Inhibitor-decorated Polymer Conjugates Targeting Fibroblast Activation Protein
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F17%3A00481818" target="_blank" >RIV/61388963:_____/17:00481818 - isvavai.cz</a>
Alternative codes found
RIV/61389013:_____/17:00481818 RIV/00216208:11110/17:10364980 RIV/00216208:11310/17:10364980
Result on the web
<a href="http://dx.doi.org/10.1021/acs.jmedchem.7b00767" target="_blank" >http://dx.doi.org/10.1021/acs.jmedchem.7b00767</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.jmedchem.7b00767" target="_blank" >10.1021/acs.jmedchem.7b00767</a>
Alternative languages
Result language
angličtina
Original language name
Inhibitor-decorated Polymer Conjugates Targeting Fibroblast Activation Protein
Original language description
Proteases are directly involved in cancer pathogenesis. Expression of fibroblast activation protein (FAP) is upregulated in stromal fibroblasts in more than 90% of epithelial cancers and is associated with tumor progression. FAP expression is minimal or absent in most normal adult tissues, suggesting its promise as a target for the diagnosis or treatment of various cancers. Here, we report preparation of a polymer conjugate (an iBody) containing a FAP-specific inhibitor as the targeting ligand. The iBody inhibits both human and mouse FAP with low nanomolar inhibition constants but does not inhibit close FAP homologues dipeptidyl peptidase IV, dipeptidyl peptidase 9, and prolyl oligopeptidase. We demonstrate the applicability of this iBody for the isolation of FAP from cell lysates and blood serum as well as for its detection by ELISA, Western blot, flow cytometry, and confocal microscopy. Our results show the iBody is a useful tool for FAP targeting in vitro and potentially also for specific anticancer drug delivery.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10608 - Biochemistry and molecular biology
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Journal of Medicinal Chemistry
ISSN
0022-2623
e-ISSN
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Volume of the periodical
60
Issue of the periodical within the volume
20
Country of publishing house
US - UNITED STATES
Number of pages
9
Pages from-to
8385-8393
UT code for WoS article
000414114300010
EID of the result in the Scopus database
2-s2.0-85032436419