The synthesis and antiviral properties of acyclic nucleoside analogues with a phosphonomethoxy fragment in the side chain.

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：: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：: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：BACKGROUND:Fatty liver, or steatosis, is a condition of excess accumulation of lipids, mainly under form of triglycerides (TG), in the liver, and it is the hallmark of non-alcoholic fatty liver disease (NAFLD). NAFLD is the most common liver disorder world-wide and it has frequently been associated with obesity, hyperl...

journal_title：Current medicinal chemistry

authors： Vergani L

更新日期：2019-01-01 00:00:00

abstract：:Chronic Obstructive Pulmonary Disease (COPD) is a progressive respiratory disorder characterized by irreversible chronic inflammation and airflow obstruction. It affects more than 64 million patients worldwide and it is predicted to become the third cause of death in the industrialized world by 2030. Currently availab...

journal_title：Current medicinal chemistry

authors： Pirozzi F,Ren K,Murabito A,Ghigo A

更新日期：2019-01-01 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：:Poisoning of DNA topoisomerase I is the mechanism by which camptothecins interfere with tumor growth. Although the clinical use of camptothecins has had a significant impact on cancer therapy, de novo or acquired clinical resistance to these drugs is common. Clinical resistance to camptothecins is still a poorly under...

journal_title：Current medicinal chemistry

authors： Beretta GL,Gatti L,Perego P,Zaffaroni N

更新日期：2013-01-01 00:00:00

abstract：:This review covers the compounds isolated from marine sponges with neuroprotective activities during the period between 1999 and 2014 based on their chemical structures, collections sites, sponge taxonomy and neuroprotective effects. These compounds were isolated from marine sponges collected from 18 countries, most o...

journal_title：Current medicinal chemistry

authors： Alghazwi M,Kan YQ,Zhang W,Gai WP,Yan XX

更新日期：2016-01-01 00:00:00

abstract：:COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of arachidonic acid to prostaglandins, played a pivotal role in inflammatory process. Different from other family members, COX-2 was barely detectable in normal physiological conditions and highly inducible during acute inflammatory response ...

journal_title：Current medicinal chemistry

authors： Cui J,Jia J

更新日期：2020-09-17 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：:Cholecystokinin (CCK) is an important neuro-intestinal peptide hormone produced by the enteroendocrine I-cells in the upper part of small intestine. Protein- and fat-enriched food plays an important role in triggering CCK secretion from the intestine. Carbohydrates stimulate only small amounts of CCK release. The CCK-...

journal_title：Current medicinal chemistry

authors： Wang HH,Portincasa P,Wang DQ

更新日期：2019-01-01 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：:Breakdown of glucose under physiological conditions gives rise to glucose degradation products (GDPs). GDPs are also formed during heat sterilization of glucose-containing peritoneal dialysis fluids (PD-fluids). In PD-fluids GDPs have been shown in many different in vitro assays to be responsible for adverse effects s...

journal_title：Current medicinal chemistry

authors： Ortiz A,Wieslander A,Linden T,Santamaria B,Sanz A,Justo P,Sanchez-Niño MD,Benito A,Kjellstrand P

更新日期：2006-01-01 00:00:00

abstract：BACKGROUND:Excessive norepinephrine (NE) release in the ischemic heart elicits severe and often lethal arrhythmias. Resident cardiac mast cells synthesize and store active renin, which is released upon degranulation, causing the activation of a local cardiac renin-angiotensin system (RAS) responsible for NE release and...

journal_title：Current medicinal chemistry

authors： Marino A,Levi R

更新日期：2018-01-01 00:00:00

abstract：:Nanomedicine is certainly one of the scientific and technological challenges of the coming years. In particular, biodegradable nanoparticles formulated from poly (D,L-lactide-co-glycolide) (PLGA) have been extensively investigated for sustained and targeted delivery of different agents, including recombinant proteins,...

journal_title：Current medicinal chemistry

authors： Tosi G,Bortot B,Ruozi B,Dolcetta D,Vandelli MA,Forni F,Severini GM

更新日期：2013-01-01 00:00:00

abstract：:Giving a glance to the report of Wound Care Market by Product updated in 2017, we can see that wound care market is expected to reach USD 22.01 billion by 2022 from USD 18.35 billion at a CAGR of 3.7%. Numerous factors are driving the growth of this market, including the increasing prevalence of chronic wounds and acu...

journal_title：Current medicinal chemistry

authors： Polerà N,Badolato M,Perri F,Carullo G,Aiello F

更新日期：2019-01-01 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：:The glomerulonephritides are a collection of separate diseases with differing pathogeneses that collectively are common and important causes of renal disease. Effective, non-toxic immunomodulatory treatments for glomerulonephritis are lacking. This review will focus on our understanding of the role of leukocytes in im...

journal_title：Current medicinal chemistry

authors： Kitching AR,Holdsworth SR,Hickey MJ

更新日期：2008-01-01 00:00:00

abstract：:Recent results using animal models of inflammatory skin conditions have shown that blockers of the voltage-gated potassium channel, Kv1.3 hold great promise for clinical utility. Kv1.3 blockers act as immunosuppressants by modulating the various subsets of inflammatory T and B cells involved in autoimmune disorders. W...

journal_title：Current medicinal chemistry

authors： Nguyen W,Howard BL,Neale DS,Thompson PE,White PJ,Wulff H,Manallack DT

更新日期：2010-01-01 00:00:00

abstract：:Protein kinase B/AKT plays a central role in cancer. The serine/threonine kinase is overexpressed or constitutively active in many cancers and has been validated as a therapeutic target for cancer treatment. However, targeting the kinase activity has revealed itself to be a challenge due to non-selectivity of the comp...

journal_title：Current medicinal chemistry

authors： Meuillet EJ

更新日期：2011-01-01 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：:Nature as a source of inspiration has been shown to have a great beneficial impact on the development of new computational methodologies. In this scenario, analyses of the interactions between a protein target and a ligand can be simulated by biologically inspired algorithms (BIAs). These algorithms mimic biological s...

journal_title：Current medicinal chemistry

authors： Heberlé G,de Azevedo WF Jr

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Glioblastoma multiforme (GBM) is the most common malignant primary brain tumor, with an incidence of 3.19 cases per 100,000 person years and remarkably poor prognosis showing a 5-year survival rate of 4-5%, and only a 26-33% survival rate at 2 years in clinical trials. OBJECTIVE:In this paper, we review the...

journal_title：Current medicinal chemistry

authors： Batash R,Asna N,Schaffer P,Francis N,Schaffer M

更新日期：2017-01-01 00:00:00

abstract：:Ornithine transcarbamylase (OTC; EC 2.1.3.3) is a one-carbon-unit transferring enzyme that synthesizes citrulline using ornithine and carbamoylphosphate as substrates. It is involved in the metabolic transformation of arginine and proline, and it participates in the urea cycle in vertebrates and in the formation of pu...

journal_title：Current medicinal chemistry

authors： Díaz-Muñoz M,Hernández-Muñoz R

更新日期：2010-01-01 00:00:00

abstract：:Amyloid beta peptide (Aβ) is recognised as a main feature of Alzheimer's disease (AD). Increasing evidence suggests that small soluble oligomers of Aβ are the toxic form of the peptide and may instigate AD. Different factors including some key residues within Aβ molecule, the cell membrane, prion protein and metals pl...

journal_title：Current medicinal chemistry

authors： Jamasbi E,Wade JD,Separovic F,Hossain MA

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

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：:Histone Deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis, and cell cycle arrest in cancer cells. Recently, their use has been clinically validated in cancer patients resulting in the approval b...

journal_title：Current medicinal chemistry

authors： Cappellacci L,Perinelli DR,Maggi F,Grifantini M,Petrelli R

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Post-translational modification (PTM) crosstalk is a young research field. However, there is now evidence of the extraordinary characterization of the different proteoforms and their interactions in a biological environment that PTM crosstalk studies can describe. Besides gene expression and phosphorylation ...

journal_title：Current medicinal chemistry

authors： Hernandez-Valladares M,Wangen R,Berven FS,Guldbrandsen A

更新日期：2019-01-01 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