Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation.

Shimon, Ilan; Taylor, John E.; Dong, Jesse Z.; Bitonte, R A; Kim, S; Morgan, Barry A.; Coy, David H.; Culler, Michael D.; Melmed, Shlomo

doi:10.1172/jci119225

Cited by 297 publications

(196 citation statements)

References 62 publications

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“…Bim 23745, Bim 23120 and Bim 23206 are fully selective analogs for the SSTR1, 2 and 5 subtypes respectively, as can be seen from the IC 50 s presented in Table 1. This is the ¢rst report showing the binding a¤nities for these three analogs and the method used for determining the K i is as reported in [9]. In our experiments these three compounds were used as speci¢c ligands for the individual SST receptor subtypes 1, 2 and 5.…”

Section: Sstr Subtype Expression In Sy5y Cellsmentioning

confidence: 93%

“…1, we observed the expression of all ¢ve SSTR subtypes in SY5Y cells. Receptor binding assays were performed using membrane preparations obtained from transfected CHO-K1 cells expressing the human SSTR subtypes 1^5 as described previously [9]. The IC 50 values for the compounds used in our experiments are shown in Table 1.…”

Section: Sstr Subtype Expression In Sy5y Cellsmentioning

confidence: 99%

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Selective stimulation of somatostatin receptor subtypes: differential effects on Ras/MAP kinase pathway and cell proliferation in human neuroblastoma cells

Cattaneo

Taylor²,

Culler³

et al. 2000

FEBS Letters

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In previous studies we have showed that somatostatin (SST) inhibits cell division, mitogen-activated protein (MAP) kinase and Ras activity in the human neuroblastoma cell line SY5Y. In the present study, we have assessed the role of a series of SST analogs, three of which were selective for SSTR1, SSTR2 or SSTR5, in these cellular events. All the analogs inhibited forskolin-induced cAMP accumulation. Selective stimulation of SSTR1 or SSTR2 but not of SSTR5 inhibited platelet-derived growth factor (PDGF)-induced [ 3 H]thymidine incorporation. The three analogs inhibited PDGF-stimulated MAP kinase activity, at least at an early time. In contrast, none of the analogs used individually was able to inhibit PDGFstimulated Ras activity. A combined stimulation of SSTR2 and SSTR5 was necessary to obtain a significant inhibitory effect, suggesting the possibility of receptor heterodimerization. These results indicate that SST inhibition of Ras and MAP kinase activities takes place via different pathways and that SST inhibition of PDGF-induced cell proliferation occurs via a Rasindependent pathway. ß

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Section: Sstr Subtype Expression In Sy5y Cellsmentioning

confidence: 93%

Section: Sstr Subtype Expression In Sy5y Cellsmentioning

confidence: 99%

Selective stimulation of somatostatin receptor subtypes: differential effects on Ras/MAP kinase pathway and cell proliferation in human neuroblastoma cells

Cattaneo

Taylor²,

Culler³

et al. 2000

FEBS Letters

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“…Agonists A very recent study (Ludvigsen et al, 2007) evaluated the effects of the following agonists on insulin and glucagon secretion from isolated rat pancreatic islets: SOM230 (panagonist), SSTR1-selective (BIM-23926 IC50 of 3.6 nM for SSTR1 and > 800 nM for other SSTRs (Zatelli et al, 2002)), SSTR2-selective (BIM-23120, IC50 of 0.34 nM for SSTR2, and over 200 nM for other SSTRs (Zatelli et al, 2001;Zatelli et al, 2002;Shimon et al, 1997b;Shimon et al, 1997a;Saveanu et al, 2001)) and SSTR5-selective (BIM-23206, IC50 of 2.4 nM for SSTR5 and more than 15 nM for other 4 SSTRs). SOM230 was a superior inhibitor of insulin secretion as compared to octreotide or SST-14 after a longer incubation period of 48 hours.…”

Section: In Vitro Studiesmentioning

confidence: 99%

Function and expression of somatostatin receptors of the endocrine pancreas

Strowski

Blake

2008

Molecular and Cellular Endocrinology

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“…While in contrast Smith et al found a predominance of sst2 rather than sst5 (68). It is generally accepted that sst2 and sst5 are involved in the regulation of growth hormone, prolactin and TSH (69).…”

Section: Somatostatin Analoguesmentioning

confidence: 89%

Pharmacological management of Cushing's syndrome: an update

Dang

Trainer

2007

Arq Bras Endocrinol Metab

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The treatment of choice for Cushing's syndrome remains surgical. The role for medical therapy is twofold. Firstly it is used to control hypercortisolaemia prior to surgery to optimize patient's preoperative state and secondly, it is used where surgery has failed and radiotherapy has not taken effect. The main drugs used inhibit steroidogenesis and include metyrapone, ketoconazole, and mitotane. RESUMOManejo Farmacológico da Síndrome de Cushing: Uma Atualização. O tratamento de escolha para a síndrome de Cushing ainda é a cirurgia. O papel da terapia medicamentosa é duplo: ele é usado para controlar o hipercortisolismo antes da cirurgia e otimizar o estado pré-operatório do paciente e, adicionalmente, quando ocorre falha cirúrgica e a radioterapia ainda não se mostrou efetiva. Os principais medicamentos são empregados para inibir a esteroidogênese e incluem: metirapona, cetoconazol e mitotano. Medicamentos visando o eixo hipotálamo-hipofisário têm sido investigados, mas seu papel na prática clínica permanece limitado, embora o agonista PPAR-γ e análogo de somatostatina, som-230 (pasireotídeo), requeira estudos adicionais. A única droga que age perifericamente no receptor glicocorticóide é a mifepristona (RU486). O manejo da síndrome de Cushing deve envolver uma combinação terapêutica atuando em diferentes vias da hipercortisolemia, mas o monitoramento dessa terapia ainda permanece um desafio. (Arq Bras Endocrinol Metab

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Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation.

Cited by 297 publications

References 62 publications

Selective stimulation of somatostatin receptor subtypes: differential effects on Ras/MAP kinase pathway and cell proliferation in human neuroblastoma cells

Selective stimulation of somatostatin receptor subtypes: differential effects on Ras/MAP kinase pathway and cell proliferation in human neuroblastoma cells

Function and expression of somatostatin receptors of the endocrine pancreas

Pharmacological management of Cushing's syndrome: an update

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