Erratum: Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907)

Article abstract of DOI:10.1021/jacs.0c05753

This addition corrects several errors in the chemical drawings in the article. The correction has no influence on the data or conclusions of the work. The configuration of the chiral carbon in Figure 1 in the main text was originally drawn as S. The corrected figure shown here depicts the R enantiomer used in this work. (Figure presented) In the Supporting Information PDF files, the configuration of the chiral carbon of the BTK binder in supplementary Table 1 (page S9), supplementary Figure 4 (page S13), and several of the synthetic schemes (pages S17-S42) was originally drawn and marked as S by error. The corrected supplementary file depicts the R enantiomer, which was the sole enantiomer used in the work. The linker in the right panel of supplementary Table 1 (page S9) was missing two carbons in the drawing, and the linker size written for compound PG15 (RC-0b) in the table was incorrect. The corrected supplementary file contains the correct drawings and linker sizes.

Full text of DOI:10.1021/jacs.0c05753

pubs.acs.org/JACS
Addition/Correction
Correction to Efficient Targeted Degradation via Reversible and
Irreversible Covalent PROTACs
Ronen Gabizon, Amit Shraga, Paul Gehrtz, Ella Livnah, Yamit Shorer, Neta Gurwicz, Liat Avram,
Tamar Unger, Hila Aharoni, Shira Albeck, Alexander Brandis, Ziv Shulman, Ben-Zion Katz,
Yair Herishanu, and Nir London*
J. Am. Chem. Soc. 2020. DOI: 10.1021/jacs.9b13907
Cite This: https://dx.doi.org/10.1021/jacs.0c05753
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sı Supporting Information
his addition corrects several errors in the chemical
The corrected supplementary file contains the correct drawings
T
drawings in the article. The correction has no influence
on the data or conclusions of the work.
The configuration of the chiral carbon in Figure 1 in the main
text was originally drawn as S. The corrected figure shown here
depicts the R enantiomer used in this work.
and linker sizes.
ASSOCIATED CONTENT
■
*
sı Supporting Information
The Supporting Information is available free of charge at
https://pubs.acs.org/doi/10.1021/jacs.0c05753.
Additional information including detailed experimental
methods, description of the reversible covalent BTK
PROTAC library and its degradation results in two cell
lines, BTK degradation by PROTACs in Ramos cells, data
on cellular penetration of PROTACs, time dependency of
BTK degradation, validation of CRBN-mediated degra-
dation, kinetic studies of BTK labeling using LC/MS,
GSH effect on labeling, proteomics selectivity analysis for
the PROTACs at additional concentrations, B cell
receptor signaling inhibition data, detailed synthetic
protocols for preparation of compounds with high-
resolution mass spectrometry and NMR analysis (PDF)
Figure 1. Structures of reversible covalent, irreversible covalent and
noncovalent BTK PROTACs described in this study. The electrophilic
moieties are highlighted in red.
In the Supporting Information PDF files, the configuration of
the chiral carbon of the BTK binder in supplementary Table 1
(
page S9), supplementary Figure 4 (page S13), and several of
the synthetic schemes (pages S17−S42) was originally drawn
and marked as S by error. The corrected supplementary file
depicts the R enantiomer, which was the sole enantiomer used in
the work.
The linker in the right panel of supplementary Table 1 (page
S9) was missing two carbons in the drawing, and the linker size
written for compound PG15 (RC-0b) in the table was incorrect.
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XXXX American Chemical Society
https://dx.doi.org/10.1021/jacs.0c05753
J. Am. Chem. Soc. XXXX, XXX, XXX−XXX
A