{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,1,20]],"date-time":"2026-01-20T01:52:04Z","timestamp":1768873924611,"version":"3.49.0"},"reference-count":48,"publisher":"Wiley","issue":"4-5","license":[{"start":{"date-parts":[[2018,4,15]],"date-time":"2018-04-15T00:00:00Z","timestamp":1523750400000},"content-version":"vor","delay-in-days":14,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Journal of Peptide Science"],"published-print":{"date-parts":[[2018,4]]},"abstract":"<jats:p>Interleukin (IL)\u201315 is an inflammatory cytokine that constitutes a validated therapeutic target in some immunopathologies, including rheumatoid arthritis (RA). Previously, we identified an IL\u201015 antagonist peptide named [K6T]P8, with potential therapeutic application in RA. In the current work, the metabolic stability of this peptide in synovial fluids from RA patients was studied. Moreover, [K6T]P8 peptide was labeled with <jats:sup>99m<\/jats:sup>Tc to investigate its stability in human plasma and its biodistribution pattern in healthy rats. The biological activity of [K6T]P8 peptide and its dimer was evaluated in CTLL\u20102 cells, using 3 different additives to improve the solubility of these peptides. The half\u2010life of [K6T]P8 in human synovial fluid was 5.88\u00a0\u00b1\u00a01.73\u00a0minutes, and the major chemical modifications included peptide dimerization, cysteinylation, and methionine oxidation. Radiolabeling of [K6T]P8 with <jats:sup>99m<\/jats:sup>Tc showed a yield of approximately 99.8%. The <jats:sup>99m<\/jats:sup>Tc\u2010labeled peptide was stable in a 30\u2010fold molar excess of cysteine and in human plasma, displaying a low affinity to plasma proteins. Preliminary biodistribution studies in healthy Wistar rats suggested a slow elimination of the peptide through the renal and hepatic pathways. Although citric acid, sucrose, and Tween 80 enhanced the solubility of [K6T]P8 peptide and its dimer, only the sucrose did not interfere with the <jats:italic>in vitro<\/jats:italic> proliferation assay used to assess their biological activity. The results here presented, reinforce nonclinical characterization of the [K6T]P8 peptide, a potential agent for the treatment of RA and other diseases associated with IL\u201015 overexpression.<\/jats:p>","DOI":"10.1002\/psc.3078","type":"journal-article","created":{"date-parts":[[2018,4,15]],"date-time":"2018-04-15T18:29:29Z","timestamp":1523816969000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["<i>In vitro<\/i> and <i>in vivo<\/i> characterization of an interleukin\u201015 antagonist peptide by metabolic stability, <sup>99m<\/sup>Tc\u2010labeling, and biological activity assays"],"prefix":"10.1002","volume":"24","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-9428-5606","authenticated-orcid":false,"given":"Yunier","family":"Rodr\u00edguez\u2010\u00c1lvarez","sequence":"first","affiliation":[{"name":"Pharmaceutical Department Center for Genetic Engineering and Biotechnology  Avenue 31, PO Box 6162 Havana 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