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Published Erratum
. 2021 Feb 22;2(2):670-671.
doi: 10.1039/d1cb90008k. eCollection 2021 Apr 1.

Correction: Fragment-based covalent ligand discovery

Wenchao Lu  1   2 , Milka Kostic  1 , Tinghu Zhang  1   2 , Jianwei Che  1   2   3 , Matthew P Patricelli  4 , Lyn H Jones  3 , Edward T Chouchani  1   5 , Nathanael S Gray  1   2
Affiliations
Published Erratum

Correction: Fragment-based covalent ligand discovery

Wenchao Lu et al. RSC Chem Biol. .

Abstract

[This corrects the article DOI: 10.1039/D0CB00222D.].

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Figures

Fig. 2
Fig. 2. The structures of representative well-characterized electrophilic fragments identified from target-based screening strategies in recent years. (A) KRAS-G12C allele-specific covalent fragment (6H05) identified from tethering screen, which was further elaborated to compound 12.31 This inspired numerous groups to develop further optimized inhibitors, within which AMG51033 and MRTX84936 successfully entered clinical trials. (B) Compound 5 targets the active cysteine (C885) of HOIP.37 (C) OTUB2-COV-1 targets the active cysteine (C51) of OTUB2 and NUDT7-COV-1 target C73 of NUDT7.38 (D) Sulfopin targets the active cysteine of Pin1 (C113).39 (E) Representative covalent fragment scaffolds target the active cysteine (C145) of SARS-COV-2 main protease (Mpro).40
See this image and copyright information in PMC

Erratum for

  • Fragment-based covalent ligand discovery.
    Lu W, Kostic M, Zhang T, Che J, Patricelli MP, Jones LH, Chouchani ET, Gray NS. Lu W, et al. RSC Chem Biol. 2021 Feb 9;2(2):354-367. doi: 10.1039/d0cb00222d. eCollection 2021 Apr 1. RSC Chem Biol. 2021. PMID: 34458789 Free PMC article. Review.

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