Current Topics in Medicinal Chemistry - Volume 16, Issue 9, 2016

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 strategies to design and develop novel drugs. Structure-based drug design/discovery (SBDD) is one of the computer-aided Read More

Phosphodiesterases (PDEs) catalyze the hydrolysis of cAMP and cGMP, thereby regulating the cyclic nucleotide signalling pathways and biological responses. PDEs inhibitors can be used clinically for treatment of several diseases including central nervous system disorders, erectile dysfunction, pulmonary hypertension, acute refractory cardiac failure, and inflammatory diseases such as chronic obstructive pulmonary disease. Ho Read More

Aberrant epigenetic control is a common phenomenon in tumour progression. The epigenetic modifications such as DNA methylation, histone modification and nucleosome remodelling are involved in the regulation of many biological processes, alteration in which can result into tumourogenesis. Histone acetylation is often associated with gene expression; however deacetylated histones generally results in gene s Read More

The cysteine biosynthetic pathway is of fundamental importance for the growth, survival, and pathogenicity of the many pathogens. This pathway is present in many species but is absent in mammals. The ability of pathogens to counteract the oxidative defences of a host is critical for the survival of these pathogens during their long latent phases, especially in anaerobic pathogens such as Entamoeba histolytica, Leishmania donov Read More

The loss of effectiveness of current antibiotics caused by the development of drug resistance has become a severe threat to public health. Current widely used antibiotics are surprisingly targeted at a few bacterial functions - cell wall, DNA, RNA, and protein biosynthesis - and resistance to them is widespread and well identified. There is therefore great interest in the discovery of novel drugs and therapies to tackle antimicrobial r Read More

The highly persistent nature of Mycobacterium tuberculosis can be attributed to its lipophilic cell wall which acts as a major barrier in the process of drug discovery against tuberculosis. Glutamine synthetase plays a major role in nitrogen metabolism and cell wall biosynthesis of pathogenic mycobacteria. The current review focuses on the structural and functional aspects of Mtb glutamine synthetase and an overview of its r Read More

Human serum albumin (HSA) is the most abundant protein in the plasma. HSA plays a central role in drug pharmacokinetics because most drugs bound to HSA are delivered to their target organ/tissues. The prodrug strategies have shown great promise for improving the activity and selectivity of drugs. Designing prodrugs based on special HSA residues, such as Cys34 and Lys residues, has been extensively studied. Therefore, t Read More

Ligand- and structure-based drug design approaches complement phenotypic and target screens, respectively, and are the two major frameworks for guiding early-stage drug discovery efforts. Since the beginning of this century, the advent of the genomic era has presented researchers with a myriad of high throughput biological data (parts lists and their interaction networks) to address efficacy and toxicity, augmenting the tra Read More

Biopolymer-based nanostructures or microstructures can be fabricated with different compositions, structures, and properties so that colloidal delivery systems can be tailored for specific applications. These structures can be assembled using various approaches, including electrospinning, coacervation, nanoprecipitation, injection, layer-by-layer deposition, and/or gelation. A major application of biopolymer-based particles is Read More

The development in sequencing technologies over the past few decades have increased the pace of decoding genetic and functional information present in the genomes of pathogenic microorganisms. The knowledge obtained through sequencing projects facilitated the identification of genes that codes for virulence factors. A major portion of genomes of pathogenic of bacteria contains genes which are classified as “hypotheti Read More