Forskning
Udskriv Udskriv
Switch language
Region Hovedstaden - en del af Københavns Universitetshospital
Udgivet

Site-SpecificCu Labeling of the Serine Protease, Active Site Inhibited Factor Seven Azide (FVIIai-N), Using Copper Free Click Chemistry

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  1. Affinity-Guided Conjugation to Antibodies for Use in Positron Emission Tomography

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  2. Oxime Coupling of Active Site Inhibited Factor Seven with a Nonvolatile, Water-Soluble Fluorine-18 Labeled Aldehyde

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  3. Molecular Targeted NIR-II Probe for Image-Guided Brain Tumor Surgery

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  4. Preclinical Study on GRPR-Targeted (68)Ga-Probes for PET Imaging of Prostate Cancer

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  5. Synthesis and Evaluation of Astatinated N-[2-(Maleimido)ethyl]-3-(trimethylstannyl)benzamide Immunoconjugates

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  1. Tumor cell MT1-MMP is dispensable for osteosarcoma tumor growth, bone degradation and lung metastasis

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  2. Limited diagnostic utility of Chromogranin A measurements in workup of neuroendocrine tumors

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  3. Blocking of efflux transporters in rats improves translational validation of brain radioligands

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

  4. Renal 123I-MIBG Uptake before and after Live-Donor Kidney Transplantation

    Publikation: Bidrag til tidsskriftTidsskriftartikelForskningpeer review

Vis graf over relationer

A method for site-specific radiolabeling of the serine protease active site inhibited factor seven (FVIIai) with64Cu has been applied using a biorthogonal click reaction. FVIIai binds to tissue factor (TF), a trans-membrane protein involved in hemostasis, angiogenesis, proliferation, cell migration, and survival of cancer cells. First a single azide moiety was introduced in the active site of this 50 kDa protease. Then a NOTA moiety was introduced via a strain promoted azide-alkyne reaction and the corresponding conjugate was labeled with64Cu. Binding to TF and the stability was evaluated in vitro. TF targeting capability of the radiolabeled conjugate was tested in vivo by positron emission tomography (PET) imaging in pancreatic human xenograft cancer mouse models with various TF expressions. The conjugate showed good stability (>91% at 16 h), an immunoreactivity of 93.5%, and a mean tumor uptake of 2.1 ± 0.2%ID/g at 15 h post injection. In conclusion, FVIIai was radiolabeled with64Cu in single well-defined position of the protein. This method can be utilized to prepare conjugates from serine proteases with the label at a specific position.

OriginalsprogEngelsk
TidsskriftBioconjugate Chemistry
Vol/bind29
Udgave nummer1
Sider (fra-til)117-125
Antal sider9
ISSN1043-1802
DOI
StatusUdgivet - 17 jan. 2018

ID: 52790211