title: Theranostic systems assembled in situ on demand by host-guest chemistry.
abstract: Theranostic systems have been explored extensively for a diagnostic therapy in the forms of polymer conjugates, implantable devices, and inorganic nanoparticles. In this work, we report theranostic systems in situ assembled by host-guest chemistry responding to a request. As a model theranostic system on demand, cucurbit[6]uril-conjugated hyaluronate (CB[6]-HA) was synthesized and decorated with FITC-spermidine (spmd) and/or formyl peptide receptor like 1 (FPRL1) specific peptide-spmd by simple mixing in aqueous solution. The resulting (FITC-spmd and/or peptide-spmd)@CB[6]-HA was successfully applied to the bioimaging of its target-specific delivery to B16F1 cells with HA receptors and its therapeutic signal transduction with elevated Ca(2+) and phosphor-extracellular signal-regulated kinase (pERK) levels in FPRL1-expressing human breast adenocarcinoma (FPRL1/MCF-7) cells. Finally, we could confirm in vitro and in vivo stability of the highly specific host-guest interaction. The on-demand theranostic platform technology using host-guest chemistry can be exploited for various bioimaging, biosensing, drug delivery, and tissue engineering applications.
authors.affiliation: National Creative Research Initiative Center for Smart Supramolecules, Department of Chemistry, Pohang University of Science and Technology (POSTECH), San 31, Hyoja-dong, Nam-gu, Pohang, Kyungbuk 790-784, Republic of Korea.
authors.forename: Hyuntae
authors.initials: H
authors.lastname: Jung
authors.forename: Kyeng Min
authors.initials: KM
authors.lastname: Park
authors.forename: Jeong-A
authors.initials: JA
authors.lastname: Yang
authors.forename: Eun Ju
authors.initials: EJ
authors.lastname: Oh
authors.forename: Don-Wook
authors.initials: DW
authors.lastname: Lee
authors.forename: Kitae
authors.initials: K
authors.lastname: Park
authors.forename: Sung Ho
authors.initials: SH
authors.lastname: Ryu
authors.forename: Sei Kwang
authors.initials: SK
authors.lastname: Hahn
authors.forename: Kimoon
authors.initials: K
authors.lastname: Kim
mesh_terms: D000230:Adenocarcinoma / Q000175:diagnosis / Q000628:therapy; D000818:Animals; D001943:Breast Neoplasms / Q000175:diagnosis / Q000628:therapy; D001952:Bridged-Ring Compounds / Q000737:chemistry / Q000627:therapeutic use; D045744:Cell Line, Tumor; D005260:Female; D016650:Fluorescein-5-isothiocyanate / Q000737:chemistry / Q000627:therapeutic use; D006801:Humans; D006820:Hyaluronic Acid / Q000737:chemistry / Q000627:therapeutic use; D007093:Imidazoles / Q000737:chemistry / Q000627:therapeutic use; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D044042:Receptors, Formyl Peptide / Q000032:analysis* / Q000737:chemistry / Q000627:therapeutic use; D044067:Receptors, Lipoxin / Q000032:analysis* / Q000737:chemistry / Q000627:therapeutic use; D013095:Spermidine / Q000737:chemistry / Q000627:therapeutic use; D047028:Macrocyclic Compounds; D000099246:Cucurbit(n)urils
chemical_list: D001952:Bridged-Ring Compounds; D016650:Fluorescein-5-isothiocyanate; D006820:Hyaluronic Acid; D007093:Imidazoles; D044042:Receptors, Formyl Peptide; D044067:Receptors, Lipoxin; D013095:Spermidine; C105101:FPR2 protein, human; C454805:cucurbit(6)uril; D047028:Macrocyclic Compounds; D000099246:Cucurbit(n)urils