{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,20]],"date-time":"2025-10-20T17:16:40Z","timestamp":1760980600592},"reference-count":50,"publisher":"Elsevier BV","issue":"10","license":[{"start":{"date-parts":[[2005,10,1]],"date-time":"2005-10-01T00:00:00Z","timestamp":1128124800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Peptides"],"published-print":{"date-parts":[[2005,10]]},"DOI":"10.1016\/j.peptides.2004.12.035","type":"journal-article","created":{"date-parts":[[2005,7,2]],"date-time":"2005-07-02T10:50:13Z","timestamp":1120301413000},"page":"2017-2025","source":"Crossref","is-referenced-by-count":10,"title":["Structure\u2013activity relationship of linear tetrapeptides Tic-DPhe-Arg-Trp-NH2 at the human melanocortin-4 receptor and effects on feeding behaviors in rat"],"prefix":"10.1016","volume":"26","author":[{"given":"Zhixiong","family":"Ye","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tanya","family":"MacNeil","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"David H.","family":"Weinberg","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rubana N.","family":"Kalyani","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rui","family":"Tang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Alison M.","family":"Strack","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Beth A.","family":"Murphy","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ralph T.","family":"Mosley","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"D.","family":"Euan MacIntyre","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Lex H.T.","family":"Van der Ploeg","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Arthur A.","family":"Patchett","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Matthew J.","family":"Wyvratt","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ravi P.","family":"Nargund","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"78","reference":[{"key":"10.1016\/j.peptides.2004.12.035_bib1","doi-asserted-by":"crossref","first-page":"2555","DOI":"10.1021\/jm00132a010","article-title":"Potent and prolonged acting cyclic lactam analogues of \u03b1-melanotropin: design based on molecular dynamics","volume":"32","author":"Al-Obeidi","year":"1989","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib2","doi-asserted-by":"crossref","first-page":"3413","DOI":"10.1021\/ja00191a044","article-title":"Design of a new class of superpotent cyclic \u03b1-melanotropins based on quenched dynamic simulations","volume":"111","author":"Al-Obeidi","year":"1989","journal-title":"J Am Chem Soc"},{"key":"10.1016\/j.peptides.2004.12.035_bib3","doi-asserted-by":"crossref","first-page":"RC26","DOI":"10.1523\/JNEUROSCI.19-18-j0004.1999","article-title":"Anatomy of an endogenous antagonist: relationship between agouti-related protein and proopiomelanocortin in brain","volume":"19","author":"Bagnol","year":"1999","journal-title":"J Neurosci"},{"key":"10.1016\/j.peptides.2004.12.035_bib4","doi-asserted-by":"crossref","first-page":"3665","DOI":"10.1021\/jm010165y","article-title":"Selective, high affinity peptide antagonists of \u03b1-melanotropin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro","volume":"44","author":"Bednarek","year":"2001","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib5","doi-asserted-by":"crossref","first-page":"209","DOI":"10.1006\/bbrc.1999.0981","article-title":"Analogs of MTII, lactam derivatives of \u03b1-melanotropin modified at the N-terminus and their selectivity at human melanocortin receptors 3, 4 and 5","volume":"261","author":"Bednarek","year":"1999","journal-title":"Biochem Biophys Res Commun"},{"key":"10.1016\/j.peptides.2004.12.035_bib6","doi-asserted-by":"crossref","first-page":"401","DOI":"10.1016\/S0196-9781(99)00048-0","article-title":"Structure-function studies on the cyclic peptide MT-II, lactam derivative of \u03b1-melanotropin","volume":"20","author":"Bednarek","year":"1999","journal-title":"Peptides"},{"key":"10.1016\/j.peptides.2004.12.035_bib7","doi-asserted-by":"crossref","first-page":"641","DOI":"10.1006\/bbrc.2001.5444","article-title":"Potent and selective peptide agonists of alpha-melanocortin action at human melanocortin receptor 4: their synthesis and biological evaluation in vitro","volume":"286","author":"Bednarek","year":"2001","journal-title":"Biochem Biophys Res Commun"},{"key":"10.1016\/j.peptides.2004.12.035_bib8","doi-asserted-by":"crossref","first-page":"3442","DOI":"10.1523\/JNEUROSCI.20-09-03442.2000","article-title":"A novel selective melanocortin-4 receptor agonist reduces food intake in rats and mice without producing aversive consequences","volume":"20","author":"Benoit","year":"2000","journal-title":"J Neurosci"},{"key":"10.1016\/j.peptides.2004.12.035_bib9","doi-asserted-by":"crossref","first-page":"157","DOI":"10.1016\/0016-6480(89)90066-X","article-title":"\u03b1-Melanotropin: the minimal active sequence in the lizard skin bioassay","volume":"73","author":"Castrucci","year":"1989","journal-title":"Gen Comp Endocrinal"},{"key":"10.1016\/j.peptides.2004.12.035_bib10","doi-asserted-by":"crossref","first-page":"145","DOI":"10.1023\/A:1008983615045","article-title":"Role of the melanocortin-4 receptor in metabolic rate and food intake in mice","volume":"9","author":"Chen","year":"2000","journal-title":"Transgenic Res"},{"key":"10.1016\/j.peptides.2004.12.035_bib11","unstructured":"Chen L, Cheung AW, Chu X, Danho W, Swistok J, Yagaloff KA. Preparation of selective linear peptides with melanocortin-4 receptor (MC4-R) agonist activity, US Patent 6600015 (2003)."},{"key":"10.1016\/j.peptides.2004.12.035_bib12","doi-asserted-by":"crossref","first-page":"2407","DOI":"10.1016\/S0960-894X(02)00459-6","article-title":"Structure\u2013activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH2 at the human melanocortin-1 and -4 receptors: arginine substitution","volume":"12","author":"Cheung","year":"2002","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.peptides.2004.12.035_bib13","doi-asserted-by":"crossref","first-page":"133","DOI":"10.1016\/S0960-894X(02)00830-2","article-title":"Structure\u2013Activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH2 at the human melanocortin-1 and -4 receptors: histidine substitution","volume":"13","author":"Cheung","year":"2003","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.peptides.2004.12.035_bib14","doi-asserted-by":"crossref","first-page":"1307","DOI":"10.1016\/S0960-894X(03)00114-8","article-title":"Structure\u2013activity relationship of cyclic peptide penta-c[Asp-His6-DPhe7-Arg8-Trp9-Lys]-NH2 at the human melanocortin-1 and -4 receptors: His6 substitution","volume":"13","author":"Cheung","year":"2003","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.peptides.2004.12.035_bib15","doi-asserted-by":"crossref","first-page":"649","DOI":"10.1016\/S0960-894X(02)01052-1","article-title":"Structure\u2013activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH2 at the human melanocortin-1 and \u20134 receptors: DPhe and Trp substitution","volume":"13","author":"Danho","year":"2003","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.peptides.2004.12.035_bib16","doi-asserted-by":"crossref","first-page":"165","DOI":"10.1038\/385165a0","article-title":"Role of melanocortinergic neurons in feeding and the agouti obesity syndrome","volume":"385","author":"Fan","year":"1997","journal-title":"Nature"},{"key":"10.1016\/j.peptides.2004.12.035_bib17","doi-asserted-by":"crossref","first-page":"3072","DOI":"10.1210\/en.141.9.3072","article-title":"The central melanocortin system can directly regulate serum insulin levels","volume":"141","author":"Fan","year":"2000","journal-title":"Endocrinology"},{"key":"10.1016\/j.peptides.2004.12.035_bib18","doi-asserted-by":"crossref","first-page":"1144","DOI":"10.1210\/jc.86.3.1144","article-title":"The melanocortin melanocyte-stimulating hormone\/adrenocorticotropin (4\u201310) decreases body fat in humans","volume":"86","author":"Fehm","year":"2001","journal-title":"J Clin Endocrinol Metab"},{"key":"10.1016\/j.peptides.2004.12.035_bib19","doi-asserted-by":"crossref","first-page":"E468","DOI":"10.1152\/ajpendo.00434.2002","article-title":"The melanocortin system","volume":"284","author":"Gantz","year":"2003","journal-title":"Am J Physiol Endocrinol Metab"},{"key":"10.1016\/j.peptides.2004.12.035_bib20","doi-asserted-by":"crossref","first-page":"6164","DOI":"10.1021\/bi010025q","article-title":"Structure-activity studies of the melanocortin-4 receptor by in vitro mutagenesis: identification of agouti-related protein (AGRP), melanocortin agonist and synthetic peptide antagonist interaction determinants","volume":"40","author":"Haskell-Luevano","year":"2001","journal-title":"Biochemistry"},{"key":"10.1016\/j.peptides.2004.12.035_bib21","doi-asserted-by":"crossref","first-page":"49","DOI":"10.1016\/S0196-9781(99)00167-9","article-title":"Structure activity studies of the melanocortin antagonist SHU9119 modified at the 6, 7, 8 and 9 positions","volume":"21","author":"Haskell-Luevano","year":"2002","journal-title":"Peptides"},{"key":"10.1016\/j.peptides.2004.12.035_bib22","first-page":"995","article-title":"Truncation studies of \u03b1-melanotropin peptides identifies tripeptide analogues exhibiting prolonged agonist bioactivity","volume":"17","author":"Haskell-Luevano","year":"1996","journal-title":"Peptides"},{"key":"10.1016\/j.peptides.2004.12.035_bib23","doi-asserted-by":"crossref","first-page":"3073","DOI":"10.1021\/jm010524p","article-title":"Structure\u2013activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the mouse melanocortin receptors: part 2 modifications at the Phe position","volume":"45","author":"Holder","year":"2002","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib24","doi-asserted-by":"crossref","first-page":"2801","DOI":"10.1021\/jm0104872","article-title":"Structure\u2013activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the mouse melanocortin receptors 1. modifications at the His position","volume":"45","author":"Holder","year":"2002","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib25","doi-asserted-by":"crossref","first-page":"325","DOI":"10.1002\/med.10064","article-title":"Melanocortin ligands: 30 years of structure\u2013activity relationship (SAR) studies","volume":"24","author":"Holder","year":"2004","journal-title":"Med Res Rev"},{"key":"10.1016\/j.peptides.2004.12.035_bib26","doi-asserted-by":"crossref","first-page":"73","DOI":"10.1016\/S0196-9781(02)00278-4","article-title":"Structure\u2013activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the mouse melanocortin receptors part 3: modifications at the Arg position","volume":"24","author":"Holder","year":"2003","journal-title":"Peptides"},{"key":"10.1016\/j.peptides.2004.12.035_bib27","doi-asserted-by":"crossref","first-page":"5736","DOI":"10.1021\/jm020296e","article-title":"Structure\u2013activity relationship of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the mouse melanocortin receptors 4. Modifications at the Trp position","volume":"45","author":"Holder","year":"2002","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib28","doi-asserted-by":"crossref","first-page":"3454","DOI":"10.1021\/jm00018a005","article-title":"Cyclic lactam \u03b1-melanotropin analogues of Ac-Nle4-c[Asp5, DPhe7 Lys10]-\u03b1-MSH (4\u201310)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors","volume":"38","author":"Hruby","year":"1995","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib29","doi-asserted-by":"crossref","first-page":"2126","DOI":"10.1021\/jm00394a033","article-title":"\u03b1-Melanotropin: the minimal active sequence in the frog skin bioassay","volume":"30","author":"Hruby","year":"1987","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib30","doi-asserted-by":"crossref","first-page":"1184","DOI":"10.1016\/S1359-6446(02)02529-1","article-title":"Nasal drug delivery: new developments and strategies","volume":"7","author":"Illum","year":"2002","journal-title":"Drug Discov Today"},{"key":"10.1016\/j.peptides.2004.12.035_bib31","doi-asserted-by":"crossref","first-page":"5006","DOI":"10.1210\/en.139.12.5006","article-title":"Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo","volume":"139","author":"Kask","year":"1998","journal-title":"Endocrinology"},{"key":"10.1016\/j.peptides.2004.12.035_bib32","doi-asserted-by":"crossref","first-page":"245","DOI":"10.1006\/bbrc.1998.8961","article-title":"Evidence that orexigenic effects of melanocortin 4 receptor antagonist HS014 are mediated by neuropeptide Y","volume":"248","author":"Kask","year":"1998","journal-title":"Biochem Biophys Res Commun"},{"key":"10.1016\/j.peptides.2004.12.035_bib33","doi-asserted-by":"crossref","first-page":"1505","DOI":"10.1021\/jm9806143","article-title":"SQ\u2014a program for rapidly producing pharmacophorically relevant molecular superpositions","volume":"42","author":"Miller","year":"1999","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib34","doi-asserted-by":"crossref","first-page":"1298","DOI":"10.1210\/me.8.10.1298","article-title":"Localization of the melanocortin-4 receptor (MC4-R) in neuroendocrine and autonomic control circuits in the brain","volume":"8","author":"Mountjoy","year":"1994","journal-title":"Mol Endocrinol"},{"key":"10.1016\/j.peptides.2004.12.035_bib35","doi-asserted-by":"crossref","first-page":"273","DOI":"10.1152\/jappl.2000.89.1.273","article-title":"Centrally administered MTII affects feeding, drinking, temperature, and activity in the Sprague\u2013Dawley rat","volume":"89","author":"Murphy","year":"2000","journal-title":"J Appl Physiol"},{"key":"10.1016\/j.peptides.2004.12.035_bib36","doi-asserted-by":"crossref","first-page":"491","DOI":"10.1016\/S0143-4179(98)90077-4","article-title":"Melanocortin mediated inhibition of feeding behavior in rats","volume":"32","author":"Murphy","year":"1998","journal-title":"Neuropeptides (Edinburgh)"},{"key":"10.1016\/j.peptides.2004.12.035_bib37","doi-asserted-by":"crossref","first-page":"1079","DOI":"10.1172\/JCI200112954","article-title":"Central melanocortin receptors regulate insulin action","volume":"108","author":"Obici","year":"2001","journal-title":"J Clin Invest"},{"key":"10.1016\/j.peptides.2004.12.035_bib38","unstructured":"Tetrapeptide 1, His-DPhe-Arg-Trp-NH2 has been reported at the human melanocortin-4 receptor previously (Ref 44, Ki=416nM and EC50=8.7nM). The smaller EC50 value than Ki value is possibly due to the use of a transient expression system for determination of EC50 since activation properties are dependent on expression level per cell."},{"key":"10.1016\/j.peptides.2004.12.035_bib39","doi-asserted-by":"crossref","first-page":"199","DOI":"10.1016\/S0896-6273(02)00969-8","article-title":"The need to feed: homeostatic and hedonic control of eating","volume":"36","author":"Saper","year":"2002","journal-title":"Neuron"},{"key":"10.1016\/j.peptides.2004.12.035_bib40","doi-asserted-by":"crossref","first-page":"5754","DOI":"10.1073\/pnas.77.10.5754","article-title":"4-Norleucine 7-d-phenylalanine-\u03b1-melanocyte-stimulating hormone: a highly potent \u03b1-melanotropin with ultralong biological activity","volume":"77","author":"Sawyer","year":"1980","journal-title":"Proc Natl Acad Sci USA"},{"key":"10.1016\/j.peptides.2004.12.035_bib41","doi-asserted-by":"crossref","first-page":"4589","DOI":"10.1021\/jm025539h","volume":"45","author":"Sebhat","year":"2002","journal-title":"J Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib42","doi-asserted-by":"crossref","first-page":"31","DOI":"10.1016\/S0065-7743(03)38005-4","article-title":"Melanocortin-4 receptor agonists and antagonists: chemistry and potential therapeutic utilities","volume":"38","author":"Sebhat","year":"2003","journal-title":"Ann Rep Med Chem"},{"key":"10.1016\/j.peptides.2004.12.035_bib43","doi-asserted-by":"crossref","first-page":"27","DOI":"10.1038\/sj.bjp.0702264","article-title":"Long term orexigenic effect of a novel melanocortin-4 receptor selective antagonist","volume":"126","author":"Skuladottir","year":"1999","journal-title":"Br J Pharmacol"},{"key":"10.1016\/j.peptides.2004.12.035_bib44","doi-asserted-by":"crossref","first-page":"137","DOI":"10.1016\/S0014-5793(99)00525-6","article-title":"Molecular analysis of a new splice variant of the human melanocortin-1 receptor","volume":"451","author":"Tan","year":"1999","journal-title":"FEBS Lett"},{"key":"10.1016\/j.peptides.2004.12.035_bib45","doi-asserted-by":"crossref","first-page":"586","DOI":"10.2174\/1389450033490858","article-title":"Melanocortins and their receptors and antagonists","volume":"4","author":"Voisey","year":"2003","journal-title":"Curr Drug Targ"},{"key":"10.1016\/j.peptides.2004.12.035_bib46","doi-asserted-by":"crossref","first-page":"1332","DOI":"10.1210\/en.141.4.1332","article-title":"The role of the dorsal vagal complex and the vagus nerve in feeding effects of melanocortin-3\/4 receptor stimulation","volume":"141","author":"Williams","year":"2000","journal-title":"Endocrinology"},{"key":"10.1016\/j.peptides.2004.12.035_bib47","doi-asserted-by":"crossref","first-page":"14900","DOI":"10.1021\/bi001684q","article-title":"Molecular determinants of ligand binding to the human melanocortin-4 receptor","volume":"39","author":"Yang","year":"2000","journal-title":"Biochemistry"},{"key":"10.1016\/j.peptides.2004.12.035_bib48","doi-asserted-by":"crossref","first-page":"239","DOI":"10.1046\/j.1467-789X.2003.00104.x","article-title":"Recent developments in our understanding of melanocortin system in the regulation of food intake","volume":"4","author":"Yang","year":"2003","journal-title":"Obes Rev"},{"key":"10.1016\/j.peptides.2004.12.035_bib49","unstructured":"Ye Z, et al. Unpublished results."},{"key":"10.1016\/j.peptides.2004.12.035_bib50","doi-asserted-by":"crossref","first-page":"627","DOI":"10.2174\/1381612033391234","article-title":"The role of melanocortin peptides and receptors in regulation of energy balance","volume":"9","author":"Zimanyi","year":"2003","journal-title":"Curr Pharm Des"}],"container-title":["Peptides"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0196978105002214?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0196978105002214?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2019,3,4]],"date-time":"2019-03-04T01:31:52Z","timestamp":1551663112000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0196978105002214"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2005,10]]},"references-count":50,"journal-issue":{"issue":"10","published-print":{"date-parts":[[2005,10]]}},"alternative-id":["S0196978105002214"],"URL":"https:\/\/doi.org\/10.1016\/j.peptides.2004.12.035","relation":{},"ISSN":["0196-9781"],"issn-type":[{"value":"0196-9781","type":"print"}],"subject":[],"published":{"date-parts":[[2005,10]]}}}