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Isolation of a Natural Killer Group 2D Small-Molecule Ligand from DNA-Encoded Chemical Libraries.
Dakhel, Sheila; Galbiati, Andrea; Migliorini, Francesca; Comacchio, Claudia; Oehler, Sebastian; Prati, Luca; Scheuermann, Jörg; Cazzamalli, Samuele; Neri, Dario; Bassi, Gabriele; Favalli, Nicholas.
Afiliación
  • Dakhel S; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Galbiati A; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Migliorini F; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Comacchio C; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Oehler S; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Prati L; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Scheuermann J; Department of Chemistry and Applied Biosciences, ETH Zürich, Vladimir-Prelog-Weg 1-5, 8093, Zürich, Switzerland.
  • Cazzamalli S; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Neri D; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Bassi G; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
  • Favalli N; Philochem AG, Libernstrasse 3, 8112, Otelfingen, Switzerland.
ChemMedChem ; 17(21): e202200350, 2022 Nov 04.
Article en En | MEDLINE | ID: mdl-35929380
Natural Killer Group 2D (NKG2D) is a homo-dimeric transmembrane protein which is typically expressed on the surface of natural killer (NK) cells, natural killer T (NKT) cells, gamma delta T (γδT) cells, activated CD8 positive T-cells and activated macrophages. Bispecific molecules, capable of bridging NKG2D with a target protein expressed on the surface of tumor cells, may be used to redirect the cytotoxic activity of NK-cells towards antigen-positive malignant T-cells. In this work, we report the discovery of a novel NKG2D small molecule binder [KD =(410±60) nM], isolated from a DNA-Encoded Chemical Library (DEL). The discovery of small organic NKG2D ligands may facilitate the generation of fully synthetic bispecific adaptors, which may serve as an alternative to bispecific antibody products and which may benefit from better tumor targeting properties.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Bibliotecas de Moléculas Pequeñas / Subfamilia K de Receptores Similares a Lectina de Células NK Idioma: En Revista: ChemMedChem Asunto de la revista: FARMACOLOGIA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Alemania
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Bibliotecas de Moléculas Pequeñas / Subfamilia K de Receptores Similares a Lectina de Células NK Idioma: En Revista: ChemMedChem Asunto de la revista: FARMACOLOGIA / QUIMICA Año: 2022 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Alemania