Structure and ligand based drug design strategies in the development of novel 5- LOX inhibitors.

abstract：:Dimerization and oligomerization of G protein-coupled receptors (GPCRs), proposed almost 30 years ago, have crucial relevance for drug design. Indeed, formation of GPCR oligomers may affect the diversity and performance by which extracellular signals are transferred to G proteins in the process of receptor transductio...

journal_title：Current medicinal chemistry

authors： Kaczor AA,Selent J

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:In the last two decades, there have been significant technological advances in the early detection of brain tumors. However, no notable improvements have been observed in the treatment of Glioblastoma Multiforme (GBM), the most common brain neoplasm coupled with the worst prognosis. GBM is characterized by a...

journal_title：Current medicinal chemistry

authors： Arévalo ÁST,Erices JI,Uribe DA,Howden J,Niechi I,Muñoz S,Martín RS,Monrás CAQ

更新日期：2017-01-01 00:00:00

abstract：:The need for innovation in research is leading to an increased use of imaging biomarkers, which have shown to reduce timings and increase productivity, thus saving costs. PET and SPECT neurotransmission imaging has shown usefulness in the discovery and development of drugs for the central nervous system, providing uni...

journal_title：Current medicinal chemistry

authors： Catafau AM,Bullich S

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND:During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. However, accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monu...

journal_title：Current medicinal chemistry

authors： O Brien Z,Moghaddam MF

更新日期：2017-01-01 00:00:00

abstract：:Functioning of G protein-coupled receptors (GPCRs) is tightly linked to the membrane environment, but a molecular level understanding of the modulation of GPCR by membrane lipids is not available. However, specific receptor-lipid interactions as well as unspecific effects mediated by the bulk properties of the membran...

journal_title：Current medicinal chemistry

authors： Sadiq SK,Guixa-Gonzalez R,Dainese E,Pastor M,De Fabritiis G,Selent J

更新日期：2013-01-01 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：: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：:G protein-coupled receptor (GPCR) (also known as seven-transmembrane domain receptor) superfamily represents the largest protein family in the human genome. These receptors respond to various physiological ligands such as photons, odors, pheromones, hormones, ions, and small molecules including amines, amino acids to ...

journal_title：Current medicinal chemistry

authors： Yonezawa T,Kurata R,Yoshida K,Murayama MA,Cui X,Hasegawa A

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND:Since Signal Transducer and Activator of Transcription 3 (STAT3) is a transcription factor which plays an important role in multiple aspects of cancer, including progression and migration, and it is constitutively activated in various human tumors, STAT3 inhibition has emerged as a validated strategy for the...

journal_title：Current medicinal chemistry

authors： Gelain A,Mori M,Meneghetti F,Villa S

更新日期：2019-01-01 00:00:00

abstract：:The signal transducers and activators of transcription (STATs) include a class of cytoplasmic signaling proteins whose role in the regulation of cell growth and survival is mediated by phosphorylation of a critical tyrosine residue within the STAT protein. This occurs in response to cytokines and growth factors modula...

journal_title：Current medicinal chemistry

authors： Lavecchia A,Di Giovanni C,Novellino E

更新日期：2011-01-01 00:00:00

abstract：:Heme is an essential molecule with contradictory biological functions. In hemoproteins such as hemoglobin and cytochromes protein-bound heme is a prosthetic group serving physiological functions as a transporter for oxygen and electrons. On the other hand free heme can have deleterious effects by generating reactive o...

journal_title：Current medicinal chemistry

authors： Wijayanti N,Katz N,Immenschuh S

更新日期：2004-04-01 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：:The evidence seems to be growing in favor of the stem cell theory of cancer with the emergence of studies demonstrating the parallel mechanisms of self renewing pathways in stem cells and particular subsets of cancer cells. The finding of leukemia stem cells and subsequently breast cancer stem cells (BCSC) further sup...

journal_title：Current medicinal chemistry

authors： Nahas GR,Patel SA,Bliss SA,Rameshwar P

更新日期：2012-01-01 00:00:00

abstract：:The present paper summarizes the possible roles of frequent and unfavourable genetic variants in cerebrovascular disorders, such as stroke and leukoaraiosis. It also approaches the topic theoretically from functional and mathematical points of view, which can help make the accumulating data on genetic variants more un...

journal_title：Current medicinal chemistry

authors： Szolnoki Z

更新日期：2009-01-01 00:00:00

abstract：:Inosine 5'-monophosphate dehydrogenase (IMPDH) catalyzes the first committed step of guanosine 5'-monophosphate (GMP) biosynthesis, and thus regulates the guanine nucleotide pool, which in turn governs proliferation. Human IMPDHs are validated targets for immunosuppressive, antiviral and anticancer drugs, but as yet m...

journal_title：Current medicinal chemistry

authors： Hedstrom L,Liechti G,Goldberg JB,Gollapalli DR

更新日期：2011-01-01 00:00:00

abstract：:Cancer cells are permanently being selected for survival and proliferation. During this process, tumor cells often co-opt basic physiological mechanisms to protect themselves from toxic chemotherapy. One of these mechanisms is the overexpression of ATP-binding cassette (ABC) drug efflux pumps leading to multidrug resi...

journal_title：Current medicinal chemistry

authors： Lorendeau D,Dury L,Nasr R,Boumendjel A,Teodori E,Gutschow M,Falson P,Di Pietro A,Baubichon-Cortay H

更新日期：2017-01-01 00:00:00

abstract：:Benzamide riboside (BR) after anabolism to an analogue of NAD, was shown to inhibit the activity of NAD-dependent enzymes such as inosine 5'-monophosphate dehydrogenase (IMPDH), the rate limiting enzyme in de novo guanylate biosynthesis, and malate dehydrogenase which is involved in the citric cycle and respiratory ch...

journal_title：Current medicinal chemistry

authors： Polgar D,Gfatter S,Uhl M,Kassie F,Leisser C,Krupitza G,Grusch M

更新日期：2002-04-01 00:00:00

abstract：: ...

journal_title：Current medicinal chemistry

authors： Poplawski T

更新日期：2019-01-01 00:00:00

abstract：:Recent advances in endoscopic techniques such as capsule endoscopy have revealed that aspirin and other nonsteroidal antiinflammatory drugs (NSAIDs) often cause mucosal lesions not only in the upper gastrointestinal tract, but also in the small intestine in humans. Gastric and duodenal lesions caused by NSAIDs can be ...

journal_title：Current medicinal chemistry

authors： Satoh H,Takeuchi K

更新日期：2012-01-01 00:00:00

abstract：:To this point, efforts to develop therapeutic peptides for intracellular applications were guided by the perception that unmodified linear peptides are highly unstable and therefore structural modifications are required to reduce proteolytic breakdown. Largely, this concept is a consequence of the fact that most resea...

journal_title：Current medicinal chemistry

authors： Zuconelli CR,Brock R,Adjobo-Hermans MJW

更新日期：2017-01-01 00:00:00

abstract：BACKGROUND:With global increase in elderly population, modern societies must find strategies to reduce the consequences of aging process; thereby decreasing the incidence of age-related neurodegenerative diseases. Oxidative stress and recently inflammation, have been pointed out as the leading causes of brain aging. Th...

journal_title：Current medicinal chemistry

authors： Sarubbo F,Moranta D,Asensio VJ,Miralles A,Esteban S

更新日期：2017-01-01 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：:Nowadays, enzymatic therapy is a very promising line of treatment for many different diseases. There is a group of disorders and conditions, caused by fibrotic and scar processes and associated with the excessive accumulation of collagen that needs to be catabolized to normalize the connective tissue content. The huma...

journal_title：Current medicinal chemistry

authors： Shekhter AB,Balakireva AV,Kuznetsova NV,Vukolova MN,Litvitsky PF,Zamyatnin AA Jr

更新日期：2019-01-01 00:00:00

abstract：:Molecular recognition and ligand binding involving proteins underlie the most important life processes within the cell, such as substrate transport, catalysis, signal transmission, receptor trafficking, gene regulation, switching on and off of biochemical pathways. Despite recent successes in predicting the structures...

journal_title：Current medicinal chemistry

authors： Morra G,Genoni A,Neves MA,Merz KM Jr,Colombo G

更新日期：2010-01-01 00:00:00

abstract：:It is well recognised that increased levels of high density lipoprotein (HDL) protect against atherosclerosis and correlate with improved prognosis for vascular disease associated events. While many of the atheroprotective effects of HDL are ascribed to the ability to remove cholesterol from the vasculature through th...

journal_title：Current medicinal chemistry

authors： Murphy AJ,Chin-Dusting JP,Sviridov D,Woollard KJ

更新日期：2009-01-01 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：: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：:The neuropeptide substance P (SP) shows a widespread distribution in both the central and peripheral nervous systems and it is known that after binding to the neurokinin-1 (NK-1) receptors, SP regulates many biological functions in the central nervous system such as emotional behaviour, stress, depression, anxiety, em...

journal_title：Current medicinal chemistry

authors： Muñoz M,Coveñas R

更新日期：2011-01-01 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：:Fabry disease (FD) is an X-linked glycosphingolipid storage disorder caused by deficient activity of the lysosomal enzyme alpha-galactosidase A. This leads to a progressive accumulation of globotriaosylceramide (Gb3) in the lysosomes of different cells and tissues, causing principally ventricular hypertrophy, renal fa...

journal_title：Current medicinal chemistry

authors： Caballero L,Climent V,Hernández-Romero D,Quintanilla MA,de la Morena G,Marín F

更新日期：2010-01-01 00:00:00