Literature DB >> 34671730

Covalent PROTACs: the best of both worlds?

Neil P Grimster1.   

Abstract

Covalent PROTACs combine the cutting edge research areas of targeted covalent inhibitors (TCIs) and proteolysis targeting chimeras (PROTACs). This nascent field of research has already demonstrated several interesting findings, and holds an immense amount of potential to expand the druggable proteome. In this opinion, we present some of these intriguing early findings and discuss the potential advantages and disadvantages of this approach. This journal is © The Royal Society of Chemistry.

Entities:  

Year:  2021        PMID: 34671730      PMCID: PMC8459387          DOI: 10.1039/d1md00191d

Source DB:  PubMed          Journal:  RSC Med Chem        ISSN: 2632-8682


  34 in total

1.  PROTAC-Mediated Degradation of Bruton's Tyrosine Kinase Is Inhibited by Covalent Binding.

Authors:  Christopher P Tinworth; Hannah Lithgow; Lars Dittus; Zuni I Bassi; Sophie E Hughes; Marcel Muelbaier; Han Dai; Ian E D Smith; William J Kerr; Glenn A Burley; Marcus Bantscheff; John D Harling
Journal:  ACS Chem Biol       Date:  2019-02-27       Impact factor: 5.100

2.  In Silico Modeling of PROTAC-Mediated Ternary Complexes: Validation and Application.

Authors:  Michael L Drummond; Christopher I Williams
Journal:  J Chem Inf Model       Date:  2019-02-15       Impact factor: 4.956

Review 3.  Proteolysis targeting chimeras (PROTACs) in 'beyond rule-of-five' chemical space: Recent progress and future challenges.

Authors:  Scott D Edmondson; Bin Yang; Charlene Fallan
Journal:  Bioorg Med Chem Lett       Date:  2019-04-20       Impact factor: 2.823

4.  10 years into the resurgence of covalent drugs.

Authors:  Elena De Vita
Journal:  Future Med Chem       Date:  2020-12-04       Impact factor: 3.808

5.  Protein degradation through covalent inhibitor-based PROTACs.

Authors:  Gang Xue; Jiahui Chen; Lihong Liu; Danli Zhou; Yingying Zuo; Tiancheng Fu; Zhengying Pan
Journal:  Chem Commun (Camb)       Date:  2020-02-04       Impact factor: 6.222

6.  A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL.

Authors:  Bingqi Tong; Jessica N Spradlin; Luiz F T Novaes; Erika Zhang; Xirui Hu; Malte Moeller; Scott M Brittain; Lynn M McGregor; Jeffrey M McKenna; John A Tallarico; Markus Schirle; Thomas J Maimone; Daniel K Nomura
Journal:  ACS Chem Biol       Date:  2020-06-25       Impact factor: 5.100

7.  Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function.

Authors:  Mai Luo; Jessica N Spradlin; Lydia Boike; Bingqi Tong; Scott M Brittain; Jeffrey M McKenna; John A Tallarico; Markus Schirle; Thomas J Maimone; Daniel K Nomura
Journal:  Cell Chem Biol       Date:  2021-01-28       Impact factor: 8.116

8.  Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs.

Authors:  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; Nir London
Journal:  J Am Chem Soc       Date:  2020-05-19       Impact factor: 15.419

9.  Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry.

Authors:  Wen-Hao Guo; Xiaoli Qi; Xin Yu; Yang Liu; Chan-I Chung; Fang Bai; Xingcheng Lin; Dong Lu; Lingfei Wang; Jianwei Chen; Lynn Hsiao Su; Krystle J Nomie; Feng Li; Meng C Wang; Xiaokun Shu; José N Onuchic; Jennifer A Woyach; Michael L Wang; Jin Wang
Journal:  Nat Commun       Date:  2020-08-26       Impact factor: 14.919

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  1 in total

1.  Cereblon covalent modulation through structure-based design of histidine targeting chemical probes.

Authors:  Justin T Cruite; Geoffrey P Dann; Jianwei Che; Katherine A Donovan; Silas Ferrao; Scott B Ficarro; Eric S Fischer; Nathanael S Gray; Fidel Huerta; Nikki R Kong; Hu Liu; Jarrod A Marto; Rebecca J Metivier; Radosław P Nowak; Breanna L Zerfas; Lyn H Jones
Journal:  RSC Chem Biol       Date:  2022-07-08
  1 in total

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