Your browser doesn't support javascript.
loading
Selection of DNA-Encoded Libraries to Protein Targets within and on Living Cells.
Cai, Bo; Kim, Dongwook; Akhand, Saeed; Sun, Yixing; Cassell, Robert J; Alpsoy, Aktan; Dykhuizen, Emily C; Van Rijn, Richard M; Wendt, Michael K; Krusemark, Casey J.
Affiliation
  • Cai B; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Kim D; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Akhand S; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Sun Y; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Cassell RJ; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Alpsoy A; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Dykhuizen EC; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Van Rijn RM; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Wendt MK; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
  • Krusemark CJ; Department of Medicinal Chemistry and Molecular Pharmacology , Purdue Center for Cancer Research, Purdue University , West Lafayette , Indiana 47907 , United States.
J Am Chem Soc ; 141(43): 17057-17061, 2019 10 30.
Article in En | MEDLINE | ID: mdl-31613623
ABSTRACT
We report the selection of DNA-encoded small molecule libraries against protein targets within the cytosol and on the surface of live cells. The approach relies on generation of a covalent linkage of the DNA to protein targets by affinity labeling. This cross-linking event enables subsequent copurification by a tag on the recombinant protein. To access targets within cells, a cyclic cell-penetrating peptide is appended to DNA-encoded libraries for delivery across the cell membrane. As this approach assesses binding of DELs to targets in live cells, it provides a strategy for selection of DELs against challenging targets that cannot be expressed and purified as active.
Subject(s)
Fulltext
Print
XML
PubMed Links
Search on Google

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Proteins / Small Molecule Libraries / Cell-Penetrating Peptides Limits: Humans Language: En Journal: J Am Chem Soc Year: 2019 Type: Article Affiliation country: United States
Fulltext
Print
XML
PubMed Links
Search on Google

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Proteins / Small Molecule Libraries / Cell-Penetrating Peptides Limits: Humans Language: En Journal: J Am Chem Soc Year: 2019 Type: Article Affiliation country: United States