Human adrenoreceptor polymorphisms: evolving recognition of clinical importance

Article Abstract:

A review was conducted on studies concerning the assessment of adrenoreceptor polymorphisms in human subjects. One study analyzed the entire coding sequence of alpha 1B-adrenoreceptor and identified three various silent polymorphisms. Another examined the relationship between beta 2-adrenoreceptor polymorphisms and the development of asthma and hypertension. It was emphasized that polymorphisms in adrenoreceptors might represent only one type of genetic variation in adrenoreceptor signalling that could impact on the expression of a disease phenotype.

Hypertension, Genetic aspects, Asthma, Genetic polymorphisms

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On criteria for functional beta3-adrenoreceptors

Article Abstract:

Atypical low stereoselectivity is not a suitable criterion for the classification of beta3-adrenoreceptors due its inconsistency. The stereoselectivity of beta3-adrenoreceptor ligands is a function of ligand affinity hence its unsuitability as a criterion for beta3- adrenoreceptor classification. An additional classification criterion, blockade by beta3-adrenoreceptor-selective antagonists, can be used to increase accuracy.

Evaluation, Ligand binding (Biochemistry)

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Schwartz and Rosenkilde reply

Article Abstract:

Philip G. Strange's assertion about the role of hydrogen-binding in the binding of adrenoceptors is correct. His claim that the paradigm of adrenoceptor binding is misleading is also correct. Given the absence of methodologies for studying such a physiological process, however, it is virtually impossible to determine and characterize the precise location and mechanics of adrenoceptor binding.

DNA-ligand interactions, DNA binding

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