Publication:
Resorufin enters the photodynamic therapy arena: a monoamine oxidase activatable agent for selective cytotoxicity

dc.contributor.coauthorAtakan, Gizem
dc.contributor.coauthorGunbas, Gorkem
dc.contributor.departmentDepartment of Chemistry
dc.contributor.departmentGraduate School of Health Sciences
dc.contributor.departmentKUBAM (Koç University Boron and Advanced Materials Application and Research Center)
dc.contributor.departmentKUTEM (Koç University Tüpraş Energy Center)
dc.contributor.departmentKUYTAM (Koç University Surface Science and Technology Center)
dc.contributor.departmentSchool of Medicine
dc.contributor.kuauthorAlmammadov, Toghrul
dc.contributor.kuauthorKölemen, Safacan
dc.contributor.kuauthorLeylek, Özen
dc.contributor.kuauthorÖzcan, Gülnihal
dc.contributor.schoolcollegeinstituteCollege of Sciences
dc.contributor.schoolcollegeinstituteGRADUATE SCHOOL OF HEALTH SCIENCES
dc.contributor.schoolcollegeinstituteResearch Center
dc.contributor.schoolcollegeinstituteSCHOOL OF MEDICINE
dc.date.accessioned2024-11-09T22:49:41Z
dc.date.issued2020
dc.description.abstractA red-absorbing, water-soluble, and iodinated resorufin derivative (R1) that can be selectively activated with a monoamine oxidase (MAO) enzyme was synthesized, and its potential as a photodynamic therapy (PDT) agent was evaluated. R1 showed high O-1(2) generation yields in aqueous solutions upon addition of MAO isoforms, and it was further tested in cell culture studies. R1 induced photocytotoxicity after being triggered by endogenous MAO enzyme in cancer cells with a much higher efficiency in SH-SYSY neuroblastoma cells with high MAO-A expression. Additionally, R1 displayed differential cytotoxicity between cancer and normal cells, without any considerable dark toxicity. To the best of our knowledge, R1 marks the first example of a resorufin-based photosensitizer (PS) as well as the first anticancer drug that is activated by a MAO enzyme. Remarkably, the target PDT agent was obtained only in three steps as a result of versatile resorufin chemistry.
dc.description.indexedbyWOS
dc.description.indexedbyScopus
dc.description.indexedbyPubMed
dc.description.issue12
dc.description.openaccessNO
dc.description.sponsoredbyTubitakEuN/A
dc.description.sponsorshipKoc University
dc.description.sponsorshipMiddle East Technical University-BAP
dc.description.sponsorshipEuropean Research Council (ERC) under the European Union's Horizon 2020 research and innovation program [852614] Koc University Seed Funding, Middle East Technical University-BAP. The research leading to these results has received funding from the European Research Council (ERC) under the European Union's Horizon 2020 research and innovation program (Grant agreement No. [852614]).
dc.description.volume11
dc.identifier.doi10.1021/acsmedchemlett.0c00484
dc.identifier.issn1948-5875
dc.identifier.scopus2-s2.0-85097846704
dc.identifier.urihttps://doi.org/10.1021/acsmedchemlett.0c00484
dc.identifier.urihttps://hdl.handle.net/20.500.14288/6547
dc.identifier.wos599586900017
dc.keywordsPhotodynamic therapy
dc.keywordsActivatable photosensitizers
dc.keywordsResorufin
dc.keywordsCancer cell selectivity
dc.keywordsMnoamine oxidase
dc.language.isoeng
dc.publisherAmer Chemical Soc
dc.relation.ispartofAcs Medicinal Chemistry Letters
dc.subjectChemistry
dc.subjectMedicinal
dc.titleResorufin enters the photodynamic therapy arena: a monoamine oxidase activatable agent for selective cytotoxicity
dc.typeJournal Article
dspace.entity.typePublication
local.contributor.kuauthorAlmammadov, Toghrul
local.contributor.kuauthorLeylek, Özen
local.contributor.kuauthorÖzcan, Gülnihal
local.contributor.kuauthorKölemen, Safacan
local.publication.orgunit1College of Sciences
local.publication.orgunit1GRADUATE SCHOOL OF HEALTH SCIENCES
local.publication.orgunit1SCHOOL OF MEDICINE
local.publication.orgunit1Research Center
local.publication.orgunit2Department of Chemistry
local.publication.orgunit2KUYTAM (Koç University Surface Science and Technology Center)
local.publication.orgunit2KUBAM (Koç University Boron and Advanced Materials Application and Research Center)
local.publication.orgunit2KUTEM (Koç University Tüpraş Energy Center)
local.publication.orgunit2School of Medicine
local.publication.orgunit2Graduate School of Health Sciences
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