title: Neurotensin branched peptide as a tumor-targeting agent for human bladder cancer.
abstract: Despite recent advances in multimodal therapy, bladder cancer still ranks ninth in worldwide cancer incidence. New molecules which might improve early diagnosis and therapeutic efficiency for tumors of such high epidemiological impact therefore have very high priority. In the present study, the tetrabranched neurotensin peptide NT4 was conjugated with functional units for cancer-cell imaging or therapy and was tested on bladder cancer cell lines and specimens from bladder cancer surgical resections, in order to evaluate its potential for targeted personalized therapy of bladder cancer. Fluorophore-conjugated NT4 distinguished healthy and cancer tissues with good statistical significance (P < 0.05). NT4 conjugated to methotrexate or gemcitabine was cytotoxic for human bladder cancer cell lines at micromolar concentrations. Their selectivity for bladder cancer tissue and capacity to carry tracers or drugs make NT4 peptides candidate tumor targeting agents for tracing cancer cells and for personalized therapy of human bladder cancer.
authors.affiliation: Department of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.
authors.forename: Jlenia
authors.initials: J
authors.lastname: Brunetti
authors.affiliation: Department of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Falciani
authors.affiliation: Department of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.
authors.forename: Barbara
authors.initials: B
authors.lastname: Lelli
authors.affiliation: Department of Urology, University of Florence, Careggi Hospital, 50139 Florence, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Minervini
authors.affiliation: Department of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.
authors.forename: Niccolò
authors.initials: N
authors.lastname: Ravenni
authors.affiliation: Department of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.
authors.forename: Lorenzo
authors.initials: L
authors.lastname: Depau
authors.affiliation: Department of Urology, University of Florence, Careggi Hospital, 50139 Florence, Italy.
authors.forename: Giampaolo
authors.initials: G
authors.lastname: Siena
authors.affiliation: Department of Chemistry, University of Florence, 50019 Florence, Italy.
authors.forename: Eleonora
authors.initials: E
authors.lastname: Tenori
authors.affiliation: Department of Chemistry, University of Florence, 50019 Florence, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Menichetti
authors.affiliation: Department of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.
authors.forename: Alessandro
authors.initials: A
authors.lastname: Pini
authors.affiliation: Department of Urology, University of Florence, Careggi Hospital, 50139 Florence, Italy.
authors.forename: Marco
authors.initials: M
authors.lastname: Carini
authors.affiliation: Department of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.
authors.forename: Luisa
authors.initials: L
authors.lastname: Bracci
mesh_terms: D000368:Aged; D000369:Aged, 80 and over; D000970:Antineoplastic Agents / Q000494:pharmacology; D001706:Biopsy; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D003841:Deoxycytidine / Q000031:analogs & derivatives / Q000494:pharmacology; D004705:Endocytosis / Q000187:drug effects; D005260:Female; D005453:Fluorescence; D006801:Humans; D008297:Male; D008727:Methotrexate / Q000494:pharmacology; D008875:Middle Aged; D009496:Neurotensin / Q000494:pharmacology / Q000627:therapeutic use*; D011485:Protein Binding / Q000187:drug effects; D001749:Urinary Bladder Neoplasms / Q000188:drug therapy* / Q000473:pathology; D000093542:Gemcitabine
chemical_list: D000970:Antineoplastic Agents; D003841:Deoxycytidine; D009496:Neurotensin; D008727:Methotrexate; D000093542:Gemcitabine