Pituitary tumours: the sst/D2 receptors as molecular targets.
Somatostatin (SS) and dopamine (DA) are among the key regulators of hormone secretion by the anterior pituitary gland. Concordantly, SS and DA receptors are expressed in the different pituitary cell types. SS receptors (sst) have a predominant inhibitory role in the regulation of growth hormone (GH) secretion, although the secretion of other pituitary hormones, e.g. prolactin (PRL), thyroid stimulating hormone (TSH) and adrenocorticotropic hormone (ACTH) is regulated by SS as well. DA receptors, in particular the D2 receptor (D2), has an important regulatory role in the control of PRL secretion. The inhibitory effects by SS and DA may be influenced by physiological feedback mechanisms, in part also involving modulation of pituitary sst and D2 expression. Pituitary tumours express both sst and/or D2 receptors. Targeting SS and DA receptors is used clinically to control hormonal hypersecretion by pituitary tumours, as well as tumour growth. The sst subtype, as well as the co-expression of sst and D2, has significant impact on the possibility to treat patients with pituitary tumours with SS analogues and DA agonists. In this review the current knowledge on the expression and functional roles of sst and D2 in pituitary tumours is discussed.
Hofland
Leo J
LJ
Department of Internal Medicine, Division of Endocrinology, Erasmus Medical Center, Rotterdam, The Netherlands. l.hofland@erasmusmc.nl
Feelders
Richard A
RA
de Herder
Wouter W
WW
Lamberts
Steven W J
SW
D018491:Dopamine Agonists / Q000627:therapeutic use; D006801:Humans; D010902:Pituitary Gland / Q000378:metabolism; D010911:Pituitary Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D017481:Receptors, Somatostatin / Q000378:metabolism*; D013004:Somatostatin / Q000031:analogs & derivatives / Q000627:therapeutic use
D018491:Dopamine Agonists; D017448:Receptors, Dopamine D2; D017481:Receptors, Somatostatin; D013004:Somatostatin