Erratum: Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907) (2024)

Abstract

His 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. 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.

Original languageEnglish
Pages (from-to)11316
Number of pages1
JournalJournal of the American Chemical Society
Volume142
Issue number25
DOIs
StatePublished - 24 Jun 2020

Bibliographical note

Publisher Copyright:
© 2020 American Chemical Society

Access to Document

Other files and links

Fingerprint

Dive into the research topics of 'Erratum: Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907)'. Together they form a unique fingerprint.

View full fingerprint

Cite this

  • APA
  • Author
  • BIBTEX
  • Harvard
  • Standard
  • RIS
  • Vancouver

Gabizon, R., Shraga, A., Gehrtz, P., Livnah, E., Shorer, Y., Gurwicz, N., Avram, L., Unger, T., Aharoni, H., Albeck, S., Brandis, A., Shulman, Z., Katz, B. Z., Herishanu, Y., & London, N. (2020). Erratum: Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907). Journal of the American Chemical Society, 142(25), 11316. https://doi.org/10.1021/jacs.0c05753

Gabizon, Ronen ; Shraga, Amit ; Gehrtz, Paul et al. / Erratum : Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907). In: Journal of the American Chemical Society. 2020 ; Vol. 142, No. 25. pp. 11316.

@article{ae17e8174cf74645bee4e91d378b1fff,

title = "Erratum: Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907)",

abstract = "His 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. 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.",

author = "Ronen Gabizon and Amit Shraga and Paul Gehrtz and Ella Livnah and Yamit Shorer and Neta Gurwicz and Liat Avram and Tamar Unger and Hila Aharoni and Shira Albeck and Alexander Brandis and Ziv Shulman and Katz, {Ben Zion} and Yair Herishanu and Nir London",

note = "Publisher Copyright: {\textcopyright} 2020 American Chemical Society",

year = "2020",

month = jun,

day = "24",

doi = "10.1021/jacs.0c05753",

language = "אנגלית",

volume = "142",

pages = "11316",

journal = "Journal of the American Chemical Society",

issn = "0002-7863",

publisher = "American Chemical Society",

number = "25",

}

Gabizon, R, Shraga, A, Gehrtz, P, Livnah, E, Shorer, Y, Gurwicz, N, Avram, L, Unger, T, Aharoni, H, Albeck, S, Brandis, A, Shulman, Z, Katz, BZ, Herishanu, Y & London, N 2020, 'Erratum: Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907)', Journal of the American Chemical Society, vol. 142, no. 25, pp. 11316. https://doi.org/10.1021/jacs.0c05753

Erratum: Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907). / Gabizon, Ronen; Shraga, Amit; Gehrtz, Paul et al.
In: Journal of the American Chemical Society, Vol. 142, No. 25, 24.06.2020, p. 11316.

Research output: Contribution to journalComment/debate

TY - JOUR

T1 - Erratum

T2 - Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907)

AU - Gabizon, Ronen

AU - Shraga, Amit

AU - Gehrtz, Paul

AU - Livnah, Ella

AU - Shorer, Yamit

AU - Gurwicz, Neta

AU - Avram, Liat

AU - Unger, Tamar

AU - Aharoni, Hila

AU - Albeck, Shira

AU - Brandis, Alexander

AU - Shulman, Ziv

AU - Katz, Ben Zion

AU - Herishanu, Yair

AU - London, Nir

N1 - Publisher Copyright:© 2020 American Chemical Society

PY - 2020/6/24

Y1 - 2020/6/24

N2 - His 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. 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.

AB - His 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. 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.

UR - http://www.scopus.com/inward/record.url?scp=85087095397&partnerID=8YFLogxK

U2 - 10.1021/jacs.0c05753

DO - 10.1021/jacs.0c05753

M3 - ???researchoutput.researchoutputtypes.contributiontojournal.comment???

C2 - 32520539

AN - SCOPUS:85087095397

SN - 0002-7863

VL - 142

SP - 11316

JO - Journal of the American Chemical Society

JF - Journal of the American Chemical Society

IS - 25

ER -

Gabizon R, Shraga A, Gehrtz P, Livnah E, Shorer Y, Gurwicz N et al. Erratum: Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907). Journal of the American Chemical Society. 2020 Jun 24;142(25):11316. doi: 10.1021/jacs.0c05753

Erratum: Efficient targeted degradation via reversible and irreversible covalent PROTACs (Journal American Chemical Society (2020) DOI: 10.1021/jacs.9b13907) (2024)

FAQs

What are the problems with PROTACs? ›

PROTACs' unique structure makes it challenging to meet Lipinski's Rule of Five, which is designed for small molecules. PROTAC drugs have poor permeability, which means poor druggability for oral administration. And the correlation between in vitro and in vivo permeability is weak.

Are PROTACs reversible? ›

Only when the PROTAC molecule binds to the active site of the targeted protein, the nearby cysteine side chain can react with the α-cyano-acrylamide group to form a stable covalent bond. Once the targeted protein is degraded, the reversible covalent PROTAC can be regenerated.

Do PROTACs break the rule of 5? ›

As PROTACs do not follow Lipinski's 'Rule of 5', these molecules face drug metabolism and pharmaco*kinetic challenges. A detailed section on absorption, distribution, metabolism, and excretion of degraders is provided wherein we discuss methodologies and strategies to surmount the challenges faced by these molecules.

Do PROTACs cross the blood brain barrier? ›

Therefore, well-designed PROTACs can cross the BBB through receptor-mediated transcytosis or through carrier-mediated endocytosis due to biologically and physically systemic structures based on the structuralism propounded by Dr. Lévi-Strauss.

Are PROTACs degraders? ›

PROTACs are heterobifunctional molecules that degrade target proteins by hijacking the ubiquitin–proteasome system. Currently, about 20–25% of all protein targets are being studied, and most works focus on their enzymatic functions.

What are the advantages of PROTACs over small molecule inhibitors? ›

Small Molecule Inhibitors. PROTACs can overcome most of the limitations of small molecule inhibitors, and they offer several advantages of the traditional concepts of drug discovery by targeted protein degradation. First, PROTACs can affect non-enzymatic functions by degrading whole proteins.

Are PROTACs orally bioavailable? ›

PROTACs in clinical trials

All seven CRBN PROTACs are administered orally in the clinical studies and the oral bioavailability in mice has been reported for four of them (all have F >30%). By contrast, DT-2216 has a very low bioavailability (F <0.03%, mouse) and is administered by intravenous infusion.

What is the difference between molecular glue and PROTACs? ›

Molecular glues enhance interactions, altering protein functions or stability, while PROTACs initiate a sequence of events leading to the targeted protein's degradation. This difference in action reflects their varied potential in therapeutic applications.

Top Articles
Latest Posts
Article information

Author: Margart Wisoky

Last Updated:

Views: 5555

Rating: 4.8 / 5 (78 voted)

Reviews: 85% of readers found this page helpful

Author information

Name: Margart Wisoky

Birthday: 1993-05-13

Address: 2113 Abernathy Knoll, New Tamerafurt, CT 66893-2169

Phone: +25815234346805

Job: Central Developer

Hobby: Machining, Pottery, Rafting, Cosplaying, Jogging, Taekwondo, Scouting

Introduction: My name is Margart Wisoky, I am a gorgeous, shiny, successful, beautiful, adventurous, excited, pleasant person who loves writing and wants to share my knowledge and understanding with you.