Matches in SemOpenAlex for { <https://semopenalex.org/work/W3136394584> ?p ?o ?g. }
- W3136394584 endingPage "1222" @default.
- W3136394584 startingPage "1214" @default.
- W3136394584 abstract "Positron Emission Tomography (PET) imaging with antibody-based contrast agents frequently uses the radioisotopes [64Cu]Cu2+ and [89Zr]Zr4+. The macrobicyclic chelator commonly known as sarcophagine (sar) is ideal for labeling receptor-targeted biomolecules with [64Cu]Cu2+. The siderophore chelator, desferrioxamine-B (dfo), has been widely used to incorporate [89Zr]Zr4+ into antibodies. Here, we describe new bifunctional chelators of sar and dfo: these chelators have been functionalized with dibromomaleimides (dbm), that enable site-specific and highly stable attachment of molecular cargoes to reduced, solvent-accessible, interstrand native disulfide groups. The new sar-dbm and dfo-dbm derivatives can be easily conjugated with the IgG antibody trastuzumab via reaction with reduced interstrand disulfide groups to give site-specifically modified dithiomaleamic acid (dtm) conjugates, sar-dtm-trastuzumab and dfo-dtm-trastuzumab, in which interstrand disulfides are rebridged covalently with a small molecule linker. Both sar- and dfo-dtm-trastuzumab conjugates have been radiolabeled with [64Cu]Cu2+ and [89Zr]Zr4+, respectively, in near quantitative radiochemical yield (>99%). Serum stability studies, in vivo PET imaging, and biodistribution analyses using these radiolabeled immunoconjugates demonstrate that both [64Cu]Cu-sar-dtm-trastuzumab and [89Zr]Zr-dfo-dtm-trastuzumab possess high stability in biological milieu. Dibromomaleimide technology can be easily applied to enable stable, site-specific attachment of radiolabeled chelators, such as sar and dfo, to native interstrand disulfide regions of antibodies, enabling tracking of antibodies with PET imaging." @default.
- W3136394584 created "2021-03-29" @default.
- W3136394584 creator A5000200207 @default.
- W3136394584 creator A5011196912 @default.
- W3136394584 creator A5020585135 @default.
- W3136394584 creator A5021417954 @default.
- W3136394584 creator A5023837325 @default.
- W3136394584 creator A5050310576 @default.
- W3136394584 creator A5060026431 @default.
- W3136394584 creator A5061001964 @default.
- W3136394584 creator A5071380280 @default.
- W3136394584 creator A5075237619 @default.
- W3136394584 creator A5076782756 @default.
- W3136394584 creator A5090174053 @default.
- W3136394584 date "2021-03-16" @default.
- W3136394584 modified "2023-10-16" @default.
- W3136394584 title "New Bifunctional Chelators Incorporating Dibromomaleimide Groups for Radiolabeling of Antibodies with Positron Emission Tomography Imaging Radioisotopes" @default.
- W3136394584 cites W1761681552 @default.
- W3136394584 cites W1964083777 @default.
- W3136394584 cites W1975639913 @default.
- W3136394584 cites W1979415145 @default.
- W3136394584 cites W1984552257 @default.
- W3136394584 cites W1992175481 @default.
- W3136394584 cites W1999794575 @default.
- W3136394584 cites W2008386216 @default.
- W3136394584 cites W2023687344 @default.
- W3136394584 cites W2035411389 @default.
- W3136394584 cites W2040477831 @default.
- W3136394584 cites W2046180004 @default.
- W3136394584 cites W2046185660 @default.
- W3136394584 cites W2047980903 @default.
- W3136394584 cites W2054845147 @default.
- W3136394584 cites W2064895892 @default.
- W3136394584 cites W2079218447 @default.
- W3136394584 cites W2082253198 @default.
- W3136394584 cites W2085607173 @default.
- W3136394584 cites W2086114352 @default.
- W3136394584 cites W2098577546 @default.
- W3136394584 cites W2098686036 @default.
- W3136394584 cites W2115269770 @default.
- W3136394584 cites W2116150122 @default.
- W3136394584 cites W2120920314 @default.
- W3136394584 cites W2144782918 @default.
- W3136394584 cites W2153699864 @default.
- W3136394584 cites W2327088034 @default.
- W3136394584 cites W2471482226 @default.
- W3136394584 cites W2558931128 @default.
- W3136394584 cites W2595729256 @default.
- W3136394584 cites W2596270747 @default.
- W3136394584 cites W2755901993 @default.
- W3136394584 cites W2762743006 @default.
- W3136394584 cites W2786202881 @default.
- W3136394584 cites W2787760690 @default.
- W3136394584 cites W2887050230 @default.
- W3136394584 cites W2898597200 @default.
- W3136394584 cites W2900304141 @default.
- W3136394584 cites W2901272595 @default.
- W3136394584 cites W2913361482 @default.
- W3136394584 cites W2922471286 @default.
- W3136394584 cites W2963810811 @default.
- W3136394584 cites W2983379295 @default.
- W3136394584 cites W3004068744 @default.
- W3136394584 cites W3008516230 @default.
- W3136394584 cites W3009413300 @default.
- W3136394584 cites W3010600514 @default.
- W3136394584 cites W3034512705 @default.
- W3136394584 doi "https://doi.org/10.1021/acs.bioconjchem.0c00710" @default.
- W3136394584 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/8299457" @default.
- W3136394584 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/33724798" @default.
- W3136394584 hasPublicationYear "2021" @default.
- W3136394584 type Work @default.
- W3136394584 sameAs 3136394584 @default.
- W3136394584 citedByCount "6" @default.
- W3136394584 countsByYear W31363945842021 @default.
- W3136394584 countsByYear W31363945842022 @default.
- W3136394584 countsByYear W31363945842023 @default.
- W3136394584 crossrefType "journal-article" @default.
- W3136394584 hasAuthorship W3136394584A5000200207 @default.
- W3136394584 hasAuthorship W3136394584A5011196912 @default.
- W3136394584 hasAuthorship W3136394584A5020585135 @default.
- W3136394584 hasAuthorship W3136394584A5021417954 @default.
- W3136394584 hasAuthorship W3136394584A5023837325 @default.
- W3136394584 hasAuthorship W3136394584A5050310576 @default.
- W3136394584 hasAuthorship W3136394584A5060026431 @default.
- W3136394584 hasAuthorship W3136394584A5061001964 @default.
- W3136394584 hasAuthorship W3136394584A5071380280 @default.
- W3136394584 hasAuthorship W3136394584A5075237619 @default.
- W3136394584 hasAuthorship W3136394584A5076782756 @default.
- W3136394584 hasAuthorship W3136394584A5090174053 @default.
- W3136394584 hasBestOaLocation W31363945841 @default.
- W3136394584 hasConcept C111919701 @default.
- W3136394584 hasConcept C134306372 @default.
- W3136394584 hasConcept C136339569 @default.
- W3136394584 hasConcept C150903083 @default.
- W3136394584 hasConcept C161790260 @default.
- W3136394584 hasConcept C178790620 @default.
- W3136394584 hasConcept C185592680 @default.
- W3136394584 hasConcept C197336794 @default.