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Front Cover: Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity (ChemMedChem 1/2020)
Author(s) -
Pillow Thomas H.,
Adhikari Pragya,
Blake Robert A.,
Chen Jinhua,
Del Rosario Geoffrey,
Deshmukh Gauri,
Figueroa Isabel,
Gascoigne Karen E.,
Kamath Amrita V.,
Kaufman Susan,
Kleinheinz Tracy,
Kozak Katherine R.,
Latifi Brandon,
Leipold Douglas D.,
Sing Li Chun,
Li Ruina,
Mulvihill Melinda M.,
O'Donohue Aimee,
Rowntree Rebecca K.,
Sadowsky Jack D.,
Wai John,
Wang Xinxin,
Wu Cong,
Xu Zijin,
Yao Hui,
Yu ShangFan,
Zhang Donglu,
Zang Richard,
Zhang Hongyan,
Zhou Hao,
Zhu Xiaoyu,
Dragovich Peter S.
Publication year - 2020
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900683
Subject(s) - conjugate , ubiquitin ligase , chemistry , linker , fusion protein , front cover , proteasome , antibody , chimeric antigen receptor , cleavage (geology) , microbiology and biotechnology , ubiquitin , in vivo , biophysics , raft , biochemistry , biology , cover (algebra) , immunotherapy , recombinant dna , immunology , computer science , immune system , mathematics , mathematical analysis , fracture (geology) , engineering , operating system , paleontology , mechanical engineering , gene , polymer , organic chemistry , copolymer
The Front Cover shows the intracellular delivery of a chimeric protein degrader via an antibody conjugate. The antibody–degrader conjugate is stable in circulation and, upon binding to an antigen on the cell surface, is trafficked to the lysosome. Antibody catabolism and linker cleavage subsequently release the free chimeric degrader and allow it to form a trimeric complex between a target protein and a ubiquitin ligase. This complex promotes ubiquitination of the target protein resulting in its degradation via the cellular proteasome. More information can be found in the Full Paper by Full Paper by Peter S. Dragovich, Thomas H. Pillow et al. on page 19 in Issue 1, 2020 (DOI: 10.1002/cmdc.201900497).