PUBLICATION
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma
- Authors
- Zhang, K., Huang, L., Lai, F., Lin, S., Tian, H., Wu, D., Chena, X., Xu, H.
- ID
- ZDB-PUB-220602-7
- Date
- 2022
- Source
- Bioorganic & medicinal chemistry letters 71: 128825 (Journal)
- Registered Authors
- Keywords
- PI3K/HDAC dual inhibitor, cancer treatment, diffuse large B-cell lymphoma
- MeSH Terms
-
- Animals
- Apoptosis
- Cell Line, Tumor
- Histone Deacetylase Inhibitors*/pharmacology
- Histone Deacetylase Inhibitors*/therapeutic use
- Humans
- Lymphoma, Large B-Cell, Diffuse*/drug therapy
- Lymphoma, Large B-Cell, Diffuse*/metabolism
- Lymphoma, Large B-Cell, Diffuse*/pathology
- Phosphatidylinositol 3-Kinases/metabolism
- Phosphoinositide-3 Kinase Inhibitors/pharmacology
- Xenograft Model Antitumor Assays
- Zebrafish
- PubMed
- 35644299 Full text @ Bioorg. Med. Chem. Lett.
Citation
Zhang, K., Huang, L., Lai, F., Lin, S., Tian, H., Wu, D., Chena, X., Xu, H. (2022) Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma. Bioorganic & medicinal chemistry letters. 71:128825.
Abstract
The synergistic anti-tumor effect by simultaneous inhibitions of PI3K and HDAC has been verified to provide the rationality of PI3K/HDAC dual inhibitors for cancer treatment. Notably, the outstanding effect of PI3K/HDAC dual inhibitors against DLBCL has been paid much attention, especially for RR-DLBCL. Our previously reported 4-methylquinazoine scaffold based PI3K/HDAC dual inhibitors could suppress the growth of solid tumors and hematologic malignancies both in vitro and in vivo, validating the potential as new therapeutic agents for cancer. In this research, we further investigated the anti-tumor activity of one of our compounds against DLBCL cell lines and in vivo zebrafish xenograft model as well as the underlying mechanism, hoping to provide a novel therapeutic agent for treating DLBCL.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping