Current Pharmaceutical Design - Volume 9, Issue 11, 2003

Giardiasis is a protozoal disease infecting 200 million people throughout the world. Giardiasis is widespread primarily in developing countries. Infections are correlated with poor hygienic conditions, poor water quality control, and overcrowding. There are very few therapeutics currently available, and drug development to treat giardiasis is hampered mainly by socioeconomic obstacles. This article presents the history of Read More

This review summarizes some of the published attempts to incorporate protein and NMR structures in the design of new antibiotics that specifically target Cell Wall biosynthesis. Most of the steps involved in peptidglycan synthesis have been investigated as potential strategies against cell wall inhibition. Structural information has been most useful in the design of molecules in the Mur enzyme pathway, penicillin binding proteins Read More

During its development in the host red cell, the human malarial parasite causes profound alteration in the permeability of the host cell membrane. These membrane transport systems(s) play a role in the development of the intra-erythrocytic parasite in its need to take up solutes and nutrients from the extracellular medium and the disposal of metabolic wastes. Importantly, the properties of these parasite induced transport sys Read More

In the last several decades the plants, animals and microbes from the marine environment have revealed a portion of what is clearly a tremendous resource for structurally diverse and bioactive secondary metabolites. Many of these extraordinarily sophisticated and bioactive natural products can be isolated in significant quantities without great difficulty. As a result these readily available bioactive natural products provide valu Read More

Drug discovery is an expensive, slow and high risk enterprise. Only one in ten of the agents that enter clinical development is successful, with an average cost of $500-800 million and a typical time-scale of 10-15 years from preclincal discovery research to regulatory approval. On the other hand, many new targets are emerging from genome sequencing and the improved understanding of molecular pathology. Also, new tec Read More

Nuclear Medicine involves studying the time course of radioactive tracers and the physiological response of the body in vivo using external imaging devices. These devices are quantitative and can be used to assay tracer concentrations. This chapter briefly discusses the historical milieu, current state-of-the-art in terms of both single photon and positron tomography (SPECT and PET), and shows a semi-quantitative example of mo Read More

Positron emission tomography (PET) provides the oncologist with information on tumour diagnosis, and treatment response monitoring. Mathematical modelling of tissue data, and online plasma radioactive metabolite profiling, enables important tissue kinetic parameters relating to the uptake, distribution and washout as well as arterial input function to be derived. The resultant kinetic data allow for not only diagnosi Read More

Positron Emission Tomography (PET) offers an exciting opportunity to monitor key pathways involved in malignant transformation due to the ability to radiolabel and image the behaviour of biological probes. In this review, we will describe how PET can use various radiolabelled compounds to monitor various targets including ligand-receptor interactions using 16α-[18F]fluoro-17β-oestradiol (FES) pathways involved in metabolis Read More