisms and nucleotide metabolism is considered a promising a...

journal_title：Current medicinal chemistry

authors： Valente M,Vidal AE,González-Pacanowska D

更新日期：2019-01-01 00:00:00