PPAR ligands for metabolic disorders.

abstract：:Low drug productivity has been a significant problem of the pharmaceutical industry for several decades even though numerous novel technologies were introduced during this period. Currently pharmacologic dogma, "single drug, single target, single disease", is at the root of the lack of drug productivity. From a system...

journal_title：Current topics in medicinal chemistry

authors： Ye H,Wei J,Tang K,Feuers R,Hong H

更新日期：2016-01-01 00:00:00

abstract：:This review discusses the state of the art, challenges and perspectives in recent applications of electrochemistry in the life sciences. It deals mainly with the elucidation of molecular mechanisms of drug action, drug design and development, involving electron transfer, pharmaco-electrochemistry (the combination of e...

journal_title：Current topics in medicinal chemistry

authors： de Paiva YG,da Rocha Ferreira F,Silva TL,Labbe E,Buriez O,Amatore C,Fonseca Goulart MO

更新日期：2015-01-01 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：:Characteristic symptoms of schizophrenia and bipolar disorders have been described and classified about a century ago. Each of these disorders may cause considerable impairment reflecting substantial alterations in cognition, perception, and mood. Though both disease concepts are well established, psychopharmacologica...

journal_title：Current topics in medicinal chemistry

authors： Bumb JM,Enning F,Leweke FM

更新日期：2013-01-01 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：: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：:The development of computational tools for the prediction of passive transport is reviewed with particular reference to four diverse approaches: the rule-of-5, polar surface area, Volsurf and Abraham's General Solvation Equation. To illustrate the current state of the art, several examples of the application of in sil...

journal_title：Current topics in medicinal chemistry

authors： Clark DE,Grootenhuis PD

更新日期：2003-01-01 00:00:00

abstract：:The increase of pathogens being resistant to antibiotics represents a global health problem and therefore it is a pressing need to develop antibiotics with novel mechanisms of action. Host defense peptides, which have direct antimicrobial activity (also termed antimicrobial peptides) or immune modulating activity, are...

journal_title：Current topics in medicinal chemistry

authors： Lohner K

更新日期：2017-01-01 00:00:00

abstract：:Autophagy is an important basic metabolic mechanism by engulfing and degrading the unnecessary or dysfunctional cellular components within double-membered autolysosomes to maintain cellular homeostasis. Autophagy has sparkled great interest for its complicated functions in different stages of cancer, and is regarded a...

journal_title：Current topics in medicinal chemistry

authors： Li S,Wang L,Hu Y,Sheng R

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Structure-based drug design is a wide area of identification of selective inhibitors of a target of interest. From the time of the availability of three dimensional structure of the drug targets, mostly the proteins, many computational methods had emerged to address the challenges associated with drug desi...

journal_title：Current topics in medicinal chemistry

authors： Velmurugan D,Pachaiappan R,Ramakrishnan C

更新日期：2020-01-01 00:00:00

abstract：:Viral entry, the first process in the reproduction of viruses, primarily involves attachment of the viral envelope proteins to membranes of the host cell. The crucial components that play an important role in viral entry include viral surface glycoprotein gp120, viral transmembrane glycoprotein gp41, host cell glycopr...

journal_title：Current topics in medicinal chemistry

authors： Suttisintong K,Kaewchangwat N,Thanayupong E,Nerungsi C,Srikun O,Pungpo P

更新日期：2019-01-01 00:00:00

abstract：:Neglected diseases comprise a number of infectious diseases historically endemic to low- and middle-income countries, though recently they have spread to high-income countries due to human migrations. In the past, pharmaceutical companies have shown hesitant to invest in these health conditions, due to the limited ret...

journal_title：Current topics in medicinal chemistry

authors： Bellera CL,Sbaraglini ML,Talevi A

更新日期：2018-01-01 00:00:00

abstract：:An evaluation of existing and proposed Fe chelators, both synthetic and natural products, for the treatment of Fe-overload disease must address a number of issues. There are fundamental parameters that determine the efficacy of a drug: absorption, distribution, metabolism, clearance and toxicity. However, the administ...

journal_title：Current topics in medicinal chemistry

authors： Sharpe PC,Richardson DR,Kalinowski DS,Bernhardt PV

更新日期：2011-01-01 00:00:00

abstract：:Alzheimer's disease (AD) is a multifactorial complex disease. The pathogenesis of AD is very complicated, and involves the β-amyloid (Aβ) cascade, tau hyperphosphorylation, neuroinflammation, oxidative stress, mitochondrial dysfunction, reduced levels of neurotrophic factors, and damage and loss of synapses as well as...

journal_title：Current topics in medicinal chemistry

authors： Li L,Zhang L,Yang CC

更新日期：2016-01-01 00:00:00

abstract：:Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and recept...

journal_title：Current topics in medicinal chemistry

authors： Pereira TM,Franco DP,Vitorio F,Kummerle AE

更新日期：2018-01-01 00:00:00

abstract：:The neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally α-amino acids with one or more stereogenic centers due to st...

journal_title：Current topics in medicinal chemistry

authors： Vogensen SB,Greenwood JR,Bunch L,Clausen RP

更新日期：2011-01-01 00:00:00

abstract：:Understanding the mechanisms involved in the activation of an immune response is essential to many fields in human health, including vaccine development and personalized cancer immunotherapy. A central step in the activation of the adaptive immune response is the recognition, by T-cell lymphocytes, of peptides display...

journal_title：Current topics in medicinal chemistry

authors： Antunes DA,Abella JR,Devaurs D,Rigo MM,Kavraki LE

更新日期：2018-01-01 00:00:00

abstract：:(18)F-labeled amino acids are an important class of imaging agents for positron emission tomography (PET) that target the increased rates of amino acid transport by many tumor cells. This class of tracers is structurally diverse, and the biological and imaging properties of a given (18)F-labeled amino acid depends lar...

journal_title：Current topics in medicinal chemistry

authors： Huang C,McConathy J

更新日期：2013-01-01 00:00:00

abstract：:Over activation of the NMDA receptor complex has been implicated in a number of neurological conditions. The use of NMDA antagonists as therapeutic agents has been limited by serious cognitive and motor side effects. Significant efforts have been reported in the development of NR2B subtype-selective antagonists, which...

journal_title：Current topics in medicinal chemistry

authors： Layton ME,Kelly MJ 3rd,Rodzinak KJ

更新日期：2006-01-01 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：:In the last few years, there has been a great increase in our understanding of pain mechanisms. Given the complexity of the mechanisms involved in pain modulation, it is surprising that the pharmacological control of pain through the application of relatively simple analgesics can be effective. Nevertheless, the appli...

journal_title：Current topics in medicinal chemistry

authors： Mico JA,Berrocoso E,Ortega-Alvaro A,Gibert-Rahola J,Rojas-Corrales MO

更新日期：2006-01-01 00:00:00

abstract：:Compared with the increasing and widespread bacterial resistance to clinical medicines and the urgent need for cures of intractable diseases, there is a dramatic decline in the numbers of drugs reaching the market or clinical trials. Accordingly, it has become imperative to discover more rational and efficient strateg...

journal_title：Current topics in medicinal chemistry

authors： Wang T,Wu MB,Zhang RH,Chen ZJ,Hua C,Lin JP,Yang LR

更新日期：2016-01-01 00:00:00

abstract：:The first proteolytic step in the processing of amyloid precursor protein (APP) to amyloid-beta (Abeta) in the brain is performed by beta-site APP cleaving enzyme (BACE1). This enzyme is a membrane bound aspartic protease with high homology of the catalytic domain to renin and pepsin and of yet unknown physiologic fun...

journal_title：Current topics in medicinal chemistry

authors： Roggo S

更新日期：2002-04-01 00:00:00

abstract：:The atomic determination of the acetylcholine binding protein (AChBP), a molluscan cholinergic protein, homologous to the amino-terminal extracellular domain of nicotinic receptors (nAChRs), offers opportunities for the modeling of the acetylcholine binding site and its ligands. Recently, we constructed three-dimensio...

journal_title：Current topics in medicinal chemistry

authors： Grutter T,Le Novère N,Changeux JP

更新日期：2004-01-01 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：:G protein coupled receptors (GPCRs) are membrane proteins coupled with G proteins through which they transmit signals to the cytoplasm. Approximately 30% of pharmaceuticals target these receptors, even though crystal structures were scarce at the time. Furthermore, an additional 15% of GPCRs have yet to be exploited f...

journal_title：Current topics in medicinal chemistry

authors： Kontoyianni M

更新日期：2016-01-01 00:00:00

abstract：:Penile erection is a complex physiologic event resulting from the interactions of the nervous system on a highly specialized vascular organ. Activation of central nervous system melanocortinergic (MC) receptors with either endogenous or synthetic melanotropic ligands may initiate and/or facilitate spontaneous penile e...

journal_title：Current topics in medicinal chemistry

authors： King SH,Mayorov AV,Balse-Srinivasan P,Hruby VJ,Vanderah TW,Wessells H

更新日期：2007-01-01 00:00:00

abstract：:(2R,3R)-2,3-Butanediol has many industrial applications, such as it is used as an antifreeze agent and low freezing point fuel. In addition, it is particularly important to provide chiral groups in drugs. In recent years, this valuable bio-based chemical has attracted increasing attention, and significant progress has...

journal_title：Current topics in medicinal chemistry

authors： Xie NZ,Chen XR,Wang QY,Chen D,Du QS,Zhou GP,Huang RB

更新日期：2017-01-01 00:00:00

abstract：:Natural quinoline alkaloid camptothecin (CPT) is used for the treatment of colon, lung, breast and ovarian cancers still facing challenges due to low solubility in aqueous and biological fluids. Its lactone form easily converts into a toxic carboxylic form at slightly basic pH, typical in blood and tissue fluid has ra...

journal_title：Current topics in medicinal chemistry

authors： Mishra D,Yadav V,Khare P,Jyotshna,Das MR,Meena A,Shanker K

更新日期：2016-01-01 00:00:00

abstract：:Glutamate is the major excitatory neurotransmitter in the mammalian central nervous system (CNS) controlling physiological processes as learning and memory. However, the overactivation of glutamatergic neurotransmission is often related to various CNS chronic and acute diseases (epilepsy, ischaemia, Parkinson, etc.). ...

journal_title：Current topics in medicinal chemistry

authors： Gitto R,De Luca L,De Grazia S,Chimirri A

更新日期：2012-01-01 00:00:00