Work

Probing class I histone deacetylases (HDAC) with proteolysis targeting chimera (PROTAC) for the development of highly potent and selective degraders

Year: 2024

Type: article

Abstract: = 14.3 nM. Apoptotic study on leukemic cells (MV-4-11) displayed more than 50 % apoptosis took place at 100 nM. PROTAC 32a (HI31.1) showed a good margin of safety against normal cell line and proper chemical stability.

Source: Bioorganic Chemistry

DOI: 10.1016/j.bioorg.2024.107887

Authors: Hany S. Ibrahim, Menglu Guo, Sebatian Hilscher, Frank Erdmann, Matthias Schmidt, Mike Schutkowski, Chunquan Sheng, Wolfgang Sippl

Institutions: Egyptian Russian University, Martin Luther University Halle-Wittenberg, Second Military Medical University, Fudan University

Language: English

Topic: Protein Degradation and Inhibitors

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,100

Funders: Alexander von Humboldt-Stiftung, Deutsche Forschungsgemeinschaft

Awards: G1055467426, Entwicklung und biologische Charakterisierung von dualen Inhibitoren gegen den Apicomplexa Parasiten Plasmodium falciparum, Molekulares Design, Synthese und Pharmakologie von neuen und selektiven Histondesacetylase 10 (HDAC10) Inhibitoren

OpenAlex ID: W4403347883

FWCI: 0.926

Cites: 41

Cited by: 8

Related to: 10