Gene targeting--homing in on alpha 2-adrenoceptor-subtype function.
The alpha-adrenoceptor was subdivided into three subtypes: alpha 2A-, alpha 2B- and alpha 2C-adrenoceptors almost ten years ago. Since then, the search has been on to discover and develop subtype-selective agonists and antagonists, but as yet no major breakthrough has been made. In the past year, several strains of genetically engineered mice have become available, either overexpressing, totally lacking or expressing heavily modified alpha 2-adrenoceptor subtypes. Ewen MacDonald, Brian Kobilka and Mika Scheinin describe how these mice may be utilized to elucidate the physiological functions of the receptor subtypes and the properties of future subtype-selective drugs.
MacDonald
E
E
Department of Pharmacology and Toxicology, Universit of Kuopio, Finland.
Kobilka
B K
BK
Scheinin
M
M
D000316:Adrenergic alpha-Agonists / Q000494:pharmacology*; D000317:Adrenergic alpha-Antagonists / Q000494:pharmacology*; D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D015195:Drug Design; D005786:Gene Expression Regulation / Q000235:genetics; D005818:Genetic Engineering; D006801:Humans; D051379:Mice; D008969:Molecular Sequence Data; D010802:Phylogeny; D018341:Receptors, Adrenergic, alpha-2 / Q000737:chemistry / Q000145:classification / Q000235:genetics* / Q000378:metabolism; D013045:Species Specificity; D014018:Tissue Distribution
D000316:Adrenergic alpha-Agonists; D000317:Adrenergic alpha-Antagonists; D018341:Receptors, Adrenergic, alpha-2