الصفحة 1
الصفحة 1
Insights into Receptor Function and New Drug Development Targets
G-Protein Coupled receptors (GPCRs) and other receptors are significant targets for drug discovery, due to their roles in fundamental physiological processes. Among these roles are: regulation of growth, food intake, reproduction, water balance, sensory perception, blood pressure and heart rate. GPCR-directed drugs account for approximately $40 billion in sales and, of drugs at market, approximately 70% target GPCR function. The availability of combinatorial chemistry coupled with high throughput screening techniques have facilitated discovery of peptidic and non-peptidic ligands of membrane receptors. Mutant receptor models have revealed their role in health and disease and provided insight to new therapeutic approaches, based on control of protein trafficking. Understanding receptor-receptor interactions has provided one mechanism for receptor cross-talk and revealed unexpected interactions.
Hormones and the brain
Peripheral hormones have a major impact on the brain: they are able to interfere with its development, to affect release of neurotransmitters and concentrations of receptors, to trigger growth factors involved in lesion repair. These multiple actions account for their capacity to modulate a number of physiological parameters, from reproductive functions to memory, behaviour and aging. Depending upon intensity and duration of exposure, they can be either neuroprotective or neurotoxic, for instance by affecting production of free radicals. This book, based on contributions of pioneer investigators in the field, outlines the ambiguous actions of gonadal steroids (estradiol, progesterone, testosterone, inhibin and activin) and of neurosteroids, related moieties produced in the brain itself. After summarizing their multiple mechanisms of action, which involve both direct effects on neuronal membranes and activation of genes coding for specific proteins in neurons or glial cells, the book outlines the role of hormones in pathogenic processes such as mental disturbances or neurodegenerative diseases.
Hormones and social behaviour
This book concentrates on two major topics: First, the molecular and neural biology of hormone actions relevant to normal social behaviors; and Second, the clinical treatment of human patients in whom these behaviors have gone wrong.
