Use of NMR and fluorescence spectroscopy as well as theoretical conformational analysis in conformation-activity studies of cyclic enkephalin analogues.

abstract：:The recognition that malfunction of the microtubule (MT) associated protein tau is likely to play a defining role in the onset and/or progression of a number of neurodegenerative diseases, including Alzheimer's disease, has resulted in the initiation of drug discovery programs that target this protein. Tau is an endog...

journal_title：Current topics in medicinal chemistry

authors： Ballatore C,Brunden KR,Trojanowski JQ,Lee VM,Smith AB 3rd,Huryn DM

更新日期：2011-01-01 00:00:00

abstract：:Monoacylglycerol lipase (MAGL) has been recently proposed as the main enzymatic activity responsible for the in vivo hydrolysis of the most abundant endocannabinoid in the brain, the 2-arachidonoylglycerol (2-AG). The endocannabinoids, mainly anandamide (AEA) and 2-AG, are a class of lipid messengers that modulate a b...

journal_title：Current topics in medicinal chemistry

authors： Viso A,Cisneros JA,Ortega-Gutiérrez S

更新日期：2008-01-01 00:00:00

abstract：:Recent advances in synthesis of functional poly-ε-caprolactone (PCL) and its self-assembly behavior, as well as application in drug delivery have been reviewed. Three strategies including end group functionalization, postpolymerization modification and new monomer preparation have been summarized to show possibilities...

journal_title：Current topics in medicinal chemistry

authors： Xiao Y,Yuan M,Zhang J,Yan J,Lang M

更新日期：2014-01-01 00:00:00

abstract：:Cyclic peptide scaffolds are key components of signal transduction pathways in both prokaryotic and eukaryotic organisms since they act as chemical messengers that activate or inhibit specific cognate receptors. In prokaryotic organisms these peptides are utilized in non-essential pathways, such as quorum sensing, tha...

journal_title：Current topics in medicinal chemistry

authors： Mull RW,Harrington A,Sanchez LA,Tal-Gan Y

更新日期：2018-01-01 00:00:00

abstract：:Multi-drug resistant bacteria are appearing at an alarming rate and impose significant burdens on healthcare systems worldwide. Cationic peptides have shown great promise as broad spectrum antimicrobial agents with a demonstrated ability to kill resistant bacteria, however, issues such as protease susceptibility and t...

journal_title：Current topics in medicinal chemistry

authors： Hadley EB,Hancock RE

更新日期：2010-01-01 00:00:00

abstract：:Twenty-five years ago the first small molecule inhibitors of Hsp90 were identified. In the intervening years there has been dramatic progress in basic scientific understanding of the Hsp90 chaperone machinery and in the role of Hsp90 in malignancy. The first-in-class Hsp90 inhibitor 17-AAG entered into Phase I clinica...

journal_title：Current topics in medicinal chemistry

authors： Kim YS,Alarcon SV,Lee S,Lee MJ,Giaccone G,Neckers L,Trepel JB

更新日期：2009-01-01 00:00:00

abstract：:For successful drug discovery it is important to understand the fundamentals of the underlying causes and consequences of the diseases for which the drug is being developed. One such physiological process in eukaryotic cells is protein phosphorylation, which is the main post-translational modification of proteins resp...

journal_title：Current topics in medicinal chemistry

authors： Bhalla N,Estrela P

更新日期：2017-01-01 00:00:00

abstract：:The connection of microbial biosynthetic gene clusters to the small molecule metabolites they encode is central to the discovery and characterization of new metabolic pathways with ecological and pharmacological potential. With increasing microbial genome sequence information being deposited into publicly available da...

journal_title：Current topics in medicinal chemistry

authors： Trautman EP,Crawford JM

更新日期：2016-01-01 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：:Rexinoids are selective ligands for the nuclear receptors known as RXRs. They do not bind to the receptors for all-trans-retinoic acid (RARs). Many new rexinoids have been synthesized and then assayed for their ability to suppress proliferation of cancer cells, to inhibit activation of inflammatory cells of the tumor ...

journal_title：Current topics in medicinal chemistry

authors： Liby KT,Sporn MB

更新日期：2016-06-16 00:00:00

abstract：:Protein-ligand binding is among the most fundamental phenomena underlying all molecular biology, and a greater ability to more accurately and robustly predict the binding free energy of a small molecule ligand for its cognate protein is expected to have vast consequences for improving the efficiency of pharmaceutical ...

journal_title：Current topics in medicinal chemistry

authors： Abel R,Wang L,Mobley DL,Friesner RA

更新日期：2017-01-01 00:00:00

abstract：:Rhodiola as one of traditional medicines has been used for clinical treatments due to its strong antioxidant properties. Phytochemical analysis revealed the presence of flavonoids, phenylpropanoids, phenylethanol/benzyl alcohol derivatives, cyanogenic glycosides and terpenoids. The bioactive compounds had been demonst...

journal_title：Current topics in medicinal chemistry

authors： Li Y,Wu J,Shi R,Li N,Xu Z,Sun M

更新日期：2017-01-01 00:00:00

abstract：:The pharmacophore modeling in modern drug research has been applied for both bioactivity profiling and early stage of risk assessment of potential side effects and toxicity due to interactions of drug candidates with antitargets namely P-glycoprotein, hERG, cytochrome P450 and pregnane X-receptor. In this article, an ...

journal_title：Current topics in medicinal chemistry

authors： Thai KM,Ngo TD,Tran TD,Le MT

更新日期：2013-01-01 00:00:00

abstract：:In this paper we provide an overview of the status of various colchicine derivatives in preclinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard t...

journal_title：Current topics in medicinal chemistry

authors： Johnson L,Goping IS,Rieger A,Mane JY,Huzil T,Banerjee A,Luduena R,Hassani B,Winter P,Tuszynski JA

更新日期：2017-01-01 00:00:00

abstract：:Parkinson's disease (PD) is one of the most prevalent and severe neurodegenerative disease affecting more than 6.1 million people globally. It is characterized by age-related progressive deterioration of neurological functions caused by neuronal damage or neuronal death. During PD, the dopamineproducing cells in the s...

journal_title：Current topics in medicinal chemistry

authors： Kumar B,Pandey M,Fayaz F,Izneid TA,Pottoo FH,Manchanda S,Sharma A,Sahoo PK

更新日期：2020-01-01 00:00:00

abstract：:Olefin metathesis has rapidly established itself as an essential tool in the synthetic chemist's armoury. The ease of operation and functional group tolerance that is obtained with the modern generation of catalysts makes the use of metathesis an extremely attractive option when preparing medicinally interesting molec...

journal_title：Current topics in medicinal chemistry

authors： Martin WH,Blechert S

更新日期：2005-01-01 00:00:00

abstract：:Neural activity utilizes energy resources and requires replenishment of metabolites through vascular dilation. During wake, cortical neurons usually have depolarized membrane potentials and exhibit frequent spontaneous action potentials, requiring an increased metabolic delivery to activated tissue and causing blood v...

journal_title：Current topics in medicinal chemistry

authors： Schei JL,Rector DM

更新日期：2011-01-01 00:00:00

abstract：:Chronic hepatitis B virus (HBV) infection affects about 400 million people worldwide. The development of nucleoside analogs that inhibit HBV polymerase provides an important approach for treating HBV infection. The approval of lamivudine, adefovir and entecavir represents a cornerstone of hepatitis B therapy. However,...

journal_title：Current topics in medicinal chemistry

authors： Zhou XX,Littler E

更新日期：2006-01-01 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：:In recent years the development of small organic molecules modulating protein-protein interactions (P-PIs) has drawn major attention in both academic and industrial research. Despite the appreciable progress being made, targeting such extensive interaction areas with comparatively small, drug-like agents has proven to...

journal_title：Current topics in medicinal chemistry

authors： Rechfeld F,Gruber P,Hofmann J,Kirchmair J

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Antimicrobial research is being focused to look for more effective therapeutics against antibiotic-resistant infections caused by methicillin-resistant Staphylococcus aureus (MRSA). In this direction, antimicrobial peptides (AMP) appear as promising tool. OBJECTIVES:This study evaluated the antimicrobial ac...

journal_title：Current topics in medicinal chemistry

authors： Ciandrini E,Morroni G,Arzeni D,Kamysz W,Neubauer D,Kamysz E,Cirioni O,Brescini L,Baffone W,Campana R

更新日期：2018-01-01 00:00:00

abstract：:Four compounds (isoquercitrin, myricetin-3-O-glucoside, catechin and gallocatechin) were isolated from lyophilized aqueous extract of Schizolobium parahyba leaves by chromatography on Sephadex LH-20, followed by semipreparative HPLC using a C-18 column, and identified by 1H and 13C NMR. The compounds were then, tested...

journal_title：Current topics in medicinal chemistry

authors： F Vale LH,Mendes MM,Fernandes RS,Costa TR,S Hage-Melim LI,A Sousa M,Hamaguchi A,Homsi-Brandeburgo MI,Franca SC,Silva CH,Pereira PS,Soares AM,Rodrigues VM

更新日期：2011-01-01 00:00:00

abstract：:The problem in this work is the computational characterization of cyclodextrins, crown ethers and hyaluronan (HA) as hosts of inclusion complexes for nanosized drug delivery vehicles in pharmaceutical formulations. The difficulty is addressed through a computational study of some thermodynamic, geometric and topologic...

journal_title：Current topics in medicinal chemistry

authors： Torrens F,Castellano G

更新日期：2015-01-01 00:00:00

abstract：:Cytochrome P450 17A1 (CYP17A1; also P450c17and P450sccII) is a critically important enzyme in humans that catalyzes the formation of all endogenous androgens. It is an atypical cytochrome P450 enzyme in that it catalyzes two distinct types of substrate oxidation. Through its hydroxylase activity, it catalyzes the 17α-...

journal_title：Current topics in medicinal chemistry

authors： Porubek D

更新日期：2013-01-01 00:00:00

abstract：:Anticancer drug screening can accelerate drug discovery to save the lives of cancer patients, but cancer heterogeneity makes this screening challenging. The prediction of anticancer drug sensitivity is useful for anticancer drug development and the identification of biomarkers of drug sensitivity. Deep learning, as a ...

journal_title：Current topics in medicinal chemistry

authors： Tan X,Yu Y,Duan K,Zhang J,Sun P,Sun H

更新日期：2020-01-01 00:00:00

abstract：:Our understanding of glutamatergic transmission in the central nervous system has been greatly expanded with the discovery and investigation of the metabotropic glutamate receptor family. Complementing the ionotropic glutamate-gated ion channels, these G-protein coupled receptors play critical roles in neuronal and gl...

journal_title：Current topics in medicinal chemistry

authors： Niswender CM,Jones CK,Conn PJ

更新日期：2005-01-01 00:00:00

abstract：:Dipeptidyl peptidase-IV (DPP-IV) (EC 3.4.14.5) is а member of the broad class of hydrolytic enzymes which is responsible for degradation of the incretin peptide hormones regulating blood glucose levels. In this article we review the literature on natural and synthetic DPP-IV inhibitors, focusing their chemical structu...

journal_title：Current topics in medicinal chemistry

authors： Smelcerovic A,Miljkovic F,Kolarevic A,Lazarevic J,Djordjevic A,Kocic G,Anderluh M

更新日期：2015-01-01 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：:Pyridine and pyridine-fused ring systems are ubiquitous in medicinal research and demonstrate such diverse pharmacological benefits as anticonvulsant therapies, treatment for fungal and bacterial infections as well as chemotherapy agents. For example, imidazo[1,2-a]pyridines have exhibited a broad range of activity as...

journal_title：Current topics in medicinal chemistry

authors： Kishbaugh TL

更新日期：2016-01-01 00:00:00

abstract：:Artemisinin is isolated from Artemisia annua L. with peroxide-containing sesquiterpene lactone structure. Because of its unique structural characteristics and promising anticancer, antivirus activities, it has recently received increasing attention. The aim of this review is to summarize recent discoveries of artemisi...

journal_title：Current topics in medicinal chemistry

authors： Liu X,Cao J,Huang G,Zhao Q,Shen J

更新日期：2019-01-01 00:00:00