A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras
| Title: | A 'click' chemistry approach to novel entinostat (MS-275) based class I histone deacetylase proteolysis targeting chimeras |
|---|---|
| Authors: | Jasmine M Cross; Megan E Coulson; Joshua P Smalley; Wiktoria A Pytel; Ozair Ismail; Justin S Trory; Shaun M Cowley; James T Hodgkinson |
| Publication Year: | 2022 |
| Collection: | University of Leicester: Figshare |
| Subject Terms: | Science & Technology; Life Sciences & Biomedicine; Biochemistry & Molecular Biology; Chemistry; Medicinal; Pharmacology & Pharmacy; DEGRADATION; HDAC1 |
| Description: | Click chemistry was utilised to prepare a library of PROTACs based on entinostat a class I histone deacetylase (HDAC) inhibitor in clinical trials. A novel PROTAC JMC-137 was identified as a HDAC1/2 and HDAC3 degrader in HCT116 cells. However, potency was compromised compared to previously identified class I HDAC PROTACs highlighting the importance in the choice of HDAC ligand, functional group for linker attachment and positioning in PROTAC design. |
| Document Type: | article in journal/newspaper |
| Language: | unknown |
| Relation: | 2381/21618366.v1 |
| Availability: | https://figshare.com/articles/journal_contribution/A_click_chemistry_approach_to_novel_entinostat_MS-275_based_class_I_histone_deacetylase_proteolysis_targeting_chimeras/21618366 |
| Rights: | CC BY 4.0 |
| Accession Number: | edsbas.8768166F |
| Database: | BASE |