{"id":"https://openalex.org/W7225831665","doi":"https://doi.org/10.1021/acs.molpharmaceut.6c00931","title":"Novel CXCR4-Targeted Radioligands with Improved Tumor Uptake and Therapeutic Efficacy","display_name":"Novel CXCR4-Targeted Radioligands with Improved Tumor Uptake and Therapeutic Efficacy","publication_year":2026,"publication_date":"2026-11-11","ids":{"openalex":"https://openalex.org/W7225831665","doi":"https://doi.org/10.1021/acs.molpharmaceut.6c00931"},"language":"en","primary_location":{"id":"doi:10.1021/acs.molpharmaceut.6c00931","doi":"https://doi.org/10.1021/acs.molpharmaceut.6c00931","is_oa":false,"landing_page_url":"https://doi.org/10.1021/acs.molpharmaceut.6c00931","pdf_url":null,"source":{"id":"https://openalex.org/S204562082","display_name":"Molecular Pharmaceutics","issn_l":"1543-8384","issn":["1543-8384","1543-8392"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-c","doyens","jufo-2","ki-jl-1","medline","norway-1","poland-140","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Molecular Pharmaceutics","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref"],"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/A5161495227","display_name":"Itzel Renee\u0301 Astiazara\u0301n-Rasco\u0301n","orcid":"https://orcid.org/0009-0003-2503-9470","observed_orcids":["https://orcid.org/0009-0003-2503-9470"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Itzel Renee\u0301 Astiazara\u0301n-Rasco\u0301n","raw_affiliation_strings":["BC Cancer Research Institute , , , ,","University of British Columbia , , , ,"],"raw_orcid":"https://orcid.org/0009-0003-2503-9470","affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]},{"raw_affiliation_string":"University of British Columbia , , , ,","institution_ids":["https://openalex.org/I141945490"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5109993247","display_name":"Hsiou\u2010Ting Kuo","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Hsiou-Ting Kuo","raw_affiliation_strings":["BC Cancer Research Institute , , , ,"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5161487283","display_name":"Lily Li","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Lily Li","raw_affiliation_strings":["BC Cancer Research Institute , , , ,"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5078033153","display_name":"Jutta Zeisler","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Jutta Zeisler","raw_affiliation_strings":["BC Cancer Research Institute , , , ,"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5124054523","display_name":"Pauline Ng","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Pauline Ng","raw_affiliation_strings":["BC Cancer Research Institute , , , ,"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5058706376","display_name":"Helen Merkens","orcid":"https://orcid.org/0000-0003-1958-0167","observed_orcids":["https://orcid.org/0000-0003-1958-0167"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Helen Merkens","raw_affiliation_strings":["BC Cancer Research Institute , , , ,"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110856495","display_name":"Joseph Lau","orcid":"https://orcid.org/0000-0002-1510-9653","observed_orcids":["https://orcid.org/0000-0002-1510-9653"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Joseph Lau","raw_affiliation_strings":["BC Cancer Research Institute , , , ,","University of British Columbia , , , ,"],"raw_orcid":"https://orcid.org/0000-0002-1510-9653","affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]},{"raw_affiliation_string":"University of British Columbia , , , ,","institution_ids":["https://openalex.org/I141945490"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5022775390","display_name":"Kuo\u2010Shyan Lin","orcid":"https://orcid.org/0000-0002-0739-0780","observed_orcids":["https://orcid.org/0000-0002-0739-0780"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Kuo-Shyan Lin","raw_affiliation_strings":["BC Cancer Research Institute , , , ,","University of British Columbia , , , ,"],"raw_orcid":"https://orcid.org/0000-0002-0739-0780","affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]},{"raw_affiliation_string":"University of British Columbia , , , ,","institution_ids":["https://openalex.org/I141945490"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5040772609","display_name":"Fran\u00e7ois B\u00e9nard","orcid":"https://orcid.org/0000-0001-7995-3581","observed_orcids":["https://orcid.org/0000-0001-7995-3581"]},"institutions":[{"id":"https://openalex.org/I141945490","display_name":"University of British Columbia","ror":"https://ror.org/03rmrcq20","country_code":"CA","type":"education","lineage":["https://openalex.org/I141945490"]}],"countries":["CA"],"is_corresponding":false,"raw_author_name":"Franc\u0327ois Be\u0301nard","raw_affiliation_strings":["BC Cancer Research Institute , , , ,","University of British Columbia , , , ,"],"raw_orcid":"https://orcid.org/0000-0001-7995-3581","affiliations":[{"raw_affiliation_string":"BC Cancer Research Institute , , , ,","institution_ids":[]},{"raw_affiliation_string":"University of British Columbia , , , ,","institution_ids":["https://openalex.org/I141945490"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":null,"fwci":0.0,"has_fulltext":false,"cited_by_count":0,"citation_normalized_percentile":{"value":0.0,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":null,"biblio":{"volume":null,"issue":null,"first_page":null,"last_page":null},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T11395","display_name":"Radiopharmaceutical Chemistry and Applications","score":0.9994999766349792,"subfield":{"id":"https://openalex.org/subfields/2741","display_name":"Radiology, Nuclear Medicine and Imaging"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},"topics":[{"id":"https://openalex.org/T11395","display_name":"Radiopharmaceutical Chemistry and Applications","score":0.9994999766349792,"subfield":{"id":"https://openalex.org/subfields/2741","display_name":"Radiology, Nuclear Medicine and Imaging"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T11532","display_name":"Chemokine receptors and signaling","score":9.999999747378752e-05,"subfield":{"id":"https://openalex.org/subfields/2730","display_name":"Oncology"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T10522","display_name":"Medical Imaging Techniques and Applications","score":9.999999747378752e-05,"subfield":{"id":"https://openalex.org/subfields/2741","display_name":"Radiology, Nuclear Medicine and Imaging"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}}],"keywords":[],"concepts":[{"id":"https://openalex.org/C2777807558","wikidata":"https://www.wikidata.org/wiki/Q4914764","display_name":"Biodistribution","level":3,"score":0.8324000239372253},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.7031999826431274},{"id":"https://openalex.org/C2776125364","wikidata":"https://www.wikidata.org/wiki/Q169219","display_name":"Albumin","level":2,"score":0.5041999816894531},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.4749999940395355},{"id":"https://openalex.org/C67847695","wikidata":"https://www.wikidata.org/wiki/Q626478","display_name":"Radioligand","level":3,"score":0.4713999927043915},{"id":"https://openalex.org/C502942594","wikidata":"https://www.wikidata.org/wiki/Q3421914","display_name":"Cancer research","level":1,"score":0.45890000462532043},{"id":"https://openalex.org/C112705442","wikidata":"https://www.wikidata.org/wiki/Q323936","display_name":"Pharmacokinetics","level":2,"score":0.451200008392334},{"id":"https://openalex.org/C2993559085","wikidata":"https://www.wikidata.org/wiki/Q2126444","display_name":"Radionuclide therapy","level":2,"score":0.39899998903274536},{"id":"https://openalex.org/C19831878","wikidata":"https://www.wikidata.org/wiki/Q659446","display_name":"Therapeutic index","level":3,"score":0.3935000002384186},{"id":"https://openalex.org/C2780091579","wikidata":"https://www.wikidata.org/wiki/Q9377","display_name":"Kidney","level":2,"score":0.3659999966621399},{"id":"https://openalex.org/C165616093","wikidata":"https://www.wikidata.org/wiki/Q424232","display_name":"Serum albumin","level":2,"score":0.3440999984741211},{"id":"https://openalex.org/C2779931791","wikidata":"https://www.wikidata.org/wiki/Q161515","display_name":"DOTA","level":3,"score":0.33980000019073486},{"id":"https://openalex.org/C2779281246","wikidata":"https://www.wikidata.org/wiki/Q172847","display_name":"Peptide","level":2,"score":0.32409998774528503},{"id":"https://openalex.org/C207001950","wikidata":"https://www.wikidata.org/wiki/Q141124","display_name":"In vivo","level":2,"score":0.31790000200271606},{"id":"https://openalex.org/C110121322","wikidata":"https://www.wikidata.org/wiki/Q865811","display_name":"Distribution (mathematics)","level":2,"score":0.3089999854564667},{"id":"https://openalex.org/C2779338263","wikidata":"https://www.wikidata.org/wiki/Q208414","display_name":"Lymphoma","level":2,"score":0.2906999886035919},{"id":"https://openalex.org/C86807702","wikidata":"https://www.wikidata.org/wiki/Q2620381","display_name":"Bovine serum albumin","level":2,"score":0.28839999437332153},{"id":"https://openalex.org/C12823836","wikidata":"https://www.wikidata.org/wiki/Q24720618","display_name":"Chemokine receptor","level":4,"score":0.2754000127315521},{"id":"https://openalex.org/C129470790","wikidata":"https://www.wikidata.org/wiki/Q415718","display_name":"CXCR4","level":4,"score":0.27059999108314514},{"id":"https://openalex.org/C2778597219","wikidata":"https://www.wikidata.org/wiki/Q11721976","display_name":"Human serum albumin","level":2,"score":0.266400009393692},{"id":"https://openalex.org/C2776146153","wikidata":"https://www.wikidata.org/wiki/Q7281276","display_name":"Radioimmunotherapy","level":4,"score":0.2644999921321869},{"id":"https://openalex.org/C146543888","wikidata":"https://www.wikidata.org/wiki/Q425056","display_name":"Blood proteins","level":2,"score":0.26089999079704285},{"id":"https://openalex.org/C2777863537","wikidata":"https://www.wikidata.org/wiki/Q357896","display_name":"Adjuvant","level":2,"score":0.25369998812675476},{"id":"https://openalex.org/C13373296","wikidata":"https://www.wikidata.org/wiki/Q421866","display_name":"Chemokine","level":3,"score":0.25279998779296875},{"id":"https://openalex.org/C60984968","wikidata":"https://www.wikidata.org/wiki/Q389172","display_name":"Cyclic peptide","level":3,"score":0.2526000142097473},{"id":"https://openalex.org/C2776107976","wikidata":"https://www.wikidata.org/wiki/Q1786433","display_name":"Tumor microenvironment","level":3,"score":0.2508000135421753}],"mesh":[],"locations_count":1,"locations":[{"id":"doi:10.1021/acs.molpharmaceut.6c00931","doi":"https://doi.org/10.1021/acs.molpharmaceut.6c00931","is_oa":false,"landing_page_url":"https://doi.org/10.1021/acs.molpharmaceut.6c00931","pdf_url":null,"source":{"id":"https://openalex.org/S204562082","display_name":"Molecular Pharmaceutics","issn_l":"1543-8384","issn":["1543-8384","1543-8392"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-c","doyens","jufo-2","ki-jl-1","medline","norway-1","poland-140","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Molecular Pharmaceutics","raw_type":"journal-article"}],"best_oa_location":null,"sustainable_development_goals":[],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":57,"referenced_works":["https://openalex.org/W1511246213","https://openalex.org/W1970496181","https://openalex.org/W2002815709","https://openalex.org/W2018672336","https://openalex.org/W2029479572","https://openalex.org/W2040210877","https://openalex.org/W2056339573","https://openalex.org/W2104849855","https://openalex.org/W2112451160","https://openalex.org/W2112979860","https://openalex.org/W2124090816","https://openalex.org/W2128532174","https://openalex.org/W2152853006","https://openalex.org/W2339037925","https://openalex.org/W2468216259","https://openalex.org/W2610882330","https://openalex.org/W2704364151","https://openalex.org/W2768473245","https://openalex.org/W2769862145","https://openalex.org/W2786988345","https://openalex.org/W2792070967","https://openalex.org/W2795555192","https://openalex.org/W2804919400","https://openalex.org/W2892869908","https://openalex.org/W2921854203","https://openalex.org/W2975975650","https://openalex.org/W3010452159","https://openalex.org/W3042040399","https://openalex.org/W3044617764","https://openalex.org/W3082635082","https://openalex.org/W3095482518","https://openalex.org/W3107475507","https://openalex.org/W3121489625","https://openalex.org/W3135587331","https://openalex.org/W3194631534","https://openalex.org/W4206901398","https://openalex.org/W4213417823","https://openalex.org/W4214842049","https://openalex.org/W4220935308","https://openalex.org/W4221032937","https://openalex.org/W4283327273","https://openalex.org/W4283368799","https://openalex.org/W4286502365","https://openalex.org/W4296363024","https://openalex.org/W4380873592","https://openalex.org/W4394752983","https://openalex.org/W4400674190","https://openalex.org/W4401284268","https://openalex.org/W4401716131","https://openalex.org/W4402749436","https://openalex.org/W4404876122","https://openalex.org/W4408790789","https://openalex.org/W4409106099","https://openalex.org/W4411179148","https://openalex.org/W4413323154","https://openalex.org/W7126042290","https://openalex.org/W7131282542"],"related_works":[],"abstract_inverted_index":{"Abstract":[0],"Radioligands":[1],"targeting":[2],"the":[3,12,34,113,141,245,282],"C-X-C":[4],"Chemokine":[5],"Receptor":[6],"4":[7],"(CXCR4)":[8],"are":[9],"promising":[10],"for":[11,168],"diagnosis":[13],"and":[14,39,61,86,103,128,147,164,200,207,224,233,247,262],"therapy":[15,25,219],"of":[16,23,37,49,144],"multiple":[17],"tumor":[18,42,59,63,149,162,172,230,264,269,278],"types.":[19],"The":[20],"therapeutic":[21,169],"efficacy":[22],"radiopharmaceutical":[24],"can":[26,40],"be":[27],"enhanced":[28],"by":[29,112],"albumin":[30,55,137,158,258],"binders,":[31],"which":[32],"modulate":[33],"plasma":[35,142],"half-life":[36,143],"radioligands":[38,51,146,255],"increase":[41],"uptake.":[43,150],"We":[44],"report":[45],"a":[46,66,89,152,156,218,238,267],"novel":[47,90],"class":[48],"CXCR4-targeting":[50,145],"conjugated":[52],"to":[53,88,108,155,244,257,288,292],"non-covalent":[54],"binders":[56,259],"with":[57,74,99,121,123,188],"improved":[58,148],"uptake":[60,163,173,190,202,265,279],"prolonged":[62,263],"retention":[64],"in":[65,136,228,237,242,266],"lymphoma":[67],"model.":[68,270],"Four":[69,117],"4-phenylbutyric":[70],"acid":[71],"(4-PBA)":[72],"derivatives":[73],"p-MeO,":[75],"p-Cl,":[76],"p-Br,":[77],"or":[78],"p-I":[79],"substituents":[80,139],"were":[81,97,119,203],"selected":[82],"as":[83,110],"albumin-binding":[84],"motifs":[85],"coupled":[87,154,256],"CXCR4-binding":[91],"cyclic":[92],"peptide.":[93],"All":[94],"non-radioactive":[95],"standards":[96],"obtained":[98],"high":[100,105,161,261],"purity":[101],"(>95%)":[102],"showed":[104,133,160],"specific":[106],"binding":[107],"CXCR4":[109,254],"measured":[111],"radioligand":[114],"competition":[115],"assay.":[116],"peptides":[118],"labeled":[120],"[177Lu]LuCl3,":[122],">94%":[124],"radiochemical":[125],"purity.":[126],"Biodistribution":[127],"longitudinal":[129],"SPECT":[130],"imaging":[131],"studies":[132],"that":[134],"variations":[135],"binder":[138],"modulated":[140],"[177Lu]Lu-6,":[151],"peptide":[153],"4-BrPBA":[157],"binder,":[159],"tumor-to-organ":[165],"ratios":[166],"optimal":[167],"studies.":[170],"[177Lu]Lu-6":[171,221,271],"reached":[174],"23.6":[175],"\u00b1":[176,192,205,209],"4.57%":[177],"injected":[178],"activity":[179],"per":[180],"gram":[181],"(%":[182],"IA/g)":[183,195],"at":[184,213],"24":[185,214],"h":[186],"post-injection,":[187],"persistent":[189],"(12.3":[191],"2.04":[193],"%":[194,211],"after":[196],"120":[197],"h.":[198],"Blood":[199],"kidney":[201],"0.28":[204],"0.03":[206],"1.14":[208],"0.08":[210],"IA/g":[212],"h,":[215],"respectively.":[216],"In":[217],"study,":[220],"(15,":[222],"30,":[223],"60":[225],"MBq)":[226],"resulted":[227],"potent":[229],"growth":[231],"inhibition":[232],"increased":[234],"overall":[235],"survival":[236],"Z138":[239],"xenograft":[240],"model":[241],"comparison":[243],"control":[246],"[177Lu]Lu-Pentixather":[248],"groups":[249],"(p":[250],"<":[251],"0.05).":[252],"Novel":[253],"demonstrated":[260],"CXCR4-expressing":[268],"achieved":[272],"an":[273],"excellent":[274],"balance":[275],"between":[276],"maximizing":[277],"while":[280],"keeping":[281],"blood":[283],"residence":[284],"time":[285],"sufficiently":[286],"short":[287],"avoid":[289],"excessive":[290],"exposure":[291],"normal":[293],"organs.":[294]},"counts_by_year":[],"updated_date":"2026-11-12T12:28:57.059296","created_date":"2026-11-12T00:00:00"}
