{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,17]],"date-time":"2026-03-17T14:12:13Z","timestamp":1773756733301,"version":"3.50.1"},"reference-count":41,"publisher":"Wiley","issue":"8","license":[{"start":{"date-parts":[[2009,1,29]],"date-time":"2009-01-29T00:00:00Z","timestamp":1233187200000},"content-version":"vor","delay-in-days":3591,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["bpspubs.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["British J Pharmacology"],"published-print":{"date-parts":[[1999,4]]},"abstract":"<jats:p>\n<jats:list list-type=\"explicit-label\">\n<jats:list-item><jats:p>Small, N\u2010 to C\u2010terminal cyclized peptides containing the leucyl\u2010aspartyl\u2010valine (LDV) motif from fibronectin connecting segment\u20101 (CS\u20101) have been investigated for their effects on the adhesion of human T\u2010lymphoblastic leukaemia cells (MOLT\u20104) to human plasma fibronectin <jats:italic>in vitro<\/jats:italic> mediated by the integrin Very Late Antigen (VLA)\u20104 (\u03b1<jats:sub>4<\/jats:sub>\u03b2<jats:sub>1<\/jats:sub>, CD49d\/CD29).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Cyclo(\u2010isoleucyl\u2010leucyl\u2010aspartyl\u2010valyl\u2010aminohexanoyl\u2010) (c(ILDV\u2010NH(CH<jats:sub>2<\/jats:sub>)<jats:sub>5<\/jats:sub>CO)) was approximately 5 fold more potent (IC<jats:sub>50<\/jats:sub> 3.6\u00b10.44\u2003\u03bc<jats:sc>M<\/jats:sc>) than the 25\u2010amino acid linear CS\u20101 peptide. Cyclic peptides containing two more or one less methylene groups had similar potency to c(ILDV\u2010NH(CH<jats:sub>2<\/jats:sub>)<jats:sub>5<\/jats:sub>CO) while a compound containing three less methylene groups, c(ILDV\u2010NH(CH<jats:sub>2<\/jats:sub>)<jats:sub>2<\/jats:sub>CO), was inactive at 100\u2003\u03bc<jats:sc>M<\/jats:sc>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>c(ILDV\u2010NH(CH<jats:sub>2<\/jats:sub>)<jats:sub>5<\/jats:sub>CO) had little effect on cell adhesion mediated by two other integrins, VLA\u20105 (\u03b1<jats:sub>5<\/jats:sub>,\u03b2<jats:sub>1<\/jats:sub>, CD49e\/CD29) (K562 cell adhesion to fibronectin) or Leukocyte Function Associated molecule\u20101 (LFA\u20101, \u03b1<jats:sub>L<\/jats:sub>\u03b2<jats:sub>2<\/jats:sub>, CD11a\/CD18) (U937 cell adhesion to Chinese hamster ovary cells transfected with intercellular adhesion molecule\u20101) at concentrations up to 300\u2003\u03bc<jats:sc>M<\/jats:sc>.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>c(ILDV\u2010NH(CH<jats:sub>2<\/jats:sub>)<jats:sub>5<\/jats:sub>CO) inhibited ovalbumin delayed\u2010type hypersensitivity or oxazolone contact hypersensitivity in Balb\/c mice when dosed continuously from subcutaneous osmotic mini\u2010pumps (0.1\u201310\u2003mg\u2003kg<jats:sup>\u22121<\/jats:sup> day<jats:sup>\u22121<\/jats:sup>). Maximum inhibition (approximately 40%) was similar to that caused by the monoclonal antibody PS\/2 (7.5\u2003mg\u2003kg<jats:sup>\u22121<\/jats:sup> i.v.) directed against the \u03b1<jats:sub>4<\/jats:sub> integrin subunit.<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>c(ILDV\u2010NH(CH<jats:sub>2<\/jats:sub>)<jats:sub>5<\/jats:sub>CO) also inhibited oxazolone contact hypersensitivity when dosed intravenously 20\u2003h after oxazolone challenge (1\u201310\u2003mg\u2003kg<jats:sup>\u22121<\/jats:sup>). Ear swelling was reduced at 3\u2003h and 4\u2003h but not at 1\u2003h and 2\u2003h post\u2010dose (10\u2003mg\u2003kg<jats:sup>\u22121<\/jats:sup>).<\/jats:p><\/jats:list-item>\n<jats:list-item><jats:p>Small molecule VLA\u20104 inhibitors derived from c(ILDV\u2010NH(CH<jats:sub>2<\/jats:sub>)<jats:sub>5<\/jats:sub>CO) may be useful as anti\u2010inflammatory agents.<\/jats:p><\/jats:list-item>\n<\/jats:list>\n<\/jats:p><jats:p><jats:italic>British Journal of Pharmacology<\/jats:italic> (1999) <jats:bold>126<\/jats:bold>, 1751\u20131760; doi:<jats:ext-link xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" ext-link-type=\"doi\" xlink:href=\"10.1038\/sj.bjp.0702511\">10.1038\/sj.bjp.0702511<\/jats:ext-link><\/jats:p>","DOI":"10.1038\/sj.bjp.0702511","type":"journal-article","created":{"date-parts":[[2005,1,28]],"date-time":"2005-01-28T19:58:52Z","timestamp":1106942332000},"page":"1751-1760","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":31,"title":["Anti\u2010inflammatory activity of c(ILDV\u2010NH(CH<sub>2<\/sub>)<sub>5<\/sub>CO), a novel, selective, cyclic peptide inhibitor of VLA\u20104\u2010mediated cell adhesion"],"prefix":"10.1111","volume":"126","author":[{"given":"Duncan","family":"Haworth","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Amanda","family":"Rees","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Peter J","family":"Alcock","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Linda J","family":"Wood","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Anand S","family":"Dutta","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"James J","family":"Gormley","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Huw B","family":"Jones","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Alec","family":"Jamieson","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Christopher F","family":"Reilly","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2009,1,29]]},"reference":[{"key":"e_1_2_6_2_1","doi-asserted-by":"publisher","DOI":"10.1093\/infdis\/152.4.668"},{"key":"e_1_2_6_3_1","doi-asserted-by":"publisher","DOI":"10.1084\/jem.173.6.1553"},{"key":"e_1_2_6_4_1","doi-asserted-by":"publisher","DOI":"10.1002\/ana.410370404"},{"key":"e_1_2_6_5_1","doi-asserted-by":"crossref","first-page":"18668","DOI":"10.1016\/S0021-9258(17)32362-1","article-title":"Cyclic RGD peptide inhibits \u03b14\u03b21 interaction with connecting segment 1 and vascular cell adhesion molecule","volume":"269","author":"CARDARELLI P.M.","year":"1994","journal-title":"J. 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