Gut hormone GPCRs: structure, function, drug discovery

Gut hormone GPCRs: structure, function, drug discovery.

Crystallization and determination of the high resolution three-dimensional structure of the β2-adrenergic receptor in 2007 was followed by structure elucidation of a number of other receptors, including those for neurotensin and glucagon. These major advances foster the understanding of structure-activity relationship of these receptors and structure-based rational design of new ligands having ...

2 GPCRs : new opportunities and challenges for drug discovery

Ethnobotany, Ethnopharmacology and Drug Discovery

     This manuscript is a review of a number of ethnobotany and ethnopharmacology texts and papers in order to arrive at current understanding and scope of ethnobotany and ethnopharmacology. It includes either a brief definition of both fields and presenting some examples on them. Also it has a glimpse on the geographical coverage of research works throughout the world, important issue of prope...

Fragment approaches in structure-based drug discovery

There has been considerable interest recently in what is known as ;fragment-based lead discovery'. The novel feature of the approach is to begin with small low-affinity compounds. The main advantage is that a larger potential chemical diversity can be sampled with fewer compounds, which is particularly important for new target classes. The approach relies on careful design of the fragment libra...

Structure-based approaches to antibiotic drug discovery.

The development of antimicrobials has advanced tremendously over the past century. However, as our production capacity increases, the threat of resistance is ever-present. To combat this resistance, two main avenues of drug discovery are being pursued: identifying new microbial proteins for which to direct drug discovery efforts, and designing innovative drugs that target existing proteins. The...