Privileged structures as leads in medicinal chemistry.

abstract：:Synthetic compounds with a tri- and tetra-substituted imidazole scaffold are known as selective inhibitors of the p38 mitogen-activated protein (MAP) kinase responsible for proinflammatory cytokine release. The scope is to review the literature describing their design, synthesis and activity studies. To date a great p...

journal_title：Current medicinal chemistry

authors： Scior T,Domeyer DM,Cuanalo-Contreras K,Laufer SA

更新日期：2011-01-01 00:00:00

abstract：:RNA aptamers are non-coding small RNAs that bind to their cognate targets with high specificity and affinity. They are generally identified by iterative rounds of in vitro selection termed SELEX (Systemic Evolution of Ligands by Exponential Enrichment). Similar to antibodies, they can inhibit, modulate and disrupt the...

journal_title：Current medicinal chemistry

authors： Li Y,Wu H,Niu Y,Hu Y,Li Q,Cao C,Cai J

更新日期：2013-01-01 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：:Various human tumors preferentially metastasize by lymphatic route and lymphovascular invasion predicts lymph node metastasis. In this review article, we will summarize recent literature data concerning lymphangiogenesis, focusing on tumor lymphangiogenesis. In detail, we try to answer some important questions related...

journal_title：Current medicinal chemistry

authors： Raica M,Ribatti D

更新日期：2010-01-01 00:00:00

abstract：:Correct QSAR analysis requires reliable measured or calculated logP values, being logP the most frequently utilized and most important physico-chemical parameter in such studies. Since the publication of theoretical fundamentals of logP prediction, many commercial software solutions are available. These programs are a...

journal_title：Current medicinal chemistry

authors： Eros D,Kövesdi I,Orfi L,Takács-Novák K,Acsády G,Kéri G

更新日期：2002-10-01 00:00:00

abstract：:Inosine monophosphate dehydrogenase (IMPDH) catalyzes the conversion of IMP to XMP with the concomitant reduction of NAD to NADH. This reaction is the rate-limiting step in guanine nucleotide biosynthesis. IMPDH is a proven target for immunosuppressive, anticancer and antiviral chemotherapy, and may also be a target f...

journal_title：Current medicinal chemistry

authors： Hedstrom L

更新日期：1999-07-01 00:00:00

abstract：:Obesity is a chronic disease characterized by the accumulation of excess adipose tissue associated with an increased risk of multiple morbidities and mortality. At the present time, only three drugs have been approved by the Food and Drug Administration (FDA) for the treatment of obesity. Agonists and antagonists of s...

journal_title：Current medicinal chemistry

authors： Rivera G,Bocanegra-García V,Galiano S,Cirauqui N,Ceras J,Pérez S,Aldana I,Monge A

更新日期：2008-01-01 00:00:00

abstract：:Targeted therapy has been recently highlighted due to the reduction of side effects and improvement in overall efficacy and survival to different types of cancers. Considering the approval of many monoclonal antibodies in the last twenty years, cancer treatment can be accomplished by the combination of monoclonal anti...

journal_title：Current medicinal chemistry

authors： Petrilli R,Pinheiro DP,de Cássia Evangelista de Oliveira F,Galvão GF,Marques LGA,Lopez RFV,Pessoa C,Eloy JO

更新日期：2020-05-25 00:00:00

abstract：:Obesity, associated with a series of complications such as diabetes, hypertension, and heart disease, is a great threat to human health and leads to increased morbidity and mortality. Despite the presence of anti-obesity agents on the market, the application of these drugs is limited because of their typical side effe...

journal_title：Current medicinal chemistry

authors： Qiu Y,Yu H,Zeng R,Guo S,Daniyal M,Deng Z,Wang A,Wang W

更新日期：2020-01-01 00:00:00

abstract：:Thalidomide (N-alpha-phthalimidoglutarimide) was used widely as a hypnotic/sedative agent in the late 1950s and the early 1960s, but had to be withdrawn from the market because of its severe teratogenicity. In spite of this, there has been a resurgence of interest in the drug in recent years due to its potential usefu...

journal_title：Current medicinal chemistry

authors： Hashimoto Y

更新日期：1998-06-01 00:00:00

abstract：:The human body is composed of 60 trillion cells, which have their origin in a fertilized egg. During development, the potential of a cell or tissue can be achieved by environmental manipulation. Then, what molecular determinants underlie or accompany the potential of the cells? To obtain a broader understanding of the...

journal_title：Current medicinal chemistry

authors： Toyoda M,Hamatani T,Okada H,Matsumoto K,Saito H,Umezawa A

更新日期：2010-01-01 00:00:00

abstract：:Poly(aminoester) dendrimers are expected to hold great promise as biodegradable nanocarriers for drug delivery due to their advantageous properties allowing their biodegradability, potentially lower toxicity and possibility of diverse chemical conjugations. The synthetic strategies for constructing such dendrimers inc...

journal_title：Current medicinal chemistry

authors： Wang Y,Quelever G,Peng L

更新日期：2012-01-01 00:00:00

abstract：:Normal somatic stem cells (SC) are naturally resistant to chemotherapeutic agents due to their expression of various membrane transporter molecules (such as MDR-1), detoxifying enzymes and DNA repair proteins. In addition, they also have a slow rate of cell turnover and therefore escape from chemotherapeutic agents th...

journal_title：Current medicinal chemistry

authors： Gangemi R,Paleari L,Orengo AM,Cesario A,Chessa L,Ferrini S,Russo P

更新日期：2009-01-01 00:00:00

abstract：:Over the past few decades, remarkable advances have been achieved in cancer therapy, including chemotherapeutic agents, their mode of application and more broader therapeutic strategies. Promising new therapeutic targets have emerged in the past ten years as a result of recent advances in our understanding of the path...

journal_title：Current medicinal chemistry

authors： Dobashi Y,Takehana T,Ooi A

更新日期：2003-12-01 00:00:00

abstract：:APN is an important zinc dependent metallo-exopeptidase; it has been considered as a suitable target for anti-cancer drug design. In this review we focus on the most effective and the most promising inhibitors of aminopeptidase N. Their binding modes to the enzyme, the attempt to explain the origin of the inhibitory a...

journal_title：Current medicinal chemistry

authors： Zhang X,Xu W

更新日期：2008-01-01 00:00:00

abstract：:Bipolar disorder (BD) is a long-term illness with mood swings which are characterized by recurrent episodes of mania/hypomania and depression, with variable interpolations of relatively asymptomatic periods, called euthymic, in which, however, some psychopathological symptoms may persist. Although mood stabilizers, su...

journal_title：Current medicinal chemistry

authors： Musenga A,Saracino MA,Sani G,Raggi MA

更新日期：2009-01-01 00:00:00

abstract：:Inflammation is a local or systemic tissue reaction caused by external or internal stimuli with the objective to remove the noxa, inhibit its further dissemination and eventually repair damaged tissue. Blood vessels and perivascular connective tissue are important regulators of the inflammatory process. After a short ...

journal_title：Current medicinal chemistry

authors： Wilting J,Becker J,Buttler K,Weich HA

更新日期：2009-01-01 00:00:00

abstract：:The efficacy of classical and molecular therapies in cancer is hampered by the occurrence of primary (intrinsic) and secondary (acquired) refractoriness of tumours to selected therapeutic regimens. Nevertheless, the increased knowledge of the genetic, molecular and metabolic mechanisms underlying cancer results in the...

journal_title：Current medicinal chemistry

authors： Rosa R,Monteleone F,Zambrano N,Bianco R

更新日期：2014-01-01 00:00:00

abstract：:Thymosin Beta-4 (Tβ4) is known as a major pleiotropic actin-sequestering protein that is involved in tumorigenesis. Tβ4 is a water-soluble protein that has different promising clinical applications in the remodeling and ulcerated tissues repair following myocardial infarction, stroke, plasticity and neurovascular remo...

journal_title：Current medicinal chemistry

authors： Bjørklund G,Dadar M,Aaseth J,Chirumbolo S

更新日期：2020-01-01 00:00:00

abstract：:Apoptotic cell death has been reported in human oocytes and preimplantation embryos under in vivo and in vitro conditions. BCL-2 family proteins comprise both anti- and pro-apoptotic members, which are likely to play a key role in controlling oocyte and early embryo survival. However, very limited data are available o...

journal_title：Current medicinal chemistry

authors： Boumela I,Assou S,Haouzi D,Déchaud H,Aït-Ahmed O,Hamamah S

更新日期：2014-01-01 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：: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：BACKGROUND:The evolutionarily conserved Hedgehog (Hh) signaling cascade is one of the key mediators of embryonic development of many metazoans. This pathway has been extensively targeted by small molecule inhibitors as its misregulation leads to various malignancies and developmental disorders. Thus, blocking this path...

journal_title：Current medicinal chemistry

authors： Khatra H,Bose C,Sinha S

更新日期：2017-01-01 00:00:00

abstract：:Factor Xa (fXa) is a critical serine protease situated at the confluence of the intrinsic and extrinsic pathways of the blood coagulation cascade. FXa catalyses the conversion of prothrombin to thrombin via the prothrombinase complex. Its singular role in thrombin generation, coupled with its potentiating effects on c...

journal_title：Current medicinal chemistry

authors： Guertin KR,Choi YM

更新日期：2007-01-01 00:00:00

abstract：:Calcium is essential for many metabolic process, including nerve function, muscle contraction, and blood clotting. The metabolic pathways that contribute to maintain serum calcium levels are bone remodeling processes, intestinal absorption and secretion, and renal handling, but hypercalcemia occurs when at least 2 of ...

journal_title：Current medicinal chemistry

authors： Lumachi F,Motta R,Cecchin D,Ave S,Camozzi V,Basso SM,Luisetto G

更新日期：2011-01-01 00:00:00

abstract：:Dose-limiting toxicity to healthy tissues is among the major hurdles in anticancer treatment along with intrinsic or acquired multi-drug resistance. Development of small molecule inhibitors (SMI) specific for antiapoptotic Bcl-2 proteins is a novel approach in a way that these antagonists are aimed to interfere with s...

journal_title：Current medicinal chemistry

authors： Bodur C,Basaga H

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:Chronic, degenerative diseases are often characterized by inflammation and aberrant angiogenesis. For these pathologies, including rheumatoid arthritis, cardiovascular and autoimmune diseases, cancer, diabetes, and obesity, current therapies have limited efficacy. OBJECTIVES:The validation of novel (chemo)p...

journal_title：Current medicinal chemistry

authors： Albini A,Bassani B,Baci D,Dallaglio K,Gallazzi M,Corradino P,Bruno A,Noonan DM

更新日期：2019-01-01 00:00:00

abstract：OBJECTIVE:We found a novel marine drug, SZ-685C, that was isolated from the secondary metabolites of a mangrove endophytic fungus (No. 1403) collected from the South China Sea, which has been reported to inhibit the proliferation of certain tumor cells. However, its anticancer mechanism remains unknown. The aims of thi...

journal_title：Current medicinal chemistry

authors： Chen CH,Xiao WW,Jiang XB,Wang JW,Mao ZG,Lei N,Fan X,Song BB,Liao CX,Wang HJ,She ZG,Zhu YH

更新日期：2013-01-01 00:00:00

abstract：:The design and development of radiolabelled steroid derivatives has been an important area of research due to their wellknown value in breast cancer targeting. The estrogen receptor (ER) and progesterone receptor (PR) are important biomarkers in the diagnosis, prognosis and follow-up of the therapeutic response of bre...

journal_title：Current medicinal chemistry

authors： Oliveira MC,Neto C,Ribeiro Morais G,Thiemann T

更新日期：2013-01-01 00:00:00

abstract：:Chagas disease is one of the most important parasitic diseases in Latin America, affecting 16 to 18 million people. Nifurtimox and Benznidazol are drugs that are commonly used in its treatment; however, these drugs produce several adverse reactions and are not effective in the chronic phase of the disease. Therefore, ...

journal_title：Current medicinal chemistry

authors： Rivera G,Bocanegra-García V,Ordaz-Pichardo C,Nogueda-Torres B,Monge A

更新日期：2009-01-01 00:00:00