Receptors as drug targets

Both enzymes and receptors are proteins, and therefore both biological structures share many fundamental similarities. Regardless their roles within a biological system are distinct from one another. 

SCHEME 5.2 General pathway for response generation from a receptor 

The similarities between enzymes and receptors allow both systems to be modeled with many of the same mathematical equations. Most treatments of receptors and enzymes appear to be very different, but the derivations and theories can largely be recycled between the two topics. 

The events initiated from the ligand-receptor complex are more complex than a simple substrate-to-product conversion by an enzyme. For this reason, receptor activity is more difficult to model mathematically than enzymatic activity. 

The primary method for determining protein structure is x-ray crystallography. Unfortunately, the receptors most frequently targeted by the pharmaceutical industry are embedded in cell membranes. The cell membrane plays a vital role in determining the overall shape of a membrane-bound receptor. Crystallization is performed in the absence of membrane lipids, so x-ray information is not representative of the true receptor structure. Therefore, reliable structural information on receptors is difficult to obtain. 

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Tobin, J. F., and Freeman, L. P. (2006). Nuclear receptors as drug targets in metabolic diseases New approaches to therapy. Trends Endocrinol. Metab. 17, 284-290. 

Tang, C. M., and Insel, P. A. (2005) Genetic variation in G-protein-coupled receptors—consequences for G-protein-coupled receptors as drug targets. Expert. Opin Then Targets. 9,1247-1265. 

R. C. Flogg, D. Bertrand (2004). Nicotinic acetylcholine receptors as drug targets. Curr. Drug Targ. CNSNeurol. Disorders 3 I23-I30. 

In the 20 years since Daly reported the potential of adenosine receptors as drug targets (Daly, 1982), considerable advances have been made in the field of purinergic receptor-related research. Although a range of neurotransmitters is known, today there is no doubt that adenosine and adenosine 5 -triphosphate (ATP) also play an important role in the process of cell to cell communication. This function leads to multiple potential indications for research on adenosine and ATP, e.g. neurodegeneration or cardiovascular diseases, but here the focus lies on adenosine s role in pain (see also review by Salter and Sollevi, 2001). 

Johnsoton GA, Chebib M, Hanrahan JR, Mewett KN (2003) GABA(C) receptors as drug targets. 

Nuclear Receptors as Drug Targets A Historical Perspective of Modern Drug Discovery... 

Nuclear Receptors as Drug Targets. Edited by Eckhard Ottow and Hilmar Weinmann Copyright 2008 WILEY-VCH Verlag GmbH Co. KGaA, Weinheim ISBN 978-3-527-31872-8... 

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