دورية أكاديمية
أعرض في EDS

The Novel SSTR3 Agonist ITF2984 Exerts Antimitotic and Proapoptotic Effects in Human Non-Functioning Pituitary Neuroendocrine Tumor (NF-PitNET) Cells.

التفاصيل البيبلوغرافية
العنوان: The Novel SSTR3 Agonist ITF2984 Exerts Antimitotic and Proapoptotic Effects in Human Non-Functioning Pituitary Neuroendocrine Tumor (NF-PitNET) Cells.
المؤلفون: Di Muro G; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy.; Department of Experimental Medicine, University Sapienza of Rome, 00100 Rome, Italy., Catalano R; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy., Treppiedi D; Endocrinology Unit, Fondazione Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS) Ca' Granda Ospedale Maggiore Policlinico, 20122 Milan, Italy., Barbieri AM; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy., Mangili F; Endocrinology Unit, Fondazione Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS) Ca' Granda Ospedale Maggiore Policlinico, 20122 Milan, Italy., Marra G; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy., Di Bari S; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy., Esposito E; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy.; PhD Program in Experimental Medicine, University of Milan, 20100 Milan, Italy., Nozza E; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy.; PhD Program in Experimental Medicine, University of Milan, 20100 Milan, Italy., Lania AG; Department of Biomedical Sciences, Humanitas University, 20090 Pieve Emanuele, Italy.; Endocrinology and Diabetology Unit, Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS) Humanitas Research Hospital, 20089 Rozzano, Italy., Ferrante E; Endocrinology Unit, Fondazione Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS) Ca' Granda Ospedale Maggiore Policlinico, 20122 Milan, Italy., Locatelli M; Neurosurgery Unit, Fondazione Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS) Ca' Granda Ospedale Maggiore Policlinico, 20122 Milan, Italy.; Department of Pathophysiology and Transplantation, University of Milan, 20122 Milan, Italy., Modena D; Preclinical R&D, Italfarmaco Group, Cinisello Balsamo, 20092 Milan, Italy., Steinkuhler C; Preclinical R&D, Italfarmaco Group, Cinisello Balsamo, 20092 Milan, Italy., Peverelli E; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy.; Endocrinology Unit, Fondazione Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS) Ca' Granda Ospedale Maggiore Policlinico, 20122 Milan, Italy., Mantovani G; Department of Clinical Sciences and Community Health, University of Milan, 20122 Milan, Italy.; Endocrinology Unit, Fondazione Istituto di Ricovero e Cura a Carattere Scientifico (IRCCS) Ca' Granda Ospedale Maggiore Policlinico, 20122 Milan, Italy.
المصدر: International journal of molecular sciences [Int J Mol Sci] 2024 Mar 23; Vol. 25 (7). Date of Electronic Publication: 2024 Mar 23.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: MDPI Country of Publication: Switzerland NLM ID: 101092791 Publication Model: Electronic Cited Medium: Internet ISSN: 1422-0067 (Electronic) Linking ISSN: 14220067 NLM ISO Abbreviation: Int J Mol Sci Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI, [2000-
مواضيع طبية MeSH: Antimitotic Agents* , Neuroendocrine Tumors*/drug therapy , Pituitary Neoplasms*/drug therapy , Pituitary Neoplasms*/genetics, Humans ; Octreotide/pharmacology ; Octreotide/therapeutic use ; Receptors, Somatostatin/genetics
مستخلص: Somatostatin receptor ligands (SRLs) with high affinity for somatostatin receptors 2 and 5 (SSTR2 and SSTR5) are poorly efficacious in NF-PitNETs, expressing high levels of SSTR3. ITF2984 is a pan-SSTR ligand with high affinity for SSTR3, able to induce SSTR3 activation and to exert antitumoral activity in the MENX rat model. The aim of this study was to test ITF2984's antiproliferative and proapoptotic effects in NF-PitNET primary cultured cells derived from surgically removed human tumors and to characterize their SSTR expression profile. We treated cells derived from 23 NF-PitNETs with ITF2984, and a subset of them with octreotide, pasireotide (SRLs with high affinity for SSTR2 or 5, respectively), or cabergoline (DRD2 agonist) and we measured cell proliferation and apoptosis. SSTR3, SSTR2, and SSTR5 expression in tumor tissues was analyzed by qRT-PCR and Western blot. We demonstrated that ITF2984 reduced cell proliferation (-40.8 (17.08)%, p < 0.001 vs. basal, n = 19 NF-PitNETs) and increased cell apoptosis (+41.4 (22.1)%, p < 0.001 vs. basal, n = 17 NF-PitNETs) in all tumors tested, whereas the other drugs were only effective in some tumors. In our model, SSTR3 expression levels did not correlate with ITF2984 antiproliferative nor proapoptotic effects. In conclusion, our data support a possible use of ITF2984 in the pharmacological treatment of NF-PitNET.
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معلومات مُعتمدة: IG 2022-27540 Italian Association for Cancer Research; 2022CZR88M MIUR- Progetti di Ricerca di Interesse Nazionale (PRIN); Ricerca Corrente Italian Ministry of Health
فهرسة مساهمة: Keywords: ITF2984; NF-PitNETs; SSTRs
المشرفين على المادة: 0 (Antimitotic Agents)
RWM8CCW8GP (Octreotide)
0 (Receptors, Somatostatin)
تواريخ الأحداث: Date Created: 20240413 Date Completed: 20240415 Latest Revision: 20240425
رمز التحديث: 20240425
مُعرف محوري في PubMed: PMC11011875
DOI: 10.3390/ijms25073606
PMID: 38612419
قاعدة البيانات: MEDLINE
الوصف
تدمد:1422-0067
DOI:10.3390/ijms25073606