{"id":"https://openalex.org/W2010951550","doi":"https://doi.org/10.2174/156802607780906591","title":"Structure-Activity Relationships of \u03b2 -MSH Derived Melanocortin-4 Receptor Peptide Agonists","display_name":"Structure-Activity Relationships of \u03b2 -MSH Derived Melanocortin-4 Receptor Peptide Agonists","publication_year":2007,"publication_date":"2007-06-01","ids":{"openalex":"https://openalex.org/W2010951550","doi":"https://doi.org/10.2174/156802607780906591","mag":"2010951550","pmid":"https://pubmed.ncbi.nlm.nih.gov/17584126"},"language":"en","primary_location":{"id":"doi:10.2174/156802607780906591","doi":"https://doi.org/10.2174/156802607780906591","is_oa":false,"landing_page_url":"https://doi.org/10.2174/156802607780906591","pdf_url":null,"source":{"id":"https://openalex.org/S107732428","display_name":"Current Topics in Medicinal Chemistry","issn_l":"1568-0266","issn":["1568-0266","1873-4294"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","jufo-1","ki-jl-1","medline","norway-1","poland-100","russia-white-list-1"],"host_organization":"https://openalex.org/P4310320079","host_organization_name":"Bentham Science Publishers","host_organization_lineage":["https://openalex.org/P4310320079"],"host_organization_lineage_names":["Bentham Science Publishers"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Current Topics in Medicinal Chemistry","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref","pubmed"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5113605408","display_name":"Liang Zeng Yan","orcid":"https://orcid.org/0000-0002-2949-7634","observed_orcids":["https://orcid.org/0000-0002-2949-7634"]},"institutions":[{"id":"https://openalex.org/I168537998","display_name":"Eli Lilly (United States)","ror":"https://ror.org/01qat3289","country_code":"US","type":"company","lineage":["https://openalex.org/I168537998"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Liang Zeng Yan","raw_affiliation_strings":["Lilly Research Laboratories, A Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. yan_liang_zeng@lilly.com","Lilly Research Laboratories, A Division of Eli Lilly and Company Lilly Corporate Center, Indianapolis, IN 46285, USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Lilly Research Laboratories, A Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. yan_liang_zeng@lilly.com","institution_ids":["https://openalex.org/I168537998"]},{"raw_affiliation_string":"Lilly Research Laboratories, A Division of Eli Lilly and Company Lilly Corporate Center, Indianapolis, IN 46285, USA","institution_ids":["https://openalex.org/I168537998"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5046610900","display_name":"Hansen M. Hsiung","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Hansen M. Hsiung","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5026792698","display_name":"Mark L. Heiman","orcid":"https://orcid.org/0000-0002-2417-9231","observed_orcids":["https://orcid.org/0000-0002-2417-9231"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Mark L. Heiman","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5046660352","display_name":"Robert A. Gadski","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Robert A. Gadski","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5052059067","display_name":"Paul J. Emmerson","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Paul J. Emmerson","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5082729075","display_name":"JeAnne L. Hertel","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"JeAnne Hertel","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":null,"display_name":"David Flora","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"David Flora","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":null,"display_name":"Patrick Edwards","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Patrick Edwards","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110015099","display_name":"D. L. Smiley","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Dave Smiley","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110949975","display_name":"Lianshan Zhang","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Lianshan Zhang","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5017553374","display_name":"Saba Husain","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Saba Husain","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5082570154","display_name":"Steven D. Kahl","orcid":"https://orcid.org/0000-0001-7085-9556","observed_orcids":["https://orcid.org/0000-0001-7085-9556"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Steven D.Kahl","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5071517746","display_name":"Richard D. DiMarchi","orcid":"https://orcid.org/0000-0003-0220-4085","observed_orcids":["https://orcid.org/0000-0003-0220-4085"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Richard D.DiMarchi","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"last","author":{"id":"https://openalex.org/A5038696393","display_name":"John P. Mayer","orcid":"https://orcid.org/0000-0002-2546-3787","observed_orcids":["https://orcid.org/0000-0002-2546-3787"]},"institutions":[{"id":"https://openalex.org/I168537998","display_name":"Eli Lilly (United States)","ror":"https://ror.org/01qat3289","country_code":"US","type":"company","lineage":["https://openalex.org/I168537998"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"John P.Mayer","raw_affiliation_strings":["Lilly Research Laboratories,Eli Lilly and Company, Lilly Corporate Center, DC 0412, Indianapolis, IN 46285, USA","Lilly Research Laboratories,Eli Lilly and Company, Lilly Corporate Center, DC 0412, Indianapolis, IN 46285, USA.,India"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Lilly Research Laboratories,Eli Lilly and Company, Lilly Corporate Center, DC 0412, Indianapolis, IN 46285, USA","institution_ids":["https://openalex.org/I168537998"]},{"raw_affiliation_string":"Lilly Research Laboratories,Eli Lilly and Company, Lilly Corporate Center, DC 0412, Indianapolis, IN 46285, USA.,India","institution_ids":["https://openalex.org/I168537998"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":0.516,"has_fulltext":false,"cited_by_count":12,"citation_normalized_percentile":{"value":0.57772727,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":87,"max":96},"biblio":{"volume":"7","issue":"11","first_page":"1052","last_page":"1067"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10489","display_name":"Regulation of Appetite and Obesity","score":0.9667999744415283,"subfield":{"id":"https://openalex.org/subfields/2807","display_name":"Endocrine and Autonomic Systems"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T10489","display_name":"Regulation of Appetite and Obesity","score":0.9667999744415283,"subfield":{"id":"https://openalex.org/subfields/2807","display_name":"Endocrine and Autonomic Systems"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10814","display_name":"Neuropeptides and Animal Physiology","score":0.013799999840557575,"subfield":{"id":"https://openalex.org/subfields/2804","display_name":"Cellular and Molecular Neuroscience"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10911","display_name":"Chemical Synthesis and Analysis","score":0.012799999676644802,"subfield":{"id":"https://openalex.org/subfields/1605","display_name":"Organic Chemistry"},"field":{"id":"https://openalex.org/fields/16","display_name":"Chemistry"},"domain":{"id":"https://openalex.org/domains/3","display_name":"Physical Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/melanocortin-4-receptor","display_name":"melanocortin-4 receptor","score":0.8999999761581421},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.8019999861717224},{"id":"https://openalex.org/keywords/peptide-agonists","display_name":"peptide agonists","score":0.8009999990463257},{"id":"https://openalex.org/keywords/obesity","display_name":"obesity","score":0.4620000123977661},{"id":"https://openalex.org/keywords/food-consumption","display_name":"dietary intake","score":0.5720000267028809},{"id":"https://openalex.org/keywords/energy-homeostasis","display_name":"energy homeostasis","score":0.8939999938011169},{"id":"https://openalex.org/keywords/proopiomelanocortin","display_name":"proopiomelanocortin","score":0.9079999923706055},{"id":"https://openalex.org/keywords/cyclic-hexapeptide","display_name":"cyclic hexapeptide","score":0.8700000047683716},{"id":"https://openalex.org/keywords/fat-metabolism","display_name":"fat metabolism","score":0.8240000009536743}],"concepts":[{"id":"https://openalex.org/C2779993316","wikidata":"https://www.wikidata.org/wiki/Q6591465","display_name":"Melanocortin","level":3,"score":0.8383749723434448},{"id":"https://openalex.org/C43295716","wikidata":"https://www.wikidata.org/wiki/Q21118676","display_name":"Melanocortin 4 receptor","level":4,"score":0.6159032583236694},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.5929442048072815},{"id":"https://openalex.org/C43790157","wikidata":"https://www.wikidata.org/wiki/Q21118678","display_name":"Melanocortin 3 receptor","level":5,"score":0.5739452242851257},{"id":"https://openalex.org/C2779281246","wikidata":"https://www.wikidata.org/wiki/Q172847","display_name":"Peptide","level":2,"score":0.5506368279457092},{"id":"https://openalex.org/C2909567013","wikidata":"https://www.wikidata.org/wiki/Q6591465","display_name":"Melanocortins","level":4,"score":0.47854217886924744},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.47543027997016907},{"id":"https://openalex.org/C126322002","wikidata":"https://www.wikidata.org/wiki/Q11180","display_name":"Internal medicine","level":1,"score":0.44831445813179016},{"id":"https://openalex.org/C2777241137","wikidata":"https://www.wikidata.org/wiki/Q24784850","display_name":"Melanocortin receptor","level":4,"score":0.4471450746059418},{"id":"https://openalex.org/C134018914","wikidata":"https://www.wikidata.org/wiki/Q162606","display_name":"Endocrinology","level":1,"score":0.3990951180458069},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.3607865869998932},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.24859225749969482},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.21903753280639648},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.18772074580192566}],"mesh":[{"descriptor_ui":"D000596","descriptor_name":"Amino Acids","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D003198","descriptor_name":"Computer Simulation","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D004220","descriptor_name":"Disulfides","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D013329","descriptor_name":"Structure-Activity Relationship","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D019824","descriptor_name":"beta-MSH","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":false},{"descriptor_ui":"D019824","descriptor_name":"beta-MSH","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D019824","descriptor_name":"beta-MSH","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D044105","descriptor_name":"Receptor, Melanocortin, Type 4","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D044105","descriptor_name":"Receptor, Melanocortin, Type 4","qualifier_ui":"Q000819","qualifier_name":"agonists","is_major_topic":true}],"locations_count":2,"locations":[{"id":"doi:10.2174/156802607780906591","doi":"https://doi.org/10.2174/156802607780906591","is_oa":false,"landing_page_url":"https://doi.org/10.2174/156802607780906591","pdf_url":null,"source":{"id":"https://openalex.org/S107732428","display_name":"Current Topics in Medicinal Chemistry","issn_l":"1568-0266","issn":["1568-0266","1873-4294"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","jufo-1","ki-jl-1","medline","norway-1","poland-100","russia-white-list-1"],"host_organization":"https://openalex.org/P4310320079","host_organization_name":"Bentham Science Publishers","host_organization_lineage":["https://openalex.org/P4310320079"],"host_organization_lineage_names":["Bentham Science Publishers"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Current Topics in Medicinal Chemistry","raw_type":"journal-article"},{"id":"pmid:17584126","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/17584126","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Current topics in medicinal chemistry","raw_type":"Journal Article"}],"best_oa_location":null,"sustainable_development_goals":[{"display_name":"Good health and well-being","score":0.9391000270843506,"id":"https://metadata.un.org/sdg/3"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":0,"referenced_works":[],"related_works":["https://openalex.org/W2126446779","https://openalex.org/W946171377","https://openalex.org/W1992673544","https://openalex.org/W2908712355","https://openalex.org/W2132903069","https://openalex.org/W7098051589","https://openalex.org/W2787923281","https://openalex.org/W4299915151","https://openalex.org/W2104494281","https://openalex.org/W2016203841"],"abstract_inverted_index":{"The":[0,24],"recent":[1],"emergence":[2],"of":[3,64,74,83,102,138,142,171,200,211],"obesity":[4,212],"as":[5,146],"a":[6,75,139,155,169],"major":[7],"health":[8],"threat":[9],"in":[10,53,71,89,92,107,112,121,159,187,208],"the":[11,16,45,65,72,118,122,136,198,209],"industrialized":[12],"world":[13],"has":[14,31],"intensified":[15],"search":[17],"for":[18,197],"novel":[19,140,193],"and":[20,38,41,60,69,96,162,181,194,204,213],"effective":[21],"pharmacologic":[22],"treatment.":[23],"proopiomelanocortin":[25],"(POMC)-melanocortin":[26],"4":[27],"receptor":[28],"(MC4R)":[29],"axis":[30],"been":[32],"shown":[33],"to":[34,135],"regulate":[35],"food":[36,94,103,177],"intake":[37,95,104,178],"energy":[39],"homeostasis":[40],"is":[42],"considered":[43],"among":[44],"most":[46],"promising":[47],"antiobesity":[48],"targets.":[49],"Our":[50],"initial":[51],"efforts":[52,133],"this":[54,84],"area":[55],"have":[56],"focused":[57],"on":[58],"affinity":[59],"selectivity":[61,165],"directed":[62],"optimization":[63,132],"native":[66],"beta-MSH(5-22)":[67],"sequence":[68],"resulted":[70],"discovery":[73],"potent":[76],"MC4R":[77,113,129,161],"agonist:":[78],"Ac-Tyr-Arg-[Cys-Glu-His-D-Phe-Arg-Trp-Cys]-NH(2)":[79],"(10).":[80],"Subcutaneous":[81],"administration":[82],"peptide":[85],"produced":[86],"an":[87,163],"excellent":[88],"vivo":[90],"efficacy":[91],"reducing":[93],"increasing":[97],"fat":[98,183],"metabolism.":[99],"Additionally,":[100],"suppression":[101],"was":[105],"observed":[106,120],"wild":[108,123],"type":[109,124],"but":[110],"not":[111],"deficient":[114],"mice,":[115],"suggesting":[116],"that":[117],"effects":[119],"mice":[125],"were":[126],"mediated":[127],"through":[128],"signaling.":[130],"Subsequent":[131],"led":[134],"identification":[137],"series":[141],"disulfide":[143],"constrained":[144],"hexapeptides":[145,153],"exemplified":[147],"by":[148,179,185],"Ac-[hCys-His-D-Phe-Arg-Trp-Cys]-NH(2)":[149],"(100).":[150],"These":[151,189],"cyclic":[152,190],"showed":[154],"further":[156],"improved":[157],"potency":[158],"binding":[160],"enhanced":[164,195],"over":[166],"MC1R.":[167],"At":[168],"dose":[170],"0.07":[172],"mg/kg":[173],"analog":[174],"102":[175],"reduced":[176],"38%":[180],"increased":[182],"utilization":[184],"58%":[186],"rats.":[188],"peptides":[191],"provide":[192],"reagents":[196],"elucidation":[199],"melanocortin":[201],"receptors":[202],"biology":[203],"may":[205],"find":[206],"applications":[207],"treatment":[210],"related":[214],"metabolic":[215],"disorders.":[216]},"counts_by_year":[{"year":2026,"cited_by_count":1},{"year":2024,"cited_by_count":1},{"year":2022,"cited_by_count":1},{"year":2021,"cited_by_count":1},{"year":2018,"cited_by_count":2},{"year":2013,"cited_by_count":1}],"updated_date":"2026-10-31T12:09:11.096373","created_date":"2016-06-24T00:00:00"}