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Beta 1- and beta 2-adrenoceptor polymorphisms and cardiovascular diseases
Kirsten Leineweber1, Gerd Heusch
1Institute for Pathophysiology, University of Essen, School of Medicine, Essen, Germany. kirsten.leineweber@bayerhealthcare.com
British Journal of Pharmacology
|May 9, 2009
Summary
Genetic variations in beta-adrenergic receptors (AR) influence cardiovascular function and drug response. These beta-AR single nucleotide polymorphisms (SNPs) may predict patient responsiveness to medications rather than cause disease.
Area of Science:
- Pharmacogenomics
- Cardiovascular Physiology
- Molecular Biology
Background:
- Beta-1 and beta-2 adrenoceptors (AR) are crucial for cardiovascular regulation.
- Polymorphisms in beta-AR genes, specifically single nucleotide polymorphisms (SNPs), are common and may alter receptor function.
- Understanding these genetic variations is key to personalized medicine in cardiovascular and pulmonary diseases.
Purpose of the Study:
- To review the functional relevance of known beta-AR SNPs.
- To explore the in vivo phenotypic consequences of these SNPs in cardiovascular and pulmonary diseases.
- To assess the predictive value of beta-AR SNPs for drug responsiveness.
Main Methods:
- Review of existing literature on beta-AR gene polymorphisms.
- Analysis of functional data from recombinant cell systems.
- Correlation of SNP genotypes with clinical phenotypes and drug responses in human studies.
Main Results:
- Specific beta-1-AR SNPs (Ser49Gly, Arg389Gly) affect receptor regulation and responsiveness.
- Beta-2-AR SNPs (Arg-19Cys, Arg16Gly, Gln27Glu, Thr164Ile) influence receptor expression, down-regulation, and stimulation response.
- Certain beta-AR SNP genotypes are associated with differential responses to agonists and antagonists, and may predict outcomes in conditions like asthma.
Conclusions:
- Beta-AR SNPs are unlikely to be disease-causing but are likely predictive of drug response.
- The Arg389Gly-beta(1)-AR polymorphism influences responsiveness to cardiovascular drugs.
- Specific beta-2-AR genotypes and haplotypes impact bronchodilator efficacy and desensitization, particularly in asthma patients.
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