Abstract：
:Histone deacetylases (HDACs) have recently emerged as key elements in epigenetic control of gene expression. Due to the implication of HDACs in a variety of diseases ranging from cancer to neurodegenerative disorder, HDAC inhibitors have received increased attention in recent years. Over the last few decades, a myriad of HDAC inhibitors containing a wide variety of structural features have been identified from natural sources. Here, we review the discovery, synthesis, biological properties, and modes of action of these naturally occurring HDAC inhibitors and consider their implications for future research.
journal_name
Curr Top Med Chemjournal_title
Current topics in medicinal chemistryauthors
Kim B,Hong Jdoi
10.2174/1568026615666141208105614subject
Has Abstractpub_date
2015-01-01 00:00:00pages
2759-82issue
24eissn
1568-0266issn
1873-4294pii
CTMC-EPUB-63859journal_volume
14pub_type
杂志文章,评审abstract：BACKGROUND:Development of acetyl- (AChE) and butyrylcholinesterase (BuChE) inhibitors belongs to viable strategies for the treatment of dementia and other diseases related to decrease in cholinergic neurotransmission. OBJECTIVE:That is why we designed twenty-two analogues of a dual AChEBuChE salicylanilide inhibitor, ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章
doi：10.2174/1568026620666200819154722
更新日期：2020-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026616666151012111046
更新日期：2016-01-01 00:00:00
abstract：:Psychiatric diagnosis has long been perceived as more of an art than a science since its foundations lie within the observation, and the self-report of the patients themselves and objective diagnostic biomarkers are lacking. Furthermore, the diagnostic tools in use not only stray away from the conventional medical fra...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026620666200131095328
更新日期：2020-01-01 00:00:00
abstract：:In general perturbation methods starts with a known exact solution of a problem and add "small" variation terms in order to approach to a solution for a related problem without known exact solution. Perturbation theory has been widely used in almost all areas of science. Bhor's quantum model, Heisenberg's matrix mecha...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026611313140011
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
pub_type： 杂志文章,评审
doi：10.2174/156802606776894447
更新日期：2006-01-01 00:00:00
abstract：:The computational assessment of drug metabolism has gained considerable interest in pharmaceutical research. Amongst others, machine learning techniques have been employed to model relationships between the chemical structure of a compound and its metabolic fate. Examples for these techniques, which were originally de...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802606778108915
更新日期：2006-01-01 00:00:00
abstract：:There are several significant setbacks including limited bioavailability, high clearance, and further current therapies require higher and frequent dosing to gain desired therapeutic effects. Nanomedicines have been widely investigated for rheumatoid arthritis (RA). Though, higher doses also increase the incidence of ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026616666160530152354
更新日期：2017-01-01 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
pub_type： 杂志文章,评审
doi：
更新日期：2017-01-01 00:00:00
abstract：:Fragment-based drug discovery (FBDD) needs a biophysical assay to complement, or even replace, biochemical screening. NMR is the best choice for this because NMR delivers many different types of data that impacts medicinal chemistry decisions. There are a multitude of different NMR methods which can be employed to the...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章
doi：10.2174/156802607782341055
更新日期：2007-01-01 00:00:00
abstract：:Hepatitis C virus (HCV) is a major cause of acute hepatitis and chronic liver disease, including cirrhosis and hepatocellular carcinoma (HCC). No vaccine is currently available to prevent hepatitis C, and the current standard of care (SOC) - pegylated interferon-α (PEG-IFN-α) in combination with ribavirin (RBV) - is o...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802610792232051
更新日期：2010-01-01 00:00:00
abstract：:Release of somatostatin into the circulation from the activated TRPV1-expressing nociceptors revealed by antidromic stimulation of dorsal roots in the rat pinpointed to a novel potential drug target on these nociceptors. The review summarizes the functional, biochemical and pharmacological evidence for a novel somatos...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802611796904852
更新日期：2011-01-01 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
pub_type： 杂志文章,评审
doi：
更新日期：2015-01-01 00:00:00
abstract：:Latest microarray-based technologies, including small molecule-, peptide-, protein- and cell-based arrays, and their applications in the field of proteomics are reviewed. ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026033452375
更新日期：2003-01-01 00:00:00
abstract：:Pronucleotides represent a promising alternative to improve the biological activity of nucleoside analogues against different viral diseases. The basic idea is to achieve nucleotide delivery into cells, bypassing limitations with intracellular formation of nucleotides from their nucleoside precursors. The cycloSal-con...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026023393183
更新日期：2002-10-01 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
pub_type： 杂志文章,评审
doi：10.2174/156802606776743101
更新日期：2006-01-01 00:00:00
abstract：:A modified version of the CORAL software (http://www.insilico.eu/coral) allows building up the classification model for the case of the Yes/No data on the anti-sarcoma activity of organic compounds. Three random splits into the sub-training, calibration, and test sets of the data for 3017 compounds were examined. The ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章
doi：10.2174/1568026611212240004
更新日期：2012-01-01 00:00:00
abstract：:This review highlights the biological importance of many polysubstituted nitro-prolines and -pyrrolidines. Their preparation using asymmetric 1,3-dipolar cycloadditions of azomethine ylides with nitroalkenes using diastereoselective and enantioselective strategies is described remarking the scope and main features of ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026614666140423112145
更新日期：2014-01-01 00:00:00
abstract：:Thiosemicarbazones (TSCNs) constitute a broad family of compounds (R1R2C=N-NH-C(S)- NR3R4), particularly attractive because many of them display some biological activity against a wide range of microorganisms and cancer cells. Their activity can be related to their electronic and structural properties, which offer a r...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章
doi：10.2174/1568026620666201022144004
更新日期：2021-01-01 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
pub_type： 杂志文章,评审
doi：10.2174/1568026611313090004
更新日期：2013-01-01 00:00:00
abstract：INTRODUCTION:Mosquito borne diseases continue to propagate and cause millions of deaths annually. They are caused either by protozoan parasites such as Plasmodium, Toxoplasma or by flaviviruses including Dengue and Zika. Among the proteome of such parasitic organisms, proteases play essential roles in events such as ho...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026617666170130122231
更新日期：2017-01-01 00:00:00
abstract：:Variable selection is a procedure used to select the most important features to obtain as much information as possible from a reduced amount of features. The selection stage is crucial. The subsequent design of a quantitative structure-activity relationship (QSAR) model (regression or discriminant) would lead to poor ...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802608786786552
更新日期：2008-01-01 00:00:00
abstract：:In 2010, the National Institutes of Health (NIH) established the Therapeutics for Rare and Neglected Diseases (TRND) program within the National Center for Advancing Translational Sciences (NCATS), which was created to stimulate drug discovery and development for rare and neglected tropical diseases through a collabor...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026613666131127160118
更新日期：2014-01-01 00:00:00
abstract：:Telomeres are structurally nucleoprotein complexes at termini of linear chromosomes and essential to chromosome stability/integrity. In normal human cells, telomere length erodes progressively with each round of cell divisions, which serves as an important barrier to uncontrolled proliferation and malignant transforma...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026620666200106145340
更新日期：2020-01-01 00:00:00
abstract：:Chemical genomics combines chemistry with molecular biology as a means of exploring the function of unknown proteins or identifying the proteins responsible for a particular phenotype induced by a small cell-permeable bioactive molecule. Chemical genomics therefore has the potential to identify and validate therapeuti...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802612801319025
更新日期：2012-01-01 00:00:00
abstract：:Leukocytes and lung structural cells contribute to the pathophysiology of asthma through the production of numerous mediators including serine proteases. Such proteases include mast cell tryptase and chymase; neutrophil elastase, cathepsin G and myeloblastin (proteinase 3); bronchial epithelial cell-derived transmembr...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/156802606776287054
更新日期：2006-01-01 00:00:00
abstract：:Computational toxicity modeling can have significant impact in the drug discovery process, especially when utilized as a sentinel filter for common drug safety liabilities, such as mutagenicity, carcinogenicity and teratogenicity. This review will focus on the strengths and limitations of the current computational mod...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026013395074
更新日期：2001-09-01 00:00:00
abstract：:Kynurenic acid (KYNA), one of the metabolites belonging to the kynurenine pathway, has been described as an important neuroprotective compound, its unbalancing being associated with several pathological conditions. In human brain, the majority of KYNA production is sustained by kynurenine aminotransferase II (KAT II)....
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章
doi：10.2174/156802611794863599
更新日期：2011-01-01 00:00:00
abstract：:Results of various projects on Mexican Indian ethnobotany and some of the subsequent pharmacological and phytochemical studies are summarised focusing both on chemical-pharmacological as well as anthropological (ethnopharmacological) aspects of our research. We have identified taste and smell properties of medicinal (...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章,评审
doi：10.2174/1568026033392570
更新日期：2003-01-01 00:00:00
abstract：:A series of novel derivatives of 1,3-oxazolidin-2-one 12a-12n has been synthesized starting from 4-nitro-(L)- phenylalanine by involving five-step reaction sequence. All the compounds were screened for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacill...
journal_title：Current topics in medicinal chemistry
pub_type： 杂志文章
doi：10.2174/15680266113139990132
更新日期：2013-08-01 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
pub_type： 杂志文章,评审
doi：10.2174/156802611794785163
更新日期：2011-01-01 00:00:00
