{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["15"],"submitter":["Kufka R"],"pubmed_abstract":["Tubugi-1 is a small cytotoxic peptide with picomolar cytotoxicity. To improve its cancer cell targeting, it was conjugated using a universal, modular disulfide derivative. This allowed conjugation to a neuropeptide-Y (NPY)-inspired peptide [K<sup>4</sup>(C-βA-),F<sup>7</sup>,L<sup>17</sup>,P<sup>34</sup>]-hNPY, acting as NPY Y1 receptor (hY1R)-targeting peptide, to form a tubugi-1-SS-NPY disulfide-linked conjugate. The cytotoxic impacts of the novel tubugi-1-NPY peptide-toxin conjugate, as well as of free tubugi-1, and tubugi-1 bearing the thiol spacer (liberated from tubugi-1-NPY conjugate), and native tubulysin A as reference were investigated by in vitro cell viability and proliferation screenings. The tumor cell lines HT-29, Colo320 (both colon cancer), PC-3 (prostate cancer), and in c"],"journal":["Beilstein journal of organic chemistry"],"pagination":["96-105"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6334802"],"repository":["biostudies-literature"],"pubmed_title":["Synthesis of a tubugi-1-toxin conjugate by a modulizable disulfide linker system with a neuropeptide Y analogue showing selectivity for hY1R-overexpressing tumor cells."],"pmcid":["PMC6334802"],"pubmed_authors":["Weber L","Kaluđerovic GN","Richter W","Wessjohann LA","Kufka R","Rennert R"],"additional_accession":[]},"is_claimable":false,"name":"Synthesis of a tubugi-1-toxin conjugate by a modulizable disulfide linker system with a neuropeptide Y analogue showing selectivity for hY1R-overexpressing tumor cells.","description":"Tubugi-1 is a small cytotoxic peptide with picomolar cytotoxicity. To improve its cancer cell targeting, it was conjugated using a universal, modular disulfide derivative. This allowed conjugation to a neuropeptide-Y (NPY)-inspired peptide [K<sup>4</sup>(C-βA-),F<sup>7</sup>,L<sup>17</sup>,P<sup>34</sup>]-hNPY, acting as NPY Y1 receptor (hY1R)-targeting peptide, to form a tubugi-1-SS-NPY disulfide-linked conjugate. The cytotoxic impacts of the novel tubugi-1-NPY peptide-toxin conjugate, as well as of free tubugi-1, and tubugi-1 bearing the thiol spacer (liberated from tubugi-1-NPY conjugate), and native tubulysin A as reference were investigated by in vitro cell viability and proliferation screenings. The tumor cell lines HT-29, Colo320 (both colon cancer), PC-3 (prostate cancer), and in c","dates":{"release":"2019-01-01T00:00:00Z","publication":"2019","modification":"2026-07-16T17:32:27.89Z","creation":"2025-05-29T19:42:06.974Z"},"accession":"S-EPMC6334802","cross_references":{"pubmed":["30680044"],"doi":["10.3762/bjoc.15.11"]}}