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001-es BibID:	BIBFORM082392
035-os BibID:	(PMID)31614426 (cikkazonosító)5027 (scopus)85073444152 (wos)000498822800059
Első szerző:	Pethő Lilla
Cím:	Suitability of GnRH Receptors for Targeted Photodynamic Therapy in Head and Neck Cancers / Lilla Pethő, József Murányi, Kinga Pénzes, Bianka Gurbi, Diána Brauswetter, Gábor Halmos, Gabriella Csík, Gábor Mező
Dátum:	2019
ISSN:	1661-6596 1422-0067
Megjegyzések:	Head and neck squamous cell carcinomas (HNSCC) have a high mortality rate, although several potential therapeutic targets have already been identified. Gonadotropin-releasing hormone receptor (GnRH-R) expression is less studied in head and neck cancers, hence, we investigated the therapeutic relevance of GnRH-R targeting in HNSCC patients. Our results indicate that half of the patient-derived samples showed high GnRH-R expression, which was associated with worse prognosis, making this receptor a promising target for GnRH-based drug delivery. Photodynamic therapy is a clinically approved treatment for HNSCC, and the efficacy and selectivity may be enhanced by the covalent conjugation of the photosensitizer to a GnRH-R targeting peptide. Several native ligands, gonadotropin-releasing hormone (GnRH) isoforms, are known to target GnRH-R effectively. Therefore, different 4Lys(Bu) modified GnRH analogs were designed and conjugated to protoporphyrin IX. The receptor binding potency of the novel conjugates was measured on human pituitary and human prostate cancer cells, indicating only slightly lower GnRH-R affinity than the peptides. The in vitro cell viability inhibition was tested on Detroit-562 human pharyngeal carcinoma cells that express GnRH-R in high levels, and the results showed that all conjugates were more effective than the free protoporphyrin IX.
Tárgyszavak:	Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk GnRH GnRH-R conjugate head and neck cancer photodynamic therapy protoporphyrin targeted drug delivery
Megjelenés:	International Journal of Molecular Sciences. - 20 : 20 (2019), p. 1-17. -
További szerzők:	Murányi József Pénzes Kinga Gurbi Bianka Brauswetter Diána Halmos Gábor (1962-) (gyógyszerész, receptorfarmakológus, experimentális onkológus) Csík Gabriella Mező Gábor (1959-) (vegyész)
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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