Analysis of DNA microarray data.

abstract：:Diabetes mellitus type 2 (DMT2) is a metabolic disease characterized by a chronic increase in glycemia that promotes several long-term complications and high mortality. Some enzymes involved in glycaemic control, such as α -(1,4)-glucosidase, have now been established as novel pharmacological targets. Coumarins have s...

journal_title：Current topics in medicinal chemistry

authors： Figueroa-Benavides C,Matos MJ,Peñaloza-Amion M,Veas R,Valenzuela-Barra G,Zapata G,Delogu G,Uriarte E,Santana L,Olea-Azar C,Delporte C

更新日期：2018-01-01 00:00:00

abstract：:There exists a huge attrition rate of molecules in clinical trials. It was expected that high-throughput screening and combinatorial chemistry would make the task of producing drugs easier. However, the efforts of the past decade have not been an unvarnished success. As a result, a lot of experimental and computationa...

journal_title：Current topics in medicinal chemistry

authors： Ajay

更新日期：2002-12-01 00:00:00

abstract：:In this review the preclinical medicinal chemistry, biochemistry and clinical results achieved in the treatment of prostatic disease with dutasteride, a dual inhibitor of type 1 and type 2,5alpha-reductase are described. During the discovery phase, dutasteride was optimized to inhibit both forms of human 5 alpha-reduc...

journal_title：Current topics in medicinal chemistry

authors： Frye SV

更新日期：2006-01-01 00:00:00

abstract：:The neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) family of hormones exhibit a wide variety of biological actions on the mammalian gastrointestinal tract through known G-protein coupled receptor pathways. At least four receptor subtypes, denoted as Y(1), Y(2), Y(4) an Y(5), each with specific ...

journal_title：Current topics in medicinal chemistry

authors： Vona-Davis LC,McFadden DW

更新日期：2007-01-01 00:00:00

abstract：:Multiple Gαi protein-coupled somatostatin receptors (SSTRs) are expressed in human kidney and liver tissues. Also, aberrant cAMP signaling has been shown to play a critical role in cysto-genesis and enlargement of the human kidney and liver. Thus, somatostatin (SST) analogs become potential and promising alternatives ...

journal_title：Current topics in medicinal chemistry

authors： Sun L,Yu CY,Mackey LV,Coy DH

更新日期：2015-01-01 00:00:00

abstract：:Neuronal nicotinic acetylcholine ion channel receptors (nAChRs) exist as several subtypes and are involved in a variety of functions and disorders of the central nervous system (CNS), such as Alzheimer's and Parkinson's diseases. The lack of reliable information on the 3D structure of nAChRs prompted us to focus effor...

journal_title：Current topics in medicinal chemistry

authors： Nicolotti O,Altomare C,Pellegrini-Calace M,Carotti A

更新日期：2004-01-01 00:00:00

abstract：:One of the major events occurring at biological interfaces is the specific recognition of bioactive ligands by their receptor proteins. The elucidation of interacting partners is an immediate entrance into the discovery of medicinal leads. The method of photoaffinity labeling enables the direct probing of target prote...

journal_title：Current topics in medicinal chemistry

authors： Hatanaka Y,Sadakane Y

更新日期：2002-03-01 00:00:00

abstract：:Cancer is a multifactorial disease including interactions of complex genetic and environmental factors. Clinical efficacy of anticancer chemotherapies is hampered by various factors including multidrug resistance (MDR). There is a strong need to discover more potent novel cancer drugs to kill cancer cells selectively....

journal_title：Current topics in medicinal chemistry

authors： Kucuksayan E,Ozben T

更新日期：2017-01-01 00:00:00

abstract：:Protein kinases (Ser/Thr and Tyr) play a key role in signal transduction pathways. It has been shown that deregulation of the Cdk activity is linked to cell proliferation and cancer. Inhibition of cyclin-dependent kinases (Cdks) is an important target for potential new anti-cancer drugs. Following the discovery of Olo...

journal_title：Current topics in medicinal chemistry

authors： Haesslein JL,Jullian N

更新日期：2002-09-01 00:00:00

abstract：:In the last decade, we have been developing some gold(III) derivatives showing interesting antitumor properties and reduced systemic and renal toxicity, compared to the clinically-established reference drug cisplatin. Starting from the rationale at the base of our investigations, this review has been divided into two ...

journal_title：Current topics in medicinal chemistry

authors： Nardon C,Fregona D

更新日期：2016-01-01 00:00:00

abstract：:In recent years, relationship between free radicals and oxidative stress with aging, cancer, atherosclerosis, neurodegenerative disorders, diabetes, and inflammatory diseases became increasingly clear. Confirming the role of oxidants in numerous pathological conditions such as cancer, the antioxidants developed as the...

journal_title：Current topics in medicinal chemistry

authors： Karaaslan C,Suzen S

更新日期：2015-01-01 00:00:00

abstract：:Chagas disease and African sleeping sickness are trypanosomal infections that represent important public health problems in Latin America and Africa, respectively. The restriction of these diseases to the poorer parts of the world has meant that they have been largely neglected and limited progress has been made in th...

journal_title：Current topics in medicinal chemistry

authors： Wilkinson SR,Bot C,Kelly JM,Hall BS

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:The high sequence and structural homology among the hsp90 paralogs - Hsp90α, Hsp90β, Grp94, and Trap-1 - has made the development of paralog-specific inhibitors a challenging proposition. OBJECTIVE:This review surveys the state of developments in structural analysis, compound screening, and structure-based ...

journal_title：Current topics in medicinal chemistry

authors： Gewirth DT

更新日期：2016-01-01 00:00:00

abstract：:Interest in the chemistry and biological properties of non-nucleoside N-glycosidic compounds has gathered pace over the past several years; the occurrence of the N-glycoside moiety in glycoproteins and a range of active natural products has prompted the synthesis of a diverse spectrum of related materials with promisi...

journal_title：Current topics in medicinal chemistry

authors： Norris P

更新日期：2008-01-01 00:00:00

abstract：:In this review the conformational studies of natural enkephalins (H-Tyr-Gly-Gly-Phe-Met-OH; the [Met(5)]enkephalin and H-Tyr-Gly-Gly-Phe-Leu-OH; the [Leu(5)]enkephalin), their acyclic and cyclic analogues, including those carried out in our laboratory, performed by experimental and theoretical methods and their combin...

journal_title：Current topics in medicinal chemistry

authors： Malicka J,Czaplewski C,Groth M,Wiczk W,Oldziej S,Lankiewicz L,Ciarkowski J,Liwo A

更新日期：2004-01-01 00:00:00

abstract：:Rheumatoid Arthritis (RA) is a chronic autoimmune inflammatory disease that affects largely synovial joints. It has been postulated that activated autoreactive CD4 T cells play a key role in triggering and/or maintaining the chronic inflammatory process in RA. Dendritic cells (DCs) are antigen-presenting cells that ac...

journal_title：Current topics in medicinal chemistry

authors： Rodríguez-Fernández JL

更新日期：2013-01-01 00:00:00

abstract：:Pulmonary drug delivery represents the best way of treating lung diseases, since it allows direct delivery of the drug to the site of action, with few systemic effects. Meanwhile, the lungs may be used as a portal of entry to the body, allowing systemic delivery of drugs via the airway surfaces into the bloodstream. I...

journal_title：Current topics in medicinal chemistry

authors： d'Angelo I,Conte C,Miro A,Quaglia F,Ungaro F

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Farnesol is an acyclic sesquiterpene alcohol, endogenously synthesized via the ergosterol pathway. It is a quorum sensing molecule (QSM) that was first discovered in C. albicans, and is involved in the inhibition of hyphae formation. METHODS:This review focuses on the comprehensive details of occurrence, ch...

journal_title：Current topics in medicinal chemistry

authors： Gupta P,Sharma M,Arora N,Pruthi V,Poluri KM

更新日期：2018-01-01 00:00:00

abstract：:Notwithstanding the functional role that the aggregates of some amyloidogenic proteins can play in different organisms, protein aggregation plays a pivotal role in the pathogenesis of a large number of human diseases. One of such diseases is Alzheimer's disease (AD), where the overproduction and aggregation of the β-a...

journal_title：Current topics in medicinal chemistry

authors： Viayna E,Sabate R,Muñoz-Torrero D

更新日期：2013-01-01 00:00:00

abstract：:Tanshinones are a class of bioactive compounds present in the Chinese herbal medicine Danshen (Salvia miltiorrhiza Bunge), containing among others, abietane diterpene quinone scaffolds. Chemical synthesis and biological activity studies of natural and unnatural tanshinone derivatives have been reviewed in this article...

journal_title：Current topics in medicinal chemistry

authors： Huang H,Song C,Chang J

更新日期：2020-01-01 00:00:00

abstract：:The field of quantitative structure activity relationships (QSAR) has evolved into an integral tool for pharmaceutical discovery. It is presently an accessible technology, as can be shown by the number papers which are easily found through PubMed literature searches. At one level, QSAR is used routinely and invisibly ...

journal_title：Current topics in medicinal chemistry

authors： Sprous DG,Palmer RK,Swanson JT,Lawless M

更新日期：2010-01-01 00:00:00

abstract：:Protein-RNA interactions play crucial roles in numerous biological processes. However, detecting the interactions and binding sites between protein and RNA by traditional experiments is still time consuming and labor costing. Thus, it is of importance to develop bioinformatics methods for predicting protein-RNA intera...

journal_title：Current topics in medicinal chemistry

authors： Liu ZP,Chen L

更新日期：2016-01-01 00:00:00

abstract：:This review describes the role of nuclear receptors in the regulation of genes involved in cholesterol transport and synthetic modulators of these receptors. Increasing the efflux of cholesterol from peripheral cells, such as lipid-laden macrophages, through a process called reverse cholesterol transport (RCT) require...

journal_title：Current topics in medicinal chemistry

authors： Pelton PD,Patel M,Demarest KT

更新日期：2005-01-01 00:00:00

abstract：:Nanotechnology is revolutionizing the development of different branches of science. The investigation of nanomaterials in the battle against cancer is not an exception. The main goal of this contribution is to bring an overview about the types of organic and inorganic nanomaterials that are under investigation for its...

journal_title：Current topics in medicinal chemistry

authors： Sanchez-Dominguez CN,Gallardo-Blanco HL,Rodriguez-Rodriguez AA,Vela-Gonzalez AV,Sanchez-Dominguez M

更新日期：2014-03-01 00:00:00

abstract：:Target-Related Affinity Profiling (TRAP) is a computational drug discovery technology that is based on 'affinity fingerprints', which are molecular descriptors derived from the protein binding preferences of small molecules. The underlying concepts of TRAP are reviewed. Affinity fingerprints are compared to molecular ...

journal_title：Current topics in medicinal chemistry

authors： Beroza P,Damodaran K,Lum RT

更新日期：2005-01-01 00:00:00

abstract：AIM:The aim of this study is to synthesize, characterize and biological evaluation of 3-ethyl 5- methyl2-(2-aminoethoxy)-4-(2-chlorophenyl)-1,4-dihydropyridine-3,5-dicarboxylate derivatives. BACKGROUND:An efficient synthesis of two series of novel carbamate and sulfonamide derivatives of amlodipine, 3-ethyl 5-methyl 2...

journal_title：Current topics in medicinal chemistry

authors： Sudhana SM,Adi PJ

更新日期：2019-01-01 00:00:00

abstract：:The novel peptide hormone ghrelin has recently been recognized as an important co-regulator of growth hormone secretion and energy homeostasis. The significance of ghrelin for obesity and cachexia as well as in the regulation of growth processes is the subject of ongoing basic research as well as clinical studies. It ...

journal_title：Current topics in medicinal chemistry

authors： Horvath TL,Diano S,Tschöp M

更新日期：2003-01-01 00:00:00

abstract：:Human multidrug resistance protein (MRP/ABCC) family contains 9 members (MRP1-9) which transport a structurally diverse array of anticancer and antimicrobial drugs and several important endogenous substances including prostaglandins (PGs) and leukotrienes (LTs) with different substrate specificity. MRP1-5 can collecti...

journal_title：Current topics in medicinal chemistry

authors： Yang AK,Zhou ZW,Wei MQ,Liu JP,Zhou SF

更新日期：2010-01-01 00:00:00

abstract：:Pyrimidine and purine nucleosides and their derivatives have critical functions and pharmacological applications in the brain. Nucleosides and nucleobases are precursors of nucleotides, which serve as the energy-rich currency of intermediary metabolism and as precursors of nucleic acids. Nucleosides (e.g., adenosine) ...

journal_title：Current topics in medicinal chemistry

authors： Parkinson FE,Damaraju VL,Graham K,Yao SY,Baldwin SA,Cass CE,Young JD

更新日期：2011-01-01 00:00:00

abstract：:The emergence of multi-resistant bacteria to drugs is recognized as a major cause of the increasing number of deaths in hospitals. Killing these bacteria require multiple expensive drugs that can have side effects. Metal nanoparticles may provide a new strategy to combat them. Due the antimicrobial and antiviral prope...

journal_title：Current topics in medicinal chemistry

authors： Oktar FN,Yetmez M,Ficai D,Ficai A,Dumitru F,Pica A

更新日期：2015-01-01 00:00:00