[HTML][HTML] Somatostatin-dopamine chimeric molecules in neuroendocrine neoplasms

MC Cantone, A Dicitore, G Vitale - Journal of Clinical Medicine, 2021 - mdpi.com
… of antiproliferative activity of somatostatin analogues (SSAs) … limitations, recently, a novel
chimeric compound named TBR-… be a new molecule with relevant perspectives in the therapy of …

[HTML][HTML] Somatostatin receptors and analogs in pheochromocytoma and paraganglioma: old players in a new precision medicine world

M Patel, I Tena, A Jha, D Taieb, K Pacak - Frontiers in Endocrinology, 2021 - frontiersin.org
… in the administration of somatostatin analogs, both “cold”, … We also explore future perspectives
for SSTRs and SSAs in … Dopastatin, a novel chimeric analog with dual binding ability …

A novel somatostatin-dopamine chimera (BIM23B065) reduced GH secretion in a first-in-human clinical trial

WMI de Boon, MJ van Esdonk… - The Journal of …, 2019 - academic.oup.com
… Proof of pharmacology of BIM23B065 was shown by a reduction in GH, IGF-1, and PRL
concentrations in healthy male volunteers, supporting activity of the somatostatin analog and …

Somatostatin receptor expression and patients' response to targeted medical treatment in pituitary tumors: evidences and controversies

F Gatto, M Arvigo, D Ferone - Journal of Endocrinological Investigation, 2020 - Springer
… For these reasons, a new generation chimeric agonist for SST 2 /SST 5 /D2R (BIM-065),
has … clinical use of this chimeric molecule. Somatostatin receptor expression and medical …

Efficacy of a novel second-generation somatostatin-dopamine chimera (TBR-065) in human medullary thyroid cancer: A preclinical study

A Dicitore, MC Cantone, G Gaudenzi, D Saronni… - …, 2021 - karger.com
… Both octreotide and lanreotide (LAN), 2 somatostatin analogs (SSAs) with high affinity for
SST 2 and moderate activity for SST 5 , have shown an inhibitory effect in vitro in controlling …

[HTML][HTML] Biological and biochemical basis of the differential efficacy of first and second generation somatostatin receptor ligands in neuroendocrine neoplasms

F Gatto, F Barbieri, M Arvigo, S Thellung… - International Journal of …, 2019 - mdpi.com
… Dimerization is a novel frontier in the regulation of the activity of GPCRs. In fact, this receptor
family activity is modulated by homo-dimerization or hetero-dimerization, the latter possibly …

[HTML][HTML] Structural insights into ligand recognition and selectivity of somatostatin receptors

W Zhao, S Han, N Qiu, W Feng, M Lu, W Zhang… - Cell Research, 2022 - nature.com
Somatostatin receptors (SSTRs) play versatile roles in inhibiting the secretion of multiple
hormones such as growth hormone and thyroid-stimulating hormone, and thus are considered …

A new generation somatostatin-dopamine analogue exerts potent antitumoral actions on pituitary neuroendocrine tumor cells

MC Vázquez-Borrego, MA Gálvez-Moreno… - …, 2020 - karger.com
… is, somatostatin analogs (SSAs) or dopamine-agonists (DA). Thus, novel, chimeric somatostatin/…
Conclusions: Our results unveil a robust antitumoral effect in vitro of the novel chimeric

A novel somatostatin receptor ligand for human ACTH–and GH–secreting pituitary adenomas

D Regazzo, S Avallone… - European Journal of …, 2024 - academic.oup.com
… In conclusion, our study, the first to evaluate the effect of a novel somatostatin receptor 5-preferring
ligand, shows that HTL0030310 can restrain hormone synthesis and secretion in …

[HTML][HTML] Development of anti-somatostatin receptors CAR T cells for treatment of neuroendocrine tumors

B Mandriani, E Pellè, F Mannavola… - … for Immunotherapy of …, 2022 - ncbi.nlm.nih.gov
somatostatin receptors and somatostatin analogs as well as radiolabeled somatostatin
analogs are … We developed a second-generation chimeric antigen receptor (CAR) construct …