![]() ![]() Notably, agents with subtype selectivity have always been pursued in drug discovery targeting SSTR2, which could facilitate to improve the efficacy of potential drugs and avoid of side effects caused by off-target 4, 7, 12. Second-generation drugs have been developed and were recently reported to exhibit high safety profile 11. ![]() However, ~30% of the acromegalic patients do not respond well to octreotide 10. The first-generation drug octreotide is a biologically stable synthesized SST analog used for the treatment of acromegaly 7, 9. A series of long-acting SST analogs have been developed and explored in clinical trials 8. ![]() However, the use of SST for disease treatment is limited owing to its short half-life in the body. Previous studies have shown that SSTs and analogs are linked to decreased GH secretion, suggesting that the SSTR family may be a major therapeutic target for NETs 1. SSTRs and their endogenous ligands, somatostatin (SST) peptides, exert important physiological regulation of neuroendocrine functions 7. SSTRs, especially SSTR2, are expressed at high levels in NETs and have emerged as important biomarkers 4, 6. Somatostatin receptors (SSTRs) are members of the G protein-coupled receptor (GPCR) superfamily and contain five subtypes (SSTR1–5). Treatment of NETs include strategies that inhibit excess hormones and block hormone action 4, 5. For example, pituitary adenoma is a tumor of the pituitary gland that produces too much growth hormone (GH) and can lead to acromegaly 3. Neuroendocrine tumors (NETs) are rare and serious tumors that are commonly caused by the excessive secretion of hormones, which result in complicated clinical syndromes and disorders 1, 2. ![]()
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