Pharmacophore design of p38α MAP kinase inhibitors with either 2,4,5-trisubstituted or 1,2,4,5-tetrasubstituted imidazole scaffold.

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：BACKGROUND:Nonalcoholic fatty liver disease (NAFLD), the most common chronic liver disease, is the leading cause of cryptogenic cirrhosis and has consistently been implicated in related metabolic disorders, such as dyslipidemia and type 2 diabetes (T2D). However, the pathogenesis of NAFLD remains to be elucidated, and ...

journal_title：Current medicinal chemistry

authors： Xu G,Huang K,Zhou J

更新日期：2018-01-01 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：:Among naturally occurring isoflavones, soy isoflavones are an important class with various biological activities. Due to their phytoestrogenic structure, their effects on the brain are profound thus making the neurobiological effects of these compounds an active area of research. One such compound is daidzein, which h...

journal_title：Current medicinal chemistry

authors： Ahmed T,Javed S,Tariq A,Budzyńska B,D'Onofrio G,Daglia M,Nabavi SF,Nabavi SM

更新日期：2017-01-01 00:00:00

abstract：:Chymase stored in mast cells activates matrix metalloproteinase (MMP)-9, which may relate to the progression of sinusoidal obstruction syndrome (SOS). We investigated the preventive effect of a chymase inhibitor, TY-51469, on monocrotaline-induced SOS in hamsters. Hamsters were orally administrated with a single dose ...

journal_title：Current medicinal chemistry

authors： Masubuchi S,Komeda K,Takai S,Jin D,Tashiro K,Li ZL,Otsuki Y,Okamura H,Hayashi M,Uchiyama K

更新日期：2013-01-01 00:00:00

abstract：:Prothymosin alpha (ProTα) is a highly acidic polypeptide, ubiquitously expressed in almost all mammalian cells and tissues and consisting of 109 amino acids in humans. ProTα is known to act both, intracellularly, as an anti-apoptotic and proliferation mediator, and extracellularly, as a biologic response modifier medi...

journal_title：Current medicinal chemistry

authors： Karachaliou CE,Kalbacher H,Voelter W,Tsitsilonis OE,Livaniou E

更新日期：2020-01-01 00:00:00

abstract：:The vascular system distributes oxygen and nutrients to all tissues in the body. Additionally, the vascular system also functions in hosting and instructing tissue-specific stem and progenitor cells. Both cell- or blood-derived signals from the vascular system regulate stem cell properties in health and disease. Studi...

journal_title：Current medicinal chemistry

authors： Schildge S,Bohrer C,Pfurr S,Mammadzada K,Schachtrup K,Schachtrup C

更新日期：2014-01-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs) are zinc-endopeptidases responsible for degradation of the extracellular matrix (ECM) components including basement membrane collagen, interstitial collagen, fibronectin, and various proteoglycans, during normal remodeling and repair processes. The turnover and remodeling of ECM must b...

journal_title：Current medicinal chemistry

authors： Oikonomidi S,Kostikas K,Tsilioni I,Tanou K,Gourgoulianis KI,Kiropoulos TS

更新日期：2009-01-01 00:00:00

abstract：:From the discovery of Endothelial Progenitor Cells (EPC), these bone marrowderived precursors have been placed as crucial mediators of the endothelial repair. Accordingly, altered levels and function of EPC have been found in different scenarios of CV risk. Despite the fact that EPC exhibit important characteristics w...

journal_title：Current medicinal chemistry

authors： Rodríguez-Carrio J,López P,Suárez A

更新日期：2018-01-01 00:00:00

abstract：:Dendritic cells (DCs) are the most powerful antigen-presenting cells which link the innate and adaptive immune responses. Depending on the context DCs initiate the immune responses or contribute to immune tolerance. Any disturbance in their phenotypes and functions may initiate inflammatory or autoimmune diseases. Hen...

journal_title：Current medicinal chemistry

authors： Rahimi K,Hassanzadeh K,Khanbabaei H,Haftcheshmeh SM,Ahmadi A,Izadpanah E,Mohammadi A,Sahebkar A

更新日期：2020-05-14 00:00:00

abstract：:AG490 is a tyrphostin originally described as a Janus Activated Kinase (JAK) 2 inhibitor. AG490 also inhibits epidermal growth factor receptor (EGFR) and guanylyl cyclases (GC). More recently, AG490 was associated with oxidative stress protection in experimental acute kidney injury models. We now show that AG490 is al...

journal_title：Current medicinal chemistry

authors： Fernández-Sánchez R,Berzal S,Sánchez-Niño MD,Neria F,Gonçalves S,Calabia O,Tejedor A,Calzada MJ,Caramelo C,Deudero JJ,Ortiz A

更新日期：2012-01-01 00:00:00

abstract：:Coeliac disease is a multifactorial disease characterized by a dysregulated immune response to ingested wheat gluten and related cereal proteins. With an incidence of about 1% of the general population, it is considered the most common food intolerance disorder. The mainstay of coeliac disease treatment is strict life...

journal_title：Current medicinal chemistry

authors： Esposito C,Caputo I,Troncone R

更新日期：2007-01-01 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：: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：:Medical devices are important diagnosis and therapy tools for several diseases which include a wide range of products. Technological advances in this area have been proposed to reduce adverse complication incidences. New technologies and manufacturing processes, as well as the development of new materials or medical d...

journal_title：Current medicinal chemistry

authors： Dutra GVS,Neto WS,Dutra JPS,Machado F

更新日期：2020-01-01 00:00:00

abstract：:Sulfonyl group-containing compounds constitute an important class of therapeutical agents in medicinal chemistry presumably because of the tense chemical structure and functionality of the sulfonyl, which could not only form hydrogen bonding interactions with active site residues of biological targets but also, as inc...

journal_title：Current medicinal chemistry

authors： Chen X,Hussain S,Parveen S,Zhang S,Yang Y,Zhu C

更新日期：2012-01-01 00:00:00

abstract：:Many non-cardiovascular drugs of common clinical use cause, as an unwanted accessory property, the prolongation of the cardiac repolarisation process, due to the block of the HERG (Human Ether-a-go-go Related Gene) potassium channel, responsible for the repolarising I(Kr) current. This delayed cardiac repolarisation p...

journal_title：Current medicinal chemistry

authors： Testai L,Bianucci AM,Massarelli I,Breschi MC,Martinotti E,Calderone V

更新日期：2004-10-01 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：:alpha-Galactosylceramide (alpha-GalCer), is a glycolipid which has been identified as a ligand recognized by a special group of immune T cells, known as invariant NKT cells. alpha-GalCer can powerfully activate invariant NKT cells to produce immunoregulatory cytokines, including interferon-gamma and IL-4, and thereby ...

journal_title：Current medicinal chemistry

authors： Hayakawa Y,Godfrey DI,Smyth MJ

更新日期：2004-01-01 00:00:00

abstract：:Thrombomodulin (TM) is a membrane protein mainly expressed by endothelial cells. It is part of the anticoagulant protein C system but recently several effects were discovered which occur independently of protein C activation. TM binds thrombin and promotes the cleavage of protein C and the thrombin activatable fibrino...

journal_title：Current medicinal chemistry

authors： Wenzel J,Assmann JC,Schwaninger M

更新日期：2014-01-01 00:00:00

abstract：:Antisynthetase syndrome is a group of closely related rare diseases which clinically manifest with inflammatory myopathies, interstitial lung disease, inflammatory arthritis, skin hyperkeratosis (mechanic’s hands) and Raynaud phenomenon. The pathophysiology of antisynthetase syndrome is not entirely understood, but ge...

journal_title：Current medicinal chemistry

authors： Mirrakhimov AE

更新日期：2015-05-13 00:00:00

abstract：:Aberrant signaling caused by mutations in the RAS-RAF-MEK-ERK pathway and its upstream activators critically contributes to human tumor development. Strategies, which aim at inhibiting hyperactive signaling molecules, appear conceptually straight forward, but their translation into clinical practice has been hampered ...

journal_title：Current medicinal chemistry

authors： Zebisch A,Czernilofsky AP,Keri G,Smigelskaite J,Sill H,Troppmair J

更新日期：2007-01-01 00:00:00

abstract：:A dramatical decline in human male reproductive function has been reported for the past 20 years. Many recent epidemiological, clinical and experimental findings suggest that the reproductive dysfunction could result from prenatal and neonatal chemical compound exposure. Even if numerous studies argue for a relationsh...

journal_title：Current medicinal chemistry

authors： Gilleron J,Malassiné A,Carette D,Segretain D,Pointis G

更新日期：2011-01-01 00:00:00

abstract：:A large number of children in the autism spectrum disorder suffer from gastrointestinal (GI) conditions, such as constipation and diarrhea. Clostridium bolteae is a part of a set of pathogens being regularly detected in the stool samples of hosts affected by GI and autism symptoms. Accompanying studies have pointed ou...

journal_title：Current medicinal chemistry

authors： Pequegnat B,Monteiro MA

更新日期：2019-01-01 00:00:00

abstract：:In recent years there has been a growing interest in computer-based screening. One of the driving forces has been the increased efficiency of protein crystallography leading to the real possibility of using structure-based design as a significant contributor to the discovery of novel ligands. In 1957 after 22 years of...

journal_title：Current medicinal chemistry

authors： Glen RC,Allen SC

更新日期：2003-05-01 00:00:00

abstract：:Neonatal brain hemorrhage (NBH) of prematurity is an unfortunate consequence of preterm birth. Complications result in shunt dependence and long-term structural changes such as posthemorrhagic hydrocephalus, periventricular leukomalacia, gliosis, and neurological dysfunction. Several animal models are available to stu...

journal_title：Current medicinal chemistry

authors： Lekic T,Klebe D,Poblete R,Krafft PR,Rolland WB,Tang J,Zhang JH

更新日期：2015-01-01 00:00:00

abstract：:The deposition of β-amyloid (Aβ) plaques in the parenchymal and cortical brain is accepted as the main pathological hallmark of Alzheimer's disease (AD). According to the amyloid cascade hypothesis, the Aβ deposition in the brain appears to be a good diagnostic biomarker for AD and may also be a good predictive biomar...

journal_title：Current medicinal chemistry

authors： Cui M

更新日期：2014-01-01 00:00:00

abstract：:Cu(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) is often utilized in medicinal chemistry to make the triazole moiety as it acts as a non-classical bioisostere of the peptide bond. This useful technique can also be applied in the fragment-based assembly of molecular libraries for high-throughput screening. This mini...

journal_title：Current medicinal chemistry

authors： Fabbrizzi P,Menchi G,Guarna A,Trabocchi A

更新日期：2014-01-01 00:00:00

abstract：:Protein C is a vitamin K-dependent anticoagulant serine protease zymogen in plasma which upon activation by the thrombin-thrombomodulin complex down-regulates the coagulation cascade by degrading cofactors Va and VIIIa by limited proteolysis. In addition to its anticoagulant function, activated protein C (APC) also bi...

journal_title：Current medicinal chemistry

authors： Rezaie AR

更新日期：2010-01-01 00:00:00

abstract：:O-Prenyl secondary metabolites (3,3-dimethylallyl, geranyl-, farnesyl- and related biosynthetic derivatives) represent a class of rarely occurring natural products. In the last two decades such compounds have been found to exert promising and effective pharmacological activities, mainly in terms of anti-cancer propert...

journal_title：Current medicinal chemistry

authors： Genovese S,Fiorito S,Epifano F,Taddeo VA

更新日期：2015-01-01 00:00:00