Insights into Receptor Function and New Drug Development Targets 2006th Edition by P Michael Conn, Claude Kordon ISBN 3540344462 9783540344469 by M Conn, C Kordon & Y Christen (eds.) 3540344462, 9783540344469 instant download after payment.

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ISBN 10: 3540344462 
ISBN 13: 9783540344469
Author: P Michael Conn, Claude Kordon

We are now on the verge of viewing effector molecules and other regulatory sites as therapeutic targets for the amelioration of human and animal disease. The recognition, for example, that mutant proteins are frequently misrouted molecules, rather than functionally defective ones, changes our approach to "inborn errors of metabolism" and offers new approaches for pharmacological discovery, based on rescue of receptors, ion channels and enzymes with pharmacoperones. Ion channels, regulators of G-protein signaling and enzymes engaged in regulation, now present opportunities for drug development.

The state of our art also benefits by the availability of superior tools that allow measurement of interactions and afford unprecedented insight into the biomolecular interactions that present novel approaches to drug design.

Insights into Receptor Function and New Drug Development Targets 2006th Table of contents:

• Introduction to Receptor Function and Drug Discovery
  • The importance of receptors (e.g., GPCRs, nuclear receptors) as drug targets.
  • Evolution of drug discovery methods (combinatorial chemistry, high-throughput screening).
• G-Protein Coupled Receptors (GPCRs)
  • GPCR structure and signaling mechanisms.
  • GPCRs in physiological processes (growth, food intake, reproduction, water balance, sensory perception, blood pressure, heart rate).
  • GPCRs as major drug targets (current and future).
  • New insights into GPCR function (e.g., inverse agonism, signaling bias, oligomerization, allosteric modulation).
  • GPCRomics: Identifying and quantifying GPCR expression for drug targets.
• Nuclear Receptors
  • Functional domains of nuclear receptors (DNA-binding domain, ligand-binding domain).
  • Role of nuclear receptors in development, differentiation, and metabolic homeostasis.
  • Classic receptors vs. orphan and "adopted" orphan receptors.
  • Nuclear receptors as drug targets.
• Ion Channels
  • Ion channels as therapeutic targets.
  • Specific examples of ion channels and their role in disease.
• Protein Trafficking and Misfolded Receptors
  • The concept of pharmacoperones and rescue of misrouted or misfolded receptors.
  • Implications for "inborn errors of metabolism" and new drug development approaches.
• Regulators of G-Protein Signaling (RGS Proteins)
  • RGS proteins as potential drug targets.
  • Enhancing agonist specificity through targeting RGS proteins.
• Receptor-Receptor Interactions and Cross-Talk
  • The phenomenon of receptor complexes (e.g., dimeric GPCRs).
  • Integration of signals at the plasma membrane level.
  • New therapeutic approaches based on receptor-receptor interactions.
• Novel Ligands and Therapeutic Strategies
  • Development of peptidic and non-peptidic ligands.
  • Pepducins and their role in modulating GPCR activity.
  • Strategies for targeting orphan receptors.
  • Peptidomimetics in drug design.
• Specific Receptor Systems and Their Drug Targets (Examples might include chapters on):
  • Ghrelin receptor
  • Nociceptin receptor
  • Apelin receptor
  • Urocortin receptor
  • Leptin and melanocortin receptors (and obesity-related mutations)
  • VIP and PACAP receptors
  • Endogenous cannabinoid system
  • Glycoprotein hormone receptors
  • Metabotropic glutamate receptors
• Advanced Tools and Technologies for Receptor Research and Drug Development
  • Techniques for measuring biomolecular interactions.
  • High-throughput screening.
  • Genomic approaches for target identification.

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Tags: P Michael Conn, Claude Kordon, Receptor, Function