Fighting tumor cell survival: advances in the design and evaluation of Pim inhibitors.

abstract：:We apply noval techniques, the Scaling Index Method (SIM), which reveals local topology of the structure, and the Minkowski Functionals (MF), which provide four global topological characteristics, to assess strength of the trabecular network of the human bone. We compare capabilities of these methods with the standard...

journal_title：Current medicinal chemistry

authors： Sidorenko I,Monetti R,Bauer J,Mueller D,Rummeny E,Eckstein F,Matsuura M,Lochmueller EM,Zysset P,Raeth C

更新日期：2011-01-01 00:00:00

abstract：:The development of new drugs with potential therapeutic applications is one of the most complex and difficult process in the pharmaceutical industry. Millions of dollars and man-hours are devoted to the discovery of new therapeutical agents. As, the activity of a drug is the result of a multitude of factors such as bi...

journal_title：Current medicinal chemistry

authors： Ooms F

更新日期：2000-02-01 00:00:00

abstract：:Proteomics has unraveled important questions in the biology of cardiovascular disease and holds even greater promise for the development of novel diagnostic and prognostic biomarkers. This approach may establish early detection strategies, and monitor responses to therapies. Technological advances (most notably blue n...

journal_title：Current medicinal chemistry

authors： Balestrieri ML,Giovane A,Mancini FP,Napoli C

更新日期：2008-01-01 00:00:00

abstract：:Protein tyrosine phosphatases (PTPs) are crucial regulators for numerous biological processes in nature. The dysfunction and overexpression of many PTP members have been demonstrated to cause fatal human diseases such as cancers, diabetes, obesity, neurodegenerative diseases and autoimmune disorders. In the past decad...

journal_title：Current medicinal chemistry

authors： He XP,Xie J,Tang Y,Li J,Chen GR

更新日期：2012-01-01 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：BACKGROUND:The genus Achillea L. is rich in bioactive sesquiterpenes and flavonoids; most of the studied species exhibit several biological activities and are used as emmenagogue, wound healing and analgesic agents. Some species are also used in local folklore medicine. OBJECTIVE:Following a literature survey, we disc...

journal_title：Current medicinal chemistry

authors： Papakosta K,Grafakou ME,Barda C,Kostopoulos IV,Tsitsilonis O,Skaltsa H

更新日期：2020-01-01 00:00:00

abstract：:During this past decade, science and engineering have seen a rapid increase in interest for nanoscale materials with dimensions less than 100 nm, which lie in the intermediate state between atoms and bulk (solid) materials. Their attributes are significantly altered relative to the corresponding bulk materials as they...

journal_title：Current medicinal chemistry

authors： Banerjee R,Katsenovich Y,Lagos L,McIintosh M,Zhang X,Li CZ

更新日期：2010-01-01 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：:Galectins form a family of carbohydrate-binding proteins defined by their affinity for beta-galactosides containing glycoconjugates. The carbohydrate recognition domain (CRD) is responsible for the specificity of galectins for saccharides. This binding may result in modulated cell proliferation, cell death and cell mi...

journal_title：Current medicinal chemistry

authors： Ingrassia L,Camby I,Lefranc F,Mathieu V,Nshimyumukiza P,Darro F,Kiss R

更新日期：2006-01-01 00:00:00

abstract：:On December 23rd, 1971, President Richard Nixon signed the National Cancer Act and invested more than $ 100 million "to launch an intensive campaign to find a cure for cancer". Today, despite these considerable efforts, cancer still remains a very aggressive silent killer all over the world. Moreover, over the last de...

journal_title：Current medicinal chemistry

authors： Orlikova B,Diederich M

更新日期：2012-01-01 00:00:00

abstract：:Advanced enteropancreatic (EP) neuroendocrine tumors (NETs) can be treated with several different therapies, including chemotherapy, biotherapy, and locoregional treatments. Over the last few decades, impressive progress has been made in the biotherapy field. Three main druggable molecular targets have been studied an...

journal_title：Current medicinal chemistry

authors： Fazio N,Scarpa A,Falconi M

更新日期：2014-01-01 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：: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：:Symmetry plays a crucial role in a variety of biological processes. For instance, many protein receptors, upon activation, dimerize to its active form and subsequently produce its biological action. Hence, there is a renewal of curiosity for the synthesis of dimeric molecules (or bivalent ligands) capable, not only to...

journal_title：Current medicinal chemistry

authors： Bérubé G

更新日期：2006-01-01 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：:Nowadays, fast and sensitive methods for biomarkers detection exist, but the performance of most of them still rely centralized laboratory testing. The development of small, fast and simple to use medical devices that can help in making diagnosis accurate and with low-invasiveness is now a major challenge for nanotech...

journal_title：Current medicinal chemistry

authors： Bedin C,Crotti S,Tasciotti E,Agostini M

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Since the serendipitous discovery of the antitumor activity of cisplatin there has been a continuous surge in studies aimed at the development of new cytotoxic metal complexes. While the majority of these complexes have been designed to interact with nuclear DNA, other targets for anticancer metallodrugs att...

journal_title：Current medicinal chemistry

authors： Erxleben A

更新日期：2019-01-01 00:00:00

abstract：:Microcin J25 (MccJ25) is a plasmid-encoded peptide of 21 L-amino acids (G1-G-A-G-H5-V-P-E-Y-F10-V-G-I-G-T15-P-I-S-F-Y20-G), excreted to the medium by an Escherichia coli strain. MccJ25 is active on Gram-negative bacteria related to the producer strain, including some pathogenic strains. The four-plasmid genes mcjABCD,...

journal_title：Current medicinal chemistry

authors： Vincent PA,Morero RD

更新日期：2009-01-01 00:00:00

abstract：:Osteogenic peptides are, or have potential to be, therapies for the treatment of osteoporosis, fracture repair, and repair of loosened bone implants. Human parathyroid hormone has been approved for the treatment of post-menopausal osteoporosis. Constrained analogs of PTH and the parathyroid-hormone related peptide (PT...

journal_title：Current medicinal chemistry

authors： Willick GE,Morley P,Whitfield JF

更新日期：2004-11-01 00:00:00

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：:Obesity and metabolic syndrome represent major public health problems, and are the biggest preventable causes of death worldwide. Obesity is the leading risk factor for type 2 diabetes mellitus (T2DM), cardiovascular diseases and non-alcoholic fatty liver disease. Obesity-associated insulin resistance, which is charac...

journal_title：Current medicinal chemistry

authors： Panzhinskiy E,Ren J,Nair S

更新日期：2013-01-01 00:00:00

abstract：:Transglutaminases (TGases) are enzymes which catalyze the cross linking of a glutaminyl residue of a protein/peptide substrate to a lysyl residue of a protein/peptide co-substrate with the formation of an N-gamma-(epsilon-L-glutamyl)-L-lysine [GGEL] cross link (isopeptidic bond) and the concomitant release of ammonia....

journal_title：Current medicinal chemistry

authors： Martin A,Romito G,Pepe I,De Vivo G,Merola MR,Limatola A,Gentile V

更新日期：2006-01-01 00:00:00

abstract：:Within the pharmaceutical industry, the ultimate source of continuing profitability is the unremitting process of drug discovery. To be profitable, drugs must be marketable: legally novel, safe and relatively free of side effects, efficacious, and ideally inexpensive to produce. While drug discovery was once typified ...

journal_title：Current medicinal chemistry

authors： Hattotuwagama CK,Davies MN,Flower DR

更新日期：2006-01-01 00:00:00

abstract：BACKGROUND:Numerous studies have demonstrated that halogenated agents elicit myocardial conditioning effects when adminis-tered perioperatively in cardiac surgery. Recent evidence has been published of the benefits of maintaining exposure to halogenated agents during the early postoperative period. The enzymatic mechan...

journal_title：Current medicinal chemistry

authors： Guerrero Orriach JL,Escalona Belmonte JJ,Ramirez Aliaga M,Ramirez Fernandez A,Rodriguez Capitan MJ,Quesada Muñoz G,Raigón Ponferrada A,Alcaide Torres J,Santiago-Fernandez C,Matute Gonzalez E,Rubio Navarro M,Bautista R,Gómez Maldo

更新日期：2020-10-01 00:00:00

abstract：:Small interfering RNA (siRNA) constitutes an excellent way of knocking down genes. However, it requires the use of delivery systems to reach the target cells, especially to neuronal cells. Dendrimers are one of the most widely used synthetic nanocarriers for siRNA delivery. However, due to the complexity of the dendri...

journal_title：Current medicinal chemistry

authors： Pavan GM,Monteagudo S,Guerra J,Carrión B,Ocaña V,Rodríguez-Lopez J,Danani A,Pérez-Martínez FC,Ceña V

更新日期：2012-01-01 00:00:00

abstract：:Genito-urinary malignancies (prostate, bladder, renal and testicular cancers) rank high among human tumors with an incidence that varies with age and organ involvement. Prostate cancer is the most commonly detected male cancer followed by bladder and kidney cancers, less frequent in women. Testicular cancer, although ...

journal_title：Current medicinal chemistry

authors： Cantile M,Franco R,Schiavo G,Procino A,Cindolo L,Botti G,Cillo C

更新日期：2011-01-01 00:00:00

abstract：:The stilbene scaffold is a basic element for a number of biologically active natural and synthetic compounds, and it is considered as a privileged structure. Stilbenes exemplified by resveratrol, combretastatin A-4 and pterostilbene are of significant interest for drug research and development because of their potenti...

journal_title：Current medicinal chemistry

authors： Giacomini E,Rupiani S,Guidotti L,Recanatini M,Roberti M

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:The sterile alpha motif (Sam) domain is a small helical protein module, able to undergo homo- and hetero-oligomerization, as well as polymerization, thus forming different types of protein architectures. A few Sam domains are involved in pathological processes and consequently, they represent valuable target...

journal_title：Current medicinal chemistry

authors： Vincenzi M,Mercurio FA,Leone M

更新日期：2020-01-01 00:00:00

abstract：:Snake venoms are natural sources of biologically active molecules that are able to act selectively and specifically on different cellular targets, modulating physiological functions. Thus, these mixtures, composed mainly of proteins and peptides, provide ample and challenging opportunities and a diversified molecular ...

journal_title：Current medicinal chemistry

authors： Almeida JR,Resende LM,Watanabe RK,Carregari VC,Huancahuire-Vega S,da S Caldeira CA,Coutinho-Neto A,Soares AM,Vale N,de C Gomes PA,Marangoni S,de A Calderon L,Da Silva SL

更新日期：2017-01-01 00:00:00

abstract：BACKGROUND:Histone deacetylases (HDAC) are an important class of enzymes that play a pivotal role in epigenetic regulation of gene expression that modifies the terminal of core histones leading to remodelling of chromatin topology and thereby controlling gene expression. HDAC inhibitors (HDACi) counter this action and ...

journal_title：Current medicinal chemistry

authors： Sultana F,Manasa KL,Shaik SP,Bonam SR,Kamal A

更新日期：2019-01-01 00:00:00