Molecular pharmacology : from DNA to drug discovery by John Dickenson, Fiona Freeman, Chris Lloyd Mills, Christian

By John Dickenson, Fiona Freeman, Chris Lloyd Mills, Christian Thode, Shiva Sivasubramaniam

This textbook offers a clean, complete and available advent to the quickly increasing box of molecular pharmacology. Adopting a drug target-based, instead of the conventional organ/system established, strategy this cutting edge advisor displays the present advances and learn pattern in the direction of molecular established drug layout, derived from a close realizing of chemical responses within the physique. medicinal drugs are then adapted to slot a remedy profile, instead of the conventional approach to 'trial and mistake' drug discovery which makes a speciality of checking out chemical compounds on animals or phone cultures and matching their results to remedies.

Providing a useful source for complicated under-graduate and MSc/PhD scholars, new researchers to the sphere and practitioners for carrying on with specialist improvement, ''Molecular Pharmacology'' explores; contemporary advances and advancements within the 4 significant human drug objective households (G-protein coupled receptors, ion channels, nuclear receptors and transporters), cloning of drug objectives, transgenic animal expertise, gene remedy, pharmacogenomics and appears on the function of calcium within the phone. present - makes a speciality of leading edge strategies and methods, together with new ways to quantify organic actions in numerous platforms and how you can interpret and comprehend pharmacological facts. leading edge - highlights advances in pharmacogenomics and explores how an individual's genetic make-up affects their reaction to healing medicines and the possibility of destructive uncomfortable side effects. utilized - comprises various, real-world examples and an in depth case-study dependent bankruptcy which appears to be like at present and attainable destiny remedy techniques for cystic fibrosis. this example examine considers the relative advantages of either drug remedy for particular sessions of mutation and gene treatment to right the underlying illness. available - incorporates a finished word list, feedback for additional analyzing on the finish of every bankruptcy and an linked site that gives an entire set of figures from in the ebook.

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Extra info for Molecular pharmacology : from DNA to drug discovery

Example text

The basic function of GPCRs is to detect extracellular signals and through G-protein activation trigger intracellular signal transduction cascades that lead to cellular responses. As such GPCRs regulate a wide variety of physiological processes. Approximately 400 GPCRs are classified as olfactory receptors since they are involved in the detection of smell and taste, with the remainder defined as non-olfactory. The potential number of receptor proteins is increased further if you take into account post-transcriptional modifications such as alternative splicing of pre-mRNA (some GPCR genes contain introns; covered later in this chapter) and RNA editing.

Nature 309: 418–425. Whiting PJ (2003). GABA-A receptor subtypes in the brain: A paradigm for CNS drug discovery? Drug Discovery Today 8: 445–450. Wieland HA, L¨uddens H and Seeburg PH (1992). A single histidine in GABAA receptors is essential for benzodiazepine agonist binding. Journal of Biological Chemistry 267: 1426–1429. Wise A, Gearing K and Rees S (2002). Target validation of Gprotein coupled receptors. Drug Discovery Today 7: 235–246. Zimmerman SB, Little JW, Oshinsky CK and Gellert M (1967).

It is vitally important to establish whether the physiological properties – and hence pharmacological profiles – of the ‘cloned’ and the ‘native’ drug targets are identical. If the outcome is negative, it may be because not all of the components of a given target have yet been cloned. In this case, it would not be recommended to pursue with a screen for novel therapeutic compounds using the ‘cloned’ target. A good example that demonstrates the need to identify all of the components of a given target is the GABAA receptor, which is the major inhibitory neurotransmitter receptor in brain.

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